Ultra-short-acting beta-adrenergic receptor blocking agents. 2. (Aryloxy)propanolamines containing esters on the aryl function.
Conformationally restricted congeners of dopamine derived from 2-aminoindan.
Spiro oxazolidinedione aldose reductase inhibitors.
Synthesis and topical antiinflammatory activity of some steroidal [16 alpha, 17 alpha-d]Isoxazolidines.
Ammonium 7H-purin-6-yl 1-Thio-beta-D-glucopyranosiduronate, a latent, selective anticancer agent.
2-beta-D-Ribofuranosylthiazole-4-carboxamide, a novel potential antitumor agent for lung tumors and metastases.
1,2,5-thiadiazole 1-oxide and 1,1-dioxide derivatives. A new class of potent histamine H2-receptor antagonists.
Antiestrogenic properties of substituted benz[a]anthracene-3,9-diols.
1-Acyltriazoles as antiinflammatory agents.
Synthesis and dopaminergic properties of some exo- and endo-2-aminobenzonorbornenes designed as rigid analogue of dopamine.
Peptide sweeteners. 5. Side-chain homologues relating zwitterionic and trifluoroacetylated amino acid anilide and dipeptide sweeteners.
Antiinflammatory properties of 8-aryl-5-isopropyl-2H-1,3-dioxolo[4,5-g]quinazolin-6(5H)-ones and -thiones.
Conformation-activity study of methadone and related compounds.
Hypobetalipoproteinemic agents. 3. Variation of the polycyclic portion of 4-(1-adamantyloxy)aniline.
N-Methylnalorphine: definition of N-allyl conformation for antagonism at the opiate receptor.
Synthesis and spasmolytic activities of 2-(1,2-benzisoxazol-3-yl)-3-[[omega-(dialkylamino)alkoxy]phenyl]acrylonitriles.
Nitro and amino derivatives of lucanthone as antitumor agents.
Structure-activity relationships in potentially hallucinogenic N,N-dialkyltryptamines substituted in the benzene moiety.
2-(Aminomethyl)phenols, a new class of saluretic agents. 6. Effects of N,O-spiroannulation and subsequent quaternization.
Antimycotic azoles. 6. Synthesis and antifungal properties of terconazole, a novel triazole ketal.
Synthesis, benzodiazepine receptor binding, and anticonvulsant activity of 2,3-dihydro-3-oxo-5H-pyrido[3,4-b][1,4]benzothiazine-4-carbonitriles.
2-(6-carboxyhexyl)cyclopentanone hexylhydrazone. A potent and time-dependent inhibitor of platelet aggregation.
6-Chloro-2,3,4,5-tetrahydro-3-methyl-1H-3-benzazepine: a potent and selective antagonist of alpha 2-adrenoceptors.
Relationship between metabolism and radioprotective activity of 2-phenylthiazolidine and its m-bromo derivative.
Aza analogues of lucanthone: synthesis and antitumor and bactericidal properties.
Different receptor sites mediate opioid agonism and antagonism.
Nonsteroidal antiinflammatory agents. 2. [(Heteroarylamino)phenyl]alkanoic acids.
Replacement of aromatic or heteroaromatic groups in nonsteroidal antiinflammatory agents with the ferrocene group.
New azacannabinoids highly active in the central nervous system.
Mannich bases of 4-phenyl-3-buten-2-one: a new class of antiherpes agent.
Inhibitors of gastric acid secretion: antisecretory 2-pyridylurea derivatives.
Effects of gonadotropin releasing hormone agonists and antagonists on reproductive functions.
Neurotransmitter receptor binding and drug discovery.
Synthesis of a biologically active fluorescent muramyl dipeptide congener.
Novel fluorinated antifolates. Enzyme inhibition and cytotoxicity studies on 2'- and 3'-fluoroaminopterin.
Synthesis and antibacterial activity of some 3-[(alkylthio)methyl]quinoxaline 1-oxide derivatives.
Optical resolution, absolute configuration, and activity of the enantiomers of proxyphylline.
O-imino esters of N,N-bis(2-chloroethyl)phosphorodiamidic acid. Synthesis, X-ray structure determination, and anticancer evaluation.
Potential antiatherosclerotic agents. 2. (Aralkylamino)- and (alkylamino) benzoic acid analogues of cetaben.
Pyrimidine and triazine 3-oxide sulfates: a new family of vasodilators.
Synthesis and biological actions of highly potent and prolonged acting biotin-labeled melanotropins.
Bispyridinamines: a new class of topical antimicrobial agents as inhibitors of dental plaque.
Synthesis and antitumor activity of tropolone derivatives.
Design and synthesis of tetrahedral intermediate analogues as potential dihydroorotase inhibitors.
Phosphorus-nitrogen compounds. 24. Phosphoramide mustard carrier derivatives.
cis-4-[[[(2-Chloroethyl)nitrosoamino]carbonyl]methylamino] cyclohexanecarboxylic acid, a nitrosourea with latent activity against an experimental solid tumor.
Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives.
Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 2. Amides.
Activity of novel aminocannabinoids in baboons.
Inhibitors of inosinic acid dehydrogenase. 2-Substituted inosinic acids.
Interactions of antitumor drugs with natural DNA: 1H NMR study of binding mode and kinetics.
Synthesis of some phosphonates with antiherpetic activity.
Mitomycin C analogues with aryl substituents on the 7-amino group.
Synthesis of a novel series of (aryloxy)propanolamines: new selective beta 2-blocking agents.
Antimycotic azoles. 7. Synthesis and antifungal properties of a series of novel triazol-3-ones.
Oxidation of sparteines by cytochrome P-450: evidence against the formation of N-oxides.
Benzisoxazolones: antimicrobial and antileukemic activity.
Improved synthesis and antitumor activity of 2-bromo-2'-deoxyadenosine.
5-(Haloalkyl)-2'-deoxyuridines: a novel type of potent antiviral nucleoside analogue.
Novel bis[1,6-dihydro-6,6-dimethyl-1,3,5-triazine-2,4-diamines] as antitrypanosomal agents.
Novel vasopressin analogues that help define a minimum effective antagonist pharmacophore.
Antihypertensive (2-aminoethyl)thiourea derivatives. 1.
Synthesis and biological activities of chloroethylurea, methylurea, and nitrosourea analogues of N-deacetylmethylthiocolchicine.
Lipophilic and hydrophilic esters of 4-acetyl-2-(2-hydroxyethyl)-5,6-bis(4-chlorophenyl)-2H-pyridazin-3-one as antihypertensive agents.
10,10-Difluoro-13-dehydroprostacyclin: a chemically and metabolically stabilized potent prostacyclin.
5-substituted 2-amino-6-phenyl-4(3H)-pyrimidinones. Antiviral- and interferon-inducing agents.
Serotonin receptor affinities of psychoactive phenalkylamine analogues.
2,4-Dihydro-6-phenyl-1H-s-triazolo[4,3-a][1,4]benzoidiazepin-1-ones with antianxiety and antidepressant activity.
Preparation and biological evaluation of 2-azaergolines.
Biological significance and therapeutic potential of prostacyclin.
8-Chloro-1-methyl-6-phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines with substituents at C-4.
Synthesis of 1,3-diazepin-2-one nucleosides as transition-state inhibitors of cytidine deaminase.
Synthetic immunostimulants derived from the bacterial cell wall.
Prevention of Ames test mutagenicity by chemical modification in a series of monoamine oxidase inhibitors
1-[Ethoxyamino)methyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2-benzoxepins: a new class of antianaphylactic agents.
6-(Phenylthio)-substituted 2,3,4,5-tetrahydro-1H-3-benzazepines, a novel class of dopamine receptor antagonists and neuroleptics.
Use of acetylacetone to prepare a prodrug of cycloserine.
3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake.
2-(Aminomethyl)phenols, a new class of saluretic agents. 1. Effects of nuclear substitution.
Soft drugs. 3. A new class of anticholinergic agents.
Synthesis of some new S-alkylated derivatives of 5-mercapto-2'-deoxyuridine as potential antiviral agents.
Synthesis of 2,4-disubstituted 6-methoxy-8-aminoquinoline analogues as potential antiparasitics.
Aporphines. 30. (-)-N(2-chloroethyl)-10,11-dihydroxynor-aporphine (chloroethylnorapomorphine), a novel irreversible dopamine receptor antagonist.
Ivermectin, a new broad-spectrum antiparasitic agent.
Neuroleptic 4-aryltetrahydropyrrolo[3,4-b]indoles.
N-(aminophenyl)oxamic acids and esters as potent, orally active antiallergy agents.
Synthesis and antiallergy activity of 4-oxo-4H-pyrido[1,2-a]thieno[2,3-d]pyrimidines.
(Phenylthio)phenylamine derivatives as potential antiinflammatory compounds
Synthesis of analogues of acetylmethadol and methadol as potential narcotic antagonists.
Folate antagonists. 19. Synthesis and antimalarial effects of 6-(arylthio)-2,4-pteridinediamines.
Syntheses of 9-acridine- and 2-phenanthridinemethanols as potential antimalarials.
Inhibition of cholesterol side-chain cleavage. 3. 22-azacholesterol analogues bearing aryl-substituted side chains.
beta-Adrenergic blocking agents. alpha- and gamma-methyl(aryloxy)propanolamines.
Synthesis and adrenoceptor affinity of some highly polar beta-substituted catecholamines.
Inhibition of thymidylate synthetase by 5-alkynyl-2'-deoxyuridylates.
(-)-4-Hydroxymorphinanones: their synthesis and analgesic activity.
Interaction of 5-ethynyl-2'-deoxyuridylate with thymidylate synthetase.
Inhibition of the renin-angiotensin system. A new approach to the therapy of hypertension.
Promotion of carbohydrate oxidation in the heart by some phenylglyoxylic acids.
Synthesis and pharmacological properties of 1,2,3,4,5,6-hexahydro-1,6-methano-2-benzazocines.
Pyrimidine acyclic nucleosides. 5-Substituted 1-[(2-aminoethoxy)methyl]uracils as candidate antivirals.
Synthesis of seleno- and thioguanine-platinum(II) complexes and their antitumor activity in mice.
Piperazinylquinoxalines with central serotoninmimetic activity.
Apyrogenic, adjuvant-active N-acetylmuramyl-dipeptides.
1-beta-D-arabinofuranosyl-1H-imidazo[4,5-c]pyridine (ara-3-deazaadenine).
Imidodisulfamides. 2. Substituted 1,2,3,4-tetrahydroisoquinolinylsulfonic imides as antagonists of slow-reacting substance of anaphylaxis.
Synthesis of 4-amino-1-beta-D-ribofuranosyl-1H-pyrrolo[2,3-b]pyridine (1-deazatubercidin) as a potential antitumor agent.
Dipole moment in relation to H2 receptor histamine antagonist activity for cimetidine analogues.
Studies on prodrugs. 5. Synthesis and antimicrobial activity of N-(oxoalkyl)norfloxacin derivatives.
In the search for new anticancer drugs. 17. Linear and cyclic polyether analogues of N,N:N',N':N'',N''-tri-1,2-ethanediylphosphoric triamide and N,N:N',N':N'',N''-tri-1,2-ethanediylphosphorothioic triamide.
Thromboxane A2 synthase inhibitors. 5-(3-Pyridylmethyl)benzofuran-2-carboxylic acids.
3,17 beta-Dihydroxy-20,21-epoxy-19-norpregna-1,3,5(10)-trienes: synthesis, rearrangement, cytotoxicity, and estrogen-receptor binding.
Chemotherapeutic approaches to the treatment of the acquired immune deficiency syndrome (AIDS).
3,4-Dihydro-2-phenyl-2H-pyrano[2,3-b]pyridines with potent antirhinovirus activity.
Carbocyclic puromycin: synthesis and inhibition of protein biosynthesis.
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 3. 7-(3,5-Disubstituted [1,1'-biphenyl]-2-yl)-3,5-dihydroxy-6-heptenoic acids and their lactone derivatives.
Thiopurine methyltransferase: structure-activity relationships for benzoic acid inhibitors and thiophenol substrates.
Interaction of monoamine oxidase B with analogues of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine derived from prodine-type analgesics.
Potential antitumor agents. 47. 3'-Methylamino analogues of amsacrine with in vivo solid tumor activity.
Biologically active derivatives of gossypol: synthesis and antimalarial activities of peri-acylated gossylic nitriles.
Synthesis and dopaminergic binding of 2-aryldopamine analogues: phenethylamines, 3-benzazepines, and 9-(aminomethyl)fluorenes.
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 2. Aminoalkyl derivatives.
Novel renin inhibitors containing analogues of statine retro-inverted at the C-termini: specificity at the P2 histidine site.
Cardiotonic agents. 1. Novel 8-aryl-substituted imidazo[1,2-a]- and -[1,5-a]pyridines and imidazo[1,5-a]pyridinones as potential positive inotropic agents.
Reactive 5'-substituted 2',5'-dideoxyuridine derivatives as potential inhibitors of nucleotide biosynthesis.
C1- and C3-methyl-substituted derivatives of 7-hydroxy-2-(di-n-propylamino)tetralin: activities at central dopamine receptors.
Synthesis and antitumor activity of N-terminal proline-containing peptide-(chloroethyl)nitrosoureas.
Synthesis and physicochemical properties of thiadiazolo[3,2-a]pyrimidinesulfonamides and thiadiazolo[3,2-a]triazinesulfonamides as candidates for topically effective carbonic anhydrase inhibitors.
Thienothiopyran-2-sulfonamides: a novel class of water-soluble carbonic anhydrase inhibitors.
Zwitterionic analogues of cimetidine as H2 receptor antagonists.
Macrolides with gastrointestinal motor stimulating activity.
(5Z)-7-(2,2-Dimethyl-4-phenyl-1,3-dioxan-cis-5-yl)heptenoi c acid: a specific thromboxane A2 receptor antagonist.
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 4. Amidines.
2-Phenylpyrroles as conformationally restricted benzamide analogues. A new class of potential antipsychotics. 2.
Syntheses and adrenergic activities of ring-fluorinated epinephrines.
Synthesis and antiviral activity of various 3'-azido analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1, HTLV-III/LAV).
N-aryl 3-halogenated azetidin-2-ones and benzocarbacephems, inhibitors of beta-lactamases.
New human renin inhibitors containing an unnatural amino acid, norstatine.
Antipicornavirus activity of substituted phenoxybenzenes and phenoxypyridines.
Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 1. Hydrazines.
Preparation and antitumor activity of 7-substituted 1,2-aziridinomitosenes.
Structure-activity relationship of novel oligopeptide antiviral and antitumor agents related to netropsin and distamycin.
3-Pyrroline N-oxide bis(carbamate) tumor inhibitors as analogues of indicine N-oxide.
Synthesis and antiarrhythmic activity of novel 3-alkyl-1-[omega-[4-[(alkylsulfonyl)amino]phenyl]-omega- hydroxyalkyl]-1H-imidazolium salts and related compounds. 2.
Synthesis and evaluation of mono-, di-, and trifluoroethenyl-GABA derivatives as GABA-T inhibitors.
Antiradiation compounds. 20. 1-Methylquinolinium(and pyridinium)-2-dithioacetic acid derivatives.
Diketopiperazines as a new class of platelet-activating factor inhibitors.
N6-(2,2-diphenylethyl)adenosine, a novel adenosine receptor agonist with antipsychotic-like activity.
Stereospecificity in allergic contact dermatitis to simple substituted methylene lactone derivatives.
Central serotonin receptors as targets for drug research.
2-Phenylindoles. Effect of N-benzylation on estrogen receptor affinity, estrogenic properties, and mammary tumor inhibiting activity.
Structure-activity studies of 5-[[4-(4,5-dihydro-2-oxazolyl) phenoxy]alkyl]-3-methylisoxazoles: inhibitors of picornavirus uncoating.
1H NMR study of degradation mechanisms of oxacephem derivatives with various 3'-substituents in alkaline solution.
Rational design of 4-[(methylsulfonyl)amino]benzamides as class III antiarrhythmic agents.
Long-acting angiotensin II inhibitors containing hexafluorovaline in position 8.
An interdisciplinary approach to the design of new structures active at the beta-adrenergic receptor. Aliphatic oxime ether derivatives.
Mineralocorticoid properties of potential metabolites of 18-hydroxydeoxycorticosterone and 18-hydroxyprogesterone.
Tetracyclic pyridazines as potential psychopharmacological agents.
Synthesis and antitumor activity of tropolone derivatives. 2.
Metabolism of phencyclidine. The role of the carbinolamine intermediate in the formation of lactam and amino acid metabolites of nitrogen heterocycles.
N6-cycloalkyladenosines. Potent, A1-selective adenosine agonists.
Synthesis and antitumor activity of a series of ftorafur analogues: the effect of varying electronegativity at the 1'-position.
Synthesis and evaluation of N,N'-bis(arylsulfonyl)hydrazines as antineoplastic agents.
Structure-activity relationship in PAF-acether. 2. rac-1-O-Octadecyl-2-O-acetyl-3-O-[gamma-(dimethylamino)propyl]glycerol .
Angiotensin converting enzyme inhibitors: 1,5-benzothiazepine derivatives.
N-[[(Mercaptoacetyl)amino]benzoyl]glycines as mucolytic agents.
Substituent effects on the bioactivation of 2-(N-hydroxyacetamido)fluorenes by N-arylhydroxamic acid N,O-acyltransferase.
1,2,4-Triazolo[4,3-a]quinoxaline-1,4-diones as antiallergic agents.
On the significance of clusters in the graphical display of structure-activity data.
(1-Amino-2-propenyl) phosphonic acid, an inhibitor of alanine racemase and D-alanine:D-alanine ligase.
5-(1-piperazinyl)-1H-1,2,4-triazol-3-amines as antihypertensive agents.
Studies on prodrugs. 11. Synthesis and antimicrobial activity of N-[(4-methyl-5-methylene-2-oxo-1,3-dioxolan-4-yl)oxy]norfloxacin .
New sensitizers for photodynamic therapy: controlled synthesis of purpurins and their effect on normal tissue.
Synthesis and biological evaluation of [125I]- and [123I]-4-iododexetimide, a potent muscarinic cholinergic receptor antagonist.
2-Haloaporphines as potent dopamine agonists.
N1-alkyl-substituted derivatives of chlorpropamide as inhibitors of aldehyde dehydrogenase.
Novel indolecarboxamidotetrazoles as potential antiallergy agents.
Mono and bis(bioreductive) alkylating agents: synthesis and antitumor activities in a B16 melanoma model.
Replacement of the 3'-CH group by nitrogen in the carbocyclic analogue of thymidine.
(3-Amino-2-oxoalkyl)phosphonic acids and their analogues as novel inhibitors of D-alanine:D-alanine ligase.
A potent, tissue-selective, synthetic inhibitor of HMG-CoA reductase.
Iodoaryl analogues of dioctanoylglycerol and 1-oleoyl-2-acetylglycerol as probes for protein kinase C.
Polyfluoro 1,3-diketones as systemic insecticides.
Bifunctional antitumor compounds: synthesis and characterization of a Au(III)-streptonigrin complex with thiol-modulating properties.
A carboxy-terminus truncated analogue of angiotensin II, [Sar1]angiotensin II-(1-7)-amide, provides an entry to a new class of angiotensin II antagonists.
Hybrid cholecystokinin (CCK) antagonists: new implications in the design and modification of CCK antagonists.
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses.
Variation in the aromatic ring of cromakalim: antihypertensive activity of pyranopyridines and 6-alkyl-2H-1-benzopyrans.
Resolved pyrrolidine, piperidine, and perhydroazepine analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
Structure-based, C2 symmetric inhibitors of HIV protease.
Expedient synthesis and biochemical properties of an [125I]-labeled analogue of glyburide, a radioligand for ATP-inhibited potassium channels.
Cyclization-activated prodrugs. Basic esters of 5-bromo-2'-deoxyuridine.
NMR studies of the conjugation of mechlorethamine with glutathione.
The synthesis and antibacterial activities of quinolones containing five- and six-membered heterocyclic substituents at the 7-position.
Potent and highly selective neurokinin antagonists.
Antimicrobial properties of N3-(iodoacetyl)-L-2,3-diaminopropanoic acid-peptide conjugates.
(R)-4-oxo-5-phosphononorvaline: a new competitive glutamate antagonist at the NMDA receptor complex.
Aldosterone antagonists. 4. Synthesis and activities of steroidal 6,6-ethylene-15,16-methylene 17-spirolactones.
3-Hydroxy-3-methylglutaryl-coenzyme a reductase inhibitors. 7. Modification of the hexahydronaphthalene moiety of simvastatin: 5-oxygenated and 5-oxa derivatives.
3-Thienyl- and 3-furylaminobutyric acids. Synthesis and binding GABAB receptor studies.
A selective, reversible, competitive inhibitor of monoamine oxidase A containing no nitrogen, with negligible potentiation of tyramine-induced blood pressure rise.
Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high-affinity sigma ligands.
Delineating the pharmacophoric elements of huperzine A: importance of the unsaturated three-carbon bridge to its AChE inhibitory activity.
4'-Hydroxy-3-methoxyflavones with potent antipicornavirus activity.
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 6. Trans-6-[2-(substituted-1-naphthyl)ethyl(or ethenyl)]-3,4,5,6-tetrahydro-4-hydroxy-2H-pyran-2-ones.
Synthesis and in vitro activity of stereoisomers of a novel thromboxane receptor antagonist, (+-)-(5Z)-7-[3-endo-[(phenylsulfonyl)amino]bicyclo [2.2.1]hept-2-exo-yl]heptenoic acid.
Design, synthesis, and 5-lipoxygenase-inhibiting properties of 1-thio-substituted butadienes.
Analogues of 1,5-bis(4-amidinophenoxy)pentane (pentamidine) in the treatment of experimental Pneumocystis carinii pneumonia.
Hydroxyethylamine analogues of the p17/p24 substrate cleavage site are tight-binding inhibitors of HIV protease.
Antirhinovirus activity of 6-anilino-9-benzyl-2-chloro-9H-purines.
Cytotoxicity and antitumor activity of some tetrahedral bis(diphosphino)gold(I) chelates.
Phenyl selenones: alkyl transfer by selenium-carbon bond cleavage.
Naltrindole 5'-isothiocyanate: a nonequilibrium, highly selective delta opioid receptor antagonist.
The preparation of 2'-deoxy-2'-fluoro-1',2'-seconucleosides as potential antiviral agents.
Synthesis and antiallergy activity of N-[2-(dimethylamino)ethyl]-4-aryl-1-piperazinecarboxamide derivatives.
A radiotracer for mapping cholinergic neurons of the brain.
Purine derivatives as competitive inhibitors of human erythrocyte membrane phosphatidylinositol 4-kinase.
Synthesis and antiviral activity of monofluoro and difluoro analogues of pyrimidine deoxyribonucleosides against human immunodeficiency virus (HIV-1).
Synthesis and antifolate properties of 9-alkyl-10-deazaminopterins.
Antihypertensive dihydropyridines with 1,4,4-trisubstitution.
N-phenyl-2-pyridinecarbothioamides as gastric mucosal protectants.
Antihypertensive thiadiazoles. 2. Vasodilator activity of some 2-aryl-5-guanidino-1,3,4-thiadiazoles.
Protoberberine alkaloids as antimalarials.
The acylating potential of gamma-lactam antibacterials: base hydrolysis of bicyclic pyrazolidinones.
(+/-)-9-Amino-1,2,3,4-tetrahydroacridin-1-ol. A potential Alzheimer's disease therapeutic of low toxicity.
Preparation of 7-oxaaporphine derivatives and evaluation of their dopaminergic activity.
Platinum complexes with binding affinity for the estrogen receptor.
Thienylpyrazoloquinolines: potent agonists and inverse agonists to benzodiazepine receptors.
Synthesis of novel 3-substituted beta-carbolines as benzodiazepine receptor ligands: probing the benzodiazepine receptor pharmacophore.
Beta-substituted phenethylamines as high-affinity mechanism-based inhibitors of dopamine beta-hydroxylase.
Application of the message-address concept in the design of highly potent and selective non-peptide delta opioid receptor antagonists.
Cardiotonic agents. Synthesis and inotropic activity of a series of isoquinolin-3-ol derivatives.
7-Aminoquinolines. A novel class of agents active against herpesviruses.
5-Isoquinolinesulfonamide derivatives. 1. Synthesis and vasodilatory activity of N-(2-guanidinoethyl)-5-isoquinolinesulfonamide derivatives.
1',2'-seco-dideoxynucleosides as potential anti-HIV agents.
Dihydropyrimidines: novel calcium antagonists with potent and long-lasting vasodilative and antihypertensive activity.
Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives: stereoselective interactions.
Enkephalinase inhibitors. 1. 2,4-Dibenzylglutaric acid derivatives.
Synthesis of substrate-based inhibitors of HMG CoA reductase
Synthesis of 4-Amino-1-(-D-ribofuranosyl)pyrrolo[2,3-d]pyridazine; an entry into a novel series of adenosine analogs
An acyliminium ion route to and Anti phe-gly dipeptide mimetics
Synthesis of substituted 5-amino-8-phenyl-3H,6H-1,4,5a,8a-tetraazaacenaphthalen-3-ones, a new class of agents for the improvement of cognition.
The Interaction of Anhydroalditols with Sweet-Almond -glucosidase and Escherichia coli -galactosidase: implications for the design of potent glycosidase inhibitors
Synthesis and biological activity of MK 287 (L-680,573): a potent, specific and orally active paf receptor antagonist
Inhibitors of cholesterol biosynthesis. 4. trans-6-[2-(substituted-quinolinyl)ethenyl/ethyl]tetrahydro-4-hydroxy-2 H-pyran-2-ones, a novel series of HMG-CoA reductase inhibitors.
31P NMR and chloride ion kinetics of alkylating monoester phosphoramidates.
Inhibition of steroid 5-reductase by 3-nitrosteroids: synthesis, mechanism of inhibition, and in vivo activity.
(2,3)--methylenepenicillanic acid sulfone: synthesis and -lactamase inhibiting properties
A potent, simple derivative of an analog of the CC-1065 alkylation subunit
Tripyl-convergent total synthesis of a homochiral benzoindane-fused prostacyclin analog
Total synthesis of a homochiral arene-fused prostacyclin analog
Triply-convergent syntheses of two homochiral arene-fused prostacyclin analogs related to U68,215
11B NMR studies of an aryl boronic acid bound to chymotrypsin and subtilisin
Synthesis and biological evaluation of 3-amino-2-(4-chlorophenyl)1,1-difluoropropyl phosphonic acid
Synthesis and dopaminergic activity of the enantiomers of 6-methyl-4,5a,6,7,8-hexahydrothiazolo[4,5-f]quinolin-2-amine (PD 128483).
Probing the inhibition of leukotriene A4 hydrolase based on its aminopeptidase activity
Studies on quinazolinones. 3: 1 novel and efficient route to the synthesis of conformationally restricted analogues of ketanserin and SGB-1534 as antihypertensive agents
Synthesis of new disoxaril analogues with potent and selective anti-human rhinovirus 14 activity
Novel in vitro and in vivo inhibitors of prolyl endopeptidase
Antihypertensive benzopyran-related potassium channel activators: a role for lipophilicity
Synthesis and DNA binding properties of an amidine-linked and phenyl-containing analogue of distamycin A
Synthesis and biological activity of fluorinated intermediates of the methionine salvage pathway
Triply-convergent synthesis of a homochiral 3,3-dimethyl, 15-cyclohexyl prostacyclin analog
Synthesis and biological activivity of juvenele hormone analogues (JHA) for Trypanosoma cruzi
Synthesis and pharmacological evaluation of novel Amino-prostanoids: potent and orally effective thromboxane A2 receptor antagonists
Synthesis and pharmacological evaluation of combined thromboxane receptor antagonist/synthase inhibitors: pyridine-containing sulphonamido acids
Total synthesis of L-2,2-difluoro-2-deoxy-MYO-inositol 1,4,5-trisphosphate, a potent inhibitor of the enzymes of d-MYO-inositol 1,4,5-trisphosphate metabolism
A general synthesis of 4-alkyl/aryl substituted saccharins
Synthesis of chemoreversible prodrugs of ARA-C
Tricyclic quinoxalines as ligands for the strychnine-insensitive glycine site
Synthesis of (+/)1-Aza-carbocyclic-pyrimidine-2,3-dideoxynucleoside analogues as potential anti-HIV agents
Preparation and radiolabelling of CP-96,345, the first non-peptide substance P antagonist
2-aryl-1,2-dihydro-6,7-dimethoxyquinazoline-3-oxides with positive inotropic activity
Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine
Structural homologies among thromboxane (TXA2) receptor antagonists: Minimal pharmacophoric requirements for high affinity interaction with TXA2 receptors
Synthesis and evaluation of new protein-tyrosine kinase inhibitors. Part 1. pyridine-containing stilbenes and amides.
Synthesis and evaluation of new protein-tyrosine kinase inhibitors. Part 2. Phenylhydrazones.
26-Hydroxysqualene and derivatives: substrates and inhibitors for squalene epoxidase
Tubulin binding of conformationally restricted bis-aryl compounds
()-2-amino-2-thiazoline-4-ethanoic acid; a novel, specific GABAA receptor agonist
Restricted rotation analogs of decarboxylated S-adenosylmethionine as inhibitors of polyamine biosynthesis.
Synthesis of novel 1-nitrogen replaced carbocyclic thymidine analogs as potential anti aids agents
Cyclic aryl hydroxamic acids: synthesis and inhibition of 5-lipoxygenase
Evaluation of bouvardin, deoxybouvardin, and RA-I - RA-VII partial structures: reassignment of the pharmacophore
Synthesis of 9-[2,2-bis(hydroxymethyl)cycloprop-1-yl]guanine as a potential antiviral agent
Synthesis of a difluoromethylenephosphonate analogue of AZT 5'-triphosphate and its inhibition of HIV-1 reverse transcriptase
Avermectin analogs with a spacer between the aglycone and the disaccharide
Synthesis of 2-substituted-1,3,4-thiadiazole-5-sulphonamides as novel water-soluble inhibitors of carbonic anhydrase
Physical parameters for brian uptake: optimizing log P, log D and pKa of T H A
Interphenylene 7-oxabicyclo[2.2.1]heptanes. SQ33,961: a new potent, long-acting thromboxane antagonist
Structural requirements for the binding of colchicine analogs to tubulin: the role of the C-10 substituent
Synthesis and resolution of 7-fluorotryptophans
Design and synthesis of potent, selective, and orally active fluorine-containing renin inhibitors.
Carboxylic acid replacement structure-activity relationships in suosan type sweeteners. A sweet taste antagonist. 1.
Selective beta 3-adrenergic agonists of brown adipose tissue and thermogenesis. 1. [4-[2-[(2-Hydroxy-3-phenoxypropyl)amino]ethoxy]phenoxy]acetates.
Structure and molecular modeling of GABAA receptor antagonists.
Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications.
N-terminal alkylated derivatives of [D-Pro10]dynorphin A-(1-11) are highly selective for kappa-opioid receptors.
Persistent binding of fatty acyl derivatives of naltrexamine to opioid receptors.
Bis basic substituted diaminobenzobisthiazoles as potential antiarthritic agents.
Synthesis and substance P receptor binding activity of androstano[3,2-b]pyrimido[1,2-a]benzimidazoles.
Synthesis and antitumor activity of amino derivatives of pyridine-2-carboxaldehyde thiosemicarbazone.
Discovery of a novel class of orally active, non-peptide angiotensin II antagonists.
(R)-2-(3-mercapto-2(S)-methyl-1-oxo-propoxy)-3-(methylthio)propanoic acid, the first ultra-short-acting angiotensin converting enzyme inhibitor.
Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists.
Cardiotonic agents. Synthesis and cardiovascular properties of novel 2-arylbenzimidazoles and azabenzimidazoles.
Synthesis and antibacterial activity of some novel 6-methyl- and 6-propenyl-substituted carbapenems.
Hybrid cholecystokinin-A antagonists based on molecular modeling of lorglumide and L-364,718.
Intriguing structure-activity relations underlie the potent inhibition of HIV protease by norstatine-based peptides.
2-substituted 3-(aminooxy)propanamines as inhibitors of ornithine decarboxylase: synthesis and biological activity.
Bis(maltolato)oxovanadium(IV) is a potent insulin mimic.
Structure-activity relationships of a series of 2-amino-4-thiazole-containing renin inhibitors.
Probing the molecular basis of resistance to pyrimethamine by site-directed mutagenesis.
DNA-directed alkylating agents. 5. Acridinecarboxamide derivatives of (1,2-diaminoethane)dichloroplatinum(II).
Sulfonylureas: a new class of cancer chemotherapeutic agents.
5'-Azido-delta 8-THC: a novel photoaffinity label for the cannabinoid receptor.
Application of neural networks: quantitative structure-activity relationships of the derivatives of 2,4-diamino-5-(substituted-benzyl)pyrimidines as DHFR inhibitors.
Synthesis and pharmacological studies of N-substituted 6-[(2-aminoethyl)amino]-1,3-dimethyl-2,4(1H,3H)-pyrimidinediones, novel class III antiarrhythmic agents.
ATP-citrate lyase as a target for hypolipidemic intervention. Sulfoximine and 3-hydroxy-beta-lactam containing analogues of citric acid as potential tight-binding inhibitors.
Novel thiophene-, pyrrole-, furan-, and benzenecarboxamidotetrazoles as potential antiallergy agents.
Inhibition of human placental aromatase by novel homologated 19-oxiranyl and 19-thiiranyl steroids.
Quinazolinone cholecystokinin-B receptor ligands.
Synthesis, hydrolysis rates, supercomputer modeling, and antibacterial activity of bicyclic tetrahydropyridazinones.
Dexamethasone 21-(beta-isothiocyanatoethyl) thioether: a new affinity label for glucocorticoid receptors.
1,2,4-Triazolo[4,3-a]pyrazine derivatives with human renin inhibitory activity. 3.1 Synthesis and biological properties of aminodeoxystatine and difluorostatone derivatives.
Common stereospecificity of opioid and dopamine systems for N-butyrophenone prodine-like compounds.
R and S enantiomers of 11-hydroxy- and 10,11-dihydroxy-N-allylnoraporphine: synthesis and affinity for dopamine receptors in rat brain tissue.
Structure-activity studies of antitumor agents based on pyrrolo[1,2-a]benzimidazoles: new reductive alkylating DNA cleaving agents.
Design of potent linear PAF antagonists.
Synthesis and biological activity of galanthamine derivatives as acetylcholinesterase (AChE) inhibitors
Synthesis and preliminary evaluation of (+)-CBI-indole2: an enhanced functional analog of (+)-CC-1065
Pyrimido[5,4-b]indole derivatives. 1. A new class of potent and selective alpha 1 adrenoceptor ligands.
New pepstatin analogues: synthesis and pepsin inhibition.
Disubstituted tetrahydrofurans and dioxolanes and PAF antagonists.
New aza(nor)adamantanes are agonists at the newly identified serotonin 5-HT4 receptor and antagonists at the 5-HT3 receptor
Synthesis and anti-HIV activity of pyrrolo-[1,2-d]-(1,4)-benzodiazepin-6-ones
P-3A and ()-desacetamido P-3A: demonstration and Study of their effective functional cleavage of duplex DNA
Synthesis of reversed hydroxamic acids of indomethacin: dual inhibitors of cyclooxygenase and 5-lipoxygenase
-alkoxyphenol leukotriene B4 receptor antagonists
-alkoxyphenol leukotriene B4 receptor antagonists: effect of a chroman carboxylic acid.
Synthesis and anti-HIV activity of 3-deoxy-3-(N-hydroxyamino) analogues of nucleosides
Reversible modulation of serine protease activity by phosphonate esters
Imidazo[2-3-:6,5]dipyrido[3,2-b:2,3-e]-1,4-diazepines: non-nucleoside HIV-1 reverse transcriptase inhibitors with greater enzyme affinity than nevirapine
Semisynthesis and biological activity of taxol analogues: baccatin III 13-(N-benzoyl-(2R,3S)-3-(p-tolyl)isoserinate), baccatin III 13-(N-(p-toluoyl)-2R,3S)-3-phenylisoserinate), baccatin III 13-(N-benzoyl-(2R,3S)-3-(p-trifluoromethylphenyl)isoserinate), and baccatin III 13-(N-(p-trifluoromethylbenzoyl)-(2R,3S)-3-phenylisoserinate)
Design, synthesis and activity against human cytomegalovirus of non-phosphorylatable analogs of toyocamycin, sangivamycin and thiosangivamycin
Design, synthesis, and binding affinity of a nonpeptide mimic of somatostatin
Synthesis and enzymatic properties of a deoxy analog of phosphatidylinositol
Synthesis and biological activity of the platelet-activating factor antagonist ()-trans-2-(3-methoxy-4-phenylsulfonylethoxy-5-n-propylsulfonylphenyl)-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran (L-671,284) and its analogs
New potent enkephalin analogs containing trifluoromethylamino acid residues
Novel Biologically Active Taxol Analogues: Baccatin III 13-(N-(p-chlorobenzoyl)-(2R,3S)-3-phenylisoserinate) and Baccatin III 13-(N-benzoyl-(2R,3S)-3-(p-chlorophenyl)isoserinate)
Novel oxathiazinones as gastrin ligands : Unexpected preducts from the schotten-baumann reaction of arylsulphonyl chlorides with derivatives of aspartic acid
-Lactam peptides as potential inhibitors of the HIV gp120-CD4 interaction
CP-70,030 and CP-75,998: The first non-peptide antagonists of bombesin and gastrin releasing peptide
Synthesis and biological activity of nor- and homo-5,10-dideazatetrahydrofolic acid
RP 70676: A potent systematically available inhibitor of acyl-CoA:cholesterol O-acyl transferase (ACAT)
Cumindysoside A, a novel cytotoxic trisnortriterpene glucoside with a 14, 18-cycloapoeuphane-type skeleton from Dysoxylum cumingianum
Dopamine receptor binding properties of some 2,3,4,5-tetrahydro-1H-3-benzazepine-7-ols with non-aromatic substituents in the 5-position
Phosphonate derivatives of N9-benzylguanine: a new class of potent purine nucleoside phosphorylase inhibitors
Indazole as an indole bioisostere: 5-HT4 receptor antagonism.
Synthesis of chemically stable 9-substituted carbacyclin derivatives and their biological use
Preparation of synthons for the synthesis of protein kinase C inhibitors from rebeccamycin.
Total synthesis of myo-inositol-1-phosphate-4,5-pyrophosphate, a novel second messenger analogue, via myo-inositol-1-phosphate-4,5-bisphosphorothioate
Acid-catalyzed O-allylation of -hydroxy--amino acids: an entry into conformationally constrained dipeptide surrogates
Preparation of the enantiomers of the novel CA-sensitizer EMD 53 998
A partial pharmacophore for the platelet activating factor (PAF) receptor
Nucleotidic prodrugs of anti-HIV dideoxynucleosides
Synthesis of a potent, reversible inhibitor of interleukin-1 converting enzyme
Inhibitors of myo-inositol monophosphatase unrelated to the enzyme substrate
The effect of N-acyl substituents on the stability of monocyclic -lactam inhibitors of human leukocyte elastase
Synthesis and cyclooxygenase and 5-lipoxygenase inhibitory activity of some thiazolidene-4-one analogs of meclofenamic acid
Anti-allergic and anti-inflammatory actions of 2-(tetrazole-5-yl)-4-hydroxy-2-methyl-2H-1,2-benzothiazine-3-carboxanilide 1,1-dioxide
Taxol Photoaffinity Label: 7-(p-Azidobenzoyl)taxol Synthesis and Biological Evaluation
Synthesis and cytotoxicity of enantiomeric pairs of duocarmycin a and its 2-epimer
Synthesis, biochemical activity and behavioral effects of a series of 1,4,5,6-tetrahydropyrimidines as novel ligands for M1 receptors
Design and synthesis of azabicyclic muscarinic agonists incorporating an oxime ether functionality
Alzheimer's therapy: an approach to novel muscarinic ligands based upon the naturally occurring alkaloid himbacine.
Cholinergic agents: aldehyde, ketone, and oxime analogues of the muscarinic agonist UH5
Synthesis and structure-activity relationships of heterocyclic analogues of the functional M1 selective muscarinic agonist hexyloxy-TZTP
Acetylcholine-releasing agents as cognition enhancers. Structure-activity relationships of pyridinyl pendant groups on selected core structures.
Acetylcholine releasing agents as cognition activators. Chemistry and pharmacology of a series of ureas
Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methyl]piperidine hydrochloride (E2020) and related compounds
Semisynthetic modification of hygromycin A. 3. synthesis and antibacterial activity of aminocyclitol analogs.
Characterization of LY806303 as a potent and selective inhibitor of thrombin
Synthesis of stereochemically defined phosphonamidate-containing peptides: Inhibitors for the HIV-1 proteinase
Syntheses of new TXA2/PGH2-receptor antagonists and their biological properties
Syntheses of new metabolically stabilized TXA2/PGH2-receptor antagonists and their biological properties
Vinylogous hydroxamic acids: 5-lipoxygenase inhibitors
Structurally novel antiarrhythmic / antioxidant quinazolines
Biologically active heparin-like fragments with a non-glycosaminoglycan structure. Part 3 : o-alkylated-o-sulphated pentasaccharides.
CP-99,711: a non-peptide glucagon receptor antagonist
Thiol-induced crosslinking of human blood proteins: implications for tumor immunity.
Synthesis and pharmacological evaluation of nonacyclic and trisdecacyclic pyrazines related to cephalostatin
On the significance of the C-terminal primary amide in cholecystokinin
Toward developing peptidomimetics: Successful replacement of backbone amide bonds in tetrapeptide-based CCK-A receptor agonists
Biological properties of (R)-4-benzamido-5-oxopentanoic basic derivatives as CCK-antagonists
Benzolactams as non-peptide cholecystokinin receptor ligands
Selective ligands for cholecystokinin receptor subtypes CCK-A and CCK-B within a single structural class
The rational design and synthesis of non-peptide rhegnylogues of CCK-26-33 - a novel series of CCK-A selective ligands
The preparation of (perfluoroalkyl)imidazoles as nonpeptide angiotensin II receptor antagonists
The syntheses and binding affinities of tools for the study of angiotensin AT2 receptors
Peptide azoles: A new class of biologically-active dipeptide mmetics.
Low molecular weight neurokinin NK2 antagonists
Novel Y2-selective, reduced-size agonists of neuropeptide Y
A structure-affinity study of the amino acid side-chains in neurotensin : N and C terminal deletions and Ala-scan
Stable isosteres of neurotensin c-terminal pentapeptides derived by modification of the amide function
Induction of reversible protein-linked DNA breaks in human osteogenic sarcoma cells by novel cytocidal colchicine derivatives which inhibit DNA topoisomerase II in vitro: Absence of cross-resistance in a colchicine-resistant sub-clone
A new designed tumor selective daunomycin derivative
An unusual oxetane nucleoside as a potent antiviral agent
Cytotoxicity of ent-udoteatrial diacetate and its analogues
Conformationally constrained analogues of diacylglycerol (DAG). 4. Interaction of -alkylidene--lactones with protein kinase C (PK-C)
A new series of potent LTD4 antagonists in the styrylquinoline class.
4-Aminomethyl chromans: dependence of serotonin and dopamine binding upon aromatic ring substitution
A new type of cytotoxic annonaceous acetogenin: Giganin from goniothalamus giganteus
Inhibition of 2,3-oxidosqualene cyclase by N-alkylpiperidines
Kinase bypass: A new strategy for anti-HIV drug design
Differences in antiviral activities for isomers of a fluorinated cyclobutane nucleoside analog
Syntheis of TRP-VAL non-cleavable dipeptide transition state isosteres
Syntheses of Cyclopentane, Cyclohexene and Olefin Oxazoles as Thromboxane A2/Endoperoxide Receptor Antagonists
Thoromboxane A2/endoperoxide receptor antagonists: 1,3-Dioxane and 1,3-dioxolane analogs
The synthesis of novel 8a-aza-8a-homoerythromycin derivatives via the beckmann rearrangement of (9z)-erythromycin a oxime
Quinazolinones 1: design and synthesis of potent quinazolinone- containing AT1-selective angiotensin-II receptor antagonists
Trisnorsqualene methyl hydroxylamine: a potent dual inhibitor of mammalian squalene epoxidase and oxidosqualene cyclase
Protein damage caused by a synthetic enediyne core
Quinuclidine-based NK-1 antagonists I: 3-benzyloxy-1-azabicyclo[2.2.2]octanes
Thiopene systems. 15. Synthesis and antihypertensive activity of 7- (subsituted benzamido)-6-hydroxythieno[3,2,-b]pyrans as nwe potassium channel activitors
--didehydrotryptophan as a surrogate for -methyltryptophan in CCK peptoids related to CI-988.
Synthesis, biological activity and electrostatic properties of 3-[2-(dimethylamino)ethyl]-5-[(3-amino-1,2,4-thiadiazol-5-yl)methyl]-1H-indole, a novel 5-HT1D receptor agonist.
Addition of amines to methyl 3-dehydroquinate and 3-dehydroshikimate
Cyclic ether acetal platelet activating factor (PAF) receptor antagonists I: 3-pyridyl derivatives
Indolocarbazoles. 1. Total synthesis and protein kinase inhibiting characteristics of compounds related to K-252c.
Derivatives of quinuclidine as 5-HT3 receptor antagonists: influence of an additional carbonyl group on the recognition of chirality by the receptor.
Synthesis and DNA cleaving properties of hybrid molecules containing propargylic sulfones and minor groove binding lexitropsins
(2R, 4S, 5S)-1-(tetrahydro-4-hydroxy-5-methoxy-2-furanyl)thymine: a potent selective inhibitor of herpes simplex thymidine kinase
Insight into the catalytic mechanism of KDO8P synthase. Synthesis and evaluation of the isosteric phosphonate mimic of the putative cyclic intermediate
Synthesis and biological evaluation of a series of HIV-1 protease inhibitors
A concise enantioselective synthesis of rans-olefin dipeptide isosteres
Excitatory amino acid receptor atagonists: synthesis and pharmacology of 3-(carboxymethoxy)isoxazoles derived from AMPA
Synthesis of a potential photoaffinity labelling reagent for HIV-1 reverse transcriptase
Role of sulfonamide moiety in non-prostanoid txa2 receptor antagonist kt2-962 : modifications of this moiety and the resulting activities
Angiotensin II receptor antagonists containing a phenylpyridine element.
Synthesis and biological activity of sulfoximine-modified myristic acid analogues
A novel class of 1,3-oxathiolane nucleoside analogues having potent anti-HIV activity
Oxazole, thiazole, and imidazole derivatives of 2,6-di-tert-butylphenol as dual 5-lipoxygenase and cyclooxygenase inhibitors
Novel water soluble phosphate prodrugs of taxol possessing in vivo antitumor activity
1,24S-dihydroxy-26,27-cyclo-22-yne-vitamin D3: the side chain triple bond analogue of MC 903 (calcipotriol)
Synthesis and biological evaluation of MC 1357, a new 20-epi-23-oxa-1,25-dihydroxy-vitamin D3 analogue with potent non-classical effects
Metabolism and biological activity of 1,25(OH)2D2 and its metabolites in a chronic myelogenous leukemia cell line, rwleu-4
Vitamin D analogues: new regulators of cancer cell growth and differentiation
(1-Butyl-4-piperidinyl)methyl 8-amino-7-chloro-1,4-benzodioxane-5-carboxylate hydrochloride: a highly potent and selective 5-HT4 receptor antagonist derived from metoclopramide.
CC-1065 functional analogues possessing different electron-withdrawing substituents and leaving groups: synthesis, kinetics, and sequence specificity of reaction with DNA and biological evaluation.
The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.
Alkylpurines as immunopotentiating agents. Synthesis and antiviral activity of certain alkylguanines.
A tight binding inhibitor of 5-aminoimidazole ribonucleotide carboxylase.
Synthesis of (R,S)-2'-trans-7-hydroxy-2-[N-n-propyl-N-(3'-iodo-2'- propenyl)-amino]tetralin (trans-7-OH-PIPAT): a new D3 dopamine receptor ligand.
Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 1. Effect of nuclear modification on in vitro activity.
Antagonists of luteinising hormone-releasing hormone (LHRH). Progress towards non-peptide leads
Acid unit modifications of 1,2,4,5-substituted hydroxyacetophenones and the effect on in vitro and in vivo LTB4 receptor antagonism
Synthesis and vitro antibacterial activity of hygromycin a analogs modified at the C4 aryl position
1,25,28-trihydroxyvitamin D2 up-regulates renal vitamin D receptor without causing hypercalcemia
Synthetic pterocarpans with anti-HIV activity
The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists.
Derivatives of 1-hydroxy-3-aminopyrrolidin-2-one (HA-966). Partial agonists at the glycine site of the NMDA receptor
Studies toward structure-activity relationships of taxol: synthesis and cytotoxicity of taxol analogues with C-2 modified phenylisoserine side chains
Resistance of the 2,2,2-trifluoroethoxy aryl moiety to the cytochrome P-450 metabolism in rat liver microsomes
Design and synthesis of a DNA-cleaving metallopeptide
o-phenylphenols: potent and orally active leukotriene B4 receptor antagonists.
Modulation of GABAA receptor function by benz[e]indenes and phenanthrenes.
Isatin oximes - A novel series of bioavailable non-NMDA antagonists
The synthesis and biochemical evaluation of new A1 selective adenosine receptor agonists containing 6-hydrazinopurine moieties
Synthesis of myristic acid analogs with anti-HIV activity that may be resistant to metabolic processing by -oxidation
Structure-activity relationships of 6-substituted benzopyran-4-carbothioamide potassium channel openers
Synthesis and antibacterial activity of two catechol-bearing penems
-lactam derivatives from 1-H-1,2-diazepines
Synthesis and excitatory amino acid pharmacology of some novel quinoxalinediones
Substituted pyrrolidin-2-one biphenyltetrazoles as angiotensin II antagonists
N-oleoyl-1,2,3,4-tetrahydroisoquinolines as conformationally restricted inhibitors of acyl-CoA:cholesterol acyl transferase (ACAT)
Design of novel agents for the therapy of non-insulin dependent diabetes mellitus (NIDDM)
Quinazolinones 2: QSAR and in vivo characterization of AT1 selective AII antagonists
Synthesis of myo-inositol 1,2,4,5-tetrakisphosphate, a Ca2+-mobilising tetrakisphosphate with a potency similar to myo-inositol 1,4,5-trisphosphate
Fibrinogen receptor antagonists containing a gamma-lactam Gly-Asp isostere
Synthesis of 3-acetoxy-12-epoxy-25-hydroxy-cholesta-5,7-diene and 2-25-dihydroxyvitamin D3
Novel antagonists of 5-HT3 receptors. Synthesis and biological evaluation of piperazinylquinoxaline derivatives.
3-(Alkylamino)-4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as powerful inhibitors of insulin release from rat pancreatic B-cells: a new class of potassium channel openers?
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
Photoisomerization of a potent and selective adenosine A2 antagonist, (E)-1,3-Dipropyl-8-(3,4-dimethoxystyryl)-7-methylxanthine.
Synthesis and structure-activity studies of a series of [(hydroxybenzyl)amino]salicylates as inhibitors of EGF receptor-associated tyrosine kinase activity.
Competitive NMDA receptor antagonists: synthesis of -ketophosphonate-substituted piperidine carboxylic acid derivatives
Competitive NMDA receptor antagonists; (R)-4-Oxo-5-phosphononorvaline structure-activity relationships
Synthesis and anticonvulsant activity of the (+)- and ()-enantiomers of 1,2,3,4-tetrahydro-5-(2-phosphonoethyl)-3-isoquinolinecarboxylic acid, a competitive NMDA antagonist
Anticonvulsant activity of glycine-site NMDA antagonists. 1. 2-carboxyl prodrugs of 5,7-dichlorokynurenic acid
Anticonvulsant activity of glycine-site NMDA antagonists. 2. trans 2-carboxy-4-substituted tetrahydroquinolines.
Structure-activity relationships of a series of glycine antagonists related to 5,7-dichlorokynurenic acid and 3-(2-carboxy-6-chloroindol-3-yl)acetic acid
Structure-activity relationships of 2,3-benzodiazepine compounds with glutamate antagonistic action
New indole derivatives as potent and selective serotonin uptake inhibitors
L-708,474: The C5-cyclohexyl analogue of L-365,260, a selective high affinity ligand for the CCKB/gastrin receptor
Synthesis and cytotoxic activity of () octadecylphosphodithionyl-1-myo-inositol
Synthesis of ecdysteroid inhibitors of ecdysone biosynthesis. Inhibition of the C-25 hydroxylation.
Novel polyamide inducers of HL-60 cellular differentiation
Synthesis of non reducible inhibitors for trypanothione reductase from Trypanosoma cruzi.
Synthesis and pharmacologic activity of hydroxyacetophenone-substituted benzophenone/xanthone leukotriene B4 receptor antagonists
Diaryl ether/carboxylic acid derivatives of LY255283: Receptor antagonists of leukotriene B4
Synthesis and structure-activity relationships of a novel series of non-peptide AT2-selective angiotensin II receptor antagonists
Diesters of zaragozic acid A: Synthesis and biological activity
Synthesis of new derivatives of 8-OH-DPAT: Influence of substitution on the aromatic ring on the pharmacological profile
Pneumocandin antifungal lipopeptides. The phenolic hydroxyl is required for 1,3--glucan synthesis inhibition.
Benzofuran based angiotensin II antagonists related to GR117289: Part III; GR138950, a triflamide with high oral bioavailability.
Neurotensin receptor binding and antinociceptive activity for lipophilic N-amido neurotensin(913) analogs
Justicidin E: A new leukotriene biosynthesis inhibitor.
Synthesis and testing of substituted phenylthioribose analogs against Klebsiella pneumoniae
Conformationally restricted analogs of CP-99,994: synthesis of a spirocyclic amine
CGS 27830, a potent nonpeptide endothelin receptor antagonist
32-Methyl-32-oxylanosterols: dual-action inhibitors of cholesterol biosynthesis.
Modulation of leukocyte genetic expression by novel purine nucleoside analogues. A new approach to antitumor and antiviral agents.
Substituted 3-phenyltropane analogs of cocaine: synthesis, inhibition of binding at cocaine recognition sites, and positron emission tomography imaging.
Cyclic sulfolanes as novel and high affinity P2 ligands for HIV-1 protease inhibitors.
N-(1-methyl-5-indolyl)-N'-(3-pyridyl)urea hydrochloride: the first selective 5-HT1C receptor antagonist.
o-Chlorobenzenesulfonamidic derivatives of (aryloxy)propanolamines as beta-blocking/diuretic agents.
Phosphorus-containing inhibitors of endothelin converting enzyme: effects of the electronic nature of phosphorus on inhibitor potency.
6-[(aminoalkyl)amino]-substituted 7H-benzo[e]perimidin-7-ones as novel antineoplastic agents. Synthesis and biological evaluation.
Structure-activity relationships for mitomycins. Application of the distance and charge analysis method.
N-(arylalkyl)farnesylamines: new potent squalene synthetase inhibitors.
Synthesis and biological evaluation of antiplatelet 2-aminochromones.
Syntheses of 5'-substituted analogues of carbocyclic 3-deazaadenosine as potential antivirals.
2,2-Dialkylnaphthalen-1-ones as new potassium channel activators.
Design of potent, cyclic peptide bradykinin receptor antagonists from conformationally constrained linear peptides.
Peptidomimetic HIV protease inhibitors: phosphate prodrugs with improved biological activities.
Ethyl substitution at the 7 position extends the half-life of 10-hydroxycamptothecin in the presence of human serum albumin.
Inhibition of bone resorption by H+/K(+)-ATPase inhibitors.
Synthesis and squalene synthetase inhibitory activity of tripotassium 1-methyl-1-[(N-benzyl-N-farnesyl)aminoethylphosphinato]ethylphosphonate as a tethered analog of N-benzyl-N-farnesylamine-inorganic pyrophosphate ion pair
Synthesis, Biological Properties, and Structure-Activity Relationships of Quinoxaline Angiotensin II Receptor Antagonists
Isosteric replacement in a series of -substituted monophosphonate calcium antagonists
Amino acid bioisosteres: design of 2-quinolone derivatives as glycine-site N-methyl-D-aspartate receptor antagonists
A systematic evaluation of the inhibition of HIV-1 protease by its C- and N-terminal peptides
Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF antagonists.
A series of penicillin derived C2-symmetric inhibitors of HIV-1 proteinase: synthesis, mode of interaction, and structure-activity relationships.
N-(1-oxododecyl)-4 alpha,10-dimethyl-8-aza-trans-decal-3 beta-ol: a potent competitive inhibitor of 2,3-oxidosqualene cyclase.
Substituted 4,6-diaminoquinolines as inhibitors of C5a receptor binding.
Renin inhibitory pentols showing improved enteral bioavailability.
SR 46559 A and related aminopyridazines are potent muscarinic agonists with no cholinergic syndrome
Synthesis and evaluation of photoaffinity probes directed at lanosterol 14-demethylase (P-45014DM)
8-Polycycloalkyl-1,3-dipropylxanthines as potent and selective antagonists for A1-adenosine receptors.
Synthesis of a peptidyl 2,2-difluoro-3-aminopropionate
Conformationally restricted peptide isosteres. 2.1 Synthesis and in vitro potency of dipeptide renin inhibitors employing a 2-alkylsulfonyl-3-phenylcyclopropane carboxamide as a P3 amino acid replacement
Arylamides of hydroxylated isoquinolines as protein-tyrosine kinase inhibitors
A peptide-acridine conjugate with ribonucleolytic activity
Potential mechanism-based inhibitors of proteolytic enzymes
2,3:18,19-dioxidosqualene: synthesis and activity as a potent inhibitor of 2,3-oxidosqualene-lanosterol cyclase in rat liver microsomes
Enol lactone derivatives as inhibitors of human neutrophil elastase and trypsin-like proteases
Synthesis and phototoxicity of a series of haematoporphyrin analogues
Derivatives of naphthalimide: new potent conformationally restricted antagonists of 5-HT3 receptors.
Rigid analogs of acetylcholine can be m1-selective agonists: implications for a rational treatment strategy in Alzheimer's disease
Benzothiadiazine dioxides: A new class of potent angiotensin-II (AT1) receptor antagonists
Energy aspects of oil/water partition leading to the novel hydrophobic parameters for the analysis of quantitative structure-activity relationships.
Fluoronaphthyridines and -quinolones as antibacterial agents. 5. Synthesis and antimicrobial activity of chiral 1-tert-butyl-6-fluoro-7-substituted-naphthyridones.
omega-[(4-Phenyl-2-quinolyl)oxy]alkanoic acid derivatives: a new family of potent LTB4 antagonists.
2-(Aminomethyl)chromans that inhibit iron-dependent lipid peroxidation and protect against central nervous system trauma and ischemia.
Inhibition of collagenase by aranciamycin and aranciamycin derivatives.
p-(Methylsulfinyl)phenyl nitrogen mustard as a novel bioreductive prodrug selective against hypoxic tumors.
Renin inhibitors containing alpha-heteroatom amino acids as P2 residues.
The rotenoid core structure: Modifications to define the requirements of the toxophore.
Azasugar and glycal inhibitors of -L-fucosidase
Synthesis of RP-67,580, a new potent nonpeptide substance P antagonist
Conversion of NSAIDS into balanced dual inhibitors of cyclooxygenase and 5-lipoxygenase
Thromboxane receptor antagonist BMS-180291: A new pre-clinical lead
Aryl cyanoguanidine potassium channel openers
Benzopyranyl-cyanoguanidine potassium channel openers
HMG-CoA reductase inhibitors 4. Tetrazole series: conformational constraints and structural requirements at the hydrophobic domain.
Synthesis of stereoisomers of 1,4:3,6-dianhydrohexitol nitrate derivative, KF-14124
Synthesis and preliminary biological evaluation of 1-aminomethyl-4-substituted-4-H-pyrrolo[2,1-C][1,4] benzothiazines, a new class of calcium antagonists.
Substituted penta- and hexapeptides as potent inhibitors of herpes simplex virus type 2 ribonucleotide reductase
Synthesis of biological evaluation of 4-deshydroxy-4-methyl etoposide and teniposide analogs
C-linked pyrazole biaryl tetrazoles as antagonists of angiotensin II
Competitive NMDA antagonist that base their activity on a unique conformational effect
1,3,4-trisubstituted pyrrolidinones as scaffolds for construction of peptidomimetic cholecystokinin antagonists
()-7-deazacarbovir as a compound with potential anti-hiv and anti-hcmv properties
Novel stereoselective calcium channel ligands of the diphenylalkylamine-type
Substituted benzamides with conformationally restricted side chains. 4. Hetero-azabicyclo[x.y.0] derivatives as gastric prokinetic agents.
Structural analysis of 2-aryl-1,3-dione compounds as inhibitors of 5-lipoxygenase
The basis for slowly reversible inhibition of dehydroquinate synthase: a case of mistaken identity?
Synthesis of sodium salt of ortho-(difluoromethyl)phenyl--ketoside of N-acetylneuraminic acid : a mechanism-based inhibitor of Clostridium perfringens neuraminidase.
New hexahydroxydiphenyl derivatives as potent inhibitors of HIV replication in H9 lymphocytes
-Amino acid analogues as mechanism-based inactivators of -aminobutyric acid aminotransferase
A mechanism-based inactivator of E. coli -hydroxydecanoyl thiolester dehydrase designed to crosslink active site amino acids
Borinic acid inhibitors as probes of the factors involved in binding at the active sites of subtilisin carlsberg and -chymotrypsin
A new class of leukotriene biosynthesis inhibitors: The discovery of MK0591
Mechanism-based inactivation of mandelate racemase by propargylglycolate
The discovery of a novel calcium channel blocker related to the structure of potassium channel opener cromakalim
Neuropeptide Y (NPY) functional group mimetics: design, synthesis, and characterization as NPY receptor antagonists
Indazole and indoline as aromatic bioisosteres in the imidazole class of serotonin 5-HT3 receptor antagonists
Synthesis of L-chiro-inositol 1,4,6-trisphosphorothioate, a potent and selective inhibitor of myo-inositol 1,4,5-trisphosphate 5-phosphatase
HIV and reverse transcriptase inhibition by tannins
Synthesis of -(S)-acylamino-N-(hydroxydioxocyclobutenyl)--lactams as potential antibiotics
Synthesis and activities of 9-pyrrolo-9-deoxoerythromycin a analogs
Synthesis of 9-[2-(phosphonomethoxy)ethylamino]adenine and 9-[(phosphonomethoxy)acetamido]adenine, analogues of a potent anti-HIV acyclonucleotide
Pyrrole analogues of the pyrrolidinone moiety of the potassium channel activator cromakalim as relaxants of guinea pig trachealis.
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 6. The first water-soluble ACAT inhibitor with lipid-regulating activity.
Synthesis and antifungal activity of 1,3,2-benzodithiazole S-oxides.
Structure-based design of HIV protease inhibitors: 4-hydroxycoumarins and 4-hydroxy-2-pyrones as non-peptidic inhibitors.
6,7,8,9-Tetrahydro-N,N-di-n-propyl-3H-benzindol-8-amines. Derivatives as potent and orally active serotonin 5-HT1A receptor agonists.
Structure-activity relationship studies of N-sulfonyl analogs of cocaine: role of ionic interaction in cocaine binding.
Synthesis and evaluation of nicotine analogs as neuronal nicotinic acetylcholine receptor ligands.
5-Phenyl-3-ureidobenzazepin-2-ones as cholecystokinin-B receptor antagonists.
Selective cyclooxygenase inhibitors: novel 1,2-diarylcyclopentenes are potent and orally active COX-2 inhibitors.
Multisubstrate inhibition of 4-hydroxybenzoate 3-monooxygenase.
The synthesis and in vitro evaluation of a 99mtechnetium-nitroimidazole complex based on a bis(amine-phenol) ligand: comparison to BMS-181321.
Androgen receptor affinity of 5'-acyl furanosteroids.
5-(Nonyloxy)tryptamine: a novel high-affinity 5-HT1D beta serotonin receptor agonist.
Synthesis and quantitative structure-activity relationships of anticonvulsant 2,3,6-triaminopyridines.
Synthesis of new acyclic pyrimidine nucleoside analogs as potential antiviral drugs.
Synthesis and opioid activity of 7-oxygenated 2,3,4,4a,5,6,7,7a-octahydro-1H-benzofuro[3,2-e]isoquinolin-9-ols.
2-Azetidinones as inhibitors of cholesterol absorption.
Retro-binding tripeptide thrombin active-site inhibitors: discovery, synthesis, and molecular modeling.
Structure-based design of inhibitors of purine nucleoside phosphorylase. 5. 9-Deazahypoxanthines.
GABAA receptor agonists, partial agonists, and antagonists. Design and therapeutic prospects.
Synthesis and in vitro cardiovascular activity of 4-aryl-2,3,3a,4-tetrahydro-1h-pyrrolo[2,1-c][1,4]benzothiazin-1-ones and 7-acetoxy-6-phenyl-7a,8,9,10-tetrahydropyrrolo [2,1,-d][1,5]benzothiazepin-10-one.
Synthesis and biological activity of intercalator substituted bile steroids
Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon
Syntheses of new bacteriochlorins and their antitumor activity
Bisindolylmaleimide inhibitors of protein kinase C. Further conformational restriction of a tertiary amine side chain.
The synthesis of 2,2,24- trisubstituted oxetanes as new azole antifungal agents
Inhibition of oxidosqualene cyclase by substituted quinolizidines
Synthesis and pharmacological characterization of ABT-200: a putative novel antidepressant combining potent -2 antagonism with moderate NE uptake inhibition
The role of oxygen in the photoinduced antiviral activity of hypericin
Potent, acid-stable and orally active macrolide-type motilin receptor agonists, GM-611 and the derivatives
Preparative chiral HPLC separation of all possible stereoisomers of LY191704 and LY266111 and their in vitro inhibition of human types 1 and 2 steroid 5-reductases
Synthesis of -estradiol-3-benzoate-17-(succinyl-12A-tetracycline): A potential bone-seeking estrogen
Heteroaromatic Taxol Analogues: The Chemistry and Biological Activities of 3-Furyl and 3-Pyridyl Substituted Taxanes
Design and synthesis of a prototype model antagonist of tachykinin NK-2 receptor
Design and synthesis of novel muscarinic agonists containing the 1,2,4-triazine ring as an ester bioisostere
Design of a potent 5-HT4 receptor agonist with nanomolar affinity
Tyrosinase inhibitory flavonoids fromheterotheca inuloides and their structural functions
Structural basis for the differential RXR & RAR activity of stilbene retinoid analogs
The contribution to binding of the pyranoside substituents in the excised binding domain of FK-506
L-161,638: A potent AT2selective quinazolinone angiotensin II binding inhibitor
Pseudopeptide inhibitors of aminopeptidases containing the [CH(CN)NH] surrogate as a transition-state MIMIC
Isolation and structure of the symmetrical disteroidal alkaloids cephalostatin 12 and cephalostatin 13
Synthesis and biological character of 1-hydroxylated vitamin D3 Analogues
Mapping the melatonin receptor. 2. synthesis and biological activity of indole derived melatonin analogues with restricted conformations of the C-3 amidoethane side chain
Synthesis and biological activity of 14-hydroxydocetaxel
Synthesis and study of a non macrocyclic FK506 derivative.
Synthesis and structure - anti-tumor-promoting activity relationship of monogalactosyl diacylglycerols
Synthesis and in vitro antibacterial activity of new semi-synthetic noviosylcoumarin antibiotics: chemical modification at the C-3 ester
Preparation and antitumor activity of [N-alkyl-Ala2]RA-VII, antitumor cyclic hexapeptide
Macrolide-type motilin receptor agonists: Assessment of the biological value of the 2- and 4-hydroxyl groups of acid-stable 8,9-anhydroerythromycin A 6,9-hemiacetals
The synthesis and serine -lactamase inhibitory activity of some phosphonamidate analogues of dipeptides
Design and synthesis of a prototypical non-peptidic inhibitor model for the enzme renin
6-isoxazolinyl and isoxazolidinyl substituted quinazolinones as angiotensin II receptor antagonists
Synthesis and biological evaluation of the potent isoxazolidinyl angiotensin II receptor antagonist CL332,877 and its enantiomers.
Synthesis of a series of brominated 1-phenyl-2-pyridylethenes as inhibitors of the protein-tyrosine kinase p56lck
Synthesis and antiproliferative activity of 15-oxoprostaglandins: Contribution of the -chain enone group to cytotoxicity
The first synthesis of a C-9 carbonyl modified baccatin III derivative and its conversion to novel taxol and taxotere analogues
Non-peptide fibrinogen receptor antagonists. 3. design and discovery of a centrally constrained inhibitor
Analogs of the marine natural product scalaradial lacking the ,-unsaturated aldehyde: effects on human synovial fluid phospholipase A2 and macrophage lipid mediator production
Norleucine as a replacement for methionine in phosphatase-resistant linear and cyclic peptides which bind to p85 SH2 domains
Phenol based tripeptide inhibitors of ras farnesyl protein transferase
Synthesis of the potent and selective atypical -adrenergic agonist SR 59062A.
5-Aryl-, butenolide, a new class of antibacterial derived from the N-aryl oxazolidinone DUP 721
Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents
Synthesis and in vitro cytotoxicity of diastereoisomerically modified dolastatin 15 analogues
Identification and characterisation of the isomers of cyclothiazide responsible for potentiating ampa current.
Synthesis and RNA cleaving activities of polyamine derived novel artificial ribonuclease
Substituent effects of benzopyran-4-(N-cyano)-carboxamidine potassium channel openers for selectivity to guinea pig trachealis
A new approach to synthesis of vinblastine analogs. Addition of organozinc reagents to the dihydropyridinium ion generated by fragmentative coupling to catharanthine and vindoline.
Synthesis and glutamate antagonist activity of 4-phosphonoalkylquinoline derivatives: A novel class of non-NMDA antagonist
Dual metalloprotease inhibitors. III. utilization of bicyclic and monocyclic diazepinone based mercaptoacetyls
Thia-prostanoid analogs with combined thromboxane receptor antagonist/thromboxane synthase inhibitor activities. Synthesis and pharmacological evaluation
Latent leishmanicidal activity of quinazolinones and 1,2,4-triazoloquinazolinones
Antineoplastic agents 315. Isolation and structure of the marine sponge cancer cell growth inhibitor phakellistatin 5
Vasoactive eicosanoids: Synthesis of 12,20-dihydroxyeicosa-5(Z),8(Z),10(E),14(Z)-tetraenoic acid via a novel chiral bis-lactol
N-linked analogs of retinoid O-glucuronides: potential cancer chemopreventive/chemotherapeutic agents
Acyclic NK1 antagonists: Replacements for the benzhydryl group.
Argatroban analogs: Synthesis, thrombin inhibitory activity and cell permeability of aminoheterocyclic guanidine surrogates
Phenytoin derivatives as potent ligands
Dual metalloprotease inhibitors. IV. Utilization of thiazepines and thiazines as constrained peptidomimetic surrogates in mercaptoacyl dipeptides
Novel conformationally constrained HIV-1 protease inhibitors: rational design, enzyme inhibition, and X-ray structure of an enzyme-inhibtor complex
Synthesis and structure activity relationships of alkyl substituted analogues of the functional M1 selective muscarinic receptor agonist xanomeline
A comparative molecular field analysis derived model of the binding of taxol analogues to microtubules
Synthesis and anti-HCMV activity of 9-[[(ethoxyhydroxyphosphinyl)methoxy]methoxy]guanine, an isostere of PMEG monoethyl ester
Benzolactam growth hormone secretagogues: Carboxamides as replacements for the 2-tetrazole moiety of L-692,429
A new hydroxyethylamine class of HIV-1 protease inhibitors with high antiviral potency and oral bioavailability
Synthesis and anti-tumour activity of 6-methyl derivatives of flavone-8-acetic acid (FAA)
Synthesis, chemical half-life and decomposition of new N3-(substituted) derivatives of CCNU
The synthesis and evaluation of peptidyl aspartyl aldehydes as inhibitors of ice.
Synthesis and biological evaluation of new LTA4 analogs
Synthesis and Biological Evaluation of New Leukotriene Analogs.
()11-Amino-2,6-dimethyl-1,2,3,4-tetrahydro-6H-quinindolin-1-one, a novel gabaA modulator with potential anxiolytic activity
Structure-activity studies of synthetic FKBP ligands as peptidyl-prolyl isomerase inhibitors
Synthesis and structure-activity relationships of macrocyclic FKBP ligands
Design, synthesis and evaluation of dual domain FKBP ligands
4-[5-(2,3-dihydroxyphenyl)pentyloxy]-2-hydroxy-3-propylbenzoic acid (Ro 24-0553): an orally active 5-lipoxygenase inhibitor with antiinflammatory activity
Synthesis and structure-activity relationships of pyrrolidine-modified analogs of the potent cholinergic channel activator, ABT 418
Structure and synthesis of clausenaquinone-a. A novel carbazolequinone alkaloid and bioactive principle from Clausena excavata
Synthesis of new thiazinoindole derivatives and their evaluation as inhibitors of human leukocyte elastase and other related serine proteases
Conformationally constrained analogues of diacylglycerol. 9.1 the effect of side-chain orientation on the protein kinase C (PK-C) binding affinity of -lactones
Diphenylborinic acid is a strong inhibitor of serine proteases
Penazetidine A, an alkaloid inhibitor of protein kinase C
Highly water soluble taxol derivatives: 2-polyethyleneglycol esters as potential prodrugs
Ketones related to the benzoate 5-HT4 receptor antagonist RS-23597 are high affinity partial agonists
Piperidine-ether based hNK1 antagonists 1: Determination of the relative and absolute stereochemical requirements
Solid phase synthesis of trypanothione disulfide
Synthesis of etoposide phosphate, BMY-40481: A water-soluble clinically active prodrug of etoposide
Stereoselectivity of the positive inotropic effects of newer diazinone-cardiotonics
Non-peptide-based inhibitors of human immunodeficiency virus-1 protease
Synthesis and biological activity of a potent antiplatelet 7-aminofurochromone
Potent glycosidase inhibitors, N-phenyl cyclic isourea derivatives of 5-amino- and 5-amino-1-C-(hydroxymethyl)-cyclopentane-1,2,3,4-tetraols
5-Cyano-2-thiouracils and their derivatives: a new class of leishmanicides
Antineoplastic agents 323. Isolation and structure of phakellistatin 6 from a Chuuk archipelago marine sponge
Structure-activity relationships of the non-peptidyl growth hormone secretagogue L-692,429
Synthesis and sar of 2h-1,2,4-benzothiadiazine-1,1-dioxide-3- carboxylic acid derivatives as novel potent glycine antagonists of the nmda receptor-channel complex
Potent and selective inhibitors of gelatinase-A 2. carboxylic and phosphonic acid derivatives
The synthesis and evaluation of flexible analogues of the topoisomerase I inhibitor, camptothecin
Carbocyclic analogues of hydroxyethylamine containing inhibitors of HIV proteinase
Synthesis and evaluation of pyridyl analogs of L-735,524: Potent HIV-1 protease inhibitors
Total synthesis of a novel benz[A]anthracycline analog of the antitumor agent 4-demethoxydaunorubicin
Potent triazolinone-based angiotensin II receptor antagonists with equivalent affinity for both the AT1 and AT2 subtypes
Synthesis and biological properties of a new series of anti-MRSA -lactams; 2-(thiazol-2-ylthio)carbapenems
The design of dipeptide helical mimetics: the synthesis and biological activity of trisubstituted indanes
Design and synthesis of new leads for PKC bisubstrate inhibitors.
Structure activity of topoisomerase i poisons related to hoechst 33342
Structural optimization of alkyl-substituted 2-(7-5H-[1]benzopyrano[2,3-b]pyridyl)propionic acid as anti-inflammatory agents
Non-peptidic inhibitors of neutral endopeptidase 24.11 2. Design and pharmacology of orally active phosphonate prodrugs
AT1 selective angiotensin II antagonists with phenoxyphenylacetic acid as a biphenyl replacement part I
Thiophene derivatives as extremely high affinity P3 ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors
The effect of fluorine substitution on the haemotoxicity of Primaquine
Synthesis of FK506-Cyclosporin hybrid macrocycles
Dichotomin A, a new cyclic hexapeptide from Stellaria dichotoma L. var. lanceolata Bge
Inhibitors of acyl-coa:cholesterol acyltransferase (ACAT). 15. sulfonylurea inhibitors with excellent hypocholesterolemic activity in vivo.
Diaryl indenes and benzofurans: Novel classes of potent and selective cyclooxygenase-2 inhibitors
5-cyano-1-[3-(N-methylpyrrolidin-2R-ylmethyl)indol-5-yl] benzimidazole (CP-161,242): A potent, centrally active 5-HT1D receptor agonist and benzodiazepine partial agonist
The discovery of a novel and potent benzodiazepine receptor pharmacophore
Further structure-activity-relationship studies on A/C/D-ring analogs of complement inhibitor K-76
Inhibition of matrix metalloproteinases by N-carboxyalkyl dipeptides: Enhanced potency and selectivity with substituted P1 homophenylalanines
The synthesis of pyrazolo[4,3-c]- and imidazo[4,5-c]-Aryl[e]fused pyridines as structural analogues of 4-aminonicotinoates
Methanodibenzosuberylpiperazines as potent multidrug resistance reversal agents
Kelatorphan and related analogs: potent and selective inhibitors of leukotriene A4 hydrolase
Deoxypseudophrynaminol: a novel antibacterial alkaloid
N-substituted glycines as replacements for proline in tripeptide aldehyde thrombin inhibitors
Synthesis and structure-activity relationships of the novel homopropargylamine antimycotics.
Mechanism-based design, synthesis, and in vitro antimalarial testing of new 4-methylated trioxanes structurally related to artemisinin: the importance of a carbon-centered radical for antimalarial activity.
Articulating a pharmacophore driven synthetic strategy: Discovery of a potent substance P antagonist
A novel 3-substituted benzazepinone growth hormone secretagogue (L-692,429).
Antiinflammatory 4,5-diarylpyrroles: synthesis and QSAR.
Novel isoxazoles which interact with brain cholinergic channel receptors have intrinsic cognitive enhancing and anxiolytic activities.
Structure-activity relationships involving the catechol subunit of rolipram
Preparation of a novel series of phosphonate norstatine renin inhibitors
Novel non-squalenoid photoaffinity labels for mammalian squalene epoxidase
Vasorelaxant activity of 2-fluoromethylbenzopyran K+ channel openers
-Ketothiazole inhibitors of prolyl endopeptidase
Synthesis of new oligosaccharidyl-thio--cyclodextrins (CDS): a novel family of potent drug-targetting vectors.
Synthesis and serotonergic activity of benzofuran and dihydrogenzofuran analogues of 5-carboxamidotryptamine.
Adamantane and Nipecotic Acid Derivatives as Novel -Turn Mimics
Aminophosphonic acid containing inhibitors of human collagenase: modification of the P1 residue
Design and synthesis of 6-fluoropurine acyclonucleosides : potential prodrugs of acyclovir and ganciclovir
Synthesis of ring-a-opened isopicropodophyllins as potential DNA topoisomerase II inhibitors
Importance of parallel vectors and "hydrophobic collapse" of the aligned aromatic rings: discovery of a potent substance P antagonist.
Methionine replacements in biologically active peptides
A non-steroidal diene acid inhibitor of human type 2 stereoid 5-reductase
Synthesis and in vitro cytotoxicity of 6-vinyluridine and related compounds
Blood-brain penetration of 5-hydroxytryptamine derivatives
Two new phospholipase d inhibitors, sch 49211 and sch 49212, produced by the fungus nattrasia mangirferae
Non-peptide fibrinogen receptor antagonists. 4. Proposed three-dimensional requirements in centrally constrained inhibitors.
16-propyl derivatives of estradiol as inhibitors of 17-hydroxysteroid dehydrogenase type 1
Stereochemical approach for enzyme inhibitor design
Synthesis of 19-hydroxy docetaxel from a novel baccatin
Possible antineoplastic agents : part 14 - synthesis, activity and QSAR studies of some 1-(substituted benzenesulphonyl)-5-oxopyrrolidine-2-carboxylic acid hydrazides
Synthesis of new pyrazolo[4,3-e]1,2,4-triazolo[1,5-c] pyrimidine and 1,2,3-triazolo[4,5-e]1,2,4-triazolo[1,5-c] pyrimidine displaying potent and selective activity as A2a adenosine receptor antagonists.
Structure-activity relationships in a series of monocyclic endothelin analogues
Inhibition of steroid 5-reductase by inverted, competitive inhibitors
Orally active prodrugs of quinoline-4-carboxylic acid angiotensin II receptor antagonists
Stereospecific synthesis of a pentopyranosyl analogue of d4T monophosphate
Structure-activity relationship of novel distamycin a derivatives : synthesis and antitumor activity
Probes for narcotic receptor mediated phenomena. 19. Synthesis of (+)-4-[(alpha R)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3- methoxybenzyl]-N,N-diethylbenzamide (SNC 80): a highly selective, nonpeptide delta opioid receptor agonist.
The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential.
Synthesis and opioid receptor affinity of a series of aralkyl ethers of 6 alpha- and 6 beta-naltrexol.
Influence of amine substituents on 5-HT2A versus 5-HT2C binding of phenylalkyl- and indolylalkylamines.
Antitumor agents. 155. Synthesis and biological evaluation of 3',6,7-substituted 2-phenyl-4-quinolones as antimicrotubule agents.
Cyclopropamitosenes, novel bioreductive anticancer agents. Synthesis, electrochemistry, and biological activity of 7-substituted cyclopropamitosenes and related indolequinones.
New nonpeptide angiostensin II receptor antagonists. Synthesis, biological properties and structure-activity relationships of 3-substituted 2,6-dialkyl-4-(biphenyll)methylaminopyridine derivatives.
C-linked pyrazole biaryl tetrazoles as antagonists of angiotensin II Part II: pharmacokinetics and an efficient regioselective synthesis
5-Membered ring heterocyclic carboxylic acids as angiotensin II antagonists
Synthesis and In Vitro evaluation of fused ring heterocyle-containing angiotensin II antagonists.
Angiotensin II receptor antagonists: imidazoles and pyrroles bearing hydroxymethyl and carboxy substituents
Substituted 4H-pyrido[1,2-a]pyrimidin-4-one angiotensin II receptor antagonists.
Subtituted phenylthiophene benzoylsulfonamides with potent binding affinity to angiotensin II AT1 and AT2 receptors
Valsartan, a potent, orally active angiotensin II antagonist developed from the structurally new amino acid series
Chiral recognition of the angiotensin II (AT1) receptor by a highly potent phenoxyproline octanoamide
Potent imidazole angiotensinII antagonists: acyl sulfonamides and acyl sulfamides as tetrazole replacements
A new class of balanced AT1/AT2 angiotensin II antagonists: quinazolinone AII antagonists with acylsulfonamide and sulfonylcarbamate acidic functionalities
A conformationally restrained series of AT1-selective angiotensin II antagonists
1H-1,2,4-triazole angiotensin II receptor antagonists: N-phenylpyridinylmethyl and N-pyridinylphenylmethyl analogs of SC-50560
Increased antiviral activity of HIV protease inhibitors of the difluorostatone type bearing (R)-valinol derivatives as novel c-termini
Benzylpenicillin methyl phosphate. A penicillin prodrug that inactivates RTEM -lactamase
Inhibition of the RTEM-1 -lactamase by boronic acids
N,N-disubstituted acetamidines as high affinity sigma receptor ligands
Peptidomimetic inhibitors of renin incorporating topographically modified isosteres spanning the P1( P3)-P1' sites
Penems containing amino acid derived substituents at C-2
Synthesis and biological activity of tetracyclic carbapenems
Synthesis and biological properties of 3-[()-2-(1,2,3-Thiadiazolyl)ethenyl]-substituted cephalosporins and related compounds: new oral cephalosporins
3-phosphono-1-carba-1-dethiacephalosporins as antibacterial agents
Synthesis and -lactamase inhibitory activity of 6-hydroxyethyl thiaclavulanic acid.
Monocyclic -lactam inhibitors of human leukocyte elastase. Stereospecific synthesis and activity of 3,4-disubstituted-2-azetidinones.
Novel conversion reaction of -lactam to -lactam. Synthesis of -lactam analogs of penam and penem antibiotics.
Cyclopentenones as potential inhibitors of penicillin sensitive enzymes
Syntheses of novel 1-aminocyclopropane-1-carboxylic acid (ACC)-containing -lactams
Synthesis and antitumor activity of a new class of pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone analogs of pyrrolo[1,4]benzodiazepines (PBDs)
Rational design for cytosolic delivery of nucleoside monphosphates : SATE and DTE as enzyme-labile transient phosphate protecting groups
Enantioselective synthesis and antielastase activity of 1,3,4-trisubstituted and 3,4-disubstituted -lactam antibiotics
Derivatives of cyclosporin at position 2 as probes for cyclophilin
Design and synthesis of achiral 5-lipoxygenase inhibitors employing the cyclobutyl group
Synthesis and anti-arthritic activity of a series of 1-aryl-3-dimethylamino-1,4-dihydroisoquinolines
Synthesis and antiviral activity of 9-(phosphonoalkylnyloxy)purines: Novel acyclonucleotides
m-Alkyl, ,,-trifluoroacetophenones: A new class of potent transition state analog inhibitors of acetylcholinesterase
Preparation and biological evaluation of -fluoromethyl--methylene--butyrolactone and -butyrolactam
Phenylalkyl ketones as potent reversible inhibitors of interleukin-1 converting enzyme
1,4-Diacylpiperazine-2-(S)-[(N-aminoalkyl)carboxamides] as novel, potent substance P receptor antagonists.
Anilide tertiary carbinols: A new structural class of potent potassium channel openers
Dihydropyridine KATP potassium channel openers
Diol sulfonamides: A potent and novel class of inhibitors of human renin
The analgesic effect of epibatidine and isomers
Syntheses of new 3-oxa-methano-PGI1 derivatives and their biological properties
Cyclooxygenase and 5-lipoxygenase inhibitory activity of 2,6 di-t-butylphenols linked by a sulfur atom to 1,3,4-thiadiazoles and 1,3,4-oxadiazoles
N-2 methylated quaternary derivatives of -carboline-3-carboxylates inhibit acetylcholinesterase in vitro
Novel pseudosymmetric inhibitors of HIV-1 protease
EPSP synthase inhibitor deisgn III. Synthesis & evaluation of a new 5-oxamic acid analog of EPSP which incorporates a malonate ether as a 3-phosphate mimic
4-hydroxyphenoxymethylene bisphosphonic acid derivatives: potent, non-hydrolysable inhibitors of MYO-inositol monophosphatase
Restricted rotation analogs of S-adenosylmethionine: synthesis, evaluation as inhibitors of S-adenosylmethionine decarboxylase, and potential use as selective antitrypanosomal agents
Nucleosides and nucleotides. 117. A transition-state analogue in purine nucleotide biosynthesis: the design and synthesis of an imidazo[4,5-c]azepine nucleoside
Synthesis and 5-HT3 receptor agonist activity of arylureas derived from histamine.
DNA gyrase inhibitory and antibacterial activity of some flavones(1)
Synthesis of 6-amino-5-oxo-7-phenyl-1,4-oxazepines as conformationally constrained gauche () dipeptide mimetics
Preparation of the enantiomers of the analgesic E-3710.
Phenylphosphonate monoester analogs of cocaine. Potential haptens for the generation of catalytic antibodies
A facile synthesis of the novel Neurokinin A antagonist SR 48968
Synthesis and release of doxorubicin from a cephalosporin based prodrug by a -lactamase-immunoconjugate
Chemistry of the new immunosuppressant KH-1060: new synthons and x-ray evidence for unique side-chain geometry
High-purity porcine pancreatic lipase: novel effects in catalyzing hydrolysis of esters derived from bicyclo[3.2.0]hept-2-EN-6-OLS
1,3- And 1,5-bisbiphenylyl substituted 3-metcaptotriazoles as angiotensin II receptor antagonists
Screening chemically synthesized peptide libraries for biologically-relevant molecules
Study of stereo-requirements of substance P binding to NK1 receptors using analogues with systematic D-amino acid replacements
Identification of antibody mimotopes containing non-natural amino acids by recombinant and synthetic peptide library affinity selection methods
Novel dimeric penicillin derived inhibitors of HIV-1 proteinase: interaction with the catalytic aspartates
Biological activity of 3-aminopropyl (methyl) phosphinic acid, a potent and selective GABAB agonist with CNS activity
Endothelin receptor ligands. replacement net approach to SAR determination of potent hexapeptides
Janus compounds: dual inhibitors of proteinases
Preparation and in vitro biological evaluation of the enantiomers of the diydropyridine BMY 20014, a combination calcium and 1-adrenoreceptor antagonist
Synthesis of ingenol analogs wth affinity for protein kinase C
Centaureidin, a cytotoxic flavone from Polymnia fruticosa, inhibits tubulin polymerization
Aromatic isosteres as conformational probes for an isoprenyl subunit: application to inhibitors of squalene synthase
Synthesis of 5-glycosylamino pyrimidines. A new class of compounds with potential anti-aids activity
Preparation and evaluation of the antiaggregating and vasodilating activities of the novel 3-nitro-4(3H)-quinazolinone derivatives
Design of potent K+ channel openers by pharmacophore model
Diastereoselective synthesis of cyclopropyl phenylalanines and their incorporation into dipeptides
Synthesis, anti-human immunodeficiency virus, and anti-hepatitis B virus activity of pyrimidine oxathiolane nucleosides
A convergent synthesis of 4-(2-benzothiazoyl)piperidines with antihistamic activity
3-hydroxy-3-cyclobutene-1,2-dione: Application of novel carboxylic acid bioisostere to an in-vivo active non-tetrazole angiotensin-II antagonist
The design of a dipeptide library for screening at peptide receptor sites
Protection of the peptide bond against -chymotrypsin by the prodrug approach
Gem-cycloalkyl substituted thiol inhibitors of neutral endopeptidase 24.11. Synthesis via nucleophilic opening of 2,2-spiro--lactones
A new approach to enhance bioavailability of biologically active peptides: conjugation of a opioid agonist to -cyclodextrin
1H-1,2,4-triazole angiostensin II receptor antagonists: qC-linkedq analogs of SC-50560
Triazolinones as nonpeptide angiotensin II antagonists. 2. discovery of a potent and orally active triazolinone acylsulfonamide
New non-peptide angiotensin II receptor antagonists. 1: structure - activity relationships of a series of a series of 2(1H)-pyridinones.
The isolation and in vivo Potent Antitumor activity of clerodane diterpenoid from the oleoresin of the brazilian medicinal plant, copaifera langsdorfi desfon.
Isolation and structure of axinastatin 5 from a republic of comoros marine sponge
Acceptor analogues as potential inhibitors of bovine -1,4-galactosyl transferase
1,1-diphenyl-3-dialkylamino-1-silacyclopentane derivatives: A new class of potent and selective 5-HT2A antagonists
Analogs of UK 14,304 as 2-adrenoceptor agonists. Twist and agent polarity as design elements.
The discovery of L-699,392, a novel potent and orally active leukotriene D4 receptor antagonist
Novel cytotoxic annonaceous acetogenins: (2,4-cis and trans)-bulladecinones from annona bullata (annonaceae)
Structure-activity relationships of taxol: synthesis and biological evaluation of C2 taxol analogs
8-chlorodibenz[b,f][1,4]oxazepine-10(11H)-carboxylic acid,2-[3-[2-(furanylmethyl)thio]-1-oxopropyl]hydrazide (SC-51322): A potent PGE2 antagonist and analgesic
The effect of heteroatom substitution on a series of phosphonate inhibitors of neutral endopeptidase 24.11
1,2,5,6-tetrahydropyridine oxime ethers incorporating electron withdrawing groups are potent and selective muscarinic agonists
Isoarecolones and arecolones: selective central nicotinic agonists that cross the blood-brain barrier
Design, structure activity and x-ray crystallographic studies of pseudosymmetrical nonpeptidyl HIV-1 protease inhibitors
3,4-Di-o-()-camphanoyl-(+)-ciskhellactone and related compounds: A. new class of potent anti-HIV agents
Anti-solid tumor efficacy and preparation of N-[[1-[[2-(diethylamino)ethyl]amino]-9-oxo-9H-thioxanthen-4-yl]methyl]methanesulfonamide (win 33377) and related derivatives
Synthesis and in vitro gastrointestinal motility enhancing activity of 3-aryl-2-imidazolidinylidene propanedinitrile derivatives
Synthesis of the benzofuran analogue of ILV, a new protein kinase C (PKC) activator
Synthesis of C2-symmetric inhibitors of the HIV-1 protease, with N,N-substituted ethylenediamide and ethylenediamine linkers.
Ca2+-ATPase inhibitory activity of a locked analogue of thapsigargin
Structurally simplified squalestatins: monocyclic 1,3-dioxane analogues.
Synthesis of RPR 100893, prototype of a new series of potent and selective non peptide NK1 antagonists : the triarylperhydroisoindolols.
Novel HIV01 protease inhibitors containing A -hydroxy sulfide isostere.
Synthesis of B-NOR-4-AZA-5-androstane compound as 5-reductase inhibitor
Substituted 1,3-benzodioxole & 1,3-benzodithiole -2- carboxylates and their tetrazole analogs with potent binding affinity to the angiotensin II AT1 receptor
Synthesis of a novel ring contracted artemisinin derivative.
N-sulfonamides of benzopyran-related potassium channel openers: Conversion of glyburide insensitive smooth muscle relaxants to potent smooth muscle contractors
QSAR Study of ortho-phenylphenol leukotriene B4 receptor antagonists
Enantioselective synthesis of PD144723: a potent stereospecific anticonvulsant.
Synthesis of 1,2,4-triazine-(2H,4H)-3,5,-dione anticoccidial agents via palladium-catalyzed cross-coupling reactions
Evaluation of (2S,4S)/(2R,4R) and (2S,4R)/(2R,4S) 6,6-N,N-dimethyl-2-methyl-2-oxo-1,3-dioxa-4-hexadecyl-6,aza-2-phosphacyclooctane bromide as inhibitors for protein kinase C, carnitine octanoyltransferase, and carnitine palmitoyltransferase
Peptide based P21RAS farnesyl transferase inhibitors: systematic modification of the tetrapeptide CA1A2X motif
Chemical and plasma hydrolyses of a diphenyl -aminomethyl phosphonate prodrug inhibitor of neutral endopeptidase 24.11
Synthesis and in vitro cytotoxicity of 1,3-dioxolane-2-(2-ethanamine)-2-methanamine platinum(II) complexes
Imidazolidinones and pyrazolones as novel ACAT inhibitors: Chemistry and biological activity
Synthesis and anti-herpes activity of some a-ring functionalized dehydroabietane derivatives
Structure-activity relationships in the amino acid sidechain of L-692,429
The synthesis of 2,3-dihydro-4(1H)-quinazolinone angiotensin II receptor antagonists
N-alkyl quinuclidinium substance P antagonists
Synthesis and FKBP binding of small molecule mimics of the tricarbonyl region of FK506
Inhibition of myeloperoxidase release from rat polymorphonuclear leukocytes by a series of azachalcone derivatives.
Identification, synthesis, and characterization of a unique class of N-methyl-D-aspartate antagonists. The 6,11-ethanobenzo[b]quinolizinium cation.
The synthesis of N-hydroxy-N'-phenyloctanediamide and its inhibitory effect on proliferation of AXC rat prostate cancer cells.
Phenoxypropylamines: a new series of squalene synthase inhibitors.
Synthesis and activity of some antimalarial bisquinolines.
Nonpeptidic inhibitors of human leukocyte elastase. 6. Design of a potent, intratracheally active, pyridone-based trifluoromethyl ketone.
Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore.
Discovery of alpha 1a-adrenergic receptor antagonists based on the L-type Ca2+ channel antagonist niguldipine.
A-ring ortho-disubstituted aporphine derivatives as potential agonists or antagonists at serotonergic 5-HT1A receptors.
Application of 15N nuclear magnetic resonance spectroscopy to the determination of the stability of aryl nitrogen mustards.
Further evidence supporting the importance of and the restrictions on a carbon-centered radical for high antimalarial activity of 1,2,4-trioxanes like artemisinin.
Halicylindramides A-C, antifungal and cytotoxic depsipeptides from the marine sponge Halichondria cylindrata.
Pseudodipeptide inhibitors of protein farnesyltransferase.
Amino acid side chain descriptors for quantitative structure-activity relationship studies of peptide analogues.
Synthesis and ligand binding study of 3 beta-(4'-substituted phenyl)-2 beta-(heterocyclic)tropanes.
Synthesis and structure-activity relationships of analogs of 2'-deoxy-2'-(3-methoxybenzamido)adenosine, a selective inhibitor of trypanosomal glycosomal glyceraldehyde-3-phosphate dehydrogenase.
Synthesis and biology of 1D-3-deoxyphosphatidylinositol: a putative antimetabolite of phosphatidylinositol-3-phosphate and an inhibitor of cancer cell colony formation.
Development of a potent thrombin receptor ligand.
Development of a novel series of trialkoxyaryl derivatives as specific and competitive antagonists of platelet activating factor.
Convergent approach to water soluble camptothecin derivatives
Overcoming product inhibition of S-Adenosyl-L-methionine (SAM) synthetase: Preparation of SAM on the 30 mM scale
Substituted alkylpyridines as P3 ligands for the hydroxyethylpiperazine class of HIV-1 protease inhibitors: Improved pharmacokinetic profiles
Aliphatic replacements of the biphenyl moiety of the nonpeptidyl growth hormone secretagogues L-692,429 and L-692,585
Potent mammalian topoisomerase II inhibitors: 1-cyclopropyl-6,8-difluoro-1,4-dihydro-7-(2,6-dimethyl-4-pyridinyl)-4-substituted-quinolines
Synthesis of prodrugs and a mutual prodrug of chlorzoxazone and acetaminophen based on a masked benzoxazolone
The evaluation of 2- and 6-substituted carbocyclic nucleosides as building blocks for antisense oligonucleotides
Synthesis of antiparasitic licorice chalcones
Synthesis of myo-inositol-1-phosphatase inhibitors in which the phosphate group is replaced by less polar groups
Total synthesis of trehalase inhibitor salbostatin
Protein kinase C- inhibitors; structure-activity relationships in bis-indole series
The design, synthesis and evaluation of A,C,D-ring analogs of the fungal metabolite K-76 as complement inhibitors: a potential probe for the absolute stereochemistry at position 2
Novel trityl linked drug immunoconjugates for cancer therapy
The asymmetric synthesis of both enantiomers of eliprodil
Synthesis and antibacterial activity of men 10700, a new penem antibiotic
Synthesis and qsar of dequalinium analogues AS K+ channel blockers. investigations on the role of the 4-amino group
Synthesis of -helix substituted analogs of calcitonin gene-related peptide
Zn(II)-chelating inhibitors of carboxypeptidase A
Stereoselective synthesis and evaluation of all stereoisomers of Z4349, a novel and selective -opioid analgesic
Design and synthesis of an antitumor prodrug released by the reaction with sulfhydryl compounds
Inhibition of prolidase by phosphoenolpyruvate is biphasic. avoidance of endogenous-metabolite inactivation by cooperativity within an enzyme dimer
Z-()-1-azabicyclo[2.2.1]heptan-3-one, O-(3-aryl-2-propynyl) oximes as potential m1-subtype selective muscarinic agonists
5-O-Carboxymethyl piperazide derivatives of serotonin: a new class of potent and selective 5-HT1D receptor agonists
Synthesis, biological in vitro evaluation and stereoselectivity of ondansetron analogues: novel 5-HT2A receptor antagonists
6-Imino-1,3-oxazines: a new class of hepatoprotectants
Isophthalic acid derivatives: amino acid surrogates for the inhibition of HIV-1 protease
Structure-based drug design of nonpeptidic P2 substituents for HIV-1 protease inhibitors
A carotane sesquiterpene as a potent modulator of the Maxi-K channel from Arthrinium phaesospermum
-Mercaptoacyl dipeptides that inhibit angiotensin converting enzyme and neutral endopeptidase 24.11
Synthesis and anti-HIV activities of 2-deoxy-2,2-difluoro--L-ribofuranosyl-pyrimidine and -purine nucleosides
-Glucosidase inhibitors incorporating pyridinium as a glucosyl mimic
The synthesis and antibacterial activity of 2-carbolinyl-carbapenems: potent anti-MRSA/MRCNS agents
Synthesis and biological activity of Para-substituted 3-phenyl docetaxel analogs
Nitrogen transfer in E. coli glucosamine-6P synthase. Investigations using substrate and bisubstrate analogs
Simple compounds, 2-alkyl-2-amino-1,3-propanediols have potent immunosuppressive activity
Design, synthesis, and structure-activity relationships of 2-substituted-2-amino-1,3-propanediols: Discovery of a novel immunosuppressant, FTY720
Design and synthesis of heterocyclic analogues of mycophenolic acid as potential chemotherapeutic agents
The in vitro effects of three lysosomotropic detergents against three human tumor cell lines
Novel lignan derivatives as selective inhibitors of DNA topoisomerase II
Resolution and comparative anti-HIV evaluation of the enantiomers of calanolides A and B
Synthesis and pharmacological evaluation of a novel series of 5-aryl benzimidazole angiotensin II receptor antagonists
3-benzyl-quinolones: Novel, potent inhibitors of mammalian topoisomerase II
The combinatorial synthesis of a 30,752-compound library: discovery of SAR around the endothelin antagonist, FR-139,317
Synthesis and antifungal activities of optically active isomers of SM-8668
Synthesis and characterization of N-(acenaphth-5-yl)-N'-(4-methoxynaphth-1-yl)guanidine as a glutamate release inhibitor and potential anti-ischemic agent
Enzymatic cyclization of nicotinamide adenine dinucleotide phosphate (NADP)
Synthesis and pharmacological characterization of A-80426: A putative novel antidepressant combining -2 antagonism with 5-HT uptake inhibition
Bivalent indoles exhibiting serotonergic binding affinity
Sch 51048, a novel broad-spectrum orally active antifungal agent: Synthesis and preliminary structure-activity profile
Synthesis and estrogen receptor binding of fluorinated diethylstilbestrol derivatives
Non-peptidic inhibitors of neutral endopeptidase 24.11 1. Discovery and optimization of potency
Atropisomeric carbamoyl type inhibitors of pancreatic cholesterol esterase
Synthesis and biological activity of 1-alkylcarbonylmethyl analogues of YM022
Synthesis and biological activity of 5-heteroaryl benzodiazepines: analogues of YM022
Synthesis and NK-2 antagonist effect of 1,6-diphenyl-pyrazolo [3,4-d]-thiazolo[3,2-a]4H-pyrimidin-4-one
Platelet glycoprotein IIbIIIa receptor (GPIIbIIIa) antagonists derived from amidinoindoles
Catechol based inhibitors of 15-lipoxygenase
Time-dependent inactivation of steroid C17(20) lyase by 17-cyclopropyl ether-substituted steroids
DNA cleavage of novel propargylic sulfones. Enhancement of potency via intercalating interaction
Synthesis and in vitro cytotoxicity of cryptophycins and related analogs
2-cyanopyrrolidides as potent, stable inhibitors of dipeptidyl peptidase IV
Phosphoramidate derivatives of d4T with improved anti-HIV efficacy retain full activity in thymidine kinase-deficient cells
1-O-, 2-O- and 3-O--glycosyl-sn-glycerols: Structure - anti-tumor-promoting activity relationship
Deuterium isotope effects on porphobilinogen synthesis catalysed by 5-aminolaevulinic acid dehydratase
Thiophenesulfonamides as endothelin receptor antagonists
A simple synthesis of biaryl phospholipase A2 inhibitors: Probing hydrophobic effects
Some benzenesulfonamido-substituted valerophenones that are selective antagonists for the 5-HT2C receptor
Novel inhibitors of cell adhesion molecule expression
Synthesis and biological activities of [N-MeLeu5] didemnin B
Synthesis and biological properties of partially modified retro and retro-inverso pseudo peptides of arg-gly-asp (RGD)
A novel nitro-substituted seco-CI: Application as a reductively activated adept prodrug
Synthesis and biological evaluation of pyrido[2,3-b]pyrazine and pyrido[2,3-b]pyrazine-n-oxide as selective glycine antagonists
Liposome-like fucopeptides as sialyl lewis X mimetics
Nonpeptide glycoprotein IIB/IIIA inhibitors. 12. Potent and orally active centrally constrained thieno[2,3-c]pyridones
Synthesis and antibacterial, activity of 4-ureido trinems
Protein-ligand interactions. 6 nicotinic acetylcholine receptor agonist activity of isoquinoline alkaloids
Coumarin-based prodrugs 2. Synthesis and bioreversibility studies of an esterase-sensitive cyclic prodrug of dadle, an opioid peptide
Dual inhibition of angiotensin-converting enzyme and neutral endopeptidase by tricyclic benzazepinone thiols
Peptidomimetic inhibitors of herpes virus ribonucleotide reductase. Correlation between herpes simplex and varicella zoster virus
Pyrrolylquinoxalinediones: A new class of AMPA receptor antagonists
Small peptidic aldehyde inhibitors of human rhinovirus 3C protease
Potent cyclic urea HIV protease inhibitors with benzofused heterocycles as P2/P2 groups
Peptide inhibitors of IKB protease: Modification of the C-termini of Z-LLF-CHO
Asiaticoside mimetics as wound healing agent
Synthesis and structure-activity relationships of 9-substituted acridines as endothelin-A receptor antagonists
6-(4-Phenyl-benzyloxy-methyl) guvacine. Synthesis, GABA uptake inhibitor and muscarinic properties
Solid-phase synthesis of peptidosulfonamide containing peptides derived from Leu-enkephalin
Discovery of antirhinoviral leads by screening a combinatorial library of ureas prepared using covalent scavengers
Benzolactam growth hormone secretagogues: Replacement of the C-3 amide bond in L-692,429
Irreversible inhibitions of serine proteases by peptidyl allylic halide derivatives
Synthesis and biological activity of the neuronal calcium channel blocker 2-amino-1-(2,5-dimethoxyphenyl)-5-trifluoromethyl benzimidazole (NS-649)
Phosphonic acid and phosphinic acid tripeptides as inhibitors of glutathionylspermidine synthetase
Synthesis of ()-10,10-dimethylhuperzine A a huperzine analogue possessing a slower enzyme off-rate
Serotoninergic 5-HT3 and 5-HT4 receptor activities of dihydrobenzofuran carboxylic acid derivatives
A non-peptide ligand for the somatostatin receptor having a benzodiazepinone structure
Synthesis and analgesic activity of Epibatidine analogues
Benzylphosphonic acid inhibitors of human prostatic acid phosphatase
Phosphinic acid inhibitors of matrix metalloproteinases
Design, synthesis and in vitro activities of a series of benzimidazole/benzoxazole glycoprotein IIb/IIIa inhibitors
Synthesis and characterization of the second cysteine-rich region of mouse skin PKCGh
Synthesis of pyridinone ribonucleoside 3-O-phosphoramidites and their incorporation into oligoribonucleotides
Potent matrix metalloproteinase inhibitors: Amino-carboxylate compounds containing modifications of the P1 residue
Design, synthesis and X-ray crystallographic studies of [7.3.1] and [8.3.1] macrocyclic FKBP-12 ligands
The effect of fluorine substitution on the antimalarial activity of tebuquine
1-Hydroxy-1,4-dihydroquinoxaline-2,3-diones: Novel antagonists at NMDA receptor glycine sites
(R)-3-(6-chloro-1-isopropylbenzimidazole-4-carboxamido)quinuclidine: A high affinity ligand for the (R)-zacopride binding site
A comparison of steroidal and non-steroidal inhibitors of human steroid 5-reductase: New tricyclic aryl acid inhibitors of the type-1 isozyme
3-Hydroxy-quinolin-2-ones: Inhibitors of [3H]-glycine binding to the site associated with the NMDA receptor
Synthesis and biological activity of novel tricyclic -lactams
Synthesis of a new inhibitor of -fucosidase
Benzenesulfonamide-peptide conjugates as probes for secondary binding sites near the active site of carbonic anhydrase
The antiinfluenza activity of pyrrolo[2,3-d]pyrimidines
Design, synthesis, and characterization of dipeptide isostere containing cis-epoxide for the irreversible inactivation of HIV protease
Trishomocubanes, a new class of selective and high affinity ligands for the sigma binding site
A Non-peptidic photoactivatable antagonist for mapping the antagonist binding site of the tachykinin NK2 receptor
Optimization of retro-thiorphan for inhibition of endothelin converting enzyme
Synthesis and preliminary pharmacological evaluation of analogues of caracasanamide, a hypotensive natural product
Synthesis and antitumor activity of a new class of water soluble camptothecin derivatives
Chemical synthesis, DNA cleavage and antitumor activity of molecules with (Z)-7-sulfonyl-3-hexene-1,5-diyne functionalities
Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. The synthesis and biological activity of a series of malonester amides
From indomethacin to a selective COX-2 inhibitor: Development of indolalkanoic acids as potent and selective cyclooxygenase-2 inhibitors
Synthesis and in vitro cytotoxicity of cis-(glycolato-O,O)-[2-substituted-(4R,5R)-4,5-bis(aminomethyl)-1,3-dioxolane]platinum (II)
The N4 nitrogen of pirenzepine is responsible for selective binding of the M1 subtype human muscarinic receptor
Orally active inhibitors of stromelysin-1 (MMP-3)
New aza-thioxanthones: Synthesis and cytotoxicity
The preparation and evaluation of (+/-)-trans-1-Diazo-8-methoxy-4a-methyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthren-2-one as an inhibitor of human type-1 steroid 5-reductase
Syntheses and biological properties of novel aza-podophyllotoxin analogs prossessing pronounced antitumor activity
Chemical synthesis and biological evaluation of 1d-1,2,4,5-InsP4 and its 3-fluorinated counterpart 1d-3-F-1,2,4,5-InsP4 potent 1d-1,4,5-InsP3-like calcium mobilizing analogues
Synthesis of potential -lactam antibiotics
A water soluble benzazepine cholecystokinin-B receptor antagonist
Proctolin and related N-methylated pentapeptides selectively contract locust foregut but not rat ileum
Design, synthesis and evaluation of novel bismustard cross-linked lexitropsins
A pair of new apotirucallane triterpenes, meliavolkensins A and B, from Melia volkensii (Meliaceae)
Chemoenzymatic synthesis of enantiomers of a new retinoid to investigate the role of chirality in the biological response
Relationship between cytotoxicity and DNA-binding affinity of amidine derivatives of tetrahydroquino[4,3-b][1]benzazepines and tetrahydrobenzo[k]naphthyridines
Formation of nitrogen oxides including NO from oxidative cleavage of CN(OH) bonds: A general cytochrome P450-dependent reaction.
Influence of the absolute configuration at C-4 in the binding of d-myoinositol 1,4,5 trisphosphate analogues to IP3 receptor
Synthesis and antibacterial activity of cephalosporins having C-3 catechol-containing (pyridinium-4-thio)-methyl groups
The synthesis and biological activity of enediyne minor groove binding hybrids
Photoactivatable analogues of a Substance P non-peptidic antagonist, for probing the antagonist binding site of the NK1 receptor
Mechanism-based inactivation of porphobilinogen synthase: Substitution of ketone functionality in the substrate with a thioester
Photoinduced electron transfer for pyrenesulfonamide conjugates of tryptophan-containing peptides. Mitigation of fluoroprobe behavior in N-terminal labeling experiments
The discovery of a series of new non-indole 5HT1D agonists
Synthesis and pharmacokinetics of potent carbamate HIV-1 protease inhibitors containing novel high affinity hydroxyethylamine isosteres
Piperidine-ether based hNK1 antagonists 2: Investigation of the effect of N-substitution
The effect of Pyrrolo[3,4-c]carbazole derivatives on spinal cord ChAT activity
The enantioselective synthesis and antiinflammatory activity of novel aryl-sphingolipid PKC inhibitors
CD45 protein tyrosine phosphatase: Determination of minimal peptide length for substrate recognition and synthesis of some tyrosine-based electrophiles as potential active-site directed irreversible inhibitors
Non-peptide glycoprotein IIb/IIIa inhibitors. 6. Design and synthesis of rigid, centrally constrained non-peptide fibrinogen receptor antagonists
Synthesis of the macrolide antibiotic, oxolide
Synthesis of 4-fluoroadenosine as an inhibitor of S-adenosyl-L-homocysteine hydrolase
4,4-Diphenyl-7-perhydrothiapyrano[3,4-c]pyrrolone, a new series of substance P receptors antagonists
3-Fluoro-2-(4-methylpiperazin-1-yl)-5,12-dihydro-5-oxobenzoxazolo[3,2-a]quinoline-6-carboxylic acid: Synthesis and In vitro cytotoxic activity
Synthesis and in vitro biological evaluation of new triphenylethylene platinum (II) complexes
Tetramic acids as novel glycine site antagonists
Synthesis and fungicidal activity of 2,2-bipyridine derivatives
Vasorelaxant activity of 2-fluoroalkyl-6-nitro-2H-1-benzopyran-4-carbothioamide and -carboxamide K+ channel openers
Synthesis of non-peptide bradykinin B2 receptor antagonists
Wiedendiol-A and -B, cholesteryl ester transfer protein inhibitors from the marine sponge Xestospongia wiedenmayeri
Phosphodiesterase type IV inhibition. Structure-activity relationships of 1,3-disubstituted pyrrolidines.
Benzophenone- and indolecarboxylic acids: potent type-2 specific inhibitors of human steroid 5 alpha-reductase.
Preparation of 18F-labeled muscarinic agonist with M2 selectivity.
Novel and potent adenosine 3',5'-cyclic phosphate phosphodiesterase III inhibitors: thiazolo[4,5-b][1,6]naphthyridin-2-ones.
Novel thiazole based heterocycles as inhibitors of LFA-1/ICAM-1 mediated cell adhesion.
CCK-A receptor selective antagonists derived from the CCK-A receptor selective tetrapeptide agonist Boc-Trp-Lys(Tac)-Asp-MePhe-NH2 (A-71623).
Synthesis of tight binding inhibitors and their action on the proprotein-processing enzyme furin.
Isolation and structure of the human cancer cell growth inhibitory cyclic decapeptides phakellistatins 7, 8 and 91,2
1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists
The SAR of 6-(N-alkyl-N-acyl)-2-propyl-3-[(2-tetrazol-5-yl)biphen-4-yl)methyl]-quinazolinones as balanced affinity antagonists of the human AT1 and AT2 receptors
LTD4 Receptor binding activity of novel pyridine chromanols: qualitative correlation with pKa
Linear peptide ETA antagonists: rational design and practical derivatization of N-terminal amino- and imino-carbonylated tripeptide derivatives
Discovery of substituted 8,9-dicarboxyldibenzo [2,3:5,6] bicyclo [5.2.0] nonan-4-ones with moderate binding affinity to the endothelin ETA and ETB receptors
CCKB selective receptor ligands: novel 1,3,5-trisubstituted benzazepin-2-ones
Benzothiazolylthio carbapenems: potent anti-MRSA agents
The design of polar -turn dipeptide mimetics
Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity
The synthesis and lactamase inhibitory activity of 6-(carboxymethylene)penicillins and 7-(carboxymethylene)cephalosporins
Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 1
Structure-activity relationships of tricyclic quinoxalinediones as potent antagonists for the glycine binding site of the NMDA receptor 2
Amino azoles and azolo-azines as potential hepatoprotectants: Part III
Immunosuppressive structure-activity relationships of Brequinar and related cinchoninic acid derivatives
Synthesis and pharmacological profile of FCE 28654: A water-soluble and injectable ACAT inhibitor
Specific affinity labeling of opioid receptors in rat brain by S-activated sulfhydryldihydromorphine analogs
Palladium-catalyzed synthesis of (E)-5-(2-acylvinyl)-2-deoxyuridines and their antiviral and cytotoxic activities
Inhibition of metalloproteinase by futoenone derivatives
Synthesis of a fluorescent labeled thromboxane A2 receptor antagonist
Inactivation of carboxypeptidase a by 2-benzyl-3,4-epithiobutanoic acid
Molecular modelling of inhibitors of aromatase a novel approach
Nucleosides and nucleotides. 142. an alternative synthesis of and its antiviral activity
Modifications of the MeBmt side chain of cyclosporin A
Design, synthesis and evaluation of C/D-ring analogs of the fungal metabolite K-76 as potential complement inhibitors
Design of a new selective cysteine protease inactivator and its mechanistic implications
The development of a novel series of non-peptide tachykinin NK3 receptor selective antagonists
Constrained analogs of KCVFM with improved inhibitory properties against farnesyl transferase
Putative atypical antipsychotics with mixed dopaminergic (D1, D2) and serotonergic (5HT2) activity: The design evolution of ZD3638
Aromatic amino acid phosphoramidate di- and triesters of 3-azido-3-deoxythymidine (AZT) are non-toxic inhibitors of HIV-1 replication
Rational design of irreversible, pseudo-C2-symmetric hiv-1 protease inhibitors
2-Substituted 2-aminoethanol: Minimum essential structure for immunosuppressive activity of ISP-I (Myriocin)
The in vitro cytotoxicity and DNA alkylating ability of the simplest functional analogues of the seco CC-1065 alkylating subunit
Design and synthesis of a conformationally constrained analog of the bis(heteroaryl)piperazine (BHAP) HIV-1 reverse transcriptase inhibitor atevirdine
Diastereoselective synthesis of mixanpril, an orally active dual inhibitor of neutral endopeptidase and angiotensin converting enzyme
Synthesis and biological evaluation of 14-alkoxymorphinans.12.1 A phenethyl analogue of the -selective opioid receptor antagonist cyprodime
Synthesis and in vitro profile of a novel series of catechol benzimidazoles. The discovery of potent, selective phosphodiesterase type IV inhibitors with greatly attenuated affinity for the [3H]rolipram binding site
Diastereoselective synthesis of (2S,4R)-4-Methylglutamic acid (sym 2081): A high affinity and selective ligand at the kainate subtype of glutamate receptors
Phosphodiesterase type IV (PDE IV) inhibition. Synthesis and evaluation of a series of 1,3,4-trisubstituted pyrrolidines
Novel inhibitors of cholesteryl ester transfer protein
Dioxolane cytosine nucleosides as anti-hepatitis B agents
Novel PKC inhibitory analogs of balanol with replacement of the ester functionality
Isolation and structure of the exceptional Pterobranchia human cancer inhibitors cephalostatins 16 and 171
Inhibitors of glucosidases with related structures and inverse specificity
Non-peptide neuropeptide y antagonists derived from the histamine H2 agonist arpromidine: Role of the guanidine group
Uracil-based angiotensin II receptor antagonists
Synthesis of bisindolylmaleimide macrocycles
Synthesis and antiplatelet activity of DMP 757 analogs
Chiral spirocyclic benzopyran potassium channel openers: Evidence for the active conformation of levcromakalim
Evaluation of differential hypoxic cytotoxicity and electrochemical studies of nitro 5-deazaflavins
Novel A-ring modified camptothecins as topoisomerase I inhibitors
Increasing the cellular PKC inhibitory activity of balanol: A study of ester analogs
Heteroatom effect in the PKC inhibitory activities of perhydroazepine analogs of balanol
Synthesis of L-fucopyranosyl-4-thiodisaccharides from levoglucosenone and their inhibitory activity on -L-fucosidase
Tricyclic -lactams: total synthesis and antibacterial activity of 5- and 5-methoxy-tribactams
Discovery of selective dopamine D3 ligands: I. Dimeric 2-[4-(3-aminopropoxy)phenyl]benzimidazole antagonists
Stereochemical preferences and requirement for the 3-hydroxyl group in novel anticonvulsant 4-fluorobenzoylamino benzopyrans
Synthesis and antiviral activity of dihydroxycyclohexyl pyrimidine and purine carbocyclic nucleosides
Balanced AT1 and AT2 angiotensin II antagonists. I. New orally active 5-carboxyl imidazolyl biphenyl sulfonylureas
Rational design, synthesis, and X-ray structure of renin inhibitors with extended P1 sidechains
The synthesis and biological evaluation of hypericin analogs
Inhibition of glycosidases by substituted amidines
4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridines: potent arylacetic acid-derived AT1 antagonists with improved affinity for the AT2 receptor
Chemical modification and structure-activity relationships of pyripyropenes; potent, bioavailable inhibitor of acyl-CoA: Cholesterol O-acyltransferase (ACAT)
Evaluation of substituted benzamides as P2 ligands for symmetry-based inhibitors of HIV protease
Differential RXR & RAR activity of stilbene retinoid analogs bearing thiazole and imidazole carboxylic acids
Structural Factors affecting the kinetics of O,N-acyl transfer in potential O-peptide prodrugs
Inhibition of an HIV-1 Tat-derived peptide binding to TAR RNA by aminoglycoside antibiotics
Asymmetric synthesis of FR165914: A novel 3-adrenergic agonist with a benzocycloheptene structure
Serine protease selectivity of the thrombin inhibitor D-Phe-Pro-Agmatine and its homologs
Novel substituted indolocarbazoles as potent and selective inhibitors of protein kinase C
A carbene-generating biotinylated lactosylceramide analog as novel photoreactive substrate for GM3 synthase
Substituted 2,4-diaminoquinazolines and 2,4-diamino-8-alkylpurines as antagonists of the neurokinin-2 (NK2) receptor
Ly316340: A potent HIV-1 protease inhibitor containing a high affinity octahydrothienopyridine hydroxyethylamine isostere
Potent, orally bioavailable HIV-1 protease inhibitors containing noncoded D-amino acids
3,4-diarylthiophenes are selective COX-2 inhibitors
Gamma-lactams and related compounds as cholesterol absorption inhibitors: homologs of the beta-lactam cholesterol absorption inhibitor SCH 484611
Synthesis of Nh-acyl--aminoamides on rink resin: Inhibitors of the hematopoietic protein tyrosine phosphatase (HePTP)
Synthesis and serotonin receptor binding properties of 5-substituted 3-(1,2,5,6-tetrahydropyridin-3-yl) indoles
Morphinan cyclic imines and pyrrolidines containing a constrained phenyl group: High affinity opioid agonists
Cycloproctolin and [-Methyl-l-Tyr]-proctolin are potent antagonists of proctolin-induced inositol phosphate production in locust foregut homogenates
Thromboxane modulating agents. 1. Design of 1-[(arylsulfonyl)amino] alkylindole derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists.
A bis-[N-3-(1-hydroxy-1-methyl-ethyl)-benzyl)-cyclic urea as a HIV protease inhibitor
Synthesis of new azino fused benzimidazolium salts. a new family of DNA intercalating agents. I
Oligonucleotide duplex stability controlled by the 7-substituents of 7-deazaguanine bases
Synthesis and antitumor activity of camptothecin derivatives bearing five-membered heterocycle containing 10-substituents
Phenolic replacements for cysteine in farnesyl transferase inhibitors based on CVFM
Enantiodifferentiation of dihydropyridine PAF antagonists
Enzymatic resolution and pharmacological activity of the enantiomers of 3,5-dihydroxyphenylglycine, a metabotropic glutamate receptor agonist
Synthesis and pharmacological activity of combretastatin analogues. Naphthylcombretastatins and related compounds
Synthesis and resolution of -(aminomethyl)-4-chlorobenzeneethanesulfinic acid a potent gabaB receptor ligand
Dibenzobicyclo[2.2.2.]octane angiotensin II receptor antagonists
Synthesis of biologically active 2-benzoyl paclitaxel analogues
Phosphorous acid analogs of L-680,833, a potent monocyclic -lactam inhibitor of human leukocyte elastase
Synthesis of 1,25-dihydroxy-22-thiavitamin D3 and related analogs
Inhibitors of acyl-CoA: Cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 12. Syntheses and biological activity of structurally novel tetrazole amides
Inhibitors of acyl-CoA: Cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. 13. Design, synthesis and biological evaluation of tetrazole anilides as potent inhibitors of ACAT in vitro and hypocholesterolemic agents in vivo
Inhibitors of human leukocyte elastase. 2.1 synthesis and sar of benzisothiazolinylmethyl aryl ethers
The design of potent and stable benzisothiazolone inhibitors of human leukocyte elastase
Relationship between structure and bioavailability in a series of hydroxamate based metalloprotease inhibitors
Hydroxamate inhibitors of the matrix metallo-proteinases (MMPs) containing novel P1 heteroatom based modifications
Ace inhibitors as a template for the design of bradykinin B2 receptor antagonists
Synthesis and binding affinity of 2,3,3a,4,9,9a-hexahydro-9,4-(iminomethano)-1H-benz[f]indenes. Ligands for the PCP site of the NMDA receptor
Characterization of a continuous fluorogenic assay for calpain I. Kinetic evaluation of peptide aldehydes, halomethyl ketones and (acyloxy)methyl ketones as inhibitors of the enzyme
Synthesis and biological evaluation of new arylthiophene analogs of DuP 753
and -N-[(1-benzyl-1H-imidazol-5-yl)-alkyl]-amino acids as angiotensin II AT-1 antagonists
A novel series of highly potent 5-lipoxygenase inhibitors; 2-aryldienylbenzoxazoles
Novel indolocarbazole protein kinase c inhibitors with improved biochemical and physicochemical properties
2-aryl-indolyl maleimides - novel and potent inhibitors of protein kinase C
The synthesis of 5-substituted camptothecins as potential inhibitors of DNA topoisomerase I
N-(carbobenzyloxy)isatin: A slow binding -keto lactam inhibitor of -chymotrypsin
Tricarbonyl 6 arene chromium (0) based antitumor agents
Mechanistic support for the stepwise process for inactivation of class A -lactamases by clavulanate
Molecular design of novel PGI2 agonists without PG skeleton. IV
Synthesis and bioactivities of heterocyclic lipids as PAF antagonists. 2
Active-site conformation of 17-(3-pyridyl)androsta-5,16-dien-3-ol, a potent inhibitor of the P450 enzyme C17-hydroxylase/C17-20 lyase
Acetylcholinesterase inhibition by alkaloids of the ant's venom Monomorium minutum
16,19-cis-murisolin and murisolin a, two novel bioactive mono-tetrahydrofuran annonaceous acetogenins from Asimina triloba seeds
Synthesis and structure-activity relationships of 2-(R) and (S) pyrrolidine-modified analogs of the cholinergic channel activator, ABT-418
Stereochemical differentiation of anticonvulsant and antihypertensive effects in 4-(fluorobenzoylamino)-benzopyrans
Synthesis and evaluation of diacylhydrazines as inhibitors of the interleukin-1 converting enzyme (ICE)
An attempt to synthesize prostanoid thromboxane A2 antagonists with an additional prostacyclin like quality
Novel prostanoid thromboxane A2 antagonists
Synthesis and biological evaluation of 4-heterotribactams
Sulfoquinovosyldiacylglycerol as an -glucosidase inhibitor
Quinuclidine-based NK1 antagonists, the role of the benzhydryl
(3R, 4S)-3-Benzyl-4-bromomethyloxetan-2-one, a fast acting alternate substrate inhibitor of -chymotrypsin
Stereochemistry of the benzodiazepine based Ras farnesyltransferase inhibitors
Identification of a series of 3-(benzyloxy)-1-azabicyclo[2.2.2]octane human NK1 antagonists.
Substituted 2-azaspiro[5.3]nonan-1-ones as potent cholesterol absorption inhibitors: defining a binding conformation for SCH 48461.
Novel inhibitors for multidrug resistance: 1,3,5-triazacycloheptanes.
Inhibitors of HIV-1 protease containing the novel and potent (R)-(hydroxyethyl)sulfonamide isostere.
High affinity and selectivity on 5-HT1A receptor of 1-aryl-4-[1-tetralin)alkyl]piperazines. 2.
Farnesyl derivatives of rigid carboxylic acids-inhibitors of ras-dependent cell growth.
Quantitative binding site model generation: compass applied to multiple chemotypes targeting the 5-HT1A receptor.
Inhibitors of acyl-CoA:cholesterol O-acyltransferase. 17. Structure-activity relationships of several series of compounds derived from N-chlorosulfonyl isocyanate.
Geranylgeranyl diphosphate-based inhibitors of post-translational geranylgeranylation of cellular proteins.
Complexes of HIV-1 reverse transcriptase with inhibitors of the HEPT series reveal conformational changes relevant to the design of potent non-nucleoside inhibitors.
Selective inhibitors of monoamine oxidase. 3. Structure-activity relationship of tricyclics bearing imidazoline, oxadiazole, or tetrazole groups.
Carbohydrates in an acidic multivalent assembly: nanomolar P-selectin inhibitors.
Nonlinear quantitative structure-activity relationship for the inhibition of dihydrofolate reductase by pyrimidines.
Substituted 1,2-dihydrophthalazines: potent, selective, and noncompetitive inhibitors of the AMPA receptor.
Antitumor activity of S-(p-bromobenzyl)glutathione diesters in vitro: a structure-activity study.
5- and 7-oxa trinems: their synthesis and biological evaluation
Utilization of wieland furoxan synthesis for preparation of 4-aryl-1,2,5-oxadiazole-3-yl carbamate derivatives having potent anti-HIV activity
-Vinyllysine and -vinylarginine are time-dependent inhibitors of their cognate decarboxylases
Synthesis and pharmacological profile of new 1,3-disubstituted cyclohexanes as leukotriene B4 receptor antagonists
Lipophilic bioisosteres of nucleoside triphosphates
Synthesis, biological activity and quantitative structure-activity relationships of N-substituted-3,4-dihydro-2H-1-benzopyran derivatives
Synthesis of phosphinic acid transition state analogues for the reaction catalysed by kynureninase
Identification and biological activity of novel peptidomimetic gastrin/CCK-B receptor agonists
(Hydroxyethyl) sulfonamide HIV-1 Protease inhibitors: Identification of the 2-methylbenzoyl moiety at P-2
Glycomimetic selectin inhibitors: (-D-mannopyranosyloxy)methylbiphenyls
Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation
Inhibitors of MMP-1: an examination of P1 C gem-disubstitution in the succinamide hydroxamate series
Design of MHC class II (DR4) ligands using conformationally restricted imino acids at p3 and p5
Synthesis and biological evaluation of hybrid molecules containing the pyrroloquinoline nucleus and DNA-minor groove binders
Indolizidine derivatives as potential substance P antagonists
The synthesis of a radioligand with high potency and selectivity for CCKB/ gastrin receptors
(S)-4-amino-5-chloro-3-iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (TRIZAC), a high-affinity ligand for the 5-HT-3 receptor
Application of the Heck reaction in the synthesis of truncated naphthoic acid retinoids
Synthesis and biological activity of conformationally constrained sialyl Lewis X analogues with reduced carbohydrate character
Derivatives of 2-arylcyclopropylamine: Synthesis and interactions with 5-HT1A receptors.
Synthesis and antitumor activity of 7-substituted 20(RS)-camptothecin analogues
Potent, cell active, non-thiol tetrapeptide inhibitors of farnesyltransferase.
Azole endothelin antagonists. 1. A receptor model explains an unusual structure-activity profile.
Novel imidazothioxanthones: Synthesis, DNA binding and cytotoxicity
Synthesis and antibacterial activity of new tropone-substituted phenyloxazolidinone antibacterial agents 1. Identification of leads and importance of the tropone substitution pattern
N-terminus urea-substituted chemotactic peptides: new potent agonists and antagonists toward the neutrophil fMLF receptor.
Rapid synthesis of novel dipeptide inhibitors of human collagenase and gelatinase using solid phase chemistry
A topliss tree analysis of the HIV-protease inhibitory activity of 6-phenyl-4-hydroxy-pyran-2-ones
Acylhydrazones as M1/M3 selective muscarinic agonists
Synthesis of N-kojic-amino acid and N-kojic-amino acid-kojiate and their tyrosinase inhibitory activity
SAR of 2-benzyl-4-aminopiperidines: CGP 49823, an orally and centrally active non-peptide NK1 antagonist
Synthesis and properties of 25 and 35 linked -oligoriboadenylates
-Dicarbonyls as non-charged arginine-directed affinity labels. Novel synthetic routes to -dicarbonyl analogs of the PP60c-src SH2 domain-targeted phosphopeptide Ac-Tyr(OPO3H2)-Glu-Glu-Ile-Glu
Synthesis and structure-activity relationships of benzophenones as inhibitors of cathepsin D
IRL 2500: A potent ETB selective endothelin antagonist
Novel 1,2-diarylcyclobutenes: Selective and orally active cox-2 inhibitors
Antitumor agents 171. Cytotoxicities of lobatosides B, C, D, and E, cyclic bisdesmosides isolated from Actinostemma lobatum maxim
Synthesis and evaluation of novel 1,5-Benzodiazepines as potent and selective CCK-B ligands. Effect of the substitution of the N-5 phenyl with alkyl groups
Design of dual-acting thromboxane antagonist-synthase inhibitors by a mutual prodrug approach
Novel 4,4-bis(trifluoromethyl) imidazolines as stereospecific and orally active acyl coa: Cholesterol acyltransferase (ACAT) inhibitors and antihypercholesterolemic agents
Benzopyran selective estrogen receptor modulators (SERMs): Pharmacological effects and structural correlation with raloxifene
The design, binding affinity prediction and synthesis of macrocyclic angiotensin II AT1 and AT2 receptor antagonists
Synthesis and in vitro evaluation of 3-substituted-1-azaanthraquinones
Chemical feasibility studies of a potential coumarin-based prodrug system
Asymmetric synthesis of cis-()-(2R4S)-4-(phosphonomethyl)-2-piperidinecarboxylic acid, a potent NMDA receptor antagonist
CCK-4 restricted analogues containing a 3-oxoindolizidine skeleton
Synthesis and biological evaluation of the L-enantiomer of 2-deoxy-5-ethyl-4-thiouridine
Nucleosides and nucleotides. 150. Enzymatic synthesis of 5-phosphatidyl derivatives of (CNDAC) and their notable antitumor effects in mice1
Design, synthesis, and antitumor activity of bicyclic and isomeric analogues of illudin M
(2S,3S,5R)-2-(3,5-difluorophenyl)-3,5-dimethyl-2-morpholinol: a novel antidepressant agent and selective inhibitor of norepinephrine uptake.
Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors.
Longimicins A-D: novel bioactive acetogenins from Asimina longifolia (annonaceae) and structure-activity relationships of asimicin type of annonaceous acetogenins.
The synthesis of 5-azido-UTP and UDP-pyridoxal and their effect on the carbamoyl-phosphate synthetase (CPS II) in the mammalian multienzyme polypeptide CAD
Structure-activity relationships for macrocyclic peptidomimetic inhibitors of HIV-1 protease
Design of a novel cognitive enhancer (8S, 10aS)-8-carbamoyl-1,2,3,6,7,8,9,10a-octahydro-5H,10H-pyrrolo[1,2-a][1,4]diazocin-5,10-dione
Novel phosphotyrosine mimetics in the design of peptide ligands for pp60src SH2 domain
Synthesis and antitumor activity of novel duocarmycin derivatives
Potent fluoromethyl ketone inhibitors of recombinant human calpain I
Structure-activity relationship study on N-glycosyl moieties through model building of DNA and ellipticine N-glycoside complex
Synthesis and biological activities of a novel class of azole-containing antifungal agents
Cyclic variations of SR 233377 (WIN 33377) and effects on antitumor activity
Design and synthesis of new antagonist peptides for platelet GPIIb/IIIa receptor as anti-thrombotic agents
4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2-naphthalenecarboxamides: Selective dopamine D3 receptor partial agonists
Non-peptide fibrinogen receptor antagonists based upon a 4-substituted piperidine scaffold
Non-peptide glycoprotein IIb/IIIa inhibitors. 9. Centrally constrained alpha-sulfonamides are useful tools for exploring platelet receptor function
Design, synthesis, and evaluation of fibrinogen inhibitors, -(p-amidinophenoxy) alkanoylaspartic acid derivatives
Synthesis and antiviral activity of 2-deoxy-1,5-anhydro-D-mannitol nucleosides containing a pyrimidine base moiety
Synthesis and biological evaluation of N-(1-aziridino)-6-fluoro-quinolone-3-carboxylic acids
The development of non-steroidal dual inhibitors of both human 5-reductase isozymes
On the bioactive conformation of the gaba uptake inhibitor SK&F 89976-A
Synthesis of cystamidin a (pyrrole-3-propanamide), a reported calpain inhibitor
Neuroprotective (+) 3S, 4S cannabinoids with modified 5-side chain
Antioxidant and cholesterol lowering properties of 2,6-DI-t-butyl-4-[(dimethylphenylsilyl)methyloxy]phenol and derivatives: A new class of anti-atherogenic compounds
Adipoyl-6-aminopenicillanic acid is a substrate for deacetoxycephalosporin C synthase (DAOCS)
Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitors
The role of the C-4 side chain of kainate and dihydrokainate in EAA receptor and transporter selectivity
New heteroaryl-spaced phosphono -amino acids are competitive NMDA antagonists with analgesic activity
N-Benzylated benzimidazol-2-one derivatives: activators of large-conductance Ca2+-dependent K+ channels
Anti-human immunodeficiency and anti-hepatitis B virus activities of -l-2,3-dideoxy purine nucleosides
Design, synthesis and binding affinities of novel non-peptide mimics of somatostatin/sandostatin
Synthesis and antimicrobial activity of 4-amino trinems
Thromboxane modulating agents. 2. Thromboxane receptor antagonists derived from the thromboxane synthase inhibitor dazmegrel.
Tc-99m-labeled fibrinogen receptor antagonists: design and synthesis of cyclic RGD peptides for the detection of thrombi
Potent and selective PKC inhibitory 5-membered ring analogs of balanol with replacement of the carboxamide moiety
Synthesis of divalent -D-mannopyranosylated clusters having enhanced binding affinities towards concanavalin A and pea lectins
Preparation, antimicrobial evaluation and mutagenicity of differently substituted [2-hydroxyaryl]-[1-methyl-5-nitro-1H-2-imidazolyl]methanols
8-amino-6-(arylsulphonyl)-5-nitroquinolines: novel nonpeptide neuropeptide Y1 receptor antagonists
Sildenafil (VIAGRATM), a potent and selective inhibitor of type 5 cGMP phosphodiesterase with utility for the treatment of male erectile dysfunction
DNA threading agents: effect of sidechain bulk on DNA binding and cytotoxicity of 9-anilinoacridine-4-carboxamides
Synthesis and in vitro evaluation of sugar-modified carboranyluridines
Nucleosides and nucleotides. 152. 1-(3-C-Ethynyl--D-ribo-pentofuranosyl)uracil as a broad spectrum antitumor nucleoside
Synthesis and activity of staurosporine analogs with a lactone functionality
Synthesis of C-oxetanosyl-thiazole and its carbocyclic analog nucleosides as potential chemotherapeutic agents
Synthesis, characterization, and anti-HIV activity of some 2-p-X-phenyl-1,3-N,N-diphenyl-amidines
Synthesis and acetylcholinesterase inhibitory activity of fluorinated analogues of huperzine A
Stereoselective synthesis and biological activity of cis azetidinones as cholesterol absorption inhibitors
Pentamidine congeners. 4. DNA binding affinity and anti-Pneumocystis carinii activity of butamidine analogues
A chiral recognition element with an unusual size constraint affects the potency and selectivity for peptidomimetic inhibitors of Candida albicans myristoyl-CoA:protein N-myristoyltransferase
Synthesis and biological evaluation of 4-alkoxysubstituted trinems. Part II
Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus
Stereoselective synthesis of lewis-associated trisaccharides as E-selectin inhibitors
Synthesis of constrained thiorphan analogs as inhibitors of neutral endopeptidase
Remarkable hydrolysis of phosphodiester by neutral lanthanide(III) DO3A complexes
Oreganic acid: a potent novel inhibitor of ras farnesyl-protein transferase from an endophytic fungus
Design and synthesis of a new class of conformationally constrained inhibitors to probe the active sites of thermolysine and neutral endopeptidase 24.11
Marine sponge bis(indole) alkaloids that displace ligand binding to 1 adrenergic receptors
Non thiazolidinedione antihyperglycaemic agents. 2: -Carbon substituted -phenylpropanoic acids1
Analogs of the orally active growth hormone secretagogue L-162,752
Nucleosides and nucleotides. 155. synthesis, antitumor effects, and possible enzymatic activation mechanism of 5-phosphatidyl-2-deoxy-2-methylenecytidine (DMDC)
6-Deoxy-6-hydroxymethyl scyllo-inositol 1,2,4-trisphosphate: A potent agonist at the inositol 1,4,5-trisphosphate receptor
Design and synthesis of novel, pseudo C2 symmetric inhibitors of HIV protease
Synthesis and antiviral activity of new phosphonobutoxypurines
Preparation of N-methoxycarbonyl-N-[2-nitro-4(5)-propylthiophenyl]thiourea as prodrugs of albendazole
Recognition in molecularly imprinted polymer 2-adrenoreceptor mimics
BMS-187257, a potent, selective, and novel heterocyclic 3 adrenergic receptor agonist
New class of potent ligands for the human peripheral cannabinoid receptor
2-(Aryloxymethyl) azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands
Enantio-dependence of inducer-specific bidirectional regulation of tumor necrosis factor (TNF)-alpha production: Potent TNF- production inhibitors
Novel analogs of cyclic-ADP-ribose: 9-Cyclic etheno-ADP-ribose and cyclic etheno-CDP-ribose
Thiol inhibitors of endothelin-converting enzyme
Antimicrobial evaluation of 3,1-benzoxazin-4-ones, 3,1-benzothiazin-4-ones, 4-alkoxyquinazolin-2-carbonitriles and N-arylimino-1,2,3-dithiazoles
Alkylbenzyl ethers of hydroquinones as monoamine oxidase B inhibitors
Correlation of oxidation potential and toxicity in thiobenzamides
Synthesis of water-soluble prodrugs of the cytotoxic agent Combretastatin A4
The design and synthesis of non-peptide ligands with affinity and selectivity for tachykinin receptors
Synthesis, enzymatic phosphorylation and antiviral activity of acyclic dienyl phosphonate derivatives of guanine
Structure activity relationships of tetrahydrocannabinol analogues on human cannabinoid receptors
Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042
D-Phe-Pro-p-Amidinobenzylamine: A potent and highly selective thrombin inhibitor
Adenosine deaminase inhibitors. Synthesis and biological evaluation of chain modified analogs of (+)-EHNA
New antithrombotic RGD-mimetics with high bioavailability
Studies on the structural feature of S'1 subsite of neprilysin (EC.3.4.24.11): Stereochemical requirement for the enzyme-inhibitor docking process
A rapid synthesis of some 5-amino- nucleosides and nucleotides as potential antiviral compounds
Synthesis and antibacterial activity of lipophilic carbapenems with anti-MRSA activity
Synthesis and cytotoxic activity of phenyl-hexahydropyrrolo[3,4-c]carbazoles
Palladium-catalysed synthesis of some biologically active 5, 6-disubstituted uracils
Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series
Synthesis of ribofuranosyl glycosides of echiguanines A and B, inhibitors of phosphatidylinositol 4-kinase
Probing the specificity of the S1 binding site of M222 mutants of subtilisin B. lentus with boronic acid inhibitors
Altering the specificity of subtilisin B. Lentus by combining site-directed mutagenesis and chemical modification
Synthesis and activity of 2,6,9-trisubstituted purines
Molecular interactions of all possible regioisomers of synthetic myo-inositol phosphates with inositol 1,4,5-trisphosphate 3-kinase
Design and synthesis of sialyl Lex mimetics based on carbocyclic scaffolds derived from () quinic acid
Synthesis and structure-activity relationships of potent conformationally restricted retinoid X receptor ligands
Synthesis and structure-activity relationship of C-3 quaternary ammonium cephalosporins exhibiting anti-MRSA activities
(Dipropylamino)-tetrahydronaphthofurans: centrally acting serotonin agonists and dopamine agonists-antagonists
Synthesis and pharmacology of the 1,2-dimethylheptyl-8-THC isomers: exceptionally potent cannabinoids
Synthesis and structure-activity relationships of novel 3-Hty-substituted pneumocandins
Inhibition of nitric oxide synthase by benzoxazolones
Anti-AIDS agents. 291. Anti-HIV activity of modified podophyllotoxin derivatives
1-Oxo-3-aryl-1H-indene-2-carboxylic acid derivatives as selective inhibitors of fibroblast growth factor receptor-1 tyrosine kinase
Synthesis of 11,13-bridged progestational steroids
Synthesis of conformationally restricted progestational 13-ethylsteroids
Synthesis and in vitro cytotoxic activity of novel hexahydro-2H-pyrido[1,2-b]isoquinolines against human brain tumor cell lines
Inhibitory effects of scopadulcic acid B and its derivatives on bone resorption and osteoclast formation in vitro
Bone targeted drugs 2. synthesis of estrogens with hydroxyapatite affinity
Synthesis and anti-HIV activity of dihydroisoxazole 6-chloropurine and adenine
1,3-diaryl-2-carboxyindoles as potent non-peptide endothelin antagonists
Synthesis of phosphorus-containing amino acid analogs as inhibitors of nitric oxide synthase
(S)-(+)-2-(3'-carboxybicyclo[1.1.1]pentyl)-glycine, a structurally new group I metabotropic glutamate receptor antagonist.
N-heteroaryl-2-phenyl-3-(benzyloxy)piperidines: a novel class of potent orally active human NK1 antagonists.
7-[3-(1-piperidinyl)propoxy]chromenones as potential atypical antipsychotics.
Synthesis and characterization of pseudopeptide bradykinin B2 receptor antagonists containing the 1,3,8-triazaspiro[4.5]decan-4-one ring system.
Theoretical study of inhibition of adenosine deaminase by (8R)-coformycin and (8R)-deoxycoformycin.
3-((4-(4-Chlorophenyl)piperazin-1-yl)-methyl)-1H-pyrrolo-2,3-b-pyridine: an antagonist with high affinity and selectivity for the human dopamine D4 receptor.
Studies on selectin blockers. 2. Novel selectin blocker as potential therapeutics for inflammatory disorders.
Discovery of an orally active non-peptide fibrinogen receptor antagonist.
Chemical synthesis of benzamide adenine dinucleotide: inhibition of inosine monophosphate dehydrogenase (types I and II).
Structure-activity relationships for inhibition of inosine monophosphate dehydrogenase by nuclear variants of mycophenolic acid.
Structure-activity relationships of phomactin derivatives as platelet activating factor antagonists.
Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy.
Selectively cytotoxic diterpenes from Euphorbia poisonii.
Rationally designed inhibitors of inosine monophosphate dehydrogenase.
Smart region definition: a new way to improve the predictive ability and interpretability of three-dimensional quantitative structure-activity relationships.
9-Benzyladenines: potent and selective cAMP phosphodiesterase inhibitors.
Substituted [(4-phenylpiperazinyl)-methyl]benzamides: selective dopamine D4 agonists.
Novel and selective partial agonists of 5-HT3 receptors. 2. Synthesis and biological evaluation of piperazinopyridopyrrolopyrazines, piperazinopyrroloquinoxalines, and piperazinopyridopyrroloquinoxalines.
Potent HIV protease inhibitors containing a novel (hydroxyethyl)amide isostere.
Stabilized analogs of thymopentin. 2. 1,2- and 3,4-ketomethylene pseudopeptides.
Doxoform and Daunoform: anthracycline-formaldehyde conjugates toxic to resistant tumor cells.
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.
Fused pyrrolo[2,3-c]carbazol-6-ones: novel immunostimulants that enhance human interferon-gamma activity.
Molecular modeling and 3D-QSAR studies on the interaction mechanism of tripeptidyl thrombin inhibitors with human alpha-thrombin.
Boron-containing polyamines as DNA targeting agents for neutron capture therapy of brain tumors: synthesis and biological evaluation.
Neuronal nicotinic acetylcholine receptors as targets for drug discovery.
A 3D QSAR study of a series of HEPT analogues: the influence of conformational mobility on HIV-1 reverse transcriptase inhibition.
(+)-2-Methyl-4-carboxyphenylglycine (LY367385) selectively antagonises metabotropic glutamate mGluR1 receptors
Synthesis of trimethylated phosphonium and arsonium analogues of the osmoprotectant glycine betaine; contrasted biological activities in two bacterial species
Studies on the active conformation of the NK1 antagonist CGP 49823. Part 21. Fluoro-olefin analogs of tertiary amide rotamers.
Subsite requirements for peptide aldehyde inhibitors of human calpain I
A QSAR study of antiplatelet agents using artificial neural network - correlation with micelle-water partition coefficient
A conformational study of ligands for omega modulatory sites of GABAa receptors by NOESY NMR spectroscopy and distance geometry
Orevactaene,1 a novel binding inhibitor of HIV-1 rev protein to Rev response element (RRE) from Epicoccum nigrum WC47880
Robustaflavone, a naturally occurring biflavanoid, is a potent non-nucleoside inhibitor of hepatitis B virus replication in vitro
Amide surrogates of matrix metalloproteinase inhibitors: Urea and sulfonamide mimics
Adenosine A2A antagonists with potent anti-cataleptic activity
Synthesis of inhibitors of glutamyl-tRNA synthetase
Synthesis and biological activity of 1,2,3,4-tetrahydroquinoline and 3,4-(1H)-dihydroquinolin-2-one analogs of retinoic acid
A new series of selective dopamine D4 ligands: 3-([4-arylpiperazin-1-yl]alkylamino)-2H-1,4-benzoxazines
The development of a charged melatonin receptor ligand
Potent antiinflammatory 3-thiazole-4(5)-acetic acids of 1,2-benzisothiazole
Synthesis of triphosphonate analogues of farnesyl pyrophosphate. Inhibitors of squalene synthase and protein:farnesyl transferase
Pyrrolylquinoxalinediones: Dicarboxylates as highly potent AMPA receptor antagonists
Catalytic mechanism of KDO8P synthase: synthesis and evaluation of a putative reaction intermediate
Catalytic mechanism of KDO8P synthase. Pre-steady-state kinetic analysis using rapid chemical quench flow methods
Synthesis and biological activity of cinnamaldehydes as angiogenesis inhibitors
Investigation into the preferred conformation of gabapentin for interaction with its binding site on the 2 subunit of a calcium channel
Design and synthesis of an -mannosyl terpenoid as selective inhibitor of P-selectin
Solid-phase synthesis of hybrid thiazolidinedione-fatty acid PPAR ligands
Synthesis and antimicrobial activities of 3-N-substituted-4,5-bis(3-indolyl)oxazol-2-ones
4-Biaryl-substituted dihydropyridines with an unusual antiperiplanar conformation
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Dihydroisoquinolone RGD mimics. Exploration of the aspartate isostere
Synthesis and progesterone receptor binding affinity of substituted 1-phenyl-7-benzyl-4,5,6,7-tetrahydro-1-indazoles
Synthesis and biological evaluation of 14,15-dehydro-LTA4 analog
BMS-200475, a novel carbocyclic 2-deoxyguanosine analog with potent and selective anti-hepatitis B virus activity in vitro
Synthesis and activity of brefeldin a analogs as inducers of cancer cell differentiation and apoptosis
Synthesis and preliminary structure-activity relationships of 1-[(3-fluoro-4-pyridinyl)amino]-3-methyl-1H-indol-5-yl methyl carbamate (P10358), a novel acetylcholinesterase inhibitor
The synthesis and antitumor evaluation of unsymmetrical bis-imides
Kinetic studies of the reaction of S-nitroso-L-cysteine with L-cysteine
Potent and selective inhibitors of the Abl-kinase: phenylamino-pyrimidine (PAP) derivatives
The dipeptide neurokinin-1 receptor antagonist S19752 is a potent and long-acting inhibitor of bronchoconstriction when administered by aerosol to the guinea pig in vivo
A nonpeptidic agonist ligand of the human C5a receptor: Synthesis, binding affinity optimization and functional characterization
A simplified template approach towards the synthesis of a potent beta-3 adrenoceptor agonist at the human receptor
Antibody-mediated regio- and enantioselective resolution of a glycerol derivative
Cyclic saligenyl phosphotriesters of 2,3-dideoxy-2,3-didehydrothymidine (d4T) a new pro-nucleotide approach
Synthesis and evaluation of novel-N-[2-(bis-aryl-methoxy)ethyl-N-aralkyl-,-alkanediamines as potent and selective dopamine reuptake inhibitors: Seco analogs of GBR12935 and GBR12909
Synthesis and anti HCMV activity of 3,4-disubstituted tetrahydrofuran derived nucleosides and nucleotides: A tethered series of PME derivatives
5-HT1A and 5-HT2A ligands with anxiolytic and antipanic-like properties
Design and synthesis of a macrocyclic E-Selectin antagonist
Synthesis of irreversible HIV-1 protease inhibitors containing sulfonamide and sulfone as amide bond isosteres
Solid-phase synthesis of a N-carboxyalkyl tripeptide combinatorial library
Design and synthesis of curacin a analogs with varied side chain structures
Synthesis and biological activity of new bradykinin pseudopeptide B1 receptor agonists containing alkylic spacers
New generation dopaminergic agents. 5. Heterocyclic bioisosteres that exploit the 3-OH-N1-phenylpiperazine dopaminergic template.
Tropane-based amino acids for peptide structure-function studies: inhibitors of platelet aggregation.
Design and synthesis of a pyridone-based phosphotyrosine mimetic.
Quinazolines: combined type 3 and 4 phosphodiesterase inhibitors.
Derivatization of the C12-C13 functional groups of epothilones A, B and C.
Syntheses and antitumor activity of cis-restricted combretastatins: 5-membered heterocyclic analogues.
Anthelmintic beta-hydroxyketoamides (BKAs).
Biologically selective potassium channel openers having 1,1-diethylpropyl group.
Antiinflammatory 4,5-diarylimidazoles as selective cyclooxygenase inhibitors.
Design and synthesis of new secretory phospholipase A2 inhibitor of a phospholipid analog.
Phenylpiperazine derivatives with strong affinity for 5HT1A, D2A and D3 receptors.
The solid phase synthesis of a series of tri-substituted hydantoin ligands for the somatostatin SST5 receptor.
Design and synthesis of a biotinylated dopamine transporter ligand for the purification and labeling of dopaminergic neurons.
Carboxy-substituted 2-azetidinones as cholesterol absorption inhibitors.
Inhibition of thermolysin with nitrone-bearing substrate analogs: a new type of thermolysin inhibitors.
Immunosuppressant activity in human beta-casein fragment analogs.
Antiinflammatory effects of escins Ia, Ib, IIa, and IIb from horse chestnut, the seeds of Aesculus hippocastanum L.
Constrained -alanine based GpIIb/IIIa antagonists
Evaluation of piperidinoethoxy moiety as an antiestrogenic substituent in non-steroidal anti-estrogens: Fertility regulation
Hemisynthesis of rhazinilam analogues: structure - activity relationships on tubulin-microtubule system
Asymmetric synthesis of a conformationally constrained N-phosphonoalkyl dipeptide
Inhibition of Matrix Metalloproteinases: An examination of the S1 pocket
Syntheses and anticancer activity of ribonucleoside analogues containing thio-substituted five-membered heterocyclic base
C3-Thia and C3-carba isosteres of a carbocyclic influenza neuraminidase inhibitor, (3R,4R,5S)-4-acetamido-5-amino-3-propoxyl-1-cyclohexene-1-carboxylic acid
Design and synthesis of a possible mimic of a thrombin-binding DNA aptamer
Synthesis and receptor binding affinity of conformationally restricted retinoic acid analogues
Synthesis of (+)- and ()-2-methylarachidonyl-2-fluoroethylamide (O-689)
On the mechanism of chorismate mutases: Revisiting structural requirements for catalysis
A technetium-99m SPECT imaging agent which targets the dopamine transporter in primate brain.
Trypanocidal activity and redox potential of heterocyclic- and 2-hydroxy-naphthoquinones
p-NITROPHENYL -D-GLUCOPYRANOSIDURONIC ANALOGS AS POTENTIAL SUBSTRATES FOR -GLUCURONIDASE
In vivo immunosuppressive activity of some cyclolignans
3-[(3-Hydroxymethyl)-4-hydroxybutyl]imidazo[4,5-b]pyridinesnovel antiviral agents
Homology modeling of the ampa receptor: A quantitative predictive tool for the design of novel antagonists
Pyrrolylquinoxalinediones: The importance of pyrrolic substitution on AMPA receptor binding
4-Sulfonamidoanilide tertiary carbinols: A novel series of potassium channel openers
Synthesis and estrogen receptor binding affinities of the major human metabolites of raloxifene (LY139481)
Potent carboxylate inhibitors of stromelysin containing P2 piperazic acids and P1 biaryl moeities
Design, syntheses and potentiating activities against methicillin resistant Staphylococcus aureus of cyclic analogs of LY301621
Novel hydroxyphosphonate inhibitors of CD-45 tyrosine phosphatase
Synthesis and evaluation of putative oxocarbenium intermediate mimic in the KDO8P synthase-catalyzed reaction as a tool for the design of potent inhibitors for lipopolysaccharide biosynthesis
Dual CCK-A and -B receptor antagonists (I) C9-methyl-1,4-benzodiazepines
Resolution and biological activities of optical isomers of 1,4-diethyl-3,6-epidithiopiperazine-2,5-dione
Effects of taxoids from Taxus cuspidata on microtubule depolymerization and vincristine accumulation in MDR cells
Cross-linking and sequence specific alkylation of DNA by aziridinyl quinones. 2. Structure requirements for sequence selectivity.
The practical synthesis of a methylenebisphosphonate analogue of benzamide adenine dinucleotide: inhibition of human inosine monophosphate dehydrogenase (type I and II).
Design, synthesis, and cocrystal structure of a nonpeptide Src SH2 domain ligand.
Neuritogenic effect of epolactaene derivatives on human neuroblastoma cells which lack high-affinity nerve growth factor receptors.
Discovery of selective dopamine D4 receptor antagonists: 1-Aryloxy-3-(4-aryloxypiperidinyl)-2-propanols
The Gif system as a tool in medicinal chemistry: The oxidation of Sch 57726 under GoAggIII conditions
Studies on -lactam antibiotics. Synthesis and antibacterial activity of novel 1-methylcarbapenems related to FR21818: 5-membered ring analogs
Tetrazole is an effective Sn-3 phosphate replacement in substrate analog inhibitors of 14 kDa phospholipase A2
Enhanced DNA photocleavage and binding properties of sapphyrin-polyamine conjugates
Inhibitory effects of pentamidine analogues on spermine stimulated ligand binding to the NMDA receptor complex
The synthesis of CD-ring modified 1,25-dihydroxy vitamin D analogues: Six-membered D-ring analogues I
CETP inhibitory activity of ceramides, isolated from the gorgonian Acabaria Undulata
Synthesis and cytotoxicity of amino analogues of the potent DNA alkylating agent seco-CBI-TMI
L-373,890, An achiral, noncovalent, subnanomolar thrombin inhibitor
Synthesis and antirheumatic activity of novel tetrahydroquinoline-8-carboxylic acid derivatives
Synthesis and antirheumatic activity of novel tetrahydro-6-quinolineacetic acid derivatives
Nonpeptide glycoprotein IIb/IIIa inhibitors. 13. design and synthesis of an orally active pyrazolopiperazinone nonpeptide fibrinogen receptor antagonist
Inhibition of carboxypeptidase a by N-(4-t-Butylbenzoyl)-2-hydroxy-1-naphthaldehyde hydrazone
ADA-Bypass by lipophilic cycloSal-ddAMP pro-nucleotides A second example of the efficiency of the cycloSal-Concept
Polyclonal catalytic antibody for hetero-cycloaddition of hepta-1,3-diene with ethyl glyoxylate an approach to the synthesis of 2-nonulosonic acid analogs
New enone derivatives of oleanolic acid and ursolic acid as inhibitors of nitric oxide production in mouse macrophages
Chemoenzymatic synthesis and characterization of a new type of carbohydrate-based cationic antimicrobial agents
Analogues of trichosatin a and trapoxin B as histone deacetylase inhibitors
Peptidic prodrugs of novel aminomethyl-THF 1-methylcarbapenems
Design and synthesis of novel monocyclic -lactam inhibitors of prostate specific antigen
Prolyl endopeptidase inhibitors1: N-acyl derivatives of L-thioproline-pyrrolidine
Novel inhibitors of the prenylated protein methyltransferase reveal distinctive structural requirements
RES-701-1/endothelin-1 hybrid peptide having a potent binding activity for type B receptor
Synthesis and in vitro antibacterial activities of novel conformationally restricted hygromycin a analogues
Conformationally restricted arginine analogues as inhibitors of human nitric oxide synthase
FKBP12-binding domain analogues of FK506 are potent, nonimmunosuppressive neurotrophic agents in vitro and promote recovery in a mouse model of parkinson's disease
Mono and bis double ester prodrugs of novel aminomethyl-THF 1-methylcarbapenems
Structure-activity relationship of cantharidin derivatives to protein phosphatases 1, 2A1, and 2B
Structure-activity relationships of carbocyclic influenza neuraminidase inhibitors
Synthesis and activity of C2-substituted analogs of influenza neuraminidase inhibitor GS 4071
The synthesis and evaluation of functionalized estratropones: Potent inhibitors of tubulin polymerization
Tricyclic -lactams: Total synthesis and antibacterial activity of 5-methoxyethyl and 5-hydroxyethyl trinems
Development of a positron emission tomography radiopharmaceutical for imaging thymidine kinase gene expression: Synthesis and in vitro evaluation of 9-{3-[18F] Fluoro-1-hydroxy-2-propoxymethyl guanine
1,4-Diaryl-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids as endothelin receptor antagonists
Synthesis and anti-HIV activity of some new aminoadamantane heterocycles
The Role of 4-phosphonodifluoromethyl- and 4-phosphono-phenylalanine in the selectivity and cellular uptake of SH2 domain ligands
Nonpeptide bradykinin antagonist analogs based on a model of a Sterling-Winthrop nonpeptide bradykinin antagonist overlapped with cyclic hexapeptide bradykinin antagonist peptides
Dimeric aminoglycosides: Design, synthesis and RNA binding
Design and synthesis of a targeted set of aromatic amino acid derivatives for identification of new lead compounds
Synthesis of N-desmethyl PNQX: elaboration into an immunogenic conjugate and a radioiodinated ligand; radioimmunoassay for the AMPA/NMDA antagonist, PNQX
Novel 7-hydroxycoumarin based fluorescent labels
Synthesis of halogenated/nitrated flavone derivatives and evaluation of their affinity for the central benzodiazepine receptor
SAR study of the indole moiety of CI-988, a potent and selective CCK-B antagonist
Synthesis and phosphatase inhibitory activity of analogs of sulfircin
Lipopeptide antifungal agents: Amine conjugates of the semi-synthetic pneumocandins L-731,373 and L-733,560
Synthesis and antibacterial activity of some thio trinems
Synthesis and evaluation of benzophenone-based photoaffinity labeling analogs of prenyl pyrophosphates containing stable amide linkages
Synthesis of 7-membered cyclic hydroxyguanidines: Novel HIV-1 protease inhibitors
Serotonin 5-HT4 agonist activity of a series of meso-azanoradamantane benzamides
Synthesis and in vitro cytotoxicity of aminocoumarin platinum(II) complexes
Structure-based design of non-peptidic pyridone aldehydes as inhibitors of interleukin-1 converting enzyme
New hepatoprotective saponins, bupleurosides III, VI, IX, and XIII, from Chinese Bupleuri Radix: Structure-requirements for the cytoprotective activity in primary cultured rat hepatocytes
4-Heterocyclyl tetrahydropyridines as selective ligands for the human dopamine D4 receptor
Synthesis and biological activity of novel penem sulfoxides and sulfones
11,21-Bisphenyl-19-norpregnane derivatives are selective antiglucocorticoids
BN 80245: An E-ring modified camptothecin with potent antiproliferative and topoisomerase I inhibitory activities
Solid phase synthesis of C-terminal carbohydrate modified enkephalins
Novel 6-substituted 2-aminotetralins with potent and selective affinity for the dopamine D3 receptor
A novel class of antagonists for metabotropic glutamate receptors, 7-(Hydroxyimino)cyclopropa[b]chromen-1a-carboxylates
Adenine-arginine mimetics as bisubstrate analog inhibitors of cAMP-dependent protein kinase
(E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2- pyridinyl]-2-propenoic acid: a high-affinity leukotriene B4 receptor antagonist with oral antiinflammatory activity.
Novel phenyl nitrogen mustard and half-mustard derivatives of amidino-modified distamycin
Novel phenyl nitrogen mustard and half-mustard derivatives of distamycin A
First synthesis and cytotoxic activity of novel docetaxel analogs modified at the C18-position
Design and synthesis of 3,5-dialkylamino substituted 8H,10H-3(R),5(R),15b(S)-2,3,6,7-tetrahydro-1,5,3-dioxazepino[3,2-c]indolo[3,2-g]pteridine-7-ones
N-linked glycoside/glucuronide conjugates of retinoids: acitretin
Eicosanoid biosynthesis: differential inhibition of cytochrome P450 epoxygenase and -hydroxylase
Fluorescent molecular probes III. 2,7-Bis-(3-carboxypropyl)-5-(and-6)-carboxyfluorescein (BCPCF): a new polar dual-excitation and dual-emission pH indicator with a pKa of 7.0
Oestrone 3-O-(N-acetyl)sulphamate, a potential molecular probe of the active site of oestrone sulphatase
Synthesis and cell growth inhibitory properties of substituted (E)-1-phenylbut-1-en-3-ones
Ester prodrugs of ampicillin tailored for intracellular accumulation
Novel water-soluble analogues retaining potent antitumor activity of RA-VII, a cyclic hexapeptide from Rubia plants
Discovery of anti-influenza A virus activity of a corynanthe-type indole alkaloid, hirsutine, in vitro and the structure-activity relationship of natural and synthetic analogs
Polysubstituted 2H-pyran-2-ones: A new class of hepatoprotective agents
1,4-Bis-(2,3-epoxypropylamino)-9,10-anthracenedione and related compounds as potent antifungal and antimicrobial agents
Thermal atropisomerism of fully functionalized vancomycin CD, DE, and CDE ring systems
Cytotoxicity and actin depolymerizing activity of aplyronine A, a potent antitumor macrolide of marine origin, and the natural and artificial analogs
Nonpeptidic inhibitors of recombinant human calpain I
-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs
Potency and inactivation rates of analogues of an irreversible inhibitor of vertebrate oxidosqualene cyclase
Synthesis and biological activity of P2P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors
A convenient synthesis of pseudoceratidine and three analogs for biological evaluation
Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D3 receptor: N-benzyl modifications
Rational design, synthesis, and serine protease inhibitory activity of a novel P1-argininal derivative featuring a conformationally constrained P2P3 bicyclic lactam moiety
Replacements for lysine in l-seryl-l-lysyl dipeptide amide inhibitors of candida albicans myristoyl-CoA:protein N-myristoyltransferase
Quantitative structure-activity relationships of benzoyliminothiadiazoline derivatives as angiotensin II receptor antagonists
Synthesis and pharmacological evaluation of sulfone substituted HIV protease inhibitors
The preparation and sar of 4-(anilino), 4-(phenoxy), and 4-(thiophenoxy)-quinazolines: Inhibitors of p56lck and EGF-R tyrosine kinase activity
Peptide based inhibitors of interleukin-8: structural simplification and enhanced potency
ATP-sensitive potassium channel openers: Synthesis and antihypertensive activity of 4-bicyclyloxybenzopyrans
Mechanism-based inactivation of l-pipecolate oxidase by a sulfur-containing substrate analog, 5-thia-l-pipecolic acid
Digitalis-like compounds: Synthesis and biological evaluation of 3-(aminoalkylthio) derivatives
2-[(substituted)phenyl]-5-[1-(2-phenylazacycloheptyl)methyl]-1H-pyrroles with high affinity and selectivity for the dopamine D3 receptor
Synthesis and evaluation of imidazolidinones as nonpeptide HIV-protease inhibitors
Synthesis and evaluation of delta lactams as nonpeptide HIV-protease inhibitors
Novel inhibitors of trypanothione biosynthesis: Synthesis and evaluation of a phosphinate analog of glutathionyl spermidine (GSP), a potent, slow-binding inhibitor of GSP synthetase
Synthesis and structural optimization of 7-(3,3-disubstituted-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo-3-quinolinecarboxylic acids as antibacterial agents
Novel small molecule neurotensin antagonists: 3-(1,5-diaryl-1,5-dioxopentan-3-yl)benzoic acids
Molecular connectivity to find -blockers with low toxicity
Novel optimised quinuclidine squalene synthase inhibitors
Synthesis, molecular modeling, and biology of the 1-benzyl derivative of APDC-an apparent mGluR6 selective ligand
Synthesis and antibacterial activity of (1R, 5R, 6R)-2-tert-butyl-6-(1-hydroxyethyl)penem-3-carboxylic acid
Studies on penam sulfones III. Synthesis and -lactamase inhibitory activity of sodium (6R)-6-(-hydroxybenzyl)-2-methoxyiminomethyl-2-methylpenam-3-carboxylate 1,1-dioxide and sodium 2-acyl-2-methylpenam-3-carboxylate 1,1-dioxide
2,3-Substituted 2-azanorbornanes as polar -turn mimetics
Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor
Imidazotriazinone inhibitors of the Ca2+-calmodulin sensitive phosphodiesterase (PDE I)
SYNTHESIS AND BIOLOGICAL EVALUATION OF A FLUORINATED ANALOG OF THE -ADRENERGIC BLOCKING AGENT, METOPROLOL
SPORANDOL: A NOVEL ANTIPARASITIC BINAPHTHALENE FROM CHRYSOSPORIUM MERIDARIUM
GENISTEIN AND FLUORINATED ANALOGS SUPPRESS AGONIST-INDUCED AIRWAY SMOOTH MUSCLE CONTRACTION
PYRIDONE-BASED PEPTIDOMIMETIC INHIBITORS OF INTERLEUKIN-1-CONVERTING ENZYME (ICE)
A SHORT AND EFFICIENT SYNTHESIS OF ZAMIFENACIN A MUSCARINIC M3 RECEPTOR ANTAGONIST
SYNTHESIS AND ANTISTAPHYLOCOCCAL ACTIVITY OF NEMATOPHIN AND ITS ANALOGS
The synthesis and activity of spiroindane growth hormone secretagogues
Enzymatic synthesis of peptidyl amino alcohols and peptidyl amino aldehydes-serine proteinase inhibitors
Vasopressin trisulphide: synthesis, NMR study and affinity studies with V1 and V2 subtypes receptors
Beta-amino acid derivatives as orally active non-peptide fibrinogen receptor antagonists
Hindered rotation congeners of mazapertine: High affinity ligands for the 5-HT1A receptor
Rational design of selective thrombin inhibitors
Novel indole containing thiazolidinedione derivatives as potent euglycemic and hypolipidaemic agents
Dicarboxylic acid inhibitors of phospholipase A2
Synthesis and evaluation of halogenated dibenzodiazepines as muscarinic receptor ligands
Synthesis and cytotoxic activity of alkylidene- and alkyl-substituted camptothecins
Dihydroxypyrrolidines C-linked to galactose. Total synthesis of a specific inhibitor of -mannosidases
A novel series of matrix metalloproteinase inhibitors for the treatment of inflammatory disorders
New cyclic butyrophenone derivatives in the indole series as potential atypical antipsychotics. A simple and practical synthesis of 6-aminomethyl-tetrahydroindol-4-ones and their affinites for D2 and 5-HT2A receptors
Synthesis of CD-ring modified 1,25-dihydroxy vitamin D analogues: Five-membered D-ring analogues
Synthesis and biological evaluation of 1-hydroxy-25(R and S)-25,26-Epoxy-23-yne vitamin D3 and of 1,25(R and S),26-Trihydroxy-23-yne vitamin D3
Amide bond surrogates: A study in thiophenesulfonamide based endothelin receptor antagonists
N-aryl cinnamides: A novel class of rigid and highly potent leukotriene B4 receptor antagonists
3-chloro-4-carboxamido-6-arylpyridazines as a non-peptide class of interleukin-1 converting enzyme inhibitor
Benzothiadiazine dioxide acyclonucleosides as lead compounds for the development of new agents against human cytomegalovirus and varicella-zoster virus infections
Synthesis and binding affinity of new muscarinic ligands structurally related to oxotremorine
Potent non-peptidic dual inhibitors of endothelin-converting enzyme and neutral endopeptidase 24.11
Synthesis of an aminopropyl analog of the experimental anticancer drug tallimustine, and activation of its 4-nitrobenzylcarbamoyl prodrug by nitroreductase and NADH
Synthesis, characterization, interaction with DNA, and antitumor activity of a cis-Dichloroplatinum(II) complex linked to an intercalator via one methylene chain
Functionalized azoles and triazolo[1,5-a]pyrimidines as latent leishmanicides
Synthesis and cytotoxicity of novel artemisinin analogs
A novel RGD containing dodecapeptidomimetic which exhibits selective binding to the v3 receptor
Topoisomerase II inhibitors. Synthetic hybridization of 4-quinolones and anthracyclines
Peptide argininol inverse substrates of anisic acid: Novel inhibitors of the trypsin-like serine proteinases
Cyclic homopentapeptides 1. Analogs of tuberactinomycins and capreomycin with activity against vancomycin-resistant enterococci and Pasteurella
Preparation and antibacterial activity of pyridopyridone analogs: C-1 modifications
Antiallergic activity of some novel oligopeptides related to immunoglobulin E
Synthesis and biological activity of cyclic analogues of MPPG and MCPG as metabotropic glutamate receptor antagonists
Synthesis and antiviral evaluation of 4-hydroxymethyl-2, 3-dideoxy-3-thianucleosides and their cyclic monophosphates
Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.
(+)-7-Deaza-5'-noraristeromycin as an anti-trypanosomal agent.
Inhibition of uridine phosphorylase. Synthesis and structure-activity relationships of aryl-substituted 1-((2-hydroxyethoxy)methyl)-5-(3-phenoxybenzyl)uracil.
Synthesis and transporter binding properties of 2,3-diphenyltropane stereoisomers. Comparison to 3beta-phenyltropane-2beta-carboxylic acid esters.
Pharmacological options in the treatment of benign prostatic hyperplasia.
A 3D-QSAR study on ginkgolides and their analogues with comparative molecular field analysis.
Indole-2-carboxamide inhibitors of human liver glycogen phosphorylase.
Bis-substituted malonic acid hydroxamate derivatives as inhibitors of human neutrophil collagenase (MMP8).
Synthesis and characterization of heteroarotinoids demonstrate structure specificity relationships.
Synthesis and antimalarial activities of fluoroalkyl derivatives of dihydroartemisinin.
4-Alkynylphenyl imidazolylpropyl ethers as selective histamine H3-receptor antagonists with high oral central nervous system activity.
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
Bis-cationic heteroaromatics as macrofilaricides: synthesis of bis-amidine and bis-guanylhydrazone derivatives of substituted imidazo[1,2-a]pyridines.
Novel CDC25A phosphatase inhibitors from pyrolysis of 3-alpha-azido-B-homo-6-oxa-4-cholesten-7-one on silica gel.
Macrocyclic amino carboxylates as selective MMP-8 inhibitors.
Structure-activity relationships of the 7-substituents of 5,4'-diamino-6,8,3'-trifluoroflavone, a potent antitumor agent.
Rational design and combinatorial evaluation of enzyme inhibitor scaffolds: identification of novel inhibitors of matrix metalloproteinases.
Studies on selectin blockers. 6. Discovery of homologous fucose sugar unit necessary for E-selectin binding.
Substituted tetrahydropyrrolo[2,1-b]oxazol-5(6H)-ones and tetrahydropyrrolo[2,1-b]thiazol-5(6H)-ones as hypoglycemic agents.
Synthesis and pharmacological evaluation of new flosulide analogues, synthesized from natural safrole.
N6-(5,6-epoxynorbornyl)adenosine analogs as A1 adenosine agonists.
Design of a new class of orally active fibrinogen receptor antagonists.
3,6-Diamino-10-methylacridan: uncharged precursor of acriflavine and its unique antimicrobial activity.
Syntheses and structure-activity relationships of novel retinoid X receptor agonists.
N-(Iodopropenyl)-octahydrobenzo[f]- and -[g]quinolines: synthesis and adrenergic and dopaminergic activity studies.
6-Amino-2-(4-fluorophenyl)-4-methoxy-3- (4-pyridyl)-1H-pyrrolo[2, 3-b]pyridine (RWJ 68354): a potent and selective p38 kinase inhibitor.
1-Methoxy-agroclavine from Penicillium sp. WC75209, a novel inhibitor of the Lck tyrosine kinase.
Derivatization of soyasapogenol A and their hepatoprotective activities.
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.
Synthesis and structure-activity relationship of potent bicyclic lactam thrombin inhibitors.
Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors.
4-Phenylthiazole derivatives inhibit IL-6 secretion in osteoblastic cells and suppress bone weight loss in ovariectomized mice.
New photoaffinity analogs of paclitaxel.
Preparation of amino acid conjugates of betulinic acid with activity against human melanoma.
A study of novel antiallergic agents with eosinophilic infiltration inhibiting action.
Short synthesis and anti-rhinoviral activity of imidazo[1,2-a]pyridines: the effect of acyl groups at 3-position.
Synthesis and evaluation of hapalosin and analogs as MDR-reversing agents.
Design of scytalone dehydratase inhibitors as rice blast fungicides: (N-phenoxypropyl)-carboxamides.
A mutational study of a Diels-Alderase catalytic antibody.
Synthesis and identification of conformationally constrained selective MMP inhibitors.
The design and synthesis of ALS inhibitors from pharmacophore models.
Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics.
Synthesis and in vitro cancer cell growth inhibitory activity of monocyclic model compounds containing spongistatin triene side-chains.
Synthesis and pharmacology of a new AMPA-kainate receptor agonist with potent convulsant activity.
1-[2(R)-(2-amino-2-methylpropionylamino)-3-(1H-indol-3-yl)propionyl]- 3-benzylpiperidine-3(S)-carboxylic acid ethyl ester (L-163,540): a potent, orally bioavailable, and short-duration growth hormone secretagogue.
Synthesis and antitumor activity of new glycosides of epipodophyllotoxin, analogues of etoposide, and NK 611.
Pharmacophoric requirements for cannabinoid side chains: multiple bond and C1'-substituted delta 8-tetrahydrocannabinols.
Orally active antimalarial 3-substituted trioxanes: new synthetic methodology and biological evaluation.
New bronchodilators selected by molecular topology.
Design of new inhibitors for cdc2 kinase based on a multiple pseudosubstrate structure.
Structure-activity relationships in 2-aminodiphenylsulfides against trypanothione reductase from Trypanosoma cruzi.
Structure-activity relationship of new growth inhibitors of Trypanosoma cruzi.
Inhibition of lipid peroxidation mediated by indolizines.
Selective inhibition of the chymotrypsin-like activity of the 20S proteasome by 5-methoxy-1-indanone dipeptide benzamides.
A new strong inhibitor of beta-mannosidase.
Structure-activity relationships for antiplasmodial activity among 7-substituted 4-aminoquinolines.
Discovery and structure-activity relationship of the first non-peptide competitive human glucagon receptor antagonists.
A potent dipeptide inhibitor of dipeptidyl peptidase IV.
Synthesis and pharmacological evaluation of benzofuran-acetamides as "antineophobic" mitochondrial DBI receptor complex ligands.
Synthetic arabinofuranosyl oligosaccharides as mycobacterial arabinosyltransferase substrates.
Novel HIV-protease inhibitors containing beta-hydroxyether and -thioether dipeptide isostere surrogates: modification of the P3 ligand.
Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.
Stability of acetal and non acetal-type analogs of artemisinin in simulated stomach acid.
An enantioselective fluorimetric assay for alcohol dehydrogenases using albumin-catalyzed beta-elimination of umbelliferone.
The design and synthesis of inhibitors of the cysteinyl protease, Der p I.
Novel D-ring analogues of podophyllotoxin as potent anti-cancer agents.
Inhibition of electric eel acetylcholinesterase by porphin compounds.
Synthesis and pharmacological activities of 13-dehydro derivatives of primary prostaglandins.
Synthesis and biological evaluation of a series of 2'-fluorinated-2',3'-dideoxy-2',3'-didehydro-(L)-nucleosides.
Adenosine deaminase inhibitors. Synthesis and biological evaluation of aralkyladenines (ARADS).
Inhibitors of the bacterial cell wall biosynthesis enzyme MurD.
Conodiparines A-D, new bisindoles from Tabernaemontana. Reversal of vincristine-resistance with cultured cells.
Solid-phase synthesis of N-substituted amidinophenoxy pyridines as factor XA inhibitors.
Syntheses of 2-[(3,5-dimethyl-4-methoxypyridyl)alkyl]-benzothiazolidine derivatives as a potential gastric H+/K(+)-ATPase inhibitor.
Preparation of difluoro analogs of CCGs and their pharmacological evaluations.
The novel cyclopropapyrroloindole(CPI) bisalkylators bearing 3,3'-(1,4-phenylene)diacryloyl group as a linker.
Design and synthesis of conformationally-constrained MMP inhibitors.
Novel imidazole derivatives with subtype-selective antimuscarinic activity (2).
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors.
Design and synthesis of analogs of vitamin E: antiproliferative activity against human breast adenocarcinoma cells.
Selective alpha-1a adrenergic receptor antagonists. Effects of pharmacophore regio- and stereochemistry on potency and selectivity.
Design and synthesis of a water-soluble taxol analogue: taxol-sialyl conjugate.
Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
New growth hormone secretagogues: C-terminal modified sulfonamide-analogues of NN703.
Synthesis of novel analogues of the delta opioid ligand SNC-80 using REM resin.
Synthesis of alpha-C(1-->3)-mannopyranoside of N-acetylgalactosamine, a new beta-galactosidase inhibitor.
Thrombin inhibitors based on a propargylglycine template.
Total synthesis of an antioxidant isolated from yeast via palladium-catalyzed coupling and its application for related compounds.
Structure-activity relationship at the proximal phenyl group in a series of non-peptidyl N-type calcium channel antagonists.
Thrombin inhibitors based on [5,5] trans-fused indane lactams.
Stereoselective synthesis of a new muscarinic M3 receptor antagonist, J-104129.
Potent, orally absorbed glucagon receptor antagonists.
Ring constrained analogues of the orvinols: the furanomorphides.
Discovery of a potent, orally active, nonsteroidal androgen receptor agonist: 4-ethyl-1,2,3,4-tetrahydro-6- (trifluoromethyl)-8-pyridono[5,6-g]- quinoline (LG121071).
Synthesis and structure-activity relationships of potential anticancer agents: alkylcarbamates of 3-(9-acridinylamino)-5-hydroxymethylaniline.
4-[[2-(1-Methyl-2-pyrrolidinyl)ethyl]thio]phenol hydrochloride (SIB-1553A): a novel cognitive enhancer with selectivity for neuronal nicotinic acetylcholine receptors.
Therapeutic potential and strategies for inhibiting tumor necrosis factor-alpha.
Novel adrenoceptor antagonists with a tricyclic pyrrolodipyridazine skeleton.
Synthesis, mode of action, and biological activities of rebeccamycin bromo derivatives.
Synthesis and in vitro multidrug resistance modulating activity of a series of dihydrobenzopyrans and tetrahydroquinolines.
Design and synthesis of modified quinolones as antitumoral acridones.
Self-immolative anthracycline prodrugs for suicide gene therapy.
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
2-Amino-4-benzyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridines: novel selective beta3-adrenoceptor agonists.
Structure-activity relationships for a class of inhibitors of purine nucleoside phosphorylase.
Design and synthesis of isoxazoline derivatives as factor Xa inhibitors. 2.
Synthesis and preliminary biological evaluation of new alpha-amino amide anticonvulsants incorporating a dextromethorphan moiety.
Combinatorial search of substituted beta-cyclodextrins for phosphatase-like activity.
A "cephalosporin-like" cyclic depsipeptide: synthesis and reaction with beta-lactam-recognizing enzymes.
Adenosine receptor ligands with oxygenated N6-substituents.
5-Aryl-1,2,3,4-tetrahydrochromeno[3,4-f]quinolin-3-ones as a novel class of nonsteroidal progesterone receptor agonists: effect of A-ring modification.
A novel pyridazinone derivative as a nonprostanoid PGI2 agonist.
Synthesis and antibacterial activities of novel C(3)-aminopyrimidinyl substituted cephalosporins including against respiratory tract pathogens.
RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.
Differential antibacterial activity of moenomycin analogues on gram-positive bacteria.
Analogues of SB-203207 as inhibitors of tRNA synthetases.
Novel heterocycles as selective alpha1-adrenergic receptor antagonists.
Inhibition of vertebrate squalene epoxidase by isoprenyl gallates and phenylalkyl gallates.
Synthesis of the novel analogues of dysidiolide and their structure-activity relationship.
Use of bicuculline, a GABA antagonist, as a template for the development of a new class of ligands showing positive allosteric modulation of the GABA(A) receptor.
New multidrug resistance modulators from Atractylodis Lanceae Rhizoma.
Pharmacotherapies for treatment of cocaine abuse: preclinical aspects.
4-Heterocyclohexanone-based inhibitors of the serine protease plasmin.
Lipophilic 4-isoxazolyl-1,4-dihydropyridines: synthesis and structure-activity relationships.
Structural modification of Fas C-terminal tripeptide and its effects on the inhibitory activity of Fas/FAP-1 binding.
Synthesis of 1-(2-aminophenyl)isoquinolines and the biological activity of their cis-dichloro platinum(II) complexes.
The sulfonimidamide as a novel transition state analog for aspartic acid and metallo proteases.
Pharmacological treatment of obesity: therapeutic strategies.
Bis- and mixed-tetrahydroisoquinolinium chlorofumarates: new ultra-short-acting nondepolarizing neuromuscular blockers.
Antagonists of the platelet P2T receptor: a novel approach to antithrombotic therapy.
Antimalarial, antiproliferative, and antitumor activities of artemisinin-derived, chemically robust, trioxane dimers.
Potent and selective inhibition of varicella-zoster virus (VZV) by nucleoside analogues with an unusual bicyclic base.
Synthesis and in vitro anti-HIV activity in human monocyte-derived macrophages of 2-oxothiazolidine-4(R)-carboxylic acid derivatives.
Manipulation of the C(22)-C(27) region of rapamycin: stability issues and biological implications.
From histamine to imidazolylalkyl-sulfonamides: the design of a novel series of histamine H3-receptor antagonists.
Correlation of anti-HIV activity with structure: use of electrostatic potential and conformational analysis.
Predicting relative binding free energies of tacrine-huperzine A hybrids as inhibitors of acetylcholinesterase.
Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists.
Tetrapeptide derived inhibitors of complexation of a class II MHC: fully unnatural ligands.
Targeting nitric oxide to cancer cells: cytotoxicity studies of glyco-S-nitrosothiols.
Synthesis and antitumoral activities of marine ent-chromazonarol and related compounds.
A novel class of Na+ and Ca2+ channel dual blockers with highly potent anti-ischemic effects.
Revised structure of a homonojirimycin isomer from Aglaonema treubii: first example of a naturally occurring alpha-homoallonojirimycin.
Synthesis and evaluation of benzoxazinones as HIV-1 reverse transcriptase inhibitors. Analogs of Efavirenz (SUSTIVA).
Synthesis and opiate receptor binding properties of 17-methyl-6,7-dehydro-3,14-dihydroxy-4,5alpha-epoxy-6,7:4',5'-pyrimidin omorphinans.
Tokaramide A, a new cathepsin B inhibitor from the marine sponge Theonella aff. mirabilis.
Quantitative analysis of the kinetics of phospholipase A2 using fast atom bombardment mass spectrometry.
Synthesis and biological evaluation of 1alpha,24-dihydroxy-25-nitrovitamin D3.
The synthesis and P388 cytotoxicity of mycalazol 11 and related 5-acyl-2-hydroxymethylpyrroles.
Design, synthesis, and evaluation of azapeptides as substrates and inhibitors for human rhinovirus 3C protease.
Protein kinase C modulators bearing dicarba-CLOSO-dodecaborane as a hydrophobic pharmacophore.
Novel benzo-fused lactam scaffolds as factor Xa inhibitors.
P'-extended alpha-ketoamide inhibitors of proteasome.
Synthesis and antitumor activity of bithienyl-pyrimidine derivatives with electrostatic binding side chains.
Synthesis and antitumour activity of novel diterpenequinone salvicine and the analogs.
Design and synthesis of novel dihydropyridine alpha-1a antagonists.
2-chloro-3-substituted-1,4-naphthoquinone inactivators of human cytomegalovirus protease.
Isoxazoline GPIIb/IIIa antagonists bearing a phosphoramidate.
Design and synthesis of thiol containing inhibitors of matrix metalloproteinases.
Specific, uncompetitive inhibition of beta-galactosidases by a 5,6-isopropylidenedioxyfuro[2,3-d]isoxazole-3-methanol derivative.
Stabilization of microtubules by Combretastatin D derivatives.
Synthesis and endothelin receptor binding activity of synthetic analogues of RES-1149-2.
Structural analogues of some highly active non-competitive AMPA antagonists.
5-Thienyltryptamine derivatives as serotonin 5-HT1B/1D receptor agonists: potential treatments for migraine.
Discovery and evaluation of potent, cysteine-based alpha4beta1 integrin antagonists.
Synthesis and class III type antiarrhythmic activity of 4-aroyl (and aryl)-l-aralkylpiperazines.
Secondary amines as new pharmacophores for macrofilaricidal drug design.
Synthesis of a dihydroxythiophene analogue of catechosporines.
Antimitotic activity of moroidin, a bicyclic peptide from the seeds of Celosia argentea.
Novel peptidomimetic hematoregulatory compounds.
Synthesis of a novel class of cdc25A inhibitors from vitamin D3.
Identification of a chemical tool for the orphan nuclear receptor FXR.
Enhanced pneumocystis carinii activity of new primaquine analogues.
Design, synthesis and biological evaluation of 7-azatricyclodecanes: analogues of cocaine.
(1,4-Benzothiazinyloxy)alkylpiperazine derivatives as potential antihypertensive agents.
Active site binding modes of HIV-1 integrase inhibitors.
Syntheses and antimalarial activities of 10-substituted deoxoartemisinins.
Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography.
Adenosine deaminase inhibitors: synthesis and biological evaluation of unsaturated, aromatic, and oxo derivatives of (+)-erythro-9-(2'S-hydroxy-3'R-nonyl)adenine [(+)-EHNA].
Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
5-Azidoimidacloprid and an acyclic analogue as candidate photoaffinity probes for mammalian and insect nicotinic acetylcholine receptors.
Protease inhibitors: current status and future prospects.
3-(4-Piperidinyl)- and 3-(8-aza-bicyclo[3.2.1]oct-3-yl)-2-phenyl-1H-indoles as bioavailable h5-HT2A antagonists.
Synthesis and binding studies of some epibatidine analogues.
A new class of highly cytotoxic diketopiperazines.
Cyclopentadienyltricarbonylrheniumbenzazepines: synthesis and binding affinity.
Synthesis and activity studies of conformationally restricted alpha-ketoamide factor Xa inhibitors.
Structure-activity study on the in vitro antiprotozoal activity of glutathione derivatives.
Artificial neural network applied to prediction of fluorquinolone antibacterial activity by topological methods.
SH2-directed ligands of the Lck tyrosine kinase.
Novel and selective calcitonin-inducing agents.
AMP deaminase inhibitors. 2. Initial discovery of a non-nucleotide transition-state inhibitor series.
Structure-activity relationship studies of flavopiridol analogues.
Synthesis of neurotensin(9-13) analogues exhibiting enhanced human neurotensin receptor binding affinities.
Design and synthesis of a novel water soluble benzotetrazepinone.
Structure-activity relationships of halichondrin B analogues: modifications at C.30-C.38.
The synthesis and in vitro cytotoxic studies of novel bis-naphthalimidopropyl polyamine derivatives.
Synthesis and biological activity of 1beta-methyl-2-[5'-isoxazoloethenylpyrrolidin-3'-ylthio]carbapenems.
Isoxazolines and isoxazoles as factor Xa inhibitors.
Neurosteroid analogues. 8. Structure-activity studies of N-acylated 17a-aza-D-homosteroid analogues of the anesthetic steroids (3alpha, 5alpha)- and (3alpha,5beta)-3-hydroxypregnan-20-one.
Hypocholesterolemic and hypolipidemic activity of some novel morpholine derivatives with antioxidant activity.
Difluoroketones as inhibitors of matrix metalloprotease-13.
Inhibition of dopamine receptors by endogenous amines: binding to striatal receptors and pharmacological effects on locomotor activity.
Potent nonpeptide endothelin antagonists: synthesis and structure-activity relationships of pyrazole-5-carboxylic acids.
Synthesis and biological evaluation of analogues of bacterial lipid I.
Macrocarpins A-D, new cytotoxic nor-triterpenes from Maytenus macrocarpa.
Cyclin-dependent kinase inhibitors: useful targets in cell cycle regulation.
Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels.
sp2-bridged diaryl retinoids: effects of bridge-region substitution on retinoid X receptor (RXR) selectivity.
Synthesis of tetrakis(multifluoro-4-pyridyl)porphin derivatives as acetylcholinesterase inhibitors.
Natural and synthetic analogues of actinomycin D as Grb2-SH2 domain blockers.
Syntheses and binding affinities of 6-nitroquipazine analogues for serotonin transporter. Part 1.
Structure-activity relationships of neuropeptide Y Y1 receptor antagonists related to BIBP 3226.
Synthesis and biological activity of phenoxyphenyl oxamic acid derivatives related to L-thyronine.
Studies on the novel anti-staphyloccal compound nematophin.
CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.
Synthesis and evaluation of quinoline carboxyguanidines as antidiabetic agents.
Synthesis and HIV-1 integrase inhibitory activities of caffeoylglucosides.
Some selective reactions of moenomycin A.
Synthesis and erythropoietin receptor binding affinities of N,N-disubstituted amino acids.
Synthesis of 5-substituted analogues of huperzine A.
Inhibition of the ras-dependent mitogenic pathway by phosphopeptide prodrugs with antiproliferative properties.
Discovery and SAR of org 24598-a selective glycine uptake inhibitor.
Amino acid derived sulfonamide hydroxamates as inhibitors of procollagen C-proteinase: solid-phase synthesis of ornithine analogues.
Coupling of the antennapedia third helix to a potent antagonist of the p53/hdm2 protein-protein interaction.
Evolution of anti-HIV drug candidates. Part 2: Diaryltriazine (DATA) analogues.
Anti-AIDS agents. Part 47: Synthesis and anti-HIV activity of 3-substituted 3',4'-Di-O-(S)-camphanoyl-(3'R,4'R)-(+)-cis-khellactone derivatives.
New anti-malarial flavonol glycoside from Hydrangeae Dulcis Folium.
The discovery of novel, potent and selective PDE5 inhibitors.
Bicyclic anti-VZV nucleosides: Thieno analogues retain full antiviral activity.
Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1.
Robinlin: a novel bioactive homo-monoterpene from Robinia pseudoacacia L. (Fabaceae).
Synthesis and structure-activity relationships of 1-phenylpyrazoles as xanthine oxidase inhibitors.
Study of aminoglycoside-nucleic acid interactions by an HPLC method.
Novel inhibitors of Leishmanial dihydrofolate reductase.
Allyl and propargyl substituted penam sulfones as versatile intermediates toward the syntheses of new beta-lactamase inhibitors.
[Lys3]Didemnins as potential affinity ligands.
Novel antitumor artemisinin derivatives targeting G1 phase of the cell cycle.
Synthesis and biological activity of the 1alpha,25-dihydroxyvitamin D3 diastereomer with unnatural configuration at the rings C/D side-chain moiety.
Synthesis and antifungal activities of novel 1,3-beta-D-glucan synthase inhibitors. Part 2.
Design, synthesis and enzymatic activity of highly selective human mitochondrial thymidine kinase inhibitors.
Synthesis and hydrolytic stability studies of albendazole carrier prodrugs.
Arylsulphonyl hydroxamic acids: potent and selective matrix metalloproteinase inhibitors.
Covalently induced activation of the delta opioid receptor by a fluorogenic affinity label, 7'-(phthalaldehydecarboxamido)naltrindole (PNTI).
Property-based design: optimization of drug absorption and pharmacokinetics.
(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
Synthesis of tetrocarcin derivatives with specific inhibitory activity towards Bcl-2 functions.
Combretoxazolones: synthesis, cytotoxicity and antitumor activity.
Sorbitol dehydrogenase inhibitors (SDIs): a new potent, enantiomeric SDI, 4-[2-1R-hydroxy-ethyl)-pyrimidin-4-yl]piperazine-1-sulfonic acid dimethylamide.
Bisubstrate ketone analogues as serotonin N-acetyltransferase inhibitors.
Terminally alkylated polyamine analogues as chemotherapeutic agents.
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
Bicyclic analogues of D-myo-inositol 1,4,5-trisphosphate related to adenophostin A: synthesis and biological activity.
Phenylpiperazinylalkylamino substituted pyridazinones as potent alpha(1) adrenoceptor antagonists.
Synthesis of cytotoxic 6E-hydroximino-4-ene steroids: structure/activity studies.
The first potent and selective inhibitors of the glycine transporter type 2.
Discovery of estrogen sulfotransferase inhibitors from a purine library screen.
New 3'-azido-3'-deoxythymidin-5'-yl O-(4-hydroxyalkyl or -alkenyl or -alkylepoxide) carbonate prodrugs: synthesis and anti-HIV evaluation.
Antimalarial simplified 3-aryltrioxanes: synthesis and preclinical efficacy/toxicity testing in rodents.
A new class of symmetric bisbenzimidazole-based DNA minor groove-binding agents showing antitumor activity.
From hit to lead. Analyzing structure-profile relationships.
Synthesis of potent C(2)-symmetric, diol-based hiv-1 protease inhibitors. Investigation of thioalkyl and thioaryl P1/P1' substituents.
Quinoline-4-acetamides as sPLA(2) inhibitors.
Prodrugs of 3-amido bearing pseudomycin analogues: novel antifungal agents.
Synthesis and antiproliferative activity of some thiazolylbenzimidazole-4,7-diones.
Serotonergic and dopaminergic activities of rigidified (R)-aporphine derivatives.
Structure-activity relationships of novel anti-malarial agents. Part 2: cinnamic acid derivatives.
Synthesis and biological evaluation of DNA targeting flexible side-chain substituted beta-carboline derivatives.
Synthesis and monoamine transporter affinity of 3beta-(4-(2-pyrrolyl)phenyl)-8-azabicycl.
Exploring the relationship between binding modes of 9-(aminomethyl)-9,10-dihydroanthracene and cyproheptadine analogues at the 5-HT2A serotonin receptor.
New 5-HT1A receptor agonists possessing 1,4-benzoxazepine scaffold exhibit highly potent anti-ischemic effects.
3-Anilino-4-arylmaleimides: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).
NO-independent stimulators of soluble guanylate cyclase.
Spatial requirements of the antagonist binding site of the NK2 receptor.
HIV Rev peptides conjugated with peptide nucleic acids and their efficient binding to RRE RNA.
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.
New pyridoquinoline derivatives as potential inhibitors of the fluoroquinolone efflux pump in resistant Enterobacter aerogenes strains.
Synthesis and antibacterial activity of acylides (3-O-acyl-erythromycin derivatives): a novel class of macrolide antibiotics.
N-[3-(2-Dimethylaminoethyl)-2-methyl-1H- indol-5-yl]-4-fluorobenzamide: a potent, selective, and orally active 5-HT(1F) receptor agonist potentially useful for migraine therapy.
Synthesis and biological evaluation of myoseverin derivatives: microtubule assembly inhibitors.
[3H]N-2-(4-(N-benzamido)phenyl)propyl-2-propanesulfonamide: a novel AMPA receptor potentiator and radioligand.
AMP deaminase inhibitors. 5. Design, synthesis, and SAR of a highly potent inhibitor series.
Perspectives in animal health: old targets and new opportunities.
Molecular design, synthesis, and hypoglycemic activity of a series of thiazolidine-2,4-diones.
Analogues of amonafide and azonafide with novel ring systems.
Discovery of potent antagonists of the interaction between human double minute 2 and tumor suppressor p53.
Privileged molecules for protein binding identified from NMR-based screening.
Structural determinants of efficacy for kappa opioid receptors in the orvinol series: 7,7-spiro analogues of buprenorphine.
7-Chloro-4,5-dihydro-8-(1,2,4-triazol-4-yl)-4-oxo-1,2,4-triazolo[1, 5-a]quinoxaline-2- carboxylates as novel highly selective AMPA receptor antagonists.
Palladium-catalyzed cross-coupling reactions for the synthesis of 6, 8-disubstituted 1,7-naphthyridines: a novel class of potent and selective phosphodiesterase type 4D inhibitors.
Synthesis and cytotoxic and antitumor activity of benzo[b]pyrano[3, 2-h]acridin-7-one analogues of acronycine.
De novo design of a novel oxazolidinone analogue as a potent and selective alpha1A adrenergic receptor antagonist with high oral bioavailability.
A refined 3-dimensional QSAR of cytochrome P450 2C9: computational predictions of drug interactions.
The discovery of anthranilic acid-based MMP inhibitors. Part 1: SAR of the 3-position.
Naphthalene derivatives: A new series of selective cyclooxygenase-2 inhibitors.
Anti-Trypanosoma activity of some natural stilbenoids and synthetic related heterocyclic compounds.
Studies on 3-deoxy-D-manno-octulosonic acid 8-phosphate synthase using chorismate mutase inhibitors.
Design, synthesis, and biological activity of diiminoisoindolines as complement component 3a antagonists.
Synthesis of the first example of a C2-C3/C2'-C3'-endo unsaturated pyrrolo[2,1-c][1,4]benzodiazepine dimer.
Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS).
Flavonoids: structural requirements for antiproliferative activity on breast cancer cells.
Quinoline-3-carbothioamides and related compounds as novel immunomodulating agents.
Thiourea-based gemfibrozil analogues as HDL-elevating agents.
Novel nucleotide phosphonate analogues with potent antitumor activity.
A survey of cyclic replacements for the central diamide moiety of inhibitors of inosine monophosphate dehydrogenase.
Synthesis and NK(1)/NK(2) binding activities of a series of diacyl-substituted 2-arylpiperazines.
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity.
Design and synthesis of ethyl pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.
6-Acylamino-penam derivatives: synthesis and inhibition of cathepsins B, L, K, and S.
Six-membered cyclic ureas as HIV-1 protease inhibitors: a QSAR study based on CODESSA PRO approach. Quantitative structure-activity relationships.
Synthesis of new Targretin analogues that induce apoptosis in leukemia HL-60 cells.
Synthetic studies of cis-4-Amino-L-proline derivatives as novel lipid lowering agents.
5-Bromo (or chloro)-6-azido-5,6-dihydro-2' -deoxyuridine and -thymidine derivatives with potent antiviral activity.
Synthesis and antibacterial evaluation of novel 2-[N-Imidoylpyrrolidinyl] carbapenems.
Discovery of 5-hydroxyalkyl-4-phenylpyridines as a new class of glucagon receptor antagonists.
Amide derivatives of meclofenamic acid as selective cyclooxygenase-2 inhibitors.
2-(anilinomethyl)imidazolines as alpha1A adrenergic receptor agonists: 2'-heteroaryl and 2'-oxime ether series.
Solution and solid-phase synthesis of potent inhibitors of hepatitis C virus NS3 proteinase.
Benzylidene rhodanines as novel inhibitors of UDP-N-acetylmuramate/L-alanine ligase.
Potent P1' biphenylmethyl substituted aggrecanase inhibitors.
New readily accessible peroxides with high anti-malarial potency.
2-Amino-7-deazaadenine forms stable base pairs with cytosine and thymine.
Shikonin derivatives: synthesis and inhibition of human telomerase.
Polyhydroxylated azepanes as new motifs for DNA minor groove binding agents.
New highly active taxoids from 9beta-dihydrobaccatin-9,10-acetals. Part 2.
Arylamidrazones as novel corticotropin releasing factor receptor antagonists.
2-(Anilinomethyl)imidazolines as alpha1 adrenergic receptor agonists: the discovery of alpha1a subtype selective 2'-alkylsulfonyl-substituted analogues.
Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators.
Electrochemical and peroxidase oxidation study of N'-hydroxyguanidine derivatives as NO donors.
One-pot synthesis of benzo[b]furan and indole inhibitors of tubulin polymerization.
Acylating agents as enzyme inhibitors and understanding their reactivity for drug design.
Structurally simple trichostatin A-like straight chain hydroxamates as potent histone deacetylase inhibitors.
Lepadins D-F: antiplasmodial and antitrypanosomal decahydroquinoline derivatives from the tropical marine tunicate Didemnum sp.
Novel retinoid X receptor antagonists: specific inhibition of retinoid synergism in RXR-RAR heterodimer actions.
New stereocontrolled synthesis and biological evaluation of 5-(1'-hydroxyalkyl)-3-methylidenetetrahydro-2-furanones as potential cytotoxic agents.
Refinement and evaluation of a pharmacophore model for flavone derivatives binding to the benzodiazepine site of the GABA(A) receptor.
Synthesis and biolocalization of water-soluble sapphyrins.
Discovery of the first nonpeptide agonist of the GPR14/urotensin-II receptor: 3-(4-chlorophenyl)-3-(2- (dimethylamino)ethyl)isochroman-1-one (AC-7954).
Synthesis and cytotoxicity of 2alpha-amido docetaxel analogues.
Solid-phase synthesis of thrombin inhibitors.
Discovery of potent and selective small molecule NPY Y5 receptor antagonists.
Solid-phase synthesis and investigation of benzofurans as selective estrogen receptor modulators.
Solid-phase synthesis of dual alpha4beta1/alpha4beta7 integrin antagonists: two scaffolds with overlapping pharmacophores.
New indene-derivatives with anti-proliferative properties.
2-Arylindoles as gonadotropin releasing hormone (GnRH) antagonists: optimization of the tryptamine side chain.
Synthesis and antibacterial activity of linezolid analogues.
Antibody-catalyzed cleavage of the D-Ala-D-Lac depsipeptide: an immunological approach to the problem of vancomycin resistance.
New highly active taxoids from 9 beta-dihydrobaccatin-9,10-acetals.
Novel estimation of lipophilic behaviour of polychlorinated biphenyls.
Thiophene derivatives: a new series of potent norepinephrine and serotonin reuptake inhibitors.
Synthesis and in vitro evaluation of a novel iodinated resiniferatoxin derivative that is an agonist at the human vanilloid VR1 receptor.
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 2: SAR of the acetylenic P1' group.
Induction of apoptosis by aryl-substituted diamines: role of aromatic group substituents and distance between nitrogens.
Design and synthesis of aminophenol-based factor Xa inhibitors.
Tryptophanyl phosphoramidates as prodrugs of synadenol and its E-isomer: synthesis and biological activity.
Bromotyrosine-derived natural and synthetic products as inhibitors of mycothiol-S-conjugate amidase.
Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade.
Spirocyclic NK(1) antagonists II: [4.5]-spiroethers.
Antifungal sordarins. Synthesis and structure-activity relationships of 3',4'-fused dioxolane and dioxane derivatives.
Synthesis and evaluation of novel quinolinones as HIV-1 reverse transcriptase inhibitors.
Simplified catechin-gallate inhibitors of HIV-1 reverse transcriptase.
Alpha-ketoester-based photobiological switches: synthesis, peptide chain extension and assay against alpha-chymotrypsin.
Synthesis and structure-activity relationships of 5-substituted pyridine analogues of 3.
Inhibition of RANTES/CCR1-mediated chemotaxis by cosalane and related compounds.
Novel, potent, and selective phosphodiesterase 5 inhibitors: synthesis and biological activities of a series of 4-aryl-1-isoquinolinone derivatives.
Synthesis of 1-benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole analogues as novel antiplatelet agents.
Synthesis and screening for antiacetylcholinesterase activity of (1-benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles related to donepezil.
Oxindole derivatives as orally active potent growth hormone secretagogues.
Cyclic imides as potent and selective alpha-1A adrenergic receptor antagonists.
Synthesis of 7,8-disubstituted benzolactam-V8 and its binding to protein kinase C.
Human beta3 adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties.
Beta-D-glycosylamidines: potent, selective, and easily accessible 1-glycosidase inhibitors.
Syntheses and biological activities of a novel group of steroidal derived inhibitors for human Cdc25A protein phosphatase.
SAR of 2,6-diamino-3,5-difluoropyridinyl substituted heterocycles as novel p38MAP kinase inhibitors.
Novel thiophene derivatives for the treatment of benign prostatic hyperplasia.
Isothiazole dioxides: synthesis and inhibition of Trypanosoma brucei protein farnesyltransferase.
Synthesis of nitroindole derivatives with high affinity and selectivity for melatoninergic binding sites MT(3).
A solid-phase approach towards the synthesis of PDE5 inhibitors.
Opioid activity of 4-imidazolidinone positional analogues of Leu-Enkephalin.
Electrostatic potential surfaces of 5-HT(3)R agonists suggest accessory cation-pi site adjacent to agonist binding domain.
Antimalarial activity of yingzhaosu A analogues.
Comparison of 3D structures and AT(1) binding properties of pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones with parent antihypertensive drug irbesartan.
Corrigendum to Synthesis and anti-angiogenic activity of 6-(1,2,4-thiadiazol-5-yl)-3-amino pyridazine derivatives [Bioorg. Med. Chem. Lett. 12 (2002) 589]
Synthesis and biological evaluation of an N10-Psec substituted pyrrolo[2,1-c][1,4]benzodiazepine prodrug.
Specific accumulation and growth inhibitory effects of hybrid liposomes to hepatoma cells in vitro.
Synthesis and antiproliferative activity of a new compound containing an alpha-methylene-gamma-lactone group.
A comparative molecular field analysis (COMFA) of the structural determinants of heat-stable enterotoxins mediating activation of guanylyl cyclase C.
Antibacterial activity of G6-quaternary ammonium derivatives of a lipophilic vancomycin analogue.
Urea small molecule agonists on mouse melanocortin receptors.
Synthesis and in vitro activity of new methylenepiperidinyl and methylenepyrrolidinyl oxazolidinone antibacterial agents.
Heterocyclic thrombin inhibitors. Part 1: design and synthesis of amidino-phenoxy quinoline derivatives.
Novel inhibitors of procollagen C-proteinase. Part 2: glutamic acid hydroxamates.
Are 5'-O-carbamate-2',3'-dideoxythiacytidine new anti-HIV and anti-HBV nucleoside drugs or prodrugs?
Synthesis, biological evaluation and DNA binding properties of novel bleomycin analogues.
Tetrabiphenylporphyrin-based receptors for protein surfaces show sub-nanomolar affinity and enhance unfolding.
Suzuki cross-coupling approaches to the synthesis of bioactive 3-substituted and 5-substituted-4-methoxy-6-methyl-2-pyrones.
A specific anti-Helicobacter pylori agent NE2001: synthesis and its effect on the growth of H. pylori.
Substituted bridged phenyl piperidines: orally active growth hormone secretagogues.
Caged RNase: photoactivation of the enzyme from perfect off-state by site-specific incorporation of 2-nitrobenzyl moiety.
5-aryl-pyrazolo[3,4-b]pyridazines: potent inhibitors of glycogen synthase kinase-3 (GSK-3).
New classes of antibacterial oxazolidinones with C-5, methylene O-linked heterocyclic side chains.
Iclaprim, a novel diaminopyrimidine with potent activity on trimethoprim sensitive and resistant bacteria.
A simple stereoselective synthesis and biological evaluation of FR181157: orally active prostacyclin mimetic.
New cerebrosides from Euphorbia peplis L.: antimicrobial activity evaluation.
Substituted azoloquinolines and -quinazolines as new potent farnesyl protein transferase inhibitors.
Synthesis and anti-HIV properties of new water-soluble bis-functionalized[60]fullerene derivatives.
Novel mechanism of inhibiting beta-lactamases by sulfonylation using beta-sultams.
Synthesis and evaluation of delta-lactams (piperazones) as elastase inhibitors.
Quinoline-carboxylic acids are potent inhibitors that inhibit the binding of insulin-like growth factor (IGF) to IGF-binding proteins.
Arylaminoethyl amides as inhibitors of the cysteine protease cathepsin K-investigating P1' substituents.
2-Phenylspiroindenes: a novel class of selective estrogen receptor modulators (SERMs).
1,4-Diazepane-2-ones as novel inhibitors of LFA-1.
Cephalosporin prodrugs of paclitaxel for immunologically specific activation by L-49-sFv-beta-lactamase fusion protein.
Pyridazinones as selective cyclooxygenase-2 inhibitors.
Biological evaluation and interconversion studies of rotamers of SCH 351125, an orally bioavailable CCR5 antagonist.
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.
Hydroporphyrins as tumour photosensitizers: synthesis and photophysical studies of 2,3-dihydro-5,15-di(3,5-dihydroxyphenyl) porphyrin.
Bis-sulfonamides as endothelin receptor antagonists.
Synthesis and photoreactivity of caged blockers for glutamate transporters.
5-aryl thiazolidine-2,4-diones: discovery of PPAR dual alpha/gamma agonists as antidiabetic agents.
Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.
Differentially functionalized diamines as novel ligands for the NPY2 receptor.
Thiourea inhibitors of herpes viruses. Part 1: bis-(aryl)thiourea inhibitors of CMV.
Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines.
Anilinopyrazole as selective CDK2 inhibitors: design, synthesis, biological evaluation, and X-ray crystallographic analysis.
Synthesis and cytotoxic activity of A-ring modified betulinic acid derivatives.
Synthesis of a novel family of diterpenes and their evaluation as anti-inflammatory agents.
Structure activity studies of a novel cytotoxic benzodiazepine.
Synthesis and anticancer effect of B-ring trifluoromethylated flavonoids.
Synthesis and biological evaluation of thymine nucleosides fused with 3',4'-tetrahydrofuran ring.
Structure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications.
Nortropinyl-arylsulfonylureas as novel, reversible inhibitors of human steroid sulfatase.
Synthesis and X-ray crystal structures of substituted fluorobenzene and benzoquinone inhibitors of the tissue factor VIIa complex.
Synthesis of linked carbohydrates and evaluation of their binding for 16S RNA by mass spectrometry.
Synthesis of 2-fluoronoraristeromycin and its inhibitory activity against Plasmodium falciparum S-adenosyl-L-homocysteine hydrolase.
Discovery and initial SAR of 2-amino-5-carboxamidothiazoles as inhibitors of the Src-family kinase p56(Lck).
Hepatoprotective pyrrole derivatives of Lycium chinense fruits.
Inactivation of S-adenosyl-L-homocysteine hydrolase with novel 5'-thioadenosine derivatives. Antiviral effects.
2,4-disubstituted pyrimidines: a novel class of KDR kinase inhibitors.
Synthesis and activity of a C-8 keto pleuromutilin derivative.
Multidrug resistance reversal activity of key ningalin analogues.
Quantitative structure--activity relations for gammadelta T cell activation by phosphoantigens.
Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
Discovery of a 3-amino-6-phenyl-pyridazine derivative as a new synthetic antineuroinflammatory compound.
Identification of potent and selective mechanism-based inhibitors of the cysteine protease cruzain using solid-phase parallel synthesis.
Synthesis and biological evaluation of a new furo[2,3-h]quinolin-2(1H)-one.
Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.
6-Aryl-1,4-dihydro-benzo[d][1,3]oxazin- 2-ones: a novel class of potent, selective, and orally active nonsteroidal progesterone receptor antagonists.
Enhancement of nucleoside cytotoxicity through nucleotide prodrugs.
N-(arylacetyl)-biphenylalanines as potent VLA-4 antagonists.
Identification of unique VLA-4 antagonists from a combinatorial library.
Bioactive 4-substituted-6-methyl-2-pyrones with promising cytotoxicity against A2780 and K562 cell lines.
Antitumor agents. Part 215: antitubulin effects of cytotoxic B-ring modified allocolchicinoids.
Novel amide-based inhibitors of inosine 5'-monophosphate dehydrogenase.
Small ligands interacting with the phosphotyrosine binding pocket of the Src SH2 protein.
Design and synthesis of a novel L-dopa-entacapone codrug.
Synthesis and antimycobacterial activity of 6-arylpurines: the requirements for the N-9 substituent in active antimycobacterial purines.
Beta-C-mannosides as selectin inhibitors.
Synthesis and SAR of conformationally restricted inhibitors of soluble epoxide hydrolase.
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists.
Hydantoin derivatives as non-peptidic inhibitors of Ras farnesyl transferase.
A series of 23,24-dihydrodiscodermolide analogues with simplified lactone regions.
An efficient, asymmetric solid-phase synthesis of benzothiadiazine-substituted tetramic acids: potent inhibitors of the hepatitis C virus RNA-dependent RNA polymerase.
Beta'-hydroxy-alpha,beta-unsaturated ketones: a new pharmacophore for the design of anticancer drugs.
Discovery of novel heterocyclic factor VIIa inhibitors.
Taxoid from the needles of the Himalayan yew Taxus wallichiana with cytotoxic and immunomodulatory activities.
Heteroaromatic side-chain analogs of pregabalin.
The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.
Identification of potent phenyl imidazoles as opioid receptor agonists.
Optimization of 2-aminothiazole derivatives as CCR4 antagonists.
Vasorelaxant activity of phthalazinones and related compounds.
(R)-sila-venlafaxine: a selective noradrenaline reuptake inhibitor for the treatment of emesis.
Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors.
Disrupting antibiotic resistance propagation by inhibiting the conjugative DNA relaxase.
Identification of anti-prion compounds as efficient inhibitors of polyglutamine protein aggregation in a zebrafish model.
Diazonamide toxins reveal an unexpected function for ornithine delta-amino transferase in mitotic cell division.
New 9-thiocyanatopupukeanane sesquiterpenes from the nudibranch Phyllidia varicosa and its sponge-prey Axinyssa aculeata.
A new class of acyclic 2-alkyl-1,1,2-triaryl (Z)-olefins as selective cyclooxygenase-2 inhibitors.
Synthesis and biological evaluation of stilbene-based pure estrogen antagonists.
Rational design of 6-methylsulfonylindoles as selective cyclooxygenase-2 inhibitors.
Formation of squaric acid amides of anthracycline antibiotics. Synthesis and cytotoxic properties.
Design and synthesis of conformationally constrained 3-(N-alkylamino)propylphosphonic acids as potent agonists of sphingosine-1-phosphate (S1P) receptors.
Synthesis and evaluation of novel oxazoline MMP inhibitors.
5-Carboxamido-1,3,2-dioxaphosphorinanes, potent inhibitors of MTP.
3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction.
Biaryl guanidine inhibitors of in vitro HCV-IRES activity.
N-[2-[2-(4-Phenylbutyl)benzofuran-4-yl]cyclopropylmethyl]acetamide: an orally bioavailable melatonin receptor agonist.
Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists.
5-Amidinoindoles as dual inhibitors of coagulation factors IXa and Xa.
Plasmepsin II inhibition and antiplasmodial activity of Primaquine-Statine 'double-drugs'.
Pseudodeflectusin, a novel isochroman derivative from Aspergillus pseudodeflectus a parasite of the sea weed, Sargassum fusiform, as a selective human cancer cytotoxin.
Synthesis and biological evaluation of (-)-laulimalide analogues.
New oligomers of conduritol-F and muco-inositol. Synthesis and biological evaluation as glycosidase inhibitors.
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 1: Identification and synthesis of phenyl-tetrazolyl acetophenones.
Nonpeptidic, noncovalent inhibitors of the cysteine protease cathepsin S.
Bis[3-(4'-substituted phenyl)prop-2-ene]disulfides as a new class of antihyperlipidemic compounds.
Ceramicines B-D, new antiplasmodial limonoids from Chisocheton ceramicus.
DNA photocleavage by porphyrin-polyamine conjugates.
Pestalofones A-E, bioactive cyclohexanone derivatives from the plant endophytic fungus Pestalotiopsis fici.
Synthesis of novel 1,4-benzoxazin-3-one derivatives as inhibitors against tyrosine kinases.
Structure-activity relationships of antitubercular nitroimidazoles. 1. Structural features associated with aerobic and anaerobic activities of 4- and 5-nitroimidazoles.
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.
10-(2-oxo-2-phenylethylidene)-10H-anthracen-9-ones as highly active antimicrotubule agents: synthesis, antiproliferative activity, and inhibition of tubulin polymerization.
Structure-activity relationship analysis of novel derivatives of narciclasine (an Amaryllidaceae isocarbostyril derivative) as potential anticancer agents.
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
Synthesis and in vitro anti-Helicobacter pylori activity of N-[5-(5-nitro-2-heteroaryl)-1,3,4-thiadiazol-2-yl]thiomorpholines and related compounds.
A small molecule inhibitor of alpha4 integrin-dependent cell migration.
Sidechain-linked inhibitors of HIV-1 protease dimerization.
Design, synthesis and preliminary evaluation of novel pyrrolidine derivatives as matrix metalloproteinase inhibitors.
Alpha-mercaptoketone based histone deacetylase inhibitors.
Anthranilimide-based glycogen phosphorylase inhibitors for the treatment of Type 2 diabetes: 2. Optimization of serine and threonine ether amino acid residues.
Fluoroolefins as amide bond mimics in dipeptidyl peptidase IV inhibitors.
Discovery of piperazinylimidazo[1,2-a]pyridines as novel S4 binding elements for orally active factor Xa inhibitors.
Design and synthesis of a pyrido[2,3-d]pyrimidin-5-one class of anti-inflammatory FMS inhibitors.
Novel cholesterol biosynthesis inhibitors targeting human lanosterol 14alpha-demethylase (CYP51).
Structure-based design and synthesis of benzimidazole derivatives as dipeptidyl peptidase IV inhibitors.
Investigation of novel 7,8-disubstituted-5,10-dihydro-dibenzo[b,e][1,4]diazepin-11-ones as potent Chk1 inhibitors.
Role of benzimidazole (Bid) in the delta-opioid agonist pseudopeptide H-Dmt-Tic-NH-CH(2)-Bid (UFP-502).
Synthesis and antiviral activities of novel chiral cyanoacrylate derivatives with (E) configuration.
Hepatitis C virus NS3 protease inhibitors comprising a novel aromatic P1 moiety.
Antifungal and cytotoxic activities of some N-substituted aniline derivatives bearing a hetaryl fragment.
Synthesis of insecticidal fluorinated anthranilic diamides.
Electronic effects of para-substitution on acetophenones in the reaction of rat liver 3alpha-hydroxysteroid dehydrogenase.
N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists.
Cytotoxic simplified tubulysin analogues.
Mathemycin B, a new antifungal macrolactone from actinomycete species HIL Y-8620959.
Biologically active triterpene saponins from callus tissue of Polygala amarella.
A new tyrosine kinase inhibitor from the marine brown alga Stypopodium zonale.
ent-kaurane diterpenoids from Isodon lungshengensis.
Structure of the deacetylase LpxC bound to the antibiotic CHIR-090: Time-dependent inhibition and specificity in ligand binding.
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
First identification of Pseudomonas aeruginosa isolates producing a KPC-type carbapenem-hydrolyzing beta-lactamase.
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
Eurysterols A and B, cytotoxic and antifungal steroidal sulfates from a marine sponge of the genus Euryspongia.
Pharmacological properties of bivalent ligands containing butorphan linked to nalbuphine, naltrexone, and naloxone at mu, delta, and kappa opioid receptors.
Synthesis and biological evaluation of 2- and 3-aminobenzo[b]thiophene derivatives as antimitotic agents and inhibitors of tubulin polymerization.
Synthesis of S-dialkylarsino-3-mercapto-1,2-propanediols and evaluation of their anticancer activity.
Glutamine vinyl ester proteasome inhibitors selective for trypsin-like (beta2) subunit.
Design and synthesis of new potent dipeptidyl peptidase IV inhibitors with enhanced ex vivo duration.
Design and synthesis of novel prodrugs of 2'-deoxy-2'-methylidenecytidine activated by membrane dipeptidase overexpressed in tumor tissues.
Impact on farnesyltransferase inhibition of 4-chlorophenyl moiety replacement in the Zarnestra series.
New bioactive diterpene polyesters from Euphorbia decipiens.
Divinatorins A-C, new neoclerodane diterpenoids from the controlled sage Salvia divinorum.
Novel oxylipin metabolites from the brown alga Eisenia bicyclis.
Two new epimeric pairs of acetogenins bearing a carbonyl group from Annona cherimolia seeds.
New cytotoxic sesterterpenoids and norsesterterpenoids from two sponges of the genus Sarcotragus.
Structurally simplified macrolactone analogues of halichondrin B.
3D QSAR studies of N-4-arylacryloylpiperazin-1-yl-phenyl-oxazolidinones: a novel class of antibacterial agents.
Synthesis and anticancer activity of brefeldin A ester derivatives.
A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.
Imidazole-dioxolane compounds as isozyme-selective heme oxygenase inhibitors.
Arylpiperazines with N-acylated amino acids as 5-HT1A receptor ligands.
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids.
Phosphonic acid-containing analogues of mycophenolic acid as inhibitors of IMPDH.
Extremely potent orally active benzo[g]quinoline analogue of the dopaminergic prodrug: 1-propyl-trans-2,3,4,4a,5,7,8,9,10,10a-decahydro-1H-benzo-[g]quinolin-6-one [corrected].
The discovery of fluoropyridine-based inhibitors of the factor VIIa/TF complex--Part 2.
Pyridazines part 41: synthesis, antiplatelet activity and SAR of 2,4,6-substituted 5-(3-oxo-3-phenylprop-1-en-1-yl)- or 5-(3-phenylprop-2-enoyl)pyridazin-3(2H)-ones.
Enhanced FTase activity achieved via piperazine interaction with catalytic zinc.
Design and synthesis of promiscuous high-affinity monoamine transporter ligands: unraveling transporter selectivity.
Structure-activity relationships of alpha-amino acid ligands for the alpha2delta subunit of voltage-gated calcium channels.
Potent 2-[(pyrimidin-4-yl)amine}-1,3-thiazole-5-carbonitrile-based inhibitors of VEGFR-2 (KDR) kinase.
Novel 1alpha,25-dihydroxyvitamin D3 analogues with the side chain at C12.
2-Alkyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles as novel 5-HT6 receptor agonists.
Synthesis and in vitro pharmacological studies of C(4) modified salvinorin A analogues.
Novel, selective indole-based ECE inhibitors: lead optimization via solid-phase and classical synthesis.
Dipyridyl amines: potent metabotropic glutamate subtype 5 receptor antagonists.
Thyrotropin-releasing hormone (TRH) analogues that exhibit selectivity to TRH receptor subtype 2.
Indole-3-acetic acid antagonists of the prostaglandin D2 receptor CRTH2.
Glycodiversification for the optimization of the kanamycin class aminoglycosides.
Synthesis and pharmacological evaluation of 1H-imidazoles as ligands for the estrogen receptor and cytotoxic inhibitors of the cyclooxygenase.
Selective inhibition of MCF-7(piGST) breast tumors using glutathione transferase-derived 2-methylene-cycloalkenones.
Synthesis of classical, four-carbon bridged 5-substituted furo[2,3-d]pyrimidine and 6-substituted pyrrolo[2,3-d]pyrimidine analogues as antifolates.
Rational approach to discover multipotent anti-Alzheimer drugs.
Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme.
Novel CCR1 antagonists with oral activity in the mouse collagen induced arthritis.
Structural basis of inhibitor specificity of the human protooncogene proviral insertion site in moloney murine leukemia virus (PIM-1) kinase.
Discovery of a potent, orally available, and isoform-selective retinoic acid beta2 receptor agonist.
Heteroaryl-O-glucosides as novel sodium glucose co-transporter 2 inhibitors. Part 1.
Harbinatic acid, a novel and potent DNA polymerase beta inhibitor from Hardwickia binata.
Sesquiterpene lactones from neurolaena oaxacana
New geodiamolides from the sponge Cymbastela sp. collected in Papua New Guinea.
Isolation of two highly methylated polyketide derivatives from a yew-associated penicillium species
Secobatzellines A and B, two new enzyme inhibitors from a deep-water Caribbean sponge of the genus Batzella.
Antibacterial diterpenoid acids from Azorella compacta.
Montadial A, a cytotoxic metabolite from Bondarzewia montana.
A new bisabolene epoxide from Tussilago farfara, and inhibition of nitric oxide synthesis in LPS-activated macrophages.
Limonoids from Swietenia macrophylla and S. aubrevilleana.
Methylsulfomycin I, a new cyclic peptide antibiotic from a Streptomyces sp. HIL Y-9420704.
Oceanapiside, an antifungal bis-alpha,omega-amino alcohol glycoside from the marine sponge Oceanapia phillipensis.
Synthesis and biological properties of 2-methylene-19-nor-25-dehydro-1alpha-hydroxyvitamin D(3)-26,23-lactones--weak agonists.
Discovery of pyrazolopyrimidines as the first class of allosteric agonists for the high affinity nicotinic acid receptor GPR109A.
Phenylethyl cinnamides: a new series of alpha-glucosidase inhibitors from the leaves of Aegle marmelos.
Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.
Molecular design of potent tyrosinase inhibitors having the bibenzyl skeleton.
CYP19 (aromatase): exploring the scaffold flexibility for novel selective inhibitors.
Design and synthesis of 2-amino-isoxazolopyridines as Polo-like kinase inhibitors.
Synthesis and biological activity of enantiomeric pairs of 5-[(E)-cycloalk-2-enylidenemethyl]thiolactomycin congeners.
Tricholomalides A-C, new neurotrophic diterpenes from the mushroom Tricholoma sp.
New strongylophorines from the Okinawan marine sponge Petrosia (Strongylophora) corticata.
Discorhabdins S, T, and U, new cytotoxic pyrroloiminoquinones from a deep-water Caribbean sponge of the genus Batzella.
Isoflavans and a Stilbene from Wood of the Decay-Resistant Tropical Tree Diphysa robinioides
Novel Acetylenic Acids from the Root Bark of Paramacrolobium caeruleum: Inhibitors of 3-Hydroxy-3-methyl-glutaryl Coenzyme A Reductase
Pentagalloylglucose, a xanthine oxidase inhibitor from a Paraguayan crude drug, "Molle-i" (Schinus terebinthifolius).
Pharmacologically Active Metabolites from Symbiotic Microalgae in Okinawan Marine Invertebrates
Alkaloids from the Leaves of Prosopis juliflora
Bioactive compounds from the root of Myrsine africana.
4-Hydroxy-25-desoxyneorollinicin, a new bistetrahydrofuranoid acetogenin from Rollinia papilionella.
Isolation and characterization of an antimalarial agent of the neem tree Azadirachta indica.
Cytotoxic macrolides from a cultured marine dinoflagellate of the genus Amphidinium.
1-Aryl Tetralin Lignans from Larrea tridentata
Turbinaric acid, a cytotoxic secosqualene carboxylic acid from the brown alga Turbinaria ornata.
Terpenoids from the North Adriatic Sponge Spongia officinalis
Brominated indole alkaloids from the marine tunicate Pseudodistoma arborescens.
Isolation and identification of an antifungal naphthopyran derivative from Rhinacanthus nasutus.
Luffariolides F and G, new manoalide derivatives from the Okinawan marine sponge Luffariella sp.
The Isolation of Majusculamide C from the Sponge Ptilocaulis trachys Collected in Enewetak and Determination of the Absolute Configuration of the 2-Methyl-3-aminopentanoic Acid Residue
Structure and stereochemistry of pectinolides A-C, novel antimicrobial and cytotoxic 5,6-dihydro-alpha-pyrones from Hyptis pectinata.
Antihypertensive Activity of Corilagin and Chebulinic Acid, Tannins from Lumnitzera, racemosa
A New Brominated Indole-3-carbaldehyde from the Marine Bryozoan Zoobotryon verticillatum
An antifungal bibenzyl from the New Zealand liverwort, Plagiochila stephensoniana. Bioactivity-directed isolation, synthesis, and analysis.
Constituents of Fevillea cordifolia: New Norcucurbitacin and Cucurbitacin Glycosides
Les Chimanines, Nouvelles Quinoleines Substituees en 2, Isolees d'Une Plante Bolivienne Antiparasitaire: Galipea longiflora
Three New Bromotyrosine-Derived Metabolites of the Sponge Psammaplysilla purpurea
Knerachelins A and B, antibacterial phenylacylphenols from Knema furfuracea.
A cytotoxic beta-carboline from the bryozoan Catenicella cribraria.
Two new modified trichothecenes from Fusarium sporotrichioides.
Three New Toxic Pinolidoxins from Ascochyta pinodes
Binding of an imidazopyridoindole at imidazoline I2 receptors.
Synthesis and biological activity of new quinoxaline antibiotics of echinomycin analogues.
TMC-95A, a reversible proteasome inhibitor, induces neurite outgrowth in PC12 cells.
Scaffold of the cyclooxygenase-2 (COX-2) inhibitor carprofen provides Alzheimer gamma-secretase modulators.
Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.
N,N'-Bisbenzylidenebenzene-1,4-diamines and N,N'-Bisbenzylidenenaphthalene-1,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors.
Identification of phosphinate dipeptide analog inhibitors directed against the Plasmodium falciparum M17 leucine aminopeptidase as lead antimalarial compounds.
Discovery of 5-substituted-6-chlorouracils as efficient inhibitors of human thymidine phosphorylase.
Synthesis and in vivo activity of MK2 and MK2 substrate-selective p38alpha(MAPK) inhibitors in Werner syndrome cells.
Platelet-activating factor (PAF) receptor binding antagonists from Alpinia officinarum.
Malaria causal prophylactic activity of imidazolidinedione derivatives.
Synthesis and antitumor activity of amine analogs of irofulven.
Synthesis and antibacterial activity of potent heterocyclic oxazolidinones and the identification of RBx 8700.
Total synthesis and absolute configuration of laurenditerpenol: a hypoxia inducible factor-1 activation inhibitor.
Discovery of the first nonpeptidic, small-molecule, highly selective somatostatin receptor subtype 5 antagonists: a chemogenomics approach.
Design, synthesis, and structure-activity relationships of a novel series of 5-alkylidenepyridazin-3(2H)-ones with a non-cAMP-based antiplatelet activity.
On the intractability of estrogen-related receptor alpha as a target for activation by small molecules.
Discovery of low nanomolar non-hydroxamate inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Synthesis and antibacterial activity of some novel chiral fluorophoric biscyclic macrocycles.
Side-chain truncation of apicularen A by olefin cross-metathesis with ethylene.
Hirtusneanoside, an unsymmetrical dimeric tetrahydroxanthone from the lichen Usnea hirta.
Benzaldehyde derivatives from Sarcodontia crocea.
Bioactive p-terphenyl derivatives from a Cordyceps-colonizing isolate of Gliocladium sp.
Amphidinolides B6 and B7, cytotoxic macrolides from a symbiotic dinoflagellate Amphidinium species.
Biologically active aspidofractinine, rhazinilam, akuammiline, and vincorine alkaloids from Kopsia.
Antioxidant phenylpropanoid-substituted epicatechins from Trichilia catigua.
Design and synthesis of indane-ureido-thioisobutyric acids: A novel class of PPARalpha agonists.
Cytotoxic 5-alkylresorcinol metabolites from the leaves of Grevillea robusta.
Identification and characterization of 4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]piperidine-1-carboxylate, an orally bioavailable, brain penetrant NR2B selective N-methyl-D-aspartate receptor antagonist.
Polycationic sulfonamides for the sequestration of endotoxin.
Green tea catechins potentiate triclosan binding to enoyl-ACP reductase from Plasmodium falciparum (PfENR).
Antimicrobial ambiguines from the cyanobacterium Fischerella sp. collected in Israel.
Mono- and Di-sesquiterpenoids from Chloranthus spicatus.
2-Mercaptoimidazoles, a new class of potent CCR2 antagonists.
Synthesis and acetylcholinesterase inhibition of derivatives of huperzine B.
Syntheses of 2,4,6-trisubstituted triazines as antimalarial agents.
New conformationally locked bicyclic N,O-nucleoside analogues of antiviral drugs.
Truncated azinomycin analogues intercalate into DNA.
Novel 3-aminochromans as potential pharmacological tools for the serotonin 5-HT(7) receptor.
1-Hydroxyalkyl-3-phenylthioureas as novel HDL-elevating agents.
Structure-activity relations of azafluorenone and azaanthraquinone as antimicrobial compounds.
Structure-based design of potent and selective inhibitors of collagenase-3 (MMP-13).
2,3-Dimethoxy-5-methyl-1,4-benzoquinones and 2-methyl-1,4-naphthoquinones: glycation inhibitors with lipid peroxidation activity.
7alpha,11beta-Dimethyl-19-nortestosterone: a potent and selective androgen response modulator with prostate-sparing properties.
Analogues of the neuroprotective tripeptide Gly-Pro-Glu (GPE): synthesis and structure-activity relationships.
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase.
Solid-phase synthesis and antibacterial evaluations of N-demethylvancomycin derivatives.
New pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective PDE5 inhibitors.
Novel immunomodulator FTY720 is phosphorylated in rats and humans to form a single stereoisomer. Identification, chemical proof, and biological characterization of the biologically active species and its enantiomer.
Synthesis, biological activity, and SAR of antimycobacterial 9-aryl-, 9-arylsulfonyl-, and 9-benzyl-6-(2-furyl)purines.
Conformation mining: an algorithm for finding biologically relevant conformations.
Synthesis and in vitro and in vivo antitumor activity of 2-phenylpyrroloquinolin-4-ones.
6-Hydroxy-1,2,3,4-tetrahydro-isoquinoline-3-carboxylic acid mimics active conformation of tyrosine in opioid peptides.
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.
Regioselective oxidation of 2-amino-3-aroyl-4,5-dialkylthiophenes by DMSO.
6-Arylamino-7-chloro-quinazoline-5,8-diones as novel cytotoxic and DNA topoisomerase inhibitory agents.
Lead identification of a potent benzopyranone selective estrogen receptor modulator.
Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.
Synthesis and biological evaluation of benzimidazole-4,7-diones that inhibit vascular smooth muscle cell proliferation.
The inhibition of metallo-beta-lactamase by thioxo-cephalosporin derivatives.
Synthesis of potent sigma-1 receptor ligands via fragmentation of dextromethorphan.
Epibatidine structure-activity relationships.
Synthesis and evaluation of lasonolide A analogues.
Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.
Betulinic acid and its derivatives as anti-angiogenic agents.
Thioxanthene-derived analogs as sigma(1) receptor ligands.
Antihyperglycemic activity of 2-methyl-3,4,5-triaryl-1H-pyrroles in SLM and STZ models.
Synthesis of 7'-[123I]iodo-D-luciferin for in vivo studies of firefly luciferase gene expression.
Fluoropyrrolidine amides as dipeptidyl peptidase IV inhibitors.
Comparison of 2-phenylspiroindenes and 2-phenylspiroindenediones as estrogen receptor ligands--modeling and binding data don't agree!
A series of heterocyclic inhibitors of phenylalanyl-tRNA synthetases with antibacterial activity.
Synthesis and biological activity of selective azasugar-based TACE inhibitors.
Dipeptide nitrile inhibitors of cathepsin K.
Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Design, synthesis, and biological evaluation of 4-alkyliden-beta lactams: new products with promising antibiotic activity against resistant bacteria.
Structure-activity relationships of novel non-competitive mGluR1 antagonists: a potential treatment for chronic pain.
Novel poly(ADP-ribose) polymerase-1 inhibitors.
Bioactive bibenzyl derivatives and fluorenones from Dendrobium nobile.
Analogues of the dopamine D2 receptor antagonist L741,626: Binding, function, and SAR.
Synthesis and SAR of potent and selective androgen receptor antagonists: 5,6-Dichloro-benzimidazole derivatives.
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles.
3-Benzyl-1,3-oxazolidin-2-ones as mGluR2 positive allosteric modulators: Hit-to lead and lead optimization.
Carbonic anhydrase inhibitors. Cloning, characterization, and inhibition studies of a new beta-carbonic anhydrase from Mycobacterium tuberculosis.
Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
NMR and molecular dynamics study of the binding mode of naphthalene-N-sulfonyl-D-glutamic acid derivatives: novel MurD ligase inhibitors.
Design and synthesis of small molecule glycerol 3-phosphate acyltransferase inhibitors.
Lipophilicity of basic drugs measured by hydrophilic interaction chromatography.
Potent cytotoxic C-11 modified geldanamycin analogues.
Synthesis and QSAR evaluation of 2-(substituted phenyl)-1H-benzimidazoles and [2-(substituted phenyl)-benzimidazol-1-yl]-pyridin-3-yl-methanones.
Synthesis of novel N-protected hydrophobic phenylalanines and their application in potential antibacterials.
Securinega alkaloids from the wood of Securinega suffruticosa var. amamiensis.
Advances in development of dopaminergic aporphinoids.
Structural and functional basis of cyclooxygenase inhibition.
Ca2+ channel alpha2-delta ligands for the treatment of neuropathic pain.
N-methyl-D-aspartate antagonists and neuropathic pain: the search for relief.
Kv7 (KCNQ) channel modulators and neuropathic pain.
In vitro anti-inflammatory activity of 3-O-methyl-flavones isolated from Siegesbeckia glabrescens.
Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains.
Multi-target-directed ligands to combat neurodegenerative diseases.
SAR study of 2,3,4,14b-tetrahydro-1H-dibenzo[b,f]pyrido[1,2-d][1,4]oxazepines as progesterone receptor agonists.
Discovery of novel FMS kinase inhibitors as anti-inflammatory agents.
Identification of a potent new chemotype for the selective inhibition of PDE4.
Tri- and tetra-substituted naphthalene diimides as potent G-quadruplex ligands.
Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity.
Protective effect of nitronyl nitroxide-amino acid conjugates on liver ischemia-reperfusion induced injury in rats.
Synthesis and antihyperglycemic activity of novel N-acyl-2-arylethylamines and N-acyl-3-coumarylamines.
Sulfonamide derivatives of bridgehead substituted bicyclo[4.2.1]nonanes as gamma-secretase inhibitors.
Discovery of disubstituted cyclohexanes as a new class of CC chemokine receptor 2 antagonists.
2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists.
Design, synthesis, and studies of small molecule STAT3 inhibitors.
Conception of myeloperoxidase inhibitors derived from flufenamic acid by computational docking and structure modification.
Targeting RNA with cysteine-constrained peptides.
Discovery of potent thiosemicarbazone inhibitors of rhodesain and cruzain.
Spread in an Italian hospital of a clonal Acinetobacter baumannii strain producing the TEM-92 extended-spectrum beta-lactamase.
Mutations in fusA associated with posttherapy fusidic acid resistance in Clostridium difficile.
Complanadines C and D, new dimeric alkaloids from Lycopodium complanatum.
Inhibitory activity of stilbenes on Alzheimer's beta-amyloid fibrils in vitro.
Synthesis and trypanocidal activity of ent-kaurane glycosides.
Synthesis of 5-deazaflavin derivatives and their activation of p53 in cells.
Molecular modeling of some 1H-benzimidazole derivatives with biological activity against Entamoeba histolytica: a comparative molecular field analysis study.
Discovery and synthesis of new immunosuppressive alkaloids from the stem of Fissistigma oldhamii (Hemsl.) Merr.
Preparation of secolycorines against acetylcholinesterase.
4-Pyridone derivatives as new inhibitors of bacterial enoyl-ACP reductase FabI.
alpha-Amino acid derivatives as proton pump inhibitors and potent anti-ulcer agents.
Synthesis and evaluation of N-acetyl-L-tyrosine based compounds as PPARalpha selective activators.
Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2).
Synthesis and biological evaluation of new taxoids derived from 2-deacetoxytaxinine J.
Neuroprotective effects of kobophenol A against the withdrawal of tropic support, nitrosative stress, and mitochondrial damage in SH-SY5Y neuroblastoma cells.
6-Hydrazinopurine 2'-methyl ribonucleosides and their 5'-monophosphate prodrugs as potent hepatitis C virus inhibitors.
Synthesis and biological evaluation of rhodanine derivatives as PRL-3 inhibitors.
Synthesis and antibacterial activity of C12 des-methyl ketolides.
Synthesis and evaluation of (2-phenethyl-2H-1,2,3-triazol-4-yl)(phenyl)methanones as Kv1.5 channel blockers for the treatment of atrial fibrillation.
Synthesis and evaluation of new arylbenzo[b]thiophene and diarylthiophene derivatives as inhibitors of the NorA multidrug transporter of Staphylococcus aureus.
Orally bioavailable potent soluble epoxide hydrolase inhibitors.
First total synthesis of protoapigenone and its analogues as potent cytotoxic agents.
Design, synthesis, and biological evaluation of Plasmodium falciparum lactate dehydrogenase inhibitors.
Fine-tuning the amphiphilicity: a crucial parameter in the design of potent alpha-phenyl-N-tert-butylnitrone analogues.
Discovery of novel benzimidazoles as potent inhibitors of TIE-2 and VEGFR-2 tyrosine kinase receptors.
4- and 5-aroylindoles as novel classes of potent antitubulin agents.
Doxazolidine induction of apoptosis by a topoisomerase II independent mechanism.
High-throughput screening of drug-brain tissue binding and in silico prediction for assessment of central nervous system drug delivery.
Discovery and characterization of novel, potent, non-peptide parathyroid hormone-1 receptor antagonists.
Development of new pyrrolopyrimidine-based inhibitors of Janus kinase 3 (JAK3).
Chiral tetrahydroquinoline derivatives as potent anti-hyperalgesic agents in animal models of sustained inflammation and chronic neuropathic pain.
Synthesis and structure evaluation of a novel cantharimide and its cytotoxicity on SK-Hep-1 hepatoma cells.
Hedgehog-Gli signaling pathway inhibitors as anticancer agents.
Hair growth stimulator property of thienyl substituted pyrazole carboxamide derivatives as a CB1 receptor antagonist with in vivo antiobesity effect.
The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.
Synthesis and biological evaluation of reversible inhibitors of IdeS, a bacterial cysteine protease and virulence determinant.
Topological modeling of lipophilicity, diuretic activity, and carbonic inhibition activity of benzene sulfonamides: a molecular connectivity approach.
Myxopyronin B analogs as inhibitors of RNA polymerase, synthesis and biological evaluation.
Synthesis and cytotoxic activity of substituted luotonin A derivatives.
Screening of antimicrobial activity of diarylamines in the 2,3,5-trimethylbenzo[b]thiophene series: a structure-activity evaluation study.
Probing the activity differences of simple and complex brominated aryl compounds against 15-soybean, 15-human, and 12-human lipoxygenase.
Prospects for inhibitors of protein tyrosine phosphatase 1B as antidiabetic drugs.
Dopamine/serotonin receptor ligands. 9. Oxygen-containing midsized heterocyclic ring systems and nonrigidized analogues. A step toward dopamine D5 receptor selectivity.
Determination of the free radical scavenging activity of dihydropyran-2,4-diones.
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators.
Isosteric N-arylpiperazine replacements in a series of dihydropyridine NPY1 receptor antagonists.
3-(2-Methoxytetrahydrofuran-2-yl)pyrazoles: a novel class of potent, selective cyclooxygenase-2 (COX-2) inhibitors.
Discovery of novel heteroarylazoles that are metabotropic glutamate subtype 5 receptor antagonists with anxiolytic activity.
Synthesis and photosensitizing efficacy of isomerically pure bacteriopurpurinimides.
Novel cyclooxygenase-1 inhibitors discovered using affinity fingerprints.
Discovery of small molecule benzimidazole antagonists of the chemokine receptor CXCR3.
SAR studies of capsazepinoid bronchodilators. Part 1: The importance of the catechol moiety and aspects of the B-ring structure.
Synthesis and SAR of novel 1,1-dialkyl-2(1H)-naphthalenones as potent HCV polymerase inhibitors.
4-thiazolidinone--a biologically active scaffold.
Synthesis and anti-mycobacterial activity of (E)-N'-(monosubstituted-benzylidene)isonicotinohydrazide derivatives.
Hexahydro-pyrrolo- and hexahydro-1H-pyrido[1,2-b]pyridazin-2-ones as potent inhibitors of HCV NS5B polymerase.
Discovery of a novel class of PPARdelta partial agonists.
Synthesis of a 200-member library of squaric acid N-hydroxylamide amides.
Optimization of a series of multi-isoform PI3 kinase inhibitors.
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.
Two new cytotoxic compounds from Tapirira guianensis.
Donnaienin, a New Acetogenin Bearing a Hydroxylated Tetrahydrofuran Ring
Malyngamides M and N from the Hawaiian Red Alga Gracilaria coronopifolia
Latifolians A and B, novel JNK3 kinase inhibitors from the Papua New Guinean plant Gnetum latifolium.
Gesashidine A, a beta-carboline alkaloid with an imidazole ring from a Thorectidae sponge.
Gymnoascolides A-C: aromatic butenolides from an Australian isolate of the soil ascomycete Gymnoascus reessii.
Sesterterpenoids, terretonins A-D, and an alkaloid, asterrelenin, from Aspergillus terreus.
Sodwanone S, a triterpene from the marine sponge Axinella weltneri.
Alkamides from the leaves of Zanthoxylum syncarpum.
Antitubercular constituents from the stem wood of Cinnamomum kotoense.
Amyloid-forming propensity of the hydrophobic non-natural amino acid on the fibril-forming core peptide of human tau.
Synthesis and biological evaluation of nitric oxide-releasing derivatives of oleanolic acid as inhibitors of HepG2 cell apoptosis.
The use of ligand-based de novo design for scaffold hopping and sidechain optimization: two case studies.
Overcoming drug resistance to heme-targeted antimalarials by systematic side chain variation of 7-chloro-4-aminoquinolines.
Identification of novel ligands for the RNA pseudoknot that regulate -1 ribosomal frameshifting.
Antineoplastic agents. 558. Ampelocissus sp. cancer cell growth inhibitory constituents.
Bioactive triterpene saponins from the roots of Phytolacca americana.
Pyrazolo-pyrimidines: a novel heterocyclic scaffold for potent and selective p38 alpha inhibitors.
Structural simplification of bioactive natural products with multicomponent synthesis. 2. antiproliferative and antitubulin activities of pyrano[3,2-c]pyridones and pyrano[3,2-c]quinolones.
Bioactive polybrominated diphenyl ethers from the marine sponge Dysidea sp.
Insect antifeedant sesquiterpene acetals from the liverwort Lepidolaena clavigera. 2. structures, artifacts, and activity.
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.
Synthesis and cytotoxic evaluation of some cribrostatin-ecteinascidin analogues.
Blood-brain barrier penetration by two dermorphin tetrapeptide analogues: role of lipophilicity vs structural flexibility.
PTP1B inhibitors: synthesis and evaluation of difluoro-methylenephosphonate bioisosteres on a sulfonamide scaffold.
Isoxazolone based inhibitors of p38 MAP kinases.
Synthesis and biological evaluation of novel analogues of dictyostatin.
Synthesis of novel triheterocyclic thiazoles as anti-inflammatory and analgesic agents.
Convenient one pot synthesis and antimicrobial evaluation of some new Mannich bases carrying 4-methylthiobenzyl moiety.
Synthesis of enantiomerically pure milnacipran analogs and inhibition of dopamine, serotonin, and norepinephrine transporters.
Synthesis and crystallographic analysis of benzophenone derivatives--the potential anti-inflammatory agents.
Engineering small molecule specificity in nearly identical cellular environments.
Synthesis and biological evaluation of new 3-substituted indole derivatives as potential anti-inflammatory and analgesic agents.
Preparation of novel anthranilic acids as antibacterial agents: extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity.
Synthesis and antiproliferative activity of some novel derivatives of diospyrin, a plant-derived naphthoquinonoid.
Synthesis and antitubercular activity of phenothiazines with reduced binding to dopamine and serotonin receptors.
Potent bradykinin B1 receptor antagonists: 4-substituted phenyl cyclohexanes.
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).
Naphthyl piperazines with dual activity as 5-HT1D antagonists and 5-HT reuptake inhibitors.
Benzimidazo[1,2-c][1,2,3]thiadiazole-7-sulfonamides as inhibitors of carbonic anhydrase.
Antimicrobial and cytotoxic activity of agelasine and agelasimine analogs.
Synthesis, inhibition and binding of simple non-nitrogen inhibitors of monoamine transporters.
Rational design of inhibitors of VirA-VirG two-component signal transduction.
Antimitotic activity of 5-hydroxy-7-methoxy-2-phenyl-4-quinolones.
Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 1. Comparison with conventional ELISA.
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
Amino porphyrins as photoinhibitors of Gram-positive and -negative bacteria.
Fluorinated phenylcyclopropylamines. 2. Effects of aromatic ring substitution and of absolute configuration on inhibition of microbial tyramine oxidase.
Synthesis of novel caspase inhibitors for characterization of the active caspase proteome in vitro and in vivo.
Synthesis and cytotoxicities of dioscin derivatives with decorated chacotriosyl residues.
3-(4-Piperidinyl)indoles and 3-(4-piperidinyl)pyrrolo-[2,3-b]pyridines as ligands for the ORL-1 receptor.
Modulators of the human CCR5 receptor. Part 3: SAR of substituted 1-[3-(4-methanesulfonylphenyl)-3-phenylpropyl]-piperidinyl phenylacetamides.
Structure-activity studies of oxazolidinone analogs as RNA-binding agents.
Synthesis and antimalarial efficacy of aza-fused rhodacyanines in vitro and in the P. berghei mouse model.
Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives.
Design and synthesis of orally efficacious benzimidazoles as melanin-concentrating hormone receptor 1 antagonists.
Development of N-4,6-pyrimidine-N-alkyl-N'-phenyl ureas as orally active inhibitors of lymphocyte specific tyrosine kinase.
Probing the role of the covalent linkage of ferrocene into a chloroquine template.
New phenolic and quinone-methide triterpenes from Maytenus amazonica.
Tenellic acids A-D: new bioactive diphenyl ether derivatives from the aquatic fungus Dendrospora tenella.
New Bis(Indole) alkaloids of the topsentin class from the sponge spongosorites genitrix
A new antibiotic nortriterpene quinone methide from Maytenus catingarum.
A new 1,2-dihydroisoquinoline from the sponge petrosia similis
Pyrimido-oxazepine as a versatile template for the development of inhibitors of specific kinases.
Synthesis and biological evaluation of novel bisheterocycle-containing compounds as potential anti-influenza virus agents.
Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.
Alkylamino derivatives of 4-aminomethylpyridine as inhibitors of copper-containing amine oxidases.
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.
Allosteric Akt (PKB) inhibitors: discovery and SAR of isozyme selective inhibitors.
5-Lipoxygenase inhibition by N-hydroxycarbamates in dual-function compounds.
Synthesis and antibacterial activity of C2-fluoro, C6-carbamate ketolides, and their C9-oximes.
Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP.
N-methylsansalvamide a peptide analogues. Potent new antitumor agents.
Biaryl diamides as potent melanin concentrating hormone receptor 1 antagonists.
Ketene aminal-based lactam derivatives as a novel class of orally active FXa inhibitors.
N-Sulfonyl hydroxamate derivatives as inhibitors of class II fructose-1,6-diphosphate aldolase.
2-Cyano-4-fluoro-1-thiovalylpyrrolidine analogues as potent inhibitors of DPP-IV.
4'C-ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase.
Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping.
Arginine binding motifs: design and synthesis of galactose-derived arginine tweezers as galectin-3 inhibitors.
Design, synthesis, biological evaluation and docking studies of pterostilbene analogs inside PPARalpha.
Antiviral amphipathic oligo- and polyribonucleotides: analogue development and biological studies.
Benzodiazepines as potent and selective bradykinin B1 antagonists.
3,6-dibromocarbazole piperazine derivatives of 2-propanol as first inhibitors of cytochrome c release via Bax channel modulation.
Discovery of a novel and highly potent noncompetitive AMPA receptor antagonist.
Determination of conformer-specific partition coefficients in octanol/water systems.
Syntheses and biological properties of cysteine-reactive epibatidine derivatives.
Studies on the synthesis and anti-Osteoporosis of estrogen-GHRPs linkers.
Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.
Synthesis and antibacterial activity of pyrroloaryl-substituted oxazolidinones.
Angiotensin II AT1 receptor antagonists. Clinical implications of active metabolites.
Stereoselective synthesis of beta-lactams with polyaromatic imines: entry to new and novel anticancer agents.
Unique structure-activity relationship for 4-isoxazolyl-1,4-dihydropyridines.
Novel cationic transport agents for oligonucleotide delivery into primary leukemic cells.
Synthesis and activity of new aryl- and heteroaryl-substituted pyrazole inhibitors of the transforming growth factor-beta type I receptor kinase domain.
New nardosinanes and 19-oxygenated ergosterols from the soft coral Nephthea armata collected in Taiwan.
Antineoplastic agents. 529. Isolation and structure of nootkastatins 1 and 2 from the Alaskan yellow cedar Chamaecyparis nootkatensis.
Design and synthesis of macrocyclic inhibitors of phosphatase cdc25B.
Amidines as amide bond replacements in VLA-4 antagonists.
The design and preparation of metabolically protected new arylpiperazine 5-HT1A ligands.
Orally bioavailable small molecule ketoamide-based inhibitors of cathepsin K.
Synthesis and mitochondrial complex I inhibition of dihydroxy-cohibin A, non-THF annonaceous acetogenin analogue.
Inhibitors of Sir2: evaluation of splitomicin analogues.
Synthesis and evaluation of oxazaborolidines for antibacterial activity against Streptococcus mutans.
Reducing the peptidyl features of caspase-3 inhibitors: a structural analysis.
A medicinal chemistry perspective on artemisinin and related endoperoxides.
Synthesis and antibacterial activity of a novel class of 4'-substituted 16-membered ring macrolides derived from tylosin.
Total synthesis and anti-tubulin activity of epi-c3 analogues of cryptophycin-24.
Structural analysis and optimization of NK(1) receptor antagonists through modulation of atropisomer interconversion properties.
Inhibitors of serine proteases as potential therapeutic agents: the road from thrombin to tryptase to cathepsin G.
Conformer- and alignment-independent model for predicting structurally diverse competitive CYP2C9 inhibitors.
N-isoquinolin-5-yl-N'-aralkyl-urea and -amide antagonists of human vanilloid receptor 1.
1-alkyl-4-acylpiperazines as a new class of imidazole-free histamine H(3) receptor antagonists.
Design, synthesis, and biological evaluation of novel tricyclic HIV-1 integrase inhibitors by modification of its pyridine ring.
Design, synthesis, and evaluation of novel 6-chloro-/fluorochromone derivatives as potential topoisomerase inhibitor anticancer agents.
Triaminotriazine DNA helicase inhibitors with antibacterial activity.
Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
2-((1H-Azol-1-yl)methyl)-N-arylbenzamides: novel dual inhibitors of VEGFR-1/2 kinases.
Lipolanthionine peptides act as inhibitors of TLR2-mediated IL-8 secretion. Synthesis and structure-activity relationships.
Sarcosine based indandione hGlyT1 inhibitors.
Synthesis and in vitro antitumoral activity of new 3,5-dicyanopyridine derivatives.
Synthesis and evaluation of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic and sedative properties.
Novel antiproliferative analogs of the Taq DNA polymerase inhibitor catalpol.
Antihyperglycemic and antidyslipidemic agent from Aegle marmelos.
Synthesis of potent and tissue-selective androgen receptor modulators (SARMs): 2-(2,2,2)-Trifluoroethyl-benzimidazole scaffold.
Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA.
Novel trifluoroacetophenone derivatives as malonyl-CoA decarboxylase inhibitors.
Identification and structure-activity relationships of substituted pyridones as inhibitors of Pim-1 kinase.
N-Benzyl-N-(tetrahydro-2H-pyran-4-yl)pyrrolidin-3-amines as selective dual serotonin/noradrenaline reuptake inhibitors.
Structure-based design of benzylamino-acridine compounds as G-quadruplex DNA telomere targeting agents.
N-i-Propoxy-N-biphenylsulfonylaminobutylhydroxamic acids as potent and selective inhibitors of MMP-2 and MT1-MMP.
(R)-2-(4-Phenylbutyl)dihydrobenzofuran derivatives as melatoninergic agents.
Structure-activity relationships of dimeric PPAR agonists.
(E)-Phenyl- and -heteroaryl-substituted O-benzoyl-(or acyl)oximes as lipoprotein-associated phospholipase A2 inhibitors.
A two-state homology model of the hERG K+ channel: application to ligand binding.
Inhibition of the G2 DNA damage checkpoint by oliveroline isolated from Duguetia odorata.
Excelsione, a depsidone from an endophytic fungus isolated from the New Zealand endemic tree Knightia excelsa.
Caspofungin in combination with amphotericin B against Candida parapsilosis.
In vitro activities of cloxyquin (5-chloroquinolin-8-ol) against Mycobacterium tuberculosis.
Quinoline derivative MC1626, a putative GCN5 histone acetyltransferase (HAT) inhibitor, exhibits HAT-independent activity against Toxoplasma gondii.
Effects of glutathione and ascorbic acid on streptomycin sensitivity of Escherichia coli.
A xanthocillin-like alkaloid from the insect pathogenic fungus Cordyceps brunnearubra BCC 1395.
The effect of halide salts on the production of Gymnoascus reessii polyenylpyrroles.
Furanocembranoids from the stem bark of Croton oblongifolius.
Quinolone resistance in Helicobacter pylori isolates in Germany.
In vitro-clinical correlations for amphotericin B susceptibility in AIDS-associated cryptococcal meningitis.
Molecular mechanism of flucytosine resistance in Candida lusitaniae: contribution of the FCY2, FCY1, and FUR1 genes to 5-fluorouracil and fluconazole cross-resistance.
Hepatitis C virus (HCV) NS5B nonnucleoside inhibitors specifically block single-stranded viral RNA synthesis catalyzed by HCV replication complexes in vitro.
Simple colorimetric inhibition assay of heme crystallization for high-throughput screening of antimalarial compounds.
Selectivity fields: comparative molecular field analysis (CoMFA) of the glycine/NMDA and AMPA receptors.
5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators.
The role of the side chain in determining relative delta- and kappa-affinity in C5'-substituted analogues of naltrindole.
Peptide science: exploring the use of chemical principles and interdisciplinary collaboration for understanding life processes.
Inhibitors of inosine monophosphate dehydrogenase: SARs about the N-[3-Methoxy-4-(5-oxazolyl)phenyl moiety.
Selective substrate-based inhibitors of mammalian dimethylarginine dimethylaminohydrolase.
Farnesoid X receptor: from structure to potential clinical applications.
A bivalent ligand (KDAN-18) containing delta-antagonist and kappa-agonist pharmacophores bridges delta2 and kappa1 opioid receptor phenotypes.
Medicinal chemistry driven approaches toward novel and selective serotonin 5-HT6 receptor ligands.
Synthesis, structure-activity relationships at the GABA(A) receptor in rat brain, and differential electrophysiological profile at the recombinant human GABA(A) receptor of a series of substituted 1,2-diphenylimidazoles.
2,3-Diphenylpropionic acids as potent VLA-4 antagonists.
Design, synthesis and evaluation of 5-substituted amino-2,4-diamino-8-chloropyrimido-[4,5-b]quinolines as novel antimalarials.
Design, new synthesis, and calcilytic activity of substituted 3H-pyrimidin-4-ones.
Synthesis of novel 10-deoxoartemisinins.
Aryl sulfones: a new class of gamma-secretase inhibitors.
Design, synthesis, and biological activity of potent and selective inhibitors of mast cell tryptase.
New cytotoxic bisindole alkaloids with protein tyrosine kinase inhibitory activity from a myxomycete Lycogala epidendrum.
Synthesis, aerobic cytotoxicity, and radiosensitizing activity of novel 2,4-dinitrophenylamine tethered 5-fluorouracil and hydroxyurea.
NO-donor phenols: a new class of products endowed with antioxidant and vasodilator properties.
Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase.
Orally active thrombin inhibitors. Part 2: optimization of the P2-moiety.
Synthesis of a potent 5'-methylthioadenosine/S-adenosylhomocysteine (MTAN) inhibitor.
Design and synthesis of 7H-pyrrolo[2,3-d]pyrimidines as focal adhesion kinase inhibitors. Part 2.
Synthesis of (2E)-3-{2-[(substituted benzyl)oxy]phenyl}acrylaldehydes as novel anti-inflammatory agents.
1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists.
Development of activity-based probes for trypsin-family serine proteases.
Identification of new diamine scaffolds with activity against Mycobacterium tuberculosis.
Novel tacrine-melatonin hybrids as dual-acting drugs for Alzheimer disease, with improved acetylcholinesterase inhibitory and antioxidant properties.
Potent anti-muscarinic activity in a novel series of quinuclidine derivatives.
Synthesis and biological activity of novel 4-phenyl-1,8-naphthyridin-2(1H)-on-3-yl ureas: potent acyl-CoA:cholesterol acyltransferase inhibitor with improved aqueous solubility.
Synthesis and biological investigations of dopaminergic partial agonists preferentially recognizing the D4 receptor subtype.
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
One-pot synthesis and SAR study of cis-2,6-dialkyl-4-chloro-tetrahydropyrans.
Activity of B-nor analogues of neurosteroids on the GABA(A) receptor in primary neuronal cultures.
Discovery of indole-containing tetracycles as a new scaffold for androgen receptor ligands.
Synthesis and antitumor properties of 2,5-bis(3'-indolyl)thiophenes: analogues of marine alkaloid nortopsentin.
Prenyloxyphenylpropanoids as novel lead compounds for the selective inhibition of geranylgeranyl transferase I.
Synthesis of 3-[4'-(p-chlorophenyl)-thiazol-2'-yl]-2-[(substituted azetidinone/thiazolidinone)-aminomethyl]-6-bromoquinazolin-4-ones as anti-inflammatory agent.
Methyl spongoate, a cytotoxic steroid from the Sanya soft coral Spongodes sp.
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
E/Z-rubrolide O, an anti-inflammatory halogenated furanone from the New Zealand ascidian Synoicum n. sp.
Discovery and refinement of a new structural class of potent peptide deformylase inhibitors.
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
Urea based CCR3 antagonists employing a tetrahydro-1,3-oxazin-2-one spacer.
Synthesis and biological evaluation of a series of tangeretin-derived chalcones.
New lycorine-type alkaloid from Lycoris traubii and evaluation of antitrypanosomal and antimalarial activities of lycorine derivatives.
Fragment-based discovery of JAK-2 inhibitors.
11-Phenyl-[b,e]-dibenzazepine compounds: novel antitumor agents.
Modification of the N-terminal sulfonyl residue in 3-amidinophenylalanine-based matriptase inhibitors.
Lead identification to generate 3-cyanoquinoline inhibitors of insulin-like growth factor receptor (IGF-1R) for potential use in cancer treatment.
Discovery of novel spirocyclopropyl hydroxamate and carboxylate compounds as TACE inhibitors.
First characterization of fluoroquinolone resistance in Streptococcus suis.
Tolerance to the glycopeptides vancomycin and teicoplanin in coagulase-negative staphylococci.
Plasmid-mediated KPC-2 in a Klebsiella pneumoniae isolate from China.
Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.
Pharmacokinetics and safety of indinavir in human immunodeficiency virus-infected pregnant women.
Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate.
Docking study yields four novel inhibitors of the protooncogene Pim-1 kinase.
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.
New QSAR combined strategy for the design of A1 adenosine receptor agonists.
Imidazo[4,5-c]quinolines as inhibitors of the PI3K/PKB-pathway.
Optimization of 2,3,5-trisubstituted pyridine derivatives as potent allosteric Akt1 and Akt2 inhibitors.
Synthesis and dopamine receptor affinities of N-alkyl-11-hydroxy-2-methoxynoraporphines: N-alkyl substituents determine D1 versus D2 receptor selectivity.
The discovery of GSK221149A: a potent and selective oxytocin antagonist.
Discovery and SAR of 1,3,4-thiadiazole derivatives as potent Abl tyrosine kinase inhibitors and cytodifferentiating agents.
alpha- and beta-substituted phosphonate analogs of LPA as autotaxin inhibitors.
Discovery of a novel class of selective human CB1 inverse agonists.
Overcoming undesirable HERG potency of chemokine receptor antagonists using baseline lipophilicity relationships.
Rapid assembly of diverse and potent allosteric Akt inhibitors.
Synthesis of 2-C-hydroxymethylribofuranosylpurines as potent anti-hepatitis C virus (HCV) agents.
Brunsvicamides A-C: sponge-related cyanobacterial peptides with Mycobacterium tuberculosis protein tyrosine phosphatase inhibitory activity.
Solid-phase synthesis of quinol fatty alcohols, design of N/O-substituted quinol fatty alcohols and comparative activities on axonal growth.
Discovery of new C3aR ligands. Part 1: arginine derivatives.
Antitumor anthraquinones from an endophytic actinomycete Micromonospora lupini sp. nov.
The discovery of long acting beta2-adrenoreceptor agonists.
A new class of histamine H3 receptor antagonists derived from ligand based design.
Synthesis and preliminary evaluation of mono-[123I]iodohypericin monocarboxylic acid as a necrosis avid imaging agent.
o-Naphthalenedicarboxaldehyde derivative of 7'-aminonaltrindole as a selective delta-opioid receptor affinity label.
Discovery of novel antitumor antimitotic agents that also reverse tumor resistance.
Improved anti-osteoporosis potency and reduced endometrial membrane hyperplasia during hormone replacement therapy with estrogen-RGD peptide conjugates.
Optimization of novel combi-molecules: identification of balanced and mixed bcr-abl/DNA targeting properties.
Synthesis and matrix metalloproteinase (MMP)-12 inhibitory activity of ageladine A and its analogs.
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: preparation and opioid receptor activity of salvinicin analogues.
Endiandrin A, a potent glucocorticoid receptor binder isolated from the Australian plant Endiandra anthropophagorum.
Imidazolylmethylbenzophenones as highly potent aromatase inhibitors.
SME-2-producing Serratia marcescens isolate from Switzerland.
Efficacy of the de novo-derived antimicrobial peptide WLBU2 against oral bacteria.
Inhibition of Botrytis cinerea by New Sesquiterpenoid Compounds Obtained from the Rearrangement of Isocaryophyllene
Antimitotic and cytotoxic flavonols from Zieridium pseudobtusifolium and Acronychia porteri.
(+)-(S)-dihydroaeruginoic acid, an inhibitor of Septoria tritici and other phytopathogenic fungi and bacteria, produced by Pseudomonas fluorescens.
Antibacterial triterpenoid acids from Dillenia papuana.
Biosynthetic Study and Radioisotope Labeling of Inostamycin
Binding of quinolizidine alkaloids to nicotinic and muscarinic acetylcholine receptors.
Khusimol, a non-peptide ligand for vasopressin V1a receptors.
Zarzissine, a new cytotoxic guanidine alkaloid from the Mediterranean sponge Anchinoe paupertas.
Patuletin acetylrhamnosides from Kalanchoe brasiliensis as inhibitors of human lymphocyte proliferative activity.
Novel Ca(2+)-ATPase inhibitors from the dried root tubers of Polygonum Multiflorum.
6-Hydroxymanzamine A and 3,4-dihydromanzamine A, new alkaloids from the Okinawan marine sponge Amphimedon Sp.
Inhibition of Soybean Lipoxygenase-1 by Anacardic Acids, Cardols, and Cardanols
New chlorinated diphenyl ethers from an Aspergillus species.
Prenylated isoflavonoids from the root bark of Erythrina vogelii.
Synthesis and structure-activity relationship study of lamellarin derivatives.
Total synthesis and bioactivity of some naturally occurring pterulones.
Clathriol, a novel polyoxygenated 14beta steroid isolated from the New Zealand marine sponge Clathria lissosclera.
Abietane diterpenoids from Coleus xanthanthus.
Horiolide, a novel norditerpenoid from Indian ocean soft coral of the genus Sinularia.
Botryllamides E-H, four new tyrosine derivatives from the ascidian Botrylloides tyreum.
A New Diterpene from a Soft Coral, Sinularia dissecta
Three New Onnamide Congeners from the Okinawan Marine Sponge Theonella Sp.
Structure of Benthophoenin, a New Free Radical Scavenger Produced by Streptomyces prunicolor
Xestokerols A, B, and C, New C 29 Steroids with a Cyclopropane Ring from the Okinawan Marine Sponge Xestospongia sp.
Dictyosphaeric acids A and B: new decalactones from an undescribed Penicillium sp. obtained from the alga Dictyosphaeria versluyii.
Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors.
A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer.
Edaravone derivatives containing NO-donor functions.
Synthesis and structure-activity relationship of benzetimide derivatives as human CXCR3 antagonists.
Synthesis and biological evaluation of novel 3'-N-tert-butylsulfonyl analogues of docetaxel.
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
Design, synthesis, and acetylcholinesterase inhibitory activity of novel coumarin analogues.
Pyrrolobenzimidazoles linked to heterocycles and peptides. Design of DNA base pair specific phosphate hydrolyzing agents and novel cytotoxic agents.
Synthesis and antibacterial activity of 7-(substituted)aminomethyl quinolones.
Discovery of small-molecule inhibitors of the ATPase activity of human papillomavirus E1 helicase.
Piperazinobenzopyranones and phenalkylaminobenzopyranones: potent inhibitors of breast cancer resistance protein (ABCG2).
Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds.
Oxazine 170 induces DNA:RNA:DNA triplex formation.
Mono- and bis-thiazolium salts have potent antimalarial activity.
Methyl pyropheophorbide-a analogues: potential fluorescent probes for the peripheral-type benzodiazepine receptor. Effect of central metal in photosensitizing efficacy.
Rational design of 4-amino-5,6-diaryl-furo[2,3-d]pyrimidines as potent glycogen synthase kinase-3 inhibitors.
Morphinane alkaloid dimers from Sinomenium acutum.
Synthesis of curcumin mimics with multidrug resistance reversal activities.
Synthesis and anti-cancer activity of benzothiazole containing phthalimide on human carcinoma cell lines.
Synthesis and DNA-cleaving activity of lactenediynes conjugated with DNA-complexing moieties.
Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors.
Design and synthesis of 4-substituted indolo[3,2-e][1,2,3]triazolo[1,5-a]pyrimidine derivatives with antitumor activity.
Constrained analogues of procaine as novel small molecule inhibitors of DNA methyltransferase-1.
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1.
Synthesis and evaluation of novel 4-amino-4,6-androstadiene-3,17-dione: an analog of formestane.
Simplified YM-26734 inhibitors of secreted phospholipase A2 group IIA.
Antitumor studies. Part 5: Synthesis, antitumor activity, and molecular docking study of 5-(monosubstituted amino)-2-deoxo-2-phenyl-5-deazaflavins.
Small molecule modulators of toll-like receptors.
PASS-assisted exploration of antidepressant activity of 1,3,4-trisubstituted-beta-lactam derivatives.
Improved synthesis of 6-epi-dictyostatin and antitumor efficacy in mice bearing MDA-MB231 human breast cancer xenografts.
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins.
Virtual screening to successfully identify novel janus kinase 3 inhibitors: a sequential focused screening approach.
Transient loss of high-level mupirocin resistance in Staphylococcus aureus due to MupA polymorphism.
Beta-lactam resistance in Haemophilus parasuis Is mediated by plasmid pB1000 bearing blaROB-1.
In vitro bactericidal activity of the antiprotozoal drug miltefosine against Streptococcus pneumoniae and other pathogenic streptococci.
Activation of inhibitors by sortase triggers irreversible modification of the active site.
Synthesis of novel quinolone and quinoline-2-carboxylic acid (4-morpholin-4-yl-phenyl)amides: a late-stage diversification approach to potent 5HT1B antagonists.
Cyclopentanone ring-cleaved pleuromutilin derivatives.
Activity of linezolid against 3,251 strains of uncommonly isolated gram-positive organisms: report from the SENTRY Antimicrobial Surveillance Program.
Further pterocellins from the New Zealand marine bryozoan Pterocella vesiculosa.
3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors.
Structure-based optimization of a potent class of arylamide FMS inhibitors.
4,5-Disubstituted oxazolidinones: High affinity molecular effectors of RNA function.
Discovery and initial SAR of arylsulfonylpiperazine inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1).
Design and synthesis of tacrine-ferulic acid hybrids as multi-potent anti-Alzheimer drug candidates.
Identification of acridinyl hydrazides as potent aspartic protease inhibitors.
Bis-aryl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type 1.
Dual binding site inhibitors of B-RAF kinase.
Antibacterial activity in serum of the 3,5-diamino-piperidine translation inhibitors.
A constituent of Pterocarpus marsupium, (-)-epicatechin, as a potential antidiabetic agent.
Phototoxic and Insecticidal Activities of Chromenes and Benzofurans from Encelia
Synthesis, characterization, and preliminary in vivo tests of new poly(ethylene glycol) conjugates of the antitumor agent 10-amino-7-ethylcamptothecin.
Synthesis and structure-activity relationship study of potent cytotoxic analogues of the marine alkaloid Lamellarin D.
Design, synthesis, and evaluation of novel kazusamycin A derivatives as potent antitumor agents.
Fluorophor-labeled spermidine derivatives as fluorescent markers in optical tumor imaging.
Facile purification of honokiol and its antiviral and cytotoxic properties.
Synthesis of a novel biotin-tagged photoaffinity probe for VEGF receptor tyrosine kinases.
Discovery of A-770041, a src-family selective orally active lck inhibitor that prevents organ allograft rejection.
C8c-C15 monoseco-analogues of the phenanthroquinolizidine alkaloids julandine and cryptopleurine exhibiting potent anti-angiogenic properties.
Synthesis and interactions of 7-deoxy-, 10-deacetoxy, and 10-deacetoxy-7-deoxypaclitaxel with NCI/ADR-RES cancer cells and bovine brain microvessel endothelial cells.
Acryloylamino-salicylanilides as EGFR PTK inhibitors.
Synthesis and biological evaluation of 6-(alkyn-1-yl)furo[2,3-d]pyrimidin-2(3H)-one base and nucleoside derivatives.
Antimalarial and antiplasmodial activities of norneolignans. Syntheses and SAR.
Anthrax lethal factor protease inhibitors: synthesis, SAR, and structure-based 3D QSAR studies.
Synthesis and preliminary in vitro investigation of bivalent ligands containing homo- and heterodimeric pharmacophores at mu, delta, and kappa opioid receptors.
Synthesis, structural reassignment, and biological activity of type B MAO inhibitors based on the 5H-indeno[1,2-c]pyridazin-5-one core.
Synthesis, SAR exploration, and X-ray crystal structures of factor XIa inhibitors containing an alpha-ketothiazole arginine.
Structure-activity relationship studies of a series of antiviral and antibacterial aglycon derivatives of the glycopeptide antibiotics vancomycin, eremomycin, and dechloroeremomycin.
Potent estrogen receptor ligands based on bisphenols with a globular hydrophobic core.
Discovery of potent and selective phenylalanine based dipeptidyl peptidase IV inhibitors.
Synthesis and phosphodiesterase 5 inhibitory activity of novel pyrido[1,2-e]purin-4(3H)-one derivatives.
Design, synthesis, and evaluation of proline based melanocortin receptor ligands.
Synthesis and biological evaluation of sulfonamidooxazoles and beta-keto sulfones: selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Discovery of non-steroidal mifepristone mimetics: pyrazoline-based PR antagonists.
BCUT descriptors to predicting affinity toward A3 adenosine receptors.
Synthesis and biological evaluation of chromone carboxamides as calpain inhibitors.
Biological evaluation of Tyr6 and Ser7 modified drosocin analogues.
New piperidinyl- and 1,2,3,6-tetrahydropyridinyl-pyrimidine derivatives as selective 5-HT1A receptor agonists with highly potent anti-ischemic effects.
Structure-activity relationship of N-methyl-bisindolylmaleimide derivatives as cell death inhibitors.
Hetaryl imidazoles: a novel dual inhibitors of VEGF receptors I and II.
Synthesis and biological investigation of new 4''-malonyl tethered derivatives of erythromycin and clarithromycin.
2,4-Disubstituted piperidines as selective CC chemokine receptor 3 (CCR3) antagonists: synthesis and selectivity.
Discovery and preliminary structure-activity relationship studies of novel benzotriazine based compounds as Src inhibitors.
N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.
Syntheses and studies of quinolone-cephalosporins as potential anti-tuberculosis agents.
Thiopyrano[2,3-e]indol-2-ones: angelicin heteroanalogues with potent photoantiproliferative activity.
Novel bioactive sulfated alkene and alkanes from the mediterranean ascidian Halocynthia papillosa.
Four new neuroprotective dihydropyranocoumarins from Angelica gigas.
Prenylbicyclogermacrane diterpenoids from the formosan soft coral Nephthea pacifica.
Two new cytotoxic linderazulenes from a deep-sea gorgonian of the genus Paramuricea.
Stemoninines from the roots of Stemona tuberosa.
An antimicrobial C(14) acetylenic acid from a marine sponge Oceanapia species.
Mycalamides C and D, cytotoxic compounds from the marine sponge Stylinos n. species.
New variotin analogues from Aspergillus viridi-nutans.
Tetrahydroisoquinoline 1-carboxamides as growth hormone secretagogues.
Chiral DNA gyrase inhibitors. 3. Probing the chiral preference of the active site of DNA gyrase. Synthesis of 10-fluoro-6-methyl-6,7-dihydro-9-piperazinyl- 2H-benzo[a]quinolizin-20-one-3-carboxylic acid analogues.
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase.
Synthesis of NO-donor bisphosphonates and their in-vitro action on bone resorption.
Dynamic receptor-based pharmacophore model development and its application in designing novel HIV-1 integrase inhibitors.
Identification of small molecule chemical inhibitors of the collagen-specific chaperone Hsp47.
Discovery of a potent, selective, and efficacious class of reversible alpha-ketoheterocycle inhibitors of fatty acid amide hydrolase effective as analgesics.
Comparison of sulfamate and sulfamide groups for the inhibition of carbonic anhydrase-II by using topiramate as a structural platform.
Chemistry of Acronycine I. Carbon- 13 NMR Studies of Acronycine and Related Compounds
Antimicrobial Neolignans of Sassafras randaiense Roots
Studies on Aristolochia, I. Conversion of Aristolochic Acid-I to Aristolic Acid-One-Step Removal of a Nitro Group
Geriatrics photo quiz. Thoracic aortic aneurysm.
Carboxyatractyloside: A Compound from Xanthium strumarium and Atractylis gummifera with Plant Growth Inhibiting Properties. The Probable "Inhibitor A"
The Effect of Ultraviolet Light on the Toxicity of Natural Products Toward the Eggs of Drosophila melanogaster
Cactus Alkaloids. LIII. Coryphanthine and O-Methyl-Candicine, Two New Quaternary Alkaloids from Coryphantha greenwoodii
Bioactive Norlignan Glucosides from Curculigo capitulata
New Guaiane Metabolites from the Caribbean Gorgonian Coral, Pseudopterogorgia americana
Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay.
Phospholipase A 2 Inhibitors from an Erythrina Species from Samoa
Halishigamides AD, New Cytotoxic Oxazole-Containing Metabolites from Okinawan Sponge Halichondria sp.
Oxysporidinone: a novel, antifungal N-methyl-4-hydroxy-2-pyridone from Fusarium oxysporum.
Bioactive Terpenoids from Octocorallia. 3. A New Eunicellin-Based Diterpenoid from the Soft Coral Cladiella sphaeroides
Pyraxinine, a Novel Nitrogenous Compound from the Marine Sponge Cymbastela cantharella
Illudinic acid, a novel illudane sesquiterpene antibiotic.
Seven New Polyacetylene Derivatives, Showing Both Potent Metamorphosis-Inducing Activity in Ascidian Larvae and Antifouling Activity Against Barnacle Larvae, from the Marine Sponge Callyspongia truncata
Dolabelides C and D, Cytotoxic Macrolides Isolated from the Sea Hare Dolabella auricularia
Activity of Parthenolide at 5HT2A receptors.
Nostopeptins A and B, Elastase Inhibitors from the Cyanobacterium Nostoc minutum
Nodulisporic acid side-chain modifications: access to the 2", 3", 4", and 6" registers.
Finding discriminating structural features by reassembling common building blocks.
Design, synthesis and photochemical properties of caged bile acids.
Novel openers of Ca2+-dependent large-conductance potassium channels: symmetrical pharmacophore and electrophysiological evaluation of bisphenols.
Antiinflammatory, gastrosparing, and antiplatelet properties of new NO-donor esters of aspirin.
Synthesis of ethyl 5-phenyl-6-oxa-1-azabicyclo[3.1.0]hexane-2-carboxylate derivatives and evaluation of their antimalarial activities.
Synthesis and biological evaluation of 18-methoxycoronaridine congeners. Potential antiaddiction agents.
Antiretroviral activity of semisynthetic derivatives of glycopeptide antibiotics.
Effect of detergent on "promiscuous" inhibitors.
Higher-end serotonin receptors: 5-HT(5), 5-HT(6), and 5-HT(7).
QSAR and the rational design of long-acting dual D2-receptor/beta 2-adrenoceptor agonists.
Muraymycins, novel peptidoglycan biosynthesis inhibitors: synthesis and SAR of their analogues.
Triethylene tetraamine: a novel telomerase inhibitor.
Synthesis and binding affinity of neuropeptide Y at opiate receptors.
Identification of a novel series of selective 5-HT7 receptor antagonists.
Discovery of a potent and selective agonist of the prostaglandin EP4 receptor.
Inhibitors of Abeta production: solid-phase synthesis and SAR of alpha-hydroxycarbonyl derivatives.
Structure-activity relationship of cyclic peptide penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2) at the human melanocortin-1 and -4 receptors: His(6) substitution.
Peptoid mimics of agouti related protein.
Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy.
Antitumor activity of novel deoxoartemisinin monomers, dimers, and trimer.
Synthesis and biological evaluation of 14-alkoxymorphinans. 18. N-substituted 14-phenylpropyloxymorphinan-6-ones with unanticipated agonist properties: extending the scope of common structure-activity relationships.
Fumagalone, a reversible inhibitor of type 2 methionine aminopeptidase and angiogenesis.
CC-1065 analogues bearing different DNA-binding subunits: synthesis, antitumor activity, and preliminary toxicity study.
Bivalent biogenic amine reuptake inhibitors.
Discovery of 2-(alpha-methylbenzylamino) pyrazines as potent Type II inhibitors of FMS.
Identification of 4-hydroxyquinolines inhibitors of p300/CBP histone acetyltransferases.
Synthesis and 5-lipoxygenase inhibitory activity of new cinnamoyl and caffeoyl clusters.
Synthesis, antiplatelet and in silico evaluations of novel N-substituted-phenylamino-5-methyl-1H-1,2,3-triazole-4-carbohydrazides.
2009 Edward E Smissman Award. Pharmaceutical "gold" from neurostabilizing agents: topiramate and successor molecules.
Synthesis of aristolactam analogues and evaluation of their antitumor activity.
Design, total synthesis, and biological evaluation of neodysiherbaine A derivative as potential probes.
Synthesis and SAR of novel hydantoin derivatives as selective androgen receptor modulators.
Microwave expedited synthesis of 5-aminocamptothecin analogs: Inhibitors of hypoxia inducible factor HIF-1alpha.
Pyridine-3-propanoic acids: Discovery of dual PPARalpha/gamma agonists as antidiabetic agents.
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
Synthesis and evaluation of water-soluble docetaxel prodrugs-docetaxel esters of malic acid.
A novel ketolide class: Synthesis and antibacterial activity of a lead compound.
Synthesis of novel HIV protease inhibitors (PI) with activity against PI-resistant virus.
Synthesis of chlorogenic acid derivatives with promising antifungal activity.
2-Benzenesulfonyl-8a-benzyl-hexahydro-2H-isoquinolin-6-ones as selective glucocorticoid receptor antagonists.
Novel quinolizidinyl derivatives as antiarrhythmic agents.
Cytotoxic germacranolides and acyclic diterpenoides from the seeds of Carpesium triste.
Malaria-infected mice are cured by a single dose of novel artemisinin derivatives.
Structure-guided optimization of small molecules inhibiting human immunodeficiency virus 1 Tat association with the human coactivator p300/CREB binding protein-associated factor.
New diphenylacetylenes as probes for positron emission tomographic imaging of amyloid plaques.
Synthesis of new plant growth regulator: N-(fatty acid) O-aryloxyacetyl ethanolamine.
P2-P3 conformationally constrained ketoamide-based inhibitors of cathepsin K.
Bioactive fluorinated derivative of amphotericin B.
Discodermolide analogues as the chemical component of combination bacteriolytic therapy.
A preliminary study of the metabolic stability of a series of benzoxazinone derivatives as potent neuropeptide Y5 antagonists.
Chemical modification of the naphthoyl 3-position of JWH-015: in search of a fluorescent probe to the cannabinoid CB2 receptor.
Estrogen receptor ligands. Part 13: Dihydrobenzoxathiin SERAMs with an optimized antagonist side chain.
Synthesis and assay of isoquinoline derivatives as HIV-1 Tat-TAR interaction inhibitors.
Identification of potent type I MetAPs inhibitors by simple bioisosteric replacement. Part 2: SAR studies of 5-heteroalkyl substituted TCAT derivatives.
Synthesis and evaluation of a series of tropane analogues as novel vesicular monoamine transporter-2 ligands.
SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
A new class of high affinity thyromimetics containing a phenyl-naphthylene core.
Potent antitubulin tumor cell cytotoxins based on 3-aroyl indazoles.
Design and synthesis of anticonvulsants from a combined phthalimide-GABA-anilide and hydrazone pharmacophore.
Design and synthesis of pyrimido[4,5-b][1,4]benzothiazine derivatives, as potent 15-lipoxygenase inhibitors.
Carbonic anhydrase and matrix metalloproteinase inhibitors. Inhibition of human tumor-associated isozymes IX and cytosolic isozyme I and II with sulfonylated hydroxamates.
The use of aminoglycoside derivatives to study the mechanism of aminoglycoside 6'-N-acetyltransferase and the role of 6'-NH2 in antibacterial activity.
Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.
Lysine sulfonamides as novel HIV-protease inhibitors: optimization of the Nepsilon-acyl-phenyl spacer.
Anti-herpes simplex virus activity of substituted 1-hydroxyacridones.
Estrogenic potential of 2-alkyl-4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude.
Thermal denaturation: a method to rank slow binding, high-affinity P38alpha MAP kinase inhibitors.
The synthesis and in vitro testing of structurally novel antibiotics derived from acylnitroso Diels-Alder adducts.
Synthesis, calpain inhibitory activity, and cytotoxicity of P2-substituted proline and thiaproline peptidyl aldehydes and peptidyl alpha-ketoamides.
Synthesis and antitumor activity of two natural N-acetylglucosamine-bearing triterpenoid saponins: lotoidoside D and E.
Identification of metabolites of the tryptase inhibitor CRA-9249: observation of a metabolite derived from an unexpected hydroxylation pathway.
Guanidinylated 2,5-dideoxystreptamine derivatives as anthrax lethal factor inhibitors.
Synthesis of 3-benzyl-2-substituted quinoxalines as novel monoamine oxidase A inhibitors.
Similarity based virtual screening: a tool for targeted library design.
Fluorine-substituted cyclofenil derivatives as estrogen receptor ligands: synthesis and structure-affinity relationship study of potential positron emission tomography agents for imaging estrogen receptors in breast cancer.
Antiplasmodial and antitrypanosomal activity of bicyclic amides and esters of dialkylamino acids.
Aryl sulfonamido tetralin inhibitors of the Kv1.5 ion channel.
Synthesis and therapeutic evaluation of pyridyl based novel mTOR inhibitors.
Discovery of a novel HCV helicase inhibitor by a de novo drug design approach.
Doubly loaded cycloSaligenyl-pronucleotides - 5,5'-Bis-(cycloSaligenyl-2',3'-dideoxy-2',3'-didehydrothymidine monophosphates).
Discovery of N-{N-[(3-cyanophenyl)sulfonyl]-4(R)-cyclobutylamino-(L)-prolyl}-4-[(3',5'-dichloroisonicotinoyl) amino]-(L)-phenylalanine (MK-0668), an extremely potent and orally active antagonist of very late antigen-4.
Optimization of 5-phenyl-3-pyridinecarbonitriles as PKCtheta inhibitors.
Regioselective synthesis and biological evaluation of bis(indolyl)methane derivatized 1,4-disubstituted 1,2,3-bistriazoles as anti-infective agents.
Toward the back-up of boceprevir (SCH 503034): discovery of new extended P4-capped ketoamide inhibitors of hepatitis C virus NS3 serine protease with improved potency and pharmacokinetic profiles.
Synthesis and activity of quinolinylmethyl P1' alpha-sulfone piperidine hydroxamate inhibitors of TACE.
Novel potent BRAF inhibitors: toward 1 nM compounds through optimization of the central phenyl ring.
2,6-Diphenylthiazolo[3,2-b][1,2,4]triazoles as telomeric G-quadruplex stabilizers.
Stereoselective synthesis and preliminary evaluation of new D-3-heteroarylcarbonylalanines as ligands of the NMDA receptor.
Synthesis and antibacterial activity of C-6 carbamate ketolides, a novel series of orally active ketolide antibiotics.
Development of a polyvalent assay system for lead identification.
More potent linear peptide inhibitors of mammalian ribonucleotide reductase.
Synthesis of fluorinated analogues of SJG-136 and their DNA-binding potential.
Corrigendum to Epibatidine structureactivity relationships
Synthesis, biological evaluations, and tubulin binding poses of C-2alpha sulfur linked taxol analogues.
6-hydroxy to 6'''-amino tethered ring-to-ring macrocyclic aminoglycosides as probes for APH(3')-IIIa kinase.
Synthesis and topoisomerase poisoning activity of A-ring and E-ring substituted luotonin A derivatives.
Selective and dual action orally active inhibitors of thrombin and factor Xa.
Synthesis and biological activity of naphthalene analogues of phenstatins: naphthylphenstatins.
Bridged androstenediol analogs as ER-beta selective SERMs.
Synthesis and evaluation of isoxazole derivatives as lysophosphatidic acid (LPA) antagonists.
ERbeta ligands. Part 6: 6H-Chromeno[4,3-b]quinolines as a new series of estrogen receptor beta-selective ligands.
Novel heterocyclic thyromimetics. Part 2.
The anti-androgen effect of ganoderol B isolated from the fruiting body of Ganoderma lucidum.
Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP).
Pyrazolone methylamino piperidine derivatives as novel CCR3 antagonists.
Synthesis of marine alkaloid: 8,9-dihydrocoscinamide B and its analogues as Novel class of antileishmanial agents.
Heterocyclic alpha-helix mimetics for targeting protein-protein interactions.
Structure-activity relationship study on anti-HIV 6-desfluoroquinolones.
Novel insight in structure-activity relationship and bioanalysis of P-glycoprotein targeting highly potent tetrakishydroxymethyl substituted 3,9-diazatetraasteranes.
Inactivation of NF-kappaB components by covalent binding of (-)-dehydroxymethylepoxyquinomicin to specific cysteine residues.
A new synthetic access to furo[3,2-f]chromene analogues of an antimycobacterial.
Enzymatically activated cycloSal-d4T-monophosphates: The third generation of cycloSal-pronucleotides.
Quinols as novel therapeutic agents. 7.1 Synthesis of antitumor 4-[1-(arylsulfonyl-1H-indol-2-yl)]-4-hydroxycyclohexa-2,5-dien-1-ones by Sonogashira reactions.
Cinnamoyl compounds as simple molecules that inhibit p300 histone acetyltransferase.
Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.
Synthesis and biological evaluation of chiral alpha-aminoanilides with central antinociceptive activity.
Scutiaquinones A and B, perylenequinones from the roots of Scutia myrtina with anthelmintic activity.
Synthesis and activity studies of analogues of the rat selective toxicant norbormide.
Antimalarial activity of 1-aryl-3,3-dialkyltriazenes.
The isolation of secondary metabolites and in vitro potent anti-cancer activity of clerodermic acid from Enicosanthum membranifolium.
Novel 9a-carbamoyl- and 9a-thiocarbamoyl-3-decladinosyl-6-hydroxy and 6-methoxy derivatives of 15-membered macrolides.
Novel nitrogen mustard-armed combi-molecules for the selective targeting of epidermal growth factor receptor overexperessing solid tumors: discovery of an unusual structure-activity relationship.
Discovery of a novel series of nonsteroidal androgen receptor modulators: 5- or 6-oxachrysen-2-ones.
Phenylethynyl-pyrrolo[1,2-a]pyrazine: a new potent and selective tool in the mGluR5 antagonists arena.
Targeting ACE and ECE with dual acting inhibitors.
Synthesis and biological properties of beta-turned Abeta(31-35) constrained analogues.
Novel methylene-linked heterocyclic EP1 receptor antagonists.
Imidazo[1,2-a]pyridine derivatives as inhibitors of TNF-alpha expression in T cells.
Synthesis and biological evaluation of cyclopropyl analogues of fosmidomycin as potent Plasmodium falciparum growth inhibitors.
Aminobenzisoxazoles with biaryl P4 moieties as potent, selective, and orally bioavailable factor Xa inhibitors.
Design and synthesis of novel HIV-1 protease inhibitors incorporating oxyindoles as the P2'-ligands.
Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases.
The development of 2-benzimidazole substituted pyrimidine based inhibitors of lymphocyte specific kinase (Lck).
Synthesis and antibacterial activity of novel neamine derivatives.
Synthesis and anti-microbial activity of pyrazolylbisindoles--promising anti-fungal compounds.
Synthesis and biological evaluation of type VI beta-turn templated RGD peptidomimetics.
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
Glyceraldehyde 3-phosphate dehydrogenase is a cellular target of the insulin mimic demethylasterriquinone B1.
Biscembranoids and their probable biogenetic precursor from the Hainan soft coral Sarcophyton tortuosum.
Computer-aided rational drug design: a novel agent (SR13668) designed to mimic the unique anticancer mechanisms of dietary indole-3-carbinol to block Akt signaling.
Metabolically labile cannabinoid esters: a 'soft drug' approach for the development of cannabinoid-based therapeutic drugs.
Modification of the ceramide moiety of isoglobotrihexosylceramide on its agonist activity in stimulation of invariant natural killer T cells.
Synthesis and structure-activity relationship of novel RXR antagonists: orally active anti-diabetic and anti-obesity agents.
Synthesis and SAR of p38alpha MAP kinase inhibitors based on heterobicyclic scaffolds.
Novel thiazolones as HCV NS5B polymerase allosteric inhibitors: Further designs, SAR, and X-ray complex structure.
Serendipitous discovery of novel imidazolopyrazole scaffold as selective androgen receptor modulators.
5-HT2C antagonists based on fused heterotricyclic templates: design, synthesis and biological evaluation.
Tryptamine-based human beta3-adrenergic receptor agonists. Part 2: SAR of the methylene derivatives.
Peptide deformylase inhibitors with activity against respiratory tract pathogens.
Potent and selective conformationally restricted neuronal nitric oxide synthase inhibitors.
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands.
Synthesis of novel rhinacanthins and related anticancer naphthoquinone esters.
3-Hydroxy-4-arylsulfonyltetrahydropyranyl-3-hydroxamic acids are novel inhibitors of MMP-13 and aggrecanase.
Antituberculous activity of some aryl semicarbazone derivatives.
Synthesis and biological evaluation of flavonoids as vasorelaxant agents.
Synthesis and structure-activity relationships of novel IKK-beta inhibitors. Part 2: Improvement of in vitro activity.
Novel thiophenes and analogues with anthelmintic activity against Haemonchus contortus.
Synthesis and antiviral activity of P1' arylsulfonamide azacyclic urea HIV protease inhibitors.
P4 cap modified tetrapeptidyl alpha-ketoamides as potent HCV NS3 protease inhibitors.
D-piece modifications of the hemiasterlin analog HTI-286 produce potent tubulin inhibitors.
Ligand conformation has a definitive effect on 5-HT1A and serotonin reuptake affinity.
Antileishmanial pyrazolopyridine derivatives: synthesis and structure-activity relationship analysis.
Benzoxepin-derived estrogen receptor modulators: a novel molecular scaffold for the estrogen receptor.
Accurate prediction of the relative potencies of members of a series of kinase inhibitors using molecular docking and MM-GBSA scoring.
Substituted 5-benzyl-2-phenyl-5H-imidazo[4,5-c]pyridines: a new class of pestivirus inhibitors.
Synthesis and evaluation of thiazepines as interleukin-1beta converting enzyme (ICE) inhibitors.
Design, synthesis, and evaluation of potent and selective ligands for the dopamine 3 (D3) receptor with a novel in vivo behavioral profile.
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates.
Discovery of bioavailable 4,4-disubstituted piperidines as potent ligands of the chemokine receptor 5 and inhibitors of the human immunodeficiency virus-1.
Polyoxygenated diterpenes from the sponge Phorbas sp.
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
Meroditerpenoids from the brown alga Sargassum siliquastrum.
Hunter-killer peptide (HKP) for targeted therapy.
Lignans from the roots of Saururus chinensis.
A novel cell-penetrating peptide sequence derived by structural minimization of a snake toxin exhibits preferential nucleolar localization.
Discovery of boronic acids as novel and potent inhibitors of fatty acid amide hydrolase.
Triazine compounds as antagonists at Bv8-prokineticin receptors.
The identification, synthesis, protein crystal structure and in vitro biochemical evaluation of a new 3,4-diarylpyrazole class of Hsp90 inhibitors.
(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.
Identification of aminopiperidine benzamides as MCHr1 antagonists.
Novel and potent cyclic cyanamide-based cathepsin K inhibitors.
Regioselective synthesis and antitumor screening of some novel N-phenylpyrazole derivatives.
Design, synthesis and antimalarial activity of benzene and isoquinoline sulfonamide derivatives.
Synthesis and in vitro anti-leukemic activity of structural analogues of JS-K, an anti-cancer lead compound.
Synthesis and pharmacological evaluation of pyrazoline derivatives as new anti-inflammatory and analgesic agents.
Design and synthesis of DPP-IV inhibitors lacking the electrophilic nitrile group.
Discovery of kinase inhibitors by high-throughput docking and scoring based on a transferable linear interaction energy model.
Allosteric modulators of the alpha7 nicotinic acetylcholine receptor.
Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Large neutral amino acid transporter enables brain drug delivery via prodrugs.
Adenosine analogues as inhibitors of P2Y12 receptor mediated platelet aggregation.
Exploring inhibitor binding at the S' subsites of cathepsin L.
Synthesis of spiro[chroman-2,4'-piperidin]-4-one derivatives as acetyl-CoA carboxylase inhibitors.
Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines.
Synthesis and evaluation of photoreactive probes to elucidate iodide efflux in thyrocytes.
(-)-Cercosporamide derivatives as novel antihyperglycemic agents.
Synthesis and biological activity of novel shikonin analogues.
Curcumin is a potent DNA hypomethylation agent.
Spiro-piperidine azetidinones as potent TRPV1 antagonists.
Structure-activity delineation of quinones related to the biologically active Calothrixin B.
Synthesis of 2'-paclitaxel methyl 2-glucopyranosyl succinate for specific targeted delivery to cancer cells.
Synthesis of pyochelin-norfloxacin conjugates.
Novel antitumor agent family of 1H-benzo[c,d]indol-2-one with flexible basic side chains: synthesis and biological evaluation.
Discovery of (Z)-2-phenyl-3-(1H-pyrrol-2-yl)acrylonitrile derivatives active against Haemonchus contortus and Ctenocephalides felis (cat flea).
Synthesis and antitumor evaluation of a novel series of triaminotriazine derivatives.
Carinatumins A-C, new alkaloids from Lycopodium carinatum inhibiting acetylcholinesterase.
Synthesis and biological evaluation of thiazolidine-2-one 1,1-dioxide as inhibitors of Escherichia coli beta-ketoacyl-ACP-synthase III (FabH).
Synthesis and evaluation of prodrugs for anti-angiogenic pyrrolylmethylidenyl oxindoles.
Coriaheptocins A and B, the First Heptahydroxylated Acetogenins, Isolated from the Roots of Annona coriacea 1
Cyclic Peptides from Higher Plants. 39. Dichotomins F and G, Cyclic Peptides from Stellaria dichotoma var. lanceolata
Micropeptins 478-A and -B, Plasmin Inhibitors from the Cyanobacterium Microcystis aeruginosa
A bioactive seco-rosane diterpenoid from Vellozia candida.
New Oxygenated Sesquiterpenes from the Indonesian Soft Coral Nephthea chabrolii
Inhibition of Bacterial RNA Polymerases. Peptide Metabolites from the Cultures of Streptomyces sp.
Sodwanones K, L, and M; new triterpenes from the marine sponge Axinella weltneri.
Bioactive Terpenoids from Octocorallia. 4. Three New Cembrane-Type Diterpenoids from the Soft Coral Lobophytum schoedei
1-Hydroxyditerpenes from Two New Zealand Liverworts, Paraschistochila pinnatifolia and Trichocolea mollissima
New Agelasine Compound from the Marine Sponge Agelas mauritiana as an Antifouling Substance against Macroalgae
New anti-HIV-1, antimalarial, and antifungal compounds from Terminalia bellerica.
New Steroidal Alkaloids from the Roots of Buxus sempervirens
Stellettamide B, a new indolizidine alkaloid from a sponge of the genus Stelletta.
Bengamides and Related New Amino Acid Derivatives from the New Caledonian Marine Sponge Jaspis carteri
Anserinones A and B: new antifungal and antibacterial benzoquinones from the coprophilous fungus Podospora anserina.
Naphthalenone and Phthalide Metabolites from Lachnum papyraceum 1
New indole derivatives with free radical scavenging activity from Agrocybe cylindracea.
RKS-1778, a new mammalian cell-cycle inhibitor and a key intermediate of the [11]cytochalasin group.
New Furanoterpenoids from the Sponge Spongia officinalis
Cavernosolide, a New Sesterterpene from a Tyrrhenian Sponge
New geranyl stilbenes from Dalea purpurea with in vitro opioid receptor affinity.
Two new analogues of the cytotoxic substance BE-52211 from Streptomyces sp.
Macrolactin N, a new peptide deformylase inhibitor produced by Bacillus subtilis.
Novel aminobenzimidazoles as selective MCH-R1 antagonists for the treatment of metabolic diseases.
Discovery and in vitro/in vivo studies of tetrazole derivatives as Kv1.5 blockers.
Aza-stilbenes as potent and selective c-RAF inhibitors.
Synthesis and structural activity relationship of 11beta-HSD1 inhibitors with novel adamantane replacements.
p38 MAP kinase inhibitors. Part 5: discovery of an orally bio-available and highly efficacious compound based on the 7-amino-naphthyridone scaffold.
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.
Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.
Multivalent effects of RGD peptides obtained by nanoparticle display.
Improved therapeutic efficacy of doxorubicin through conjugation with a novel peptide drug delivery technology (Vectocell).
Novel Schiff base copper complexes of quinoline-2 carboxaldehyde as proteasome inhibitors in human prostate cancer cells.
Design, synthesis, and preliminary evaluation of doxazolidine carbamates as prodrugs activated by carboxylesterases.
Structural basis for the structure-activity relationships of peroxisome proliferator-activated receptor agonists.
Using fragment cocktail crystallography to assist inhibitor design of Trypanosoma brucei nucleoside 2-deoxyribosyltransferase.
Array synthesis of progesterone receptor antagonists: 3-aryl-1,2-diazepines.
1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR.
A three-dimensional pharmacophore model for 5-hydroxytryptamine6 (5-HT6) receptor antagonists.
Studies on the apoptotic activity of natural and synthetic retinoids: discovery of a new class of synthetic terphenyls that potently support cell growth and inhibit apoptosis in neuronal and HL-60 cells.
p53 Activation by small molecules: application in oncology.
Discovery of high-affinity ligands of sigma1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screening.
Structure-based design, synthesis, and biological evaluation of inhibitors of Mycobacterium tuberculosis type II dehydroquinase.
5'-Homoneplanocin A inhibits hepatitis B and hepatitis C.
8-Substituted 3,4-dihydroquinolinones as a novel scaffold for atypical antipsychotic activity.
Diamino-C,N-diarylpyridine positional isomers as inhibitors of lysophosphatidic acid acyltransferase-beta.
Acyl ureas as human liver glycogen phosphorylase inhibitors for the treatment of type 2 diabetes.
Kynurenamines as neural nitric oxide synthase inhibitors.
Pharmacophore modeling, docking, and principal component analysis based clustering: combined computer-assisted approaches to identify new inhibitors of the human rhinovirus coat protein.
Designed multiple ligands. An emerging drug discovery paradigm.
Design and synthesis of novel antibacterial peptide-resin conjugates.
Design, synthesis and biological evaluation of substituted dioxodibenzothiazepines and dibenzocycloheptanes as farnesyltransferase inhibitors.
Novel, potent THC/anandamide (hybrid) analogs.
Structure-activity relationship (SAR) investigations of substituted imidazole analogs as TRPV1 antagonists.
Efficient synthesis and biological evaluation of 1,2,9-trisubstituted 1,9-dihydro-6H-purin-6-ones.
Determination of 1-aryl-4-propylpiperazine pKa values: the substituent on aryl modulates basicity.
Preliminary investigations on the synthesis and antitumor activity of 3(2H)-furanones.
Design of beta-hairpin peptides for modulation of cell adhesion by beta-turn constraint.
A novel and potent VLA-4 antagonist based on trans-4-substituted cyclohexanecarboxylic acid.
Tetracyclic indole inhibitors of hepatitis C virus NS5B-polymerase.
Effect of fluorination on the pharmacological profile of 11beta isomers of fulvestrant in breast carcinoma cells.
2-Aminoimidazoles inhibitors of TGF-beta receptor 1.
The discovery of a selective, small molecule agonist for the MAS-related gene X1 receptor.
New small-molecule synthetic antimycobacterials.
Concentration-effect relationship of ceftazidime explains why the time above the MIC is 40 percent for a static effect in vivo.
Synergistic effect of posaconazole and caspofungin against clinical zygomycetes.
Colistin methanesulfonate against multidrug-resistant Acinetobacter baumannii in an in vitro pharmacodynamic model.
One-pot synthesis and antibacterial activities of pyrazolo[4',3':5,6]pyrido[2,3-d]pyrimidine-dione derivatives.
N-Glycine-sulfonamides as potent dual orexin 1/orexin 2 receptor antagonists.
Exploring the connection unit in the HDAC inhibitor pharmacophore model: novel uracil-based hydroxamates.
Identification of a potent and selective 5-HT1B receptor antagonist.
Synthesis of potent and selective serotonin 5-HT1B receptor ligands.
A new antitumor compound from the plant Oryctanthus sp. as a VEGF receptor binding inhibitor.
The synthesis and 16S A-site rRNA recognition of carbohydrate-free aminoglycosides.
Plakolide A, a new gamma-lactone from the marine sponge Plakortis sp.
Excisanin H, a novel cytotoxic 14,20-epoxy-ent-kaurene diterpenoid, and three new ent-kaurene diterpenoids from Rabdosia excisa.
Cytotoxic compounds from Mundulea chapelieri from the Madagascar Rainforest.
Four new triterpenoids from Maytenus ilicifolia.
Two new xanthone derivatives from the algicolous marine fungus Wardomyces anomalus.
Seco-prezizaane-type sesquiterpenes and an abietane-type diterpene from Illicium minwanense.
Homopseudopteroxazole, a new antimycobacterial diterpene alkaloid from Pseudopterogorgia elisabethae.
Acinospesigenin-A, -B, and -C: three new triterpenoids from Phytolacca acinosa.
Renieramycin J, a highly cytotoxic tetrahydroisoquinoline alkaloid, from a marine sponge Neopetrosia sp..
Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.
Synthesis of water-soluble prodrugs of BMS-191011: a maxi-K channel opener targeted for post-stroke neuroprotection.
Synthesis and biological evaluation of a novel phenyl substituted sydnone series as potential antitumor agents.
First total synthesis of structurally unique flavonoids and their strong anti-inflammatory effect.
3-(7-Azaindolyl)-4-arylmaleimides as potent, selective inhibitors of glycogen synthase kinase-3.
4-Substituted anilides as selective melatonin MT2 receptor agonists.
Effective irreversible alkylating reagents based on the structure of clavulones.
Synthesis and biological evaluation of pyrrolo[2,1-c][1,4]benzodiazepine (PBD) C8 cyclic amine conjugates.
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 5: Combined A- and C-ring structure-activity relationship studies.
Indoloxypropanolamine analogues as 5-HT(1A) receptor antagonists.
Design, synthesis and biological evaluation of novel lipoamino acid-based glycolipids for oral drug delivery.
Taxodistines A and B, abietane-type diterpenes from Taxodium distichum.
Alpha-diaminobutyric acid-linked hairpin polyamides.
Efficient one-pot synthesis of biologically active polysubstituted aromatic amines.
Synthesis and antibacterial activity of pyranmycin derivatives with N-1 and O-6 modifications.
Syntheses and optimization of new GS39783 analogues as positive allosteric modulators of GABA B receptors.
Phenylimidazole derivatives as specific inhibitors of bacterial enoyl-acyl carrier protein reductase FabK.
Synthetic studies of neoclerodane diterpenes from Salvia divinorum: exploration of the 1-position.
Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships.
MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus.
From docking false-positive to active anti-HIV agent.
A simple method for the preparation of PEG-6-mercaptopurine for oral administration.
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
Synthesis, structure-activity relationship and in vivo antiinflammatory efficacy of substituted dipiperidines as CCR2 antagonists.
Identifying common metalloprotease inhibitors by protein fold types using Fourier transform mass spectrometry.
Hit generation and exploration: imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases.
New biologically active epidioxysterols from Stereum hirsutum.
Design and synthesis via click chemistry of 8,9-anhydroerythromycin A 6,9-hemiketal analogues with anti-MRSA and -VRE activity.
Discovery of 1,1-dioxo-1,2,6-thiadiazine-5-carboxamide derivatives as cannabinoid-like molecules with agonist and antagonist activity.
New 1,2,3,4-tetrahydropyrrolo[3,4-b]indole derivatives as selective CB2 receptor agonists.
Effect of varying the 4''-position of arbekacin derivatives on antibacterial activity against MRSA and Pseudomonas aeruginosa.
DNA cleavage by photolysis of aryl sulfoxides.
Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.
Cryptadines A and B, novel C27N3-type pentacyclic alkaloids from Lycopodium cryptomerinum.
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.
Synthesis and evaluation of novel pyrazolidinone analogs of PGE2 as EP2 and EP4 receptors agonists.
Discovery of novel isoxazolines as anti-tuberculosis agents.
Synthesis of andrographolide derivatives and their TNF-alpha and IL-6 expression inhibitory activities.
Syntheses of novel myxopyronin B analogs as potential inhibitors of bacterial RNA polymerase.
Stereoselectivity by enantiomeric inhibitors of matrix metalloproteinase-8: new insights from molecular dynamics simulations.
Improved biochemical strategies for targeted delivery of taxoids.
Leuconoxine, kopsinitarine, kopsijasmine, and kopsinone derivatives from Kopsia.
Design and synthesis of hepatoselective, pyrrole-based HMG-CoA reductase inhibitors.
Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.
Synthesis of 2-[3,5-substituted pyrazol-1-yl]-4,6-trisubstituted triazine derivatives as antimalarial agents.
Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain.
Binding of isotryptamines and indenes at h5-HT6 serotonin receptors.
2-(Arylmethyl)-3-substituted quinuclidines as selective alpha 7 nicotinic receptor ligands.
6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists.
Muscarinic allosteric enhancers of ligand binding: pivotal pharmacophoric elements in hexamethonio-type agents.
Synthesis and pharmacology of ethylphenidate enantiomers: the human transesterification metabolite of methylphenidate and ethanol.
Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases.
Combinatorial optimization of isatin-beta-thiosemicarbazones as anti-poxvirus agents.
Discovery of a beta-MSH-derived MC-4R selective agonist.
Preparation of 3-spirocyclic indolin-2-ones as ligands for the ORL-1 receptor.
Synthesis of desthio prenylcysteine analogs: sulfur is important for biological activity.
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
Saucerneol B derivatives as human acyl-CoA: cholesterol acyltransferase inhibitors.
Brucella suis histidinol dehydrogenase: synthesis and inhibition studies of a series of substituted benzylic ketones derived from histidine.
Antibacterial nicotinamide adenine dinucleotide synthetase inhibitors: amide- and ether-linked tethered dimers with alpha-amino acid end groups.
Investigation into the P3 binding domain of m-calpain using photoswitchable diazo- and triazene-dipeptide aldehydes: new anticataract agents.
Tetrahydroisoquinoline based sulfonamide hydroxamates as potent matrix metalloproteinase inhibitors.
Peptidyl hydroxamic acids as methionine aminopeptidase inhibitors.
Synthesis and antibacterial activity of 6-O-arylpropargyl-9-oxime-11,12-carbamate ketolides.
Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia.
Reverse hydroxamate-based selective TACE inhibitors.
The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
Synthesis and activity of phosphinic tripeptide inhibitors of cathepsin C.
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Synthesis and antiangiogenic activity of exo-olefinated deoxoartemisinin derivatives.
(+)-3-[2-(Benzo[b]thiophen-2-yl)-2-oxoethyl]-1-azabicyclo[2.2.2]octane as potent agonists for the alpha7 nicotinic acetylcholine receptor.
Triaryl methane derivatives as antiproliferative agents.
Aspermytin A: a new neurotrophic polyketide isolated from a marine-derived fungus of the genus Aspergillus.
Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors.
Discovery of 2-pyrimidyl-5-amidothiophenes as potent inhibitors for AKT: synthesis and SAR studies.
Novel, orally bioavailable gamma-aminoamide CC chemokine receptor 2 (CCR2) antagonists.
Metabolism investigation leading to novel drug design 2: orally active prostacyclin mimetics. Part 5.
A novel class of AMPA receptor allosteric modulators. Part 1: design, synthesis, and SAR of 3-aryl-4-cyano-5-substituted-heteroaryl-2-carboxylic acid derivatives.
Synthesis and cytotoxicity of leinamycin antibiotic analogues.
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. 4. Opioid receptor binding properties of 8-[N-(4'-phenyl)-phenethyl)carboxamido] analogues of cyclazocine and ethylketocycalzocine.
TEM-158 (CMT-9), a new member of the CMT-type extended-spectrum beta-lactamases.
Functional characterization of TcaA: minimal requirement for teicoplanin susceptibility and role in Caenorhabditis elegans virulence.
A class of potent tyrosinase inhibitors: alkylidenethiosemicarbazide compounds.
Anti-HIV evaluation of benzo[d]isothiazole hydrazones.
Design, synthesis, structure-activity relationship and antibacterial activity series of novel imidazo fused quinolone carboxamides.
Synthesis, antimicrobial and cytotoxic activities of 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazoles.
Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities.
Antifungal unsaturated cyclic Mannich ketones and amino alcohols: study of mechanism of action.
[35S]GTP gamma S binding studies of amphiphilic drugs-activated Gi proteins: a caveat.
Biphenyl C-cyclopropylalkylamides: New scaffolds for targeting estrogen receptor beta.
Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors.
L337H mutant of rat neuronal nitric oxide synthase resembles human neuronal nitric oxide synthase toward inhibitors.
Octahydropyrrolo[3,4-c]pyrrole: a diamine scaffold for construction of either alpha4beta2 or alpha7-selective nicotinic acetylcholine receptor (nAChR) ligands. Substitutions that switch subtype selectivity.
Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.
A novel dimeric diterpene from Salvia prionitis.
Potent and selective CC-chemokine receptor-2 (CCR2) antagonists as a potential treatment for asthma.
Synthesis and evaluation of a phosphonate analogue of the soluble guanylate cyclase activator YC-1.
New triterpene glucosides, oligoporins A-C, from Oligoporus tephroleucus protect DNA from Fenton reaction.
Synthesis and antitrichinellosis activity of some bis(benzimidazol-2-yl)amines.
New celecoxib derivatives as anti-inflammatory agents.
Biochemical and structural evaluation of highly selective 2-arylbenzoxazole-based transthyretin amyloidogenesis inhibitors.
Fragment-based discovery of mexiletine derivatives as orally bioavailable inhibitors of urokinase-type plasminogen activator.
Pradefovir: a prodrug that targets adefovir to the liver for the treatment of hepatitis B.
Chemoenzymatic synthesis and antiviral evaluation of conformationally constrained and 3'-methyl-branched carbanucleosides using both enantiomers of the same building block.
Nitrogen-appended N-alkylsulfonamides as inhibitors of gamma-secretase.
Discovery of beta-benzamido hydroxamic acids as potent, selective, and orally bioavailable TACE inhibitors.
Novel thiol-based TACE inhibitors. Part 2: Rational design, synthesis, and SAR of thiol-containing aryl sulfones.
Identification of 2-amino-5-(thioaryl)thiazoles as inhibitors of nerve growth factor receptor TrkA.
A flavonoid gossypin binds to cyclin-dependent kinase 2.
Triazole derivatives as non-nucleoside inhibitors of HIV-1 reverse transcriptase--structure-activity relationships and crystallographic analysis.
Cy3-3-acylcholine: a fluorescent analogue of acetylcholine for single molecule detection.
Antimitotic quinoid triterpenes from Maytenus chuchuhuasca.
Synthesis, biological evaluation and quantitative structure-activities relationship of flavonoids as vasorelaxant agents.
Cyathusals A, B, and C, antioxidants from the fermented mushroom Cyathus stercoreus.
Synthesis, antifungal and antimicrobial activity of alkylphospholipids.
Design, synthesis, and anticonvulsant activity of some sulfamides.
Indole alkaloids produced by a marine fungus isolate of Penicillium janthinellum Biourge.
Terpenoids from the medicinal plant Maytenus ilicifolia.
3-Hydroxy-1,5-dihydro-pyrrol-2-one derivatives as advanced inhibitors of HIV integrase.
Synthesis and biological evaluation of conformationally constrained analogues of the antitubercular agent ethambutol.
CP5484, a novel quaternary carbapenem with potent anti-MRSA activity and reduced toxicity.
Trifunctional norrisolide probes for the study of Golgi vesiculation.
Effect of substituents on diarylmethanes for antitubercular activity.
Synthesis and antimalarial activity of new 1,12-bis(N,N'-acetamidinyl)dodecane derivatives.
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists.
Antiplasmodial activity of lauryl-lysine oligomers.
Daptomycin nonsusceptibility in Staphylococcus aureus with reduced vancomycin susceptibility is independent of alterations in MprF.
(2S,2'R)-analogue of LG190178 is a major active isomer.
The design and synthesis of novel alpha-ketoamide-based p38 MAP kinase inhibitors.
Synthesis and biological evaluation of 8-oxoadenine derivatives as toll-like receptor 7 agonists introducing the antedrug concept.
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
4,7-Dichloro benzothien-2-yl sulfonylaminomethyl boronic acid: first boronic acid-derived beta-lactamase inhibitor with class A, C, and D activity.
Aminofurazans as potent inhibitors of AKT kinase.
Evaluation of aldose reductase inhibition and docking studies of 6'-nitro and 6',6''-dinitrorosmarinic acids.
Synthesis and antimicrobial activity of novel pyrazolo[3,4-d]pyrimidin derivatives.
Synthesis and in vitro antiproliferative activities of quinoline derivatives.
Synthesis, biological and medicinal significance of S-glycosido-thieno[2,3-d]-pyrimidines as new anti-inflammatory and analgesic agents.
Polybioside, a neuroactive compound from the venom of the social wasp Polybia paulista.
HPLC-based activity profiling for GABA(A) receptor modulators: a new dihydroisocoumarin from Haloxylon scoparium.
Cytotoxic polyisoprenyl benzophenonoids from Garcinia subelliptica.
1-(2-(2,2,2-trifluoroethoxy)ethyl-1H-pyrazolo[4,3-d]pyrimidines as potent phosphodiesterase 5 (PDE5) inhibitors.
Diterpenoids from the feces of Trogopterus xanthipes.
Silica-supported fluoroboric acid (HBF(4)-SiO(2)) catalyzed highly productive synthesis of thiomorpholides as activators of l-asparaginase as well as the antioxidant agent.
Antibiotic indole sesquiterpene alkaloid from Greenwayodendron suaveolens with a new natural product framework.
Synthesis and structure-activity relationships of potent 4-fluoro-2-cyanopyrrolidine dipeptidyl peptidase IV inhibitors.
1-(2-METHOXYPHENYL)-4-ALKYLPIPERAZINES: EFFECT OF THE N-4 SUBSTITUENT ON THE AFFINITY AND SELECTIVITY FOR DOPAMINE D4 RECEPTOR
Benzofuran based angiotensin II antagonists related to GR117289: enhancement of potency in vitro and oral activity
Simple cis-epoxide-based inhibitors of HIV-1 protease
Total synthesis of novel conduritol related compounds capable of modulating insulin release.
4,5,6,7-Tetrahdryo-8-oxo-cycloheptimidazoles: a new class of potent non-peptide angiiotensin II receptor antagonists
Combined glycomimetic and multivalent strategies for the design of potent selectin antagonists
Tannins as selective inhibitors of protein kinase C
Synthesis and pharmacological activity of a macrocyclic benzamide
Purine 2, 3-acyclonucleosides: Improved synthesis and antiparasitic actimity
Synthesis and biological activities of new heterocyclic aromatic retinoids
Chiral carbocylic nucleosides: The synthesis and antiviral activity of 4-hydroxy and 4-fluorocarbocyclic - 2- deoxyguanosines
A general approach toward the design of mechanism-based inactivators of serine proteinases: inactivation of human leukocyte elastase by a phthalimide derivative
Reduced amide bond neurotensin 813 mimetics with potent in vivo activity
Synthesis of new imidazo[1,2-b]pyridazine isosteres of potent imidazo[4,5-b]pyridine angiotensin II antagonists
Novel indolactam-based inhibitors of matrix metalloproteinases
Synthesis and -lactamase inhibitory evaluation of novel 6-halo-2-chloromethyl-2-methylpenam-3-carboxylic acids and their sulfones and 6-halo-2-mercaptobenzothiazolylmethyl-2-methylpenam-3-carboxylic acids
Inhibition of cartilage degradation by isothiazoloquinolinones
Discovery of FK453, a novel non-xanthine adenosine A1 receptor antagonist
Electrosynthesis of 4,4-dimethyl-2-ethoxycarbonyl-5-fluoro-3-thiolanones: highly potent human type II PLA2 inhibitors
DISCOVERY OF A NOVEL CLASS OF BK CHANNEL OPENERS: ENANTIOSPECIFIC SYNTHESIS AND BK CHANNEL OPENING ACTIVITY OF 3-(5-CHLORO-2-HYDROXYPHENYL)-1,3-DIHYDRO-3-HYDROXY-6-(TRIFLUOROMETHYL)-2H-INDOL-2-ONE
Rational design of purine nucleoside phosphorylase inhibitors: Design of 2-(2-Haloethyl) and 2-ethenyl substituted quinazolinone alkylating agents.
Quinuclidine based NK-1 antagonists 2: determination of the absolute stereochemical requirements
A convenient synthesis of sulfated and sialyl oligosaccharides as potential ligands for CD22 adhesion protein
Synthesis and antitumor activity of novel cyclopropapyrroloindole (CPI) derivatives bearing bis(methoxycarbonyl) groups
Optical isomers of RP 64406: New potent antiglutamate agents
Alkyl ether analogs of the FK-506 related, immunosuppressive macrolide L-683,590 (ascomycin)
O-benzyl hydroxyproline as a bioisostere for Phe-Pro: Novel dipeptide thrombin inhibitors
Design and syntheses of 4-acylaminopyridine derivatives: Novel high affinity choline uptake enhancers II
Synthesis and antiviral evaluation of enantiomeric 2,3-dideoxy- and 2,3-didehydro-2,3-dideoxy-4-thionucleosides
Synthesis of and glycosidase inhibition by -l-homofuconojirimycin
Synthesis of 2,3-dideoxy-2,3-didehydronucleoside analogues as potential anti HIV agents
-((Tetronoyl)oxy)- and -((tetramoyl)oxy)methyl ketone inhibitors of the interleukin-1 converting enzyme (ICE)
Benzolactam growth hormone secretagogues: replacements for the 2-tetrazole moiety of L-692,429
The first selective antagonist for a GABAC receptor
-hydroxy- and -ketoester functionalized thrombin inhibitors
The squalestatins: effects of changes at the allylic centre in the C1 sidechain
Synthesis of peptidyl acetals as inhibitors of prolyl endopeptidase
Functionalized aliphatic P2/P2 analogs of HIV-1 protease inhibitor DMP323
Calcineurin has a very tight-binding pocket for the side chain of residue 4 of cyclosporin
Conformation of the CYP2D6 model substrate sparteine under physiological conditions
Arylpiperazide derivatives of phenylpiperazines as a new class of potent and selective 5-HT1B receptor antagonists
The synthesis of BRL 49653 - a novel and potent antihyperglycaemic agent
S-carbobenzoxyglutathione: a competitive inhibitor of mammalian glyoxalase II.
Structure-activity studies of highly potent cyclic [Cys4,Cys10]Melanotropin analogues.
Synthesis and characterization of a fluorescent analogue of methotrexate.
Antidepressant activity of 5-aryl-2,3,5,6-tetrahydroimidazo[2,1-a]isoquinolin-5-ols.
Synthesis and antiviral activity of carbocyclic analogues of 2'-deoxyribofuranosides of 2-amino-6-substituted-purines and of 2-amino-6-substituted-8-azapurines.
Tetrahydropyrrolo[1,2-a]quinoxalines and tetrahydropyrrolo[1,2-a]pyrido[3,2-a]pyrazines: vascular smooth muscle relaxants and antihypertensive agents.
Quantitative structure-activity relationships of 6-anilinouracils as inhibitors of Bacillus subtilis DNA polymerase III.
Potential antitumor agents. 42. Structure-activity relationships for acridine-substituted dimethyl phosphoramidate derivatives of 9-anilinoacridine.
Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues.
Antitrichomonal activity of mesoionic thiazolo[3,2-a]pyridines.
New bicyclic antidepressant agent. Synthesis and activity of napactadine and related compounds.
Synthesis and dopaminergic activity of (R)- and (S)-4-hydroxy-2-(di-n-propylamino)indan.
Glutamine-derived aldehydes for the inhibition of human rhinovirus 3C protease
Synthesis and structure-activity relationships of new acetylcholinesterase inhibitors: Morpholinoalkylcarbamoyloxyeseroline derivatives
Synthesis and biological evaluation of 2,3-diarylthiophenes as selective Cox-2 and Cox-1 inhibitors
Synthesis and pharmacological activities of a novel tripeptide mimetic dopamine prodrug
The antitumor activity of novel pyrazoloquinoline derivatives
Purification of pig and rat liver squalene epoxidase by affinity chromatography
Butyrophenone analogues: Synthesis of 2-methyl-3-ethyl-5-aminoethyl-4,5,6,7-tetrahydroindol-4-ones, and their affinities for d1, d2 and 5-ht2a receptors
Cmi-206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor
A systematic study of P1P3 spanning sidechains for the inhibition of HIV-1 protease
Synthesis and in vitro cytotoxicity of ()-acetomycin and related analogs
Isosinococuline, a novel antitumor morphinane alkaloid from Cocculus trilobus
Synthesis and bioassay of a protein tyrosine phosphatase inhibitor, dephostatin
Preparation and biological evaluation of -Trifluoromethyl-,-unsaturated carbonyl compounds
Non-peptide oxytocin antagonists: identification and synthesis of a potent camphor aminosuccinimide
Selectively deoxygenated sulfated tetrasaccharides as probes for the investigation of smooth muscle cell antiproliferative activity
Synthesis and biological evaluation of 2,3-diarylthiophenes as selective cox-2 inhibitors. part II: Replacing the heterocycle
Suppression of morphine and cocaine self-administration in rats by a mixed mu antagonist-kappa agonist (N-CBM-TAMO) and a long-acting selective D1 antagonist (AS-300)
Tetrahydrothienopyridine derivatives as novel GPIIb/IIIa antagonists
The synthesis of a hematoregulatory agent based on HP-5B containing an effective, achiral cystine replacement
Structural comparison of alkylpolyamine analogues with potent in vitro antitumor or antiparasitic activity
New simplified inhibitors of EPSP synthase: The importance of ring size for recognition at the shikimate 3-phosphate site
Novel inhibitors of influenza sialidases related to GG167 structure-activity, crystallographic and Molecular dynamics studies with 4H-pyran-2-carboxylic acid 6-carboxamides
SAR of 2-benzyl-4-aminopiperidines NK1 antagonists. Part 21. synthesis of CGP 49823
Synthesis of conformationally-restricted boropeptide thrombin inhibitors
Pyrazolo[3,4-d]pyrimidines: C4, C6 substitution leads to adenosine A1 receptor selectivity
Antioxidant properties of nitrocaffeic acids
Synthesis and biological activity of novel sialyl-lewisX conjugates
-Methanesulfonyl-L-valine as a novel, unnatural amino acid surrogate for P2 in the design of HIV protease inhibitors.
Synthesis and antitumor activity of (2R,3R)-2,3-dihydroxy- and -2,3-dialkoxy-1,4-diaminobutane platinum(II) complexes
Modifications of the isonipecotic acid fragment of SNS-032: analogs with improved permeability and lower efflux ratio.
2-Trifluoroacetylthiophene oxadiazoles as potent and selective class II human histone deacetylase inhibitors.
Potent benzimidazolone-based CGRP receptor antagonists.
Highly potent and selective chiral inhibitors of PDE5: an illustration of Pfeiffer's rule.
The first X-ray crystal structure of the glucocorticoid receptor bound to a non-steroidal agonist.
Synthesis and biological activities of novel nonpeptide angiotensin II receptor antagonists based on benzimidazole derivatives bearing a heterocyclic ring.
Synthesis and in vitro evaluation of the antifungal activities of dihydropyrimidinones.
Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation.
Benzimidazole- and benzoxazole-based inhibitors of Rho kinase.
Convergent synthesis and cruzain inhibitory activity of novel 2-(N'-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines.
Synthesis of 3,6-bicyclolides: a novel class of macrolide antibiotics.
Dihydropyrazolopyrimidine inhibitors of K(V)1.5 (I(Kur)).
Synthesis and immunostimulatory properties of the phosphorothioate analogues of cdiGMP.
Synthesis of (3,4-dimethoxyphenoxy)alkylamino acetamides as orexin-2 receptor antagonists.
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Synthesis of oxazolidinone phospholipid analogue as a new inhibitor of phospholipase A2
QSAR study of benzoquinolinones as inhibitors of human type 1 5--reductase.
Bridged gamma-carbolines and derivatives possessing selective and combined affinity for 5-HT2 and D2 receptors.
Selective inhibition of mammalian lanosterol 14 alpha-demethylase: a possible strategy for cholesterol lowering.
Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.
3,4-Dihydroxychalcones as potent 5-lipoxygenase and cyclooxygenase inhibitors.
Contribution of the CmeABC efflux pump to macrolide and tetracycline resistance in Campylobacter jejuni.
In vivo efficacy of a novel oxazolidinone compound in two mouse models of infection.
Haemophilus ducreyi is resistant to human antimicrobial peptides.
Chemotherapy of leishmaniasis part-VIII: synthesis and bioevaluation of novel chalcones.
In vivo studies of 5-arylethenylbenzofuroxans in acute murine models of Chagas' disease.
Synthesis and aldose reductase inhibitory activity of some new chromonyl-2,4-thiazolidinediones.
Design and synthesis of bisubstrate inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: overview and perspectives.
Synthesis and antimicrobial activities of a new series of 4-S-[4(1)-amino-5(1)-oxo-6(1)-substituted benzyl-4(1),5(1)-dihydro-1(1),2(1),4(1)-triazin-3-yl]mercaptoacetyl-3-arylsydnones.
The pharmacophore of a peptoid VEGF receptor 2 antagonist includes both side chain and main chain residues.
Small, non-peptide C5a receptor antagonists: part 2.
Nakijiquinones E and F, new dimeric sesquiterpenoid quinones from marine sponge.
Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-inflammatory agents.
Novel non-carboxylic acid retinoids: 1,2,4-oxadiazol-5-one derivatives.
Ultrasound promoted synthesis of 2-imidazolines in water: a greener approach toward monoamine oxidase inhibitors.
Synthesis, antimalarial activity, structure-activity relationship analysis of thieno-[3,2-b]benzothiazine S,S-dioxide analogs.
Electronically stabilized versions of the antimalarial acetal trioxanes artemether and artesunate.
Synthesis and structure-activity relationship of histone deacetylase (HDAC) inhibitors with triazole-linked cap group.
Cytotoxic pregnane steroids from the formosan soft coral Stereonephthya crystalliana.
Caminosides B-D, antimicrobial glycolipids isolated from the marine sponge Caminus sphaeroconia.
Bioactive dibenzylbutyrolactone and dibenzylbutanediol lignans from Peperomia duclouxii.
Bioactive ent-clerodane diterpenoids from the aerial parts of Baccharis gaudichaudiana.
Sphaeric acid, a new succinic acid derivative from a Sphaeropsis sp.
Two new maytansinoids from maytenus buchananii
Cytotoxic xenia diterpenoids from the soft coral Xenia umbellata.
Isolation and structure assignment of an iminotetrasaccharide from a cultured filamentous cyanobacterium Anabaena sp.
Cytotoxic oxylipins from a marine sponge Topsentia sp.
7alpha,20-epoxy-ent-kauranoids from Isodon parvifolius.
Granulatamides A and B, cytotoxic tryptamine derivatives from the soft coral Eunicella granulata.
Sundaicumones A and B, polyprenylated acylphloroglucinol derivatives from Calophyllumsundaicum with weak activity against the glucocorticoid receptor.
Synthesis and antiproliferative activity in vitro of novel (2-butynyl)thioquinolines.
Total synthesis and evaluation of C25-benzyloxyepothilone C for tubulin assembly and cytotoxicity against MCF-7 breast cancer cells.
Recent advances on phosphodiesterase 4 inhibitors for the treatment of asthma and chronic obstructive pulmonary disease.
Isoxazoles with antipicornavirus activity.
Sleep-inducing N-alkyl-5-[m-(trifluoromethyl)phenyl]-5-hydroxy-2-pyrrolidinones and N-alkyl-3-(trifluoromethyl)cinnamamides.
Alpha-adrenoreceptor reagents. 3. Synthesis of some 2-substituted 1,4-benzodioxans as selective presynaptic alpha 2-adrenoreceptor antagonists.
Echinofuran, a New Furanosesquiterpene from the Gorgonian Echinogorgia praelonga
Antimutagenic agents from natural products.
New Diol Esters Isolated from Cultures of the Dinoflagellates Prorocentrum lima and Prorocentrum concavum
Cytotoxic activity of tetraprenylphenols related to suillin, an antitumor principle from Suillus granulatus.
A Novel Class of Non-Peptidic Endothelin Antagonists Isolated from the Medicinal Herb Phyllanthus niruri
Oxygenated Clerosterols Isolated from the Marine Alga Codium arabicum
Antimicrobial Agents from Tanacetum balsamita
The Racemization of Crinitol. Resolution of Crinitol and of 3-Nonen-2-ol Enantiomers by Recycle-HPLC, via MTPA Esters
New steroid acids from Antrodia cinnamomea, a fungal parasite of Cinnamomum micranthum.
Structural Revision of Physalin H Isolated from Physalis angulata
Bioactive Guanidine Alkaloids from Pterogyne nitens
Agastaquinone, a new cytotoxic diterpenoid quinone from Agastache rugosa.
Cacospongionolide B, a new sesterterpene from the sponge Fasciospongia cavernosa.
Curacins B and C, New Antimitotic Natural Products from the Marine Cyanobacterium Lyngbya majuscula
Polytolypin, a new antifungal triterpenoid from the coprophilous fungus Polytolypa hystricis.
New cytotoxic coumarins and prenylated benzophenone derivatives from the bark of Ochrocarpos punctatus from the Madagascar rainforest.
Cytotoxic germacranolides from Inula verbascifolia subsp. methanea.
Constituents of the twigs of Hernandia ovigera that inhibit the transformation of JB6 murine epidermal cells.
Aldehyde dehydrogenase inhibitors from the mushroom Clitocybe clavipes.
Araguspongines K and L, new bioactive bis-1-oxaquinolizidine N-oxide alkaloids from Red Sea specimens of Xestospongia exigua.
Five new steroidal saponins from Solanum chrysotrichum leaves and their antimycotic activity.
New cytotoxic xenia diterpenoids from the Formosan soft coral Xenia umbellata.
Studies on Cytotoxic Constituents in Pericarps of Mallotus japonicus, V. Three New Phloroglucinol Derivatives, Butyrylmallotochromanol, Isobutyrylmallotochromanol, and Mallotojaponol
Chemistry of Sponges, VIII. Anomoian A, a Bromotyrosine Derivative from Anomoiantbella popeae
Spermine alkaloids from Schweinfurthia papilionacea.
Lyngbyatoxins B and C, two new irritants from Lyngbya majuscula.
Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.
Perylene-conjugated pyrrole polyamide as a sequence-specific fluorescent probe.
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
Structure-based design, synthesis, evaluation, and crystallographic studies of conformationally constrained Smac mimetics as inhibitors of the X-linked inhibitor of apoptosis protein (XIAP).
Polyoxygenated methyl cyclohexanoids from a terrestrial ampelomyces fungus.
Cytotoxic triterpenoid alkaloids from Buxus microphylla.
2-Arylbenzofuran Derivatives from Morus cathayana.
Anti-coxsackie virus B3 norsesquiterpenoids from the roots of Phyllanthus emblica.
Design, synthesis and identification of novel colchicine-derived immunosuppressant.
Synthesis and structure-activity relationships of gamma-carboline derivatives as potent and selective cysLT(1) antagonists.
Synthesis and biological evaluation of amide derivatives of diflunisal as potential anti-tumor agents.
Discovery and functional evaluation of diverse novel human CB(1) receptor ligands.
5-N,N-Disubstituted 5-aminopyrazole-3-carboxylic acids are highly potent agonists of GPR109b.
Synthesis and evaluation of 3''- and 4''-deoxy and -fluoro analogs of the immunostimulatory glycolipid, KRN7000.
Synthesis of novel quinoxaline derivatives and its cytotoxic activities.
Scuteflorins A and B, dihydropyranocoumarins from Scutellaria lateriflora.
Constituents of the moss Polytrichum commune.
Synthesis of 10-substituted triazolyl artemisinins possessing anticancer activity via Huisgen 1,3-dipolar cylcoaddition.
Facile synthesis and biological evaluation of a cell-permeable probe to detect redox-regulated proteins.
Three new triterpenoids from Peganum nigellastrum.
Hyperforin analogues from St. John's wort (Hypericum perforatum).
Siamenol, a new carbazole alkaloid from Murraya siamensis.
Flavonol-cinnamate cycloadducts and diamide derivatives from Aglaia laxiflora.
Sulcatin, a novel antiproliferative N-methylpyridinium alkaloid from the ascidian Microcosmus vulgaris.
Discovery of novel sphingosine kinase 1 inhibitors.
Evaluation of triazolamers as active site inhibitors of HIV-1 protease.
Identification of a critical residue in the transmembrane domain 2 of tachykinin neurokinin 3 receptor affecting the dissociation kinetics and antagonism mode of osanetant (SR 142801) and piperidine-based structures.
Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control.
Synthesis and antimicrobial activity of 7-(2-substituted phenylthiazolidinyl)-benzopyran-2-one derivatives.
Mitoxantrone analogues as ligands for a stem-loop structure of tau pre-mRNA.
Design and synthesis of novel histone deacetylase inhibitor derived from nuclear localization signal peptide.
Azaindole hydroxamic acids are potent HIV-1 integrase inhibitors.
Isoquinoline-based analogs of the cancer drug clinical candidate tipifarnib as anti-Trypanosoma cruzi agents.
Microtubule-stabilizing activity of zampanolide, a potent macrolide isolated from the Tongan marine sponge Cacospongia mycofijiensis.
Binding ensemble profiling with photoaffinity labeling (BEProFL) approach: mapping the binding poses of HDAC8 inhibitors.
Transcriptional response of Candida parapsilosis following exposure to farnesol.
Antiproliferative oleanane saponins from Meryta denhamii.
Recent developments in fragment-based drug discovery.
Microsomal prostaglandin E2 synthase-1 (mPGES-1): a novel anti-inflammatory therapeutic target.
A cycloartane incorporating a fused tetrahydrofuran ring and a cytotoxic lactam from Monocarpia marginalis.
High throughput solubility determination with application to selection of compounds for fragment screening.
Pyronane monoterpenoids from the fruit of Gardenia jasminoides.
Cytotoxic dihydroagarofuranoid sesquiterpenes from the seeds of Celastrus orbiculatus.
Novel open-chain cytochalsins from the marine-derived fungus Spicaria elegans.
Synthesis of 3',4'-epoxynoraristeromycin analogs for molecular labeling probe of S-adenosyl-l-homocysteine hydrolase.
Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.
Effect of some P-glycoprotein modulators on Rhodamine-123 absorption in guinea-pig ileum.
Synthesis and anti-hepatitis B virus evaluation of novel ethyl 6-hydroxyquinoline-3-carboxylates in vitro.
A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.
Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Discovery of potent and cell-active allosteric dual Akt 1 and 2 inhibitors.
Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Mixed tetraoxanes containing the acetone subunit as antimalarials.
A tissue-selective nonsteroidal progesterone receptor modulator: 7,9-difluoro-5-(3-methylcyclohex-2-enyl)-2,2,4-trimethyl-1,2-dihydrochromeno[3,4-f]quinoline.
Isolation of Eupalmerin, a Minor Cembranoid Diterpene from the Caribbean Gorgonian Eunicea mammosa
Tetracyclic Triterpenoids of the Fruit Coats of Azadirachta indica
Euglobal T1, a New Euglobal from Eucalyptus tereticornis
Modified Taxols, 6. Preparation of Water-Soluble Prodrugs of Taxol
Antimicrobial diterpenes of Croton sonderianus, 1. Hardwickic and 3,4-secotrachylobanoic acids.
(-)-Grandisin form Cryptocarya crassinervia.
Structure of Irniine, a Pyrrolidine Alkaloid from Arisarum vulgare
Additional cytotoxic polyacetylenes from the marine sponge Petrosia species.
Cytotoxic constituents from leaves of Aglaia elliptifolia.
Synthesis of indoleamine 2,3-dioxygenase inhibitory analogues of the sponge alkaloid exiguamine A.
Molecular characteristics for solid-state limited solubility.
Synthesis and activity of tetrapeptidic HTLV-I protease inhibitors possessing different P3-cap moieties.
Synthesis and anti-platelet evaluation of 2-benzoylaminobenzoate analogs.
Synthesis and cytotoxicity of a salicylihalamide A analogue.
Novel potent and selective thrombin inhibitors based on a central 1,4-benzoxazin-3(4H)-one scaffold.
Corymbones A and B, phloroglucinols with thyrotropin releasing hormone receptor 2 binding affinity from the flowers of Corymbia peltata.
Non-peptide gonadotropin-releasing hormone receptor antagonists.
From the selective serotonin transporter inhibitor citalopram to the selective norepinephrine transporter inhibitor talopram: synthesis and structure-activity relationship studies.
Synthesis and DNA cleaving activity of water-soluble non-conjugated thienyl tetraynes.
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Aminopyrazine CB1 receptor inverse agonists.
Preparation of piperazine derivatives as 5-HT7 receptor antagonists.
Novel substituted aminoalkylguanidines as potential antihyperglycemic and food intake-reducing agents.
Identification of non-lipid LPA3 antagonists by virtual screening.
Efficacious 11beta-hydroxysteroid dehydrogenase type I inhibitors in the diet-induced obesity mouse model.
Terretonins E and F, inhibitors of the mitochondrial respiratory chain from the marine-derived fungus Aspergillus insuetus (#).
Oral Therapy with Amlodipine and Lacidipine, 1,4-Dihydropyridine Derivatives Showing Activity against Experimental Visceral Leishmaniasis.
In vitro-selected linezolid-resistant Mycobacterium tuberculosis mutants.
Evaluation of substrate and inhibitor properties of a novel MDR modulator H17 towards transmembrane efflux pumps.
Synthesis of 2-(4-substitutedmethylpiperazin-1-yl)-N-(3,4-dihydro-3-oxo-2H-benzo[b][1,4]oxazin-7-yl)acetamides and their positive inotropic evaluation.
Mannosylated saponins based on oleanolic and glycyrrhizic acids. Towards synthetic colloidal antigen delivery systems.
Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death.
Amphotericin B-induced ion flux is markedly attenuated in phosphatidylglycerol membrane as evidenced by a newly devised fluorometric method.
Antioxidant efficacy of iridoid and phenylethanoid glycosides from the medicinal plant Teucrium chamaedris in cell-free systems.
Substituted 2-arylbenzothiazoles as kinase inhibitors: hit-to-lead optimization.
Synthesis and activity of azaterphenyl diamidines against Trypanosoma brucei rhodesiense and Plasmodium falciparum.
Discovery of a series of acrylic acids and their derivatives as chemical leads for selective EP3 receptor antagonists.
Synthesis and glycogen phosphorylase inhibitory activity of N-(beta-D-glucopyranosyl)amides possessing 1,4-benzodioxane moiety.
Synthesis and dopaminergic activity of some E-3-(piperidin-1-yl)-1-(4-substituted phenyl)prop-2-en-1-one derivatives.
Synthesis and biological evaluation of N-aryl-1,4-dihydropyridines as novel antidyslipidemic and antioxidant agents.
Janus kinase 2 inhibitors. Synthesis and characterization of a novel polycyclic azaindole.
Nonacidic inhibitors of human microsomal prostaglandin synthase 1 (mPGES 1) identified by a multistep virtual screening protocol.
Novel oxadiazole analogues derived from ethacrynic acid: design, synthesis, and structure-activity relationships in inhibiting the activity of glutathione S-transferase P1-1 and cancer cell proliferation.
Neglected tropical diseases: multi-target-directed ligands in the search for novel lead candidates against Trypanosoma and Leishmania.
Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists.
Alternaramide, a cyclic depsipeptide from the marine-derived fungus Alternaria sp. SF-5016.
Synthesis and antibacterial activity of novel 3-O-carbamoyl derivatives of clarithromycin and 11,12-cyclic carbonate azithromycin.
Asymmetric synthesis of anticancer beta-lactams via Staudinger reaction: utilization of chiral ketene from carbohydrate.
5-Substituted [1]pyrindine derivatives with antiproliferative activity.
Stolonoxides E and F, cytotoxic metabolites from the marine ascidian Stolonica socialis.
Nakijiquinones J--R, sesquiterpenoid quinones with an amine residue from okinawan marine sponges.
Bafilomycins produced in culture by Streptomyces spp. isolated from marine habitats are potent inhibitors of autophagy.
An expeditious synthesis and anticancer activity of novel 4-(3'-indolyl)oxazoles.
Heat shock protein 90: inhibitors in clinical trials.
Cytotoxic neoclerodane diterpenoids from Scutellaria barbata.
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.
New benzophenone-derived bisphosphonium salts as leishmanicidal leads targeting mitochondria through inhibition of respiratory complex II.
Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.
Synthesis and biological evaluation of botulinum neurotoxin a protease inhibitors.
N-methyl phenylalanine-rich peptides as highly versatile blood-brain barrier shuttles.
Synthesis, radiofluorination, and hypoxia-selective studies of FRAZ: A configurational and positional analogue of the clinical hypoxia marker, [18F]-FAZA.
Exploration of inhibitors for diaminopimelate aminotransferase.
Gentisides A and B, two new neuritogenic compounds from the traditional Chinese medicine Gentiana rigescens Franch.
Acyclic nucleoside phosphonates with 5-azacytosine base moiety substituted in C-6 position.
Synthesis of glycyrrhetinic acid derivatives for the treatment of metabolic diseases.
Isoxazole analogues bind the system xc- transporter: structure-activity relationship and pharmacophore model.
Microwave assisted synthesis and antimicrobial activity of 2-quinoxalinone-3-hydrazone derivatives.
Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer.
Development of carbohydrate-derived inhibitors of acid sphingomyelinase.
Novel small molecule bradykinin B1 receptor antagonists. Part 1: benzamides and semicarbazides.
Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: novel selective inhibitors of transforming growth factor-beta kinase.
New PPARgamma ligands based on 2-hydroxy-1,4-naphthoquinone: computer-aided design, synthesis, and receptor-binding studies.
Carbon-11 labeled indolylpropylamine analog as a new potential PET agent for imaging of the serotonin transporter.
Synthesis of Hsp90 inhibitor dimers as potential antitumor agents.
Identification of MMP-12 inhibitors by using biosensor-based screening of a fragment library.
Synthesis and activity of conformationally-constrained macrocyclic norstatine-based inhibitors of HIV protease
Semisynthetic modification of hygromycin A. 1. Synthesis and antibacterial activity of vinyl methyl and amide analogs.
Inhibition of antennal esterases of the egyptian armyworm Spodoptera littoralis by trifluoromethyl ketones
N-(2-pyrrolidinylmethyl)benzoxazine-8-carboxamides exhibiting high affinities for All of D2, 5-HT1 A, and 5-HT2 receptors
Benzimidazole ribonucleosides: Observation of an unexpected nitration when performing non-aqueous diazotizations with t-butyl nitrite
Synthesis and evaluation of dual domain macrocyclic FKBP12 ligands.
Tryptophan-norleucine 1,5-disubstituted tetrazoles as cis peptide bond mimics: Investigation of the bioactive conformation of a potent and selective peptide for the cholecystokinin-B receptor
Synthesis and pharmacology of 2-alkyl raloxifene analogs
Synthesis and creatine kinase inhibitory activity of non-hydrolyzable analogs of phosphocreatine
Synthesis and ion-binding properties of an immobilized bis-cysteine peptide
A new class of diacidic nonpeptide angiotensin II receptor antagonists
Dihydropyridines: a new class of angiotensin II antagonists
Conversion of acyclic nonpeptide CCK antagonists into CCK agonists
Synthesis and antiangiogenic activity of new carbohydrate derivatives
Synthetic studies on the furan ring of wortmannin
Kinetic characterization of a peptide inhibitor of trypsin isolated from a synthetic peptide combinatorial library
Novel catalytic activity of immobilized spores under reduced water activity
Synthesis, bioactivity, and DNA-cleaving ability of desferrioxamine B-nalidixic acid and anthraquinone carboxylic acid conjugates
Synthesis of 2-O-heteroaroyl taxanes: evaluation of microtubule assembly promotion and cytotoxicity
-hydroxyamide derived aminodiols as potent inhibitors of hiv protease
A highly potent series of fluoroalkyl benzoxazine pyridine-N-oxide potassium channel openers
The -iodoethoxyl group: a stable unit for radioiodination
Synthesis and 5-HT3 receptor antagonist potency of novel (endo) 3,9-diazabicyclo[3.3.1]nonan-7-amino derivatives
Synthesis of new 3-thiosubstituted carbacephem antibiotics and their activity against penicillin resistant Streptococcus pneumoniae
Synthesis of 2-O-substituted -D-Gal-(14)--D-GlcNAc-1-0-Bn as specific acceptors for -L-(13) fucosyltransferases
Identification of simpler analogs of neurotensin(913) which retain antinociceptive activity
DNA topoisomerase II inhibition by substituted 1,2,3,4-tetrahydro--carboline derivatives
Studies on the active conformation of NK1 antagonist CGP 49823. Part 1. Synthesis of conformationally restricted analogs.
The identification of a novel renin inhibitor of equivalent efficacy following oral or intravenous administration.
Sch 53823 and Sch 53825, novel fungal metabolites with phospholipase D inhibitory activity
The conserved acid binding domain model of inhibitors of protein phosphatases 1 and 2A: Molecular modelling aspects.
The synthesis and cognition enhancing effects of a series of dibenzoyl guanidines. Analogs of N,N-[[4-(aminocarbonyl)phenyl]carbonimidoyl]bis[benzamide]
Schotten-Baumann acylation of N-debenzoyltaxol; an efficient route to N-acyl taxol analogues and their biological evaluation
Synthesis and biological activity of new optically active 2-oxaisocephems: 3-(N-alkylpyridinium-4-thio)methyl derivatives
Peptoid mimics of a C2-symmetric inhibitor of the HIV-1 protease.
Development of angiotensin II antagonists with equipotent affinity for human AT1 and AT2 receptor subtypes.
Synthesis and in vitro antiandrogenic activity of 17-hydroxy-17-(-hydroxy/haloalkyn-1-yl)-4-methyl-4-aza-3-oxo-5-androstan-(1-ene)-3-ones
2-(3-hydroxypropoxy)-1,25-dihydroxyvitamin D3 (ED-71), preventive and therapeutic effects on bone mineral loss in ovariectomized rats
Photoreactive CMP-sialic acids as substrates for 2,6-sialyltransferase
Synthesis of the 4,5 diphosphonate analog of D,L-myo-inositol 4,5-diphosphate
4-oxygenated retinoids: unexpected chemopreventive potential for analogues originally synthesized as affinity labels
Structure-based design of achiral anthranilamides as P2/P2 surrogates for symmetry-based HIV protease inhibitors: design, synthesis, X-ray structure, enzyme inhibition and antiviral activity
Rapid synthesis and properties of ()-6-Deoxy-6-fluoro-myo-inositol-1,4,5-tris(phosphate) an analogue of myo-inositol-1,4,5-tris(phosphate)
Dihydro-imidazolone derivatives as angiotensin II receptor antagonists: chiral effect on the activity
Cyanoguanidine bioisosteres in potassium channel openers: Evaluation of 3,4-disubstituted-1,2,5-thiadiazole-1-oxides
N-acyl-3-alkylidenyl- and 3-alkyl azeitidin-2-ones: a new class of monocyclic -lactam antibacterial agents 2. Synthesis and structure-activity relationships of heteroatom substituted 3-isopropylidene and 3-isopropyl analogs
Increase of the anti-HIV activity of D4T in human T-cell culture by the use of the sate pronucleotide approach
Chemistry and pharmacokinetics of diarylthiophenes and terphenyls as selective COX-2 inhibitors
Topliss approach to the synthesis of biologically active substituted N-benzoyl taxol analogues
A practical and scalable synthesis of SR 142801, a tachykinin NK3 antagonist
Inhibitory effect on HT-1080 tumor cell invasion in vitro using 9-(2-hydroxyethyl)adenine 2-phosphates
Balanced angiotensin II receptor antagonists. I. The effects of biphenyl ortho-substitution on AT1/AT2 affinities
Synthesis and biological activity of C-5 modified derivatives of (+)-AJ76 and (+)-UH232: Increased dopamine D3 receptor preference and improved pharmacokinetic properties
Imidazol-1-ylalkanoate esters and their corresponding acids. A novel series of extrinsic 1H NMR probes for intracellular pH
Epoxidation of 6,7- and 10,11-oxidosqualenes by the squalene epoxidase present in rat liver microsomes
Synthesis of -difluoro and -difluoro--trifluoroketo-derivatives as potential inhibitors for Cholesterol Ester Hydrolase
Design, synthesis and molecular modeling of 3-acylamino-2- Carboxyindole NMDA receptor glycine-site antagonists
Pharmacological evaluation of combined PGI2 agonists/thromboxane synthase inhibitors. I
Structural analogues of LY292728, a highly potent xanthone dicarboxylic acid leukotriene B4 receptor antagonist: spatial positioning of the secondary acid group
S-nitrosation of proteins by N-methyl-N-nitrosoanilines
New hydroxy-amido-anthraquinones as potential antineoplastic drugs.
Cycloalkylpiperazines as HIV-1 protease inhibitors: enhanced oral absorption
The synthesis and biological activity of some known and putative metabolites of the atypical antipsychotic agent olanzapine (LY170053)
The selective inhibition of phosphodiesterase IV by benzopyran derivatives of rolipram
A new class of angiotensin II receptor antagonists with a novel acidic bioisostere
A Hammett correlation for CC-1065 and duocarmycin analogs: Magnitude of substituent electronic effects on functional reactivity
Synthesis and HIV-1 reverse transcriptase inhibition properties of two new methylenephosphonate analogues of 3-azido-3-deoxythymidine-5-triphosphate
Synthesis and structure-activity relationships of novel THF 1-methylcarbapenems II
The structural feature of S1 subsite of carboxypeptidase A
Balanced angiotensin II receptor antagonists. III. The effects of substitution at the imidazole 5-position.
Mechanism-based inactivation of E. coli -glutamylcysteine synthetase by phosphinic acid- and sulfoximine-based transition-state analogues
Analogs of UK 14,304: Structural features responsible for 2 adrenoceptor activity
2-NAP: a selective, hydrophilic, non-peptide CCKA - receptor antagonist derived from the cholecystokinin C-terminal dipeptide.
Preparation and antifungal activity of fusacandin analogs: C-6 sidechain esters
Synthesis of 1-(2-Deoxy-2-C-fluoromethyl--D-arabinofuranosyl)cytosine as a potential antineoplastic agent
Two novel, potent and selective histamine H3 receptor agonists
Isolation and X-ray crystal structure of racemic Xestospongin D from the Singapore marine sponge Niphates sp1
Bifunctional antitumor agents: a DNA interactive enediyne from the pyrrolo[9,10-b]phenanthrene template
Synthesis and pharmacological activity of SC-53228, a leukotriene B4 receptor antagonist with high intrinsic potency and selectivity
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 6. 4-substituted 3-pyridinylalkanoic acids.
Acetylcholinesterase inhibition by fused dihydroquinazoline compounds
Syntheses and antifilarial profile of 5-amino and 5,8-diamino-isoquinoline derivatives: A new class of antifilarial agents
Inhibitors of the adenovirus type 2 proteinase based on substrate-like tetrapeptide nitriles
Acyclic NK-1 antagonists: 2-benzhydryl-2-aminoethyl ethers
Synthesis and pharmacological characterization of l-trans-4-tetrazolylproline (ly300020): A novel systemically-active ampa receptor agonist
Synthesis of echiguanine analogs and their ribofuranosyl glycosides that inhibit phosphatidylinositol 4-kinase
Anti HIV-1 activity of a hydrophilic cyclosporin derivative with improved binding affinity to cyclophilin A
A novel non nucleoside compound with high in vitro anti-HIV-1 activity. Absolute stereochemistry determination
Aromatic P1 replacements for the highly potent HIV-1 protease inhibitor CRIXIVAN
Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.
Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents.
1-(2-((Z)-6-(2-(Trifluoromethyl)phenyl)hexa-3-en-1,5-diynyl)phenyl)piperidin-2-one as a new potent apoptosis agent.
Synthesis and biological evaluation of novel 2-(substituted phenylaminocarbonylmethylthio)-6-(2,6-dichlorobenzyl)-pyrimidin-4(3H)-ones as potent HIV-1 NNRTIs.
Synthesis and in vitro evaluation of aspartate transcarbamoylase inhibitors.
Natural and synthetic 2'-hydroxy-chalcones and aurones: synthesis, characterization and evaluation of the antioxidant and soybean lipoxygenase inhibitory activity.
A novel targeted delivery system utilizing a cephalosporin-oncolytic prodrug activated by an antibody -lactamase conjugate for the treatment of cancer
Imidazo[1,2-a]piperazines as mechanistic inhibitors of serine proteinases
Synthesis, siderophore, and antimicrobial evaluation of a spermidine-based tricatecholate siderophore and carbacephalosporin conjugate
A new potent inhibitor for angiotensin converting enzyme: (R,S)-captopril-F3
A new class of leukotriene biosynthesis inhibitors: The development of ((4-(4-chlorophenyl)-1-(4-(2-quinolinylmethoxy)phenyl)butyl)thio)acetic acid, L-674,636
5-HT2 antagonist activity of 3-aminomethyltetralones
Enzymic and nonenzymic lipid peroxidation: inhibition by substituted phenoxazines
Enantioselective total synthesis and pharmacologic profile of 12-deoxy-12(S)-methyl leukotriene B4
C8-substituted derivatives of 2-(dipropylamino)tetralin: Palladium-catalyzed synthesis and interactions with 5-HT1A-receptors
The function of S1 subsite pocket of carboxypeptidase A
Synthesis and evaluation of several cathechol bioisosteres as potential dopamine receptor ligands
High selectivity of novel isoguanosine analogues for the adenosine A1 receptor
Structural features of substituted purine derivatives compatible with depletion of human O6-alkylguanine-DNA alkyltransferase.
Synthesis of the -phosphonic acid analogue of kainic acid
Modeling of competitive phosphono amino acid NMDA receptor antagonists.
Synthesis and anti-HIV activity of 4'-thio-2',3'-dideoxynucleosides.
A new class of high affinity ligands for the neurokinin A NK2 receptor: psi (CH2NR) reduced peptide bond analogues of neurokinin A4-10.
Synthesis and antileukemic activity of etoposide a-ring analogs
Muscarinic agonist SAR of azaspirodioxolanes
The discovery of a new structural class of potent orally active leukotriene D4 antagonists
3-oxagranatane (3-oxa-9-azabicyclo[3.3.1]nonane) derivatives as highly potent serotonin 5-Ht3 receptor antagonists.
alpha-Methylated analogues of triiodothyroalkanoic acids: synthesis and biological activity.
Specific inhibition of HIV-1 protease by boronated porphyrins.
4-[2-[Methyl(2-phenethyl)amino]-2-oxoethyl]-8-(phenylmethoxy)-2- naphthalenecarboxylic acid: a high affinity, competitive, orally active leukotriene B4 receptor antagonist.
Design, synthesis and biological evaluation of estradiol-chlorambucil hybrids as anticancer agents.
Biochemical analysis of cellular target of S-trityl-L-cysteine derivatives using affinity matrix.
Structure-activity relationships of bacterial outer-membrane permeabilizers based on polymyxin B heptapeptides.
Acidic elements in histamine H(3) receptor antagonists.
Bioactive bromophycolides R-U from the Fijian red alga Callophycus serratus.
Inhibitory activity and selectivity of staurosporine derivatives towards protein kinase C
An efficient method for the synthesis of guanidino prodrugs
2-(1-Cyclopenten-1-yl)-2-[2-(dimethylamino)ethyl]-5-(E)-benzylidene cyclopentanone hydrochlorides: a new series of moderate cytotoxic agents
Indolocarbazole nitrogens linked by three-atom bridges: a potent new class of PKC inhibitors
Selective inhibitors of monoamine oxidase. 2. Arylamide SAR.
Synthesis and antiestrogenic activity of diaryl thioether derivatives.
Furoxans as nitric oxide donors. 4-Phenyl-3-furoxancarbonitrile: thiol-mediated nitric oxide release and biological evaluation.
Cyclopentanespiro-3H-dihydro-pyrimidinones as Angiotensin II AT1 receptor antagonists
Discovery and development of aryl-fused imidazole-based angiotensin II antagonists
Substituted lactam biphenyltetrazoles as angiotensin II mediated antihypertensives
Benzopyran potassium channel activators related to cromakalim - heterocyclic amide replacements at position 4.
Cucurbitacin F derivatives, anti-HIV principles from cowania mexicana
D-amino acids as novel P2/P3 ligands for inhibitors of HIV-1 protease
Synthesis of sulphur heterocycles as hepatoprotectants : part I
The phosphonate analog of 5-methylthioribose 1--phosphate
Design and synthesis of squalene synthase inhibitors - acylic mimics of the zaragazic acids
Design, synthesis and biological properties of structurally non-related endotoxin inhibitors
Mercaptoacyl dipeptides as dual inhibitors of angiotensin-converting enzyme and neutral endopeptidase. Preliminary structure-activity studies
Morpholine-based substance P antagonists: assessment of the 3-point binding model
GR159897 and related analogues as highly potent, orally active non-peptide neurokinin NK2 receptor antagonists.
Tetrahydroisoquinoline as a phenylalanine replacement in renin inhibitors
Investigation of the effects of synthetic, non-cytotoxic immunophilin inhibitors on MDR
Examination of peptidic ,-diamino-,-difluoroketones as inhibitors of human leukocyte elastase
Balanced angiotensin II receptor antagonists. II.1,2 4-aminomethyl- and acylaminomethylimidazoles
Novel ether derivatives of alkyl piperidines as potential sigma / 5HT2 antipsychotic agents
Differential binding and dopamine uptake activity of cocaine analogues modified at nitrogen
Substrate specificity of immobilized penicillin-G acylase towards penicillin and cephalosporin derivatives was studied. The phenylacetyl moiety can be altered at the -position with several small substituents. Depending on polarity and size of the substituent, enzyme activity decreases or increases. Insertion or deletion of atoms between the aromatic nucleus of the phenylacetyl group and the center of hydrolysis leads to substrates that are no longer recognized by the enzyme.
Synthesis and antiviral activity of a novel class of HIV-1 protease inhibitors containing a heterocyclic P1-P2 amide bond isostere
Synthesis of a galactose-fucose disaccharide mimic of sialyl Lewis X
The synthesis and biological activity of tetrahydroquinoline angiotensin II antagonists containing a substituted biphenyltetrazole group
Gem-disubstituted amino-ether based substance p antagonists
Cysteine and methionine linked by carbon pseudopeptides inhibit farnesyl transferase
Synthesis and antiviral activity of amino acid esters of ribavirin
Antifungal lipopeptides: Structure-activity relationships of 3-hydroxyglutamine-modified pneumocandin B0 derivatives
Radioprotective effects of -galactosylceramides
Synthesis of novel iodinated radioligands with high affinity and selectivity for CCK-B/gastrin receptors
Discovery of L-740,515, a potent thienopyridine cysLT1 receptor (LTD4 receptor) antagonist
Balanced AT1 and AT2 angiotensin II antagonists. II. Potent 5 -hydroxyacid imidazolyl biphenyl sulfonylureas
6,3'-Dinitroflavone, a novel high affinity ligand for the benzodiazepine receptor with potent anxiolytic properties
Synthesis of dibenzo[a,d]cycloheptanes as cytokine biosynthesis inhibitors
Synthesis and activity of cereulide, a cyclic dodecadepsipeptide ionophore as emetic toxin from Bacillus cereus
Synthesis and evaluation of water soluble indole pyrrolothiazole paf antagonists
Synthesis and evaluation of novel daunomycin-phosphate-sulfate --glucuronide and --glucoside prodrugs for application in adept
Amino acid-derived piperidides as novel CCKB ligands with anxiolytic-like properties
A novel series of arylpiperazines with high affinity and selectivity for the dopamine D3 receptor
Partial structures of the fungal toxin aflatrem, methyl-substituted 6,8-dioxabicyclo[3.2.1]octan-2-ones have anticonvulsant activity
Inhibitors of Acyl-CoA:Cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents 14. synthesis and structure-activity relationships of a novel series of sulfonamide tetrazoles
Structure activity relationships of non-peptide bradykinin B2 receptor antagonists
The synthesis, and dopamine D2 and serotonin 5-HT3 receptor affinity of 3-aza analogues (pyridyl) of 4-amino-5-chloro-2-methoxybenzamides
Cyclic sulfone-3-carboxamides as novel P2-ligands for Ro 31-8959 based HIV-1 protease inhibitors
Synthesis and bioactivities of heterocyclic lipids as PAF antagonists. 1
Potent dual antagonists of endothelin and angiotensin II receptors derived from -phenoxyphenylacetic acids (Part III)
Synthesis and binding properties of myo-inositol 4,5,6-tris(phosphate) an analogue of myo-inositol 1,4,5-tris(phosphate). Correlation with the ionization state of the molecules
Thiourea analogues of resiniferatoxin as ligands for the vanilloid receptor
2,3-Dihydro-1-benzofuran-5-ols as analogues of alpha-tocopherol that inhibit in vitro and ex vivo lipid autoxidation and protect mice against central nervous system trauma.
Synthesis of alpha-methylene-gamma-butyrolactones: a structure-activity relationship study of their allergenic power.
Synthesis of 8-methoxy-15,16-dinor-6,8,10-trichothecatriene 12,13 alpha-epoxide and 12,13 beta-epoxide as potential antineoplastic agents.
Antitumor structure-activity relations. Nitrosoureas vs. L-1210 leukemia.
Synthesis and anxiolytic activity of a series of pyrazino[1,2-a][1,4]benzodiazepine derivatives.
A novel opioid receptor site directed alkylating agent with irreversible narcotic antagonistic and reversible agonistic activities.
Bradykinin analogues containing N alpha-methyl amino acids.
Synthesis and Pharmacology of Mangostin-3,6-di-O-glucoside
Constituents of Pachygone ovata and Pharmacological Action of its Major Leaf Alkaloid
Isolation in High Yield of Citrinin From Penicillium odoratum and of Mycophenolic Acid From Penicillium brunneo-stoloniferum
Centaurepensin: A Cytotoxic Constituent of Centaurea solstitialis and C. repens (Asteraceae)
Constituents of Helenium amarum. II. Isolation and Characterization of Heleniamarin and Other Constituents
Coumarins and Cinnamic Acid From Gymnophyton Isatidicarpum
Pyrrolizidine Alkaloids From Middle Eastern Plants
Cochinolide, a new gamma-alkylidene bicyclic butenolide with antiviral activity, and its beta-glucopyranoside from Homalium cochinchinensis.
Agelasines H and I, 9-methyladenine-containing diterpenoids from an Agelas sponge.
Mediation of the cytotoxicity of lanostanoids and steroids of Ganoderma tsugae through apoptosis and cell cycle.
Jimenezin, a Novel Annonaceous Acetogenin from the Seeds of Rollinia mucosa Containing Adjacent TetrahydrofuranTetrahydropyran Ring Systems ,1
New Diterpene Lactones from the Sponge Spongia matamata
Detecting potential teratogenic alkaloids from blue cohosh rhizomes using an in vitro rat embryo culture.
Three new taxane diterpenoids from Taxus sumatrana.
Antiinsectan decaturin and oxalicine analogues from Penicillium thiersii.
Hemiterpene glucosides with anti-platelet aggregation activities from Ilex pubescens.
Bisindigotin, a TCDD antagonist from the Chinese medicinal herb Isatis indigotica.
A cytotoxic carotenoid from the marine sponge Prianos osiros.
Cytotoxic xanthones from Cudrania tricuspidata.
Microbial transformation of 20(S)-protopanaxatriol by Mucor spinosus.
Globosumones A-C, cytotoxic orsellinic acid esters from the Sonoran desert endophytic fungus Chaetomium globosum.
Penem inhibitors of bacterial signal peptidase
Semisynthesis and biological evaluation of brevifoliol 13-[N-benzoyl-(-2R,3S)-3-phenylisoserinate]
C-3-N-acyl analogs of 9(R)-dihydrotaxol: synthesis and structure activity relationships
CP-71,362, an unusually potent inhibitor of rat and dog renin
Adenosine dialdehyde analogs I: Regioselective synthesis of adenosine monoaldehydes
-Phenoxyphenylacetic acid derived angiotensin II antagonists with low nanomolar AT1/AT2 receptor subtype affinity (Part II)
Dopamine autoreceptor agonists: computational studies, synthesis and biological investigations
A novel condensed tropone-isoquinoline alkaloid, pareitropone, from Cissampelos pareira
Novel angiotensin converting enzyme inhibitors containing -hydroxy ketomethylene dipeptide isosteres
Diaryl phosphate derivatives act as pro-drugs of AZT with reduced cytotoxicity compared to the parent nucleoside
Synthesis and activity of spiroisoindolines as novel noncompetitive NMDA antagonists
Anti-histaminic activity of bromopyrrole alkaloids isolated from Caribbean Agelas sponges
Enantiomeric Composition of Trans-Dihydrodiols Formed from Meso-K-Region Arene Oxides by Microsomal Epoxide Hydrolase
Synthesis and sar of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity
Synthesis and antiviral activity of 11-azapentacyclo[6.2.1.0.0.0]decane.
Plant antitumor agents. 23. Synthesis and antileukemic activity of camptothecin analogues.
Studies of the antitumor activity of (2-alkoxyalkyl)- and (2-alkoxyalkenyl)phosphocholines.
Analgesic actions of 3-substituted 6-tert-butyl-1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines.
Effect of methoxy substitution on the adrenergic activity of three structurally related alpha 2-adrenoreceptor antagonists.
4,5-Disubstituted primaquine analogues as potential antimalarial agents.
Inactivation of thymidylate synthase at an alternate high-affinity binding site.
Enantiomers of 1-ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid: preparation and biological activity.
Synthesis and gastrointestinal pharmacology of the 4-fluoro analogue of enisoprost.
Synthesis and antiinflammatory activities of 3-(3,5-di-tert-butyl-4-hydroxybenzylidene)pyrrolidin-2-ones.
Synthesis of N-(3,6-dihydro-1(2H)-pyridinyl)benzamides with hyperglycemic-hypoglycemic activity.
Structure-activity relationships of kadsurenone analogues.
Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists.
The role of solvent-accessible surface area in determining partition coefficients.
Three new phenolic compounds from a manipulated plant cell culture, Mirabilis jalapa.
Inhibition of glucose and dehydroascorbic acid uptakes by resveratrol in human transformed myelocytic cells.
Benz[f]isoquinoline analogues as high-affinity sigma ligands.
Nor-mefloquine: Stereospecific synthesis and biological properties
Cholecystokinin analogues: The ergopeptine alkaloids as models of the active conformation of CCK
An explanation of the substituent effect of 1,3,8-trisubstituted xanthines on adenosine A1/A2 affinity.
Synthesis and biological properties of 1069C: a new synthetic antitumour agent with very low cross-resistance potential
Structure-activity relationships of the pyridazinone series of 5-lipoxygenase inhibitors
(E)-1-alkyl-[2-(1H-azol-2-yl)vinyl]pyridinium salts: theoretical analysis, synthesis and evaluation of their interaction with choline acetyltransferase.
Synthesis of chiral phosphorus mustards derived from serine
2-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity.
Synthesis of metabolically stable arylpiperazine 5-HT1A receptor agonists
Synthesis of 1-(2-Indolyl)pyridinium salts: a prodrug approach to acetylcholinesterase inhibition
(5S)-3-aryl-5-(1-piperidinylmethyl)-2-oxazolidinones, a new class of potential neuroleptics with a high affinity for sigma receptors
A novel approach to the site specific delivery of potential HMG-CoA reductase inhibitors
Synthesis and activity in cognition-related tests of novel 2-benzoylamino-4-oxoquinazolines
MDL 74147, a novel selective and soluble inhibitor of human renin. Synthesis, structure-activity relationship, species and protease selectivities.
DuP 747: a new, potent, kappa opioid analgesic. Synthesis and pharmacology1.
A novel and selective class of azabicyclic muscarinic agonists incorporating an N-methoxy imidoyl halide or nitrile functionality
The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex) derivaties
Synthesis and anti-herpes activity of 5-trifluorovinyl-2-deoxyuridine
The use of synthetic phosphopeptides for epitope mapping of the s1-casein phosphopeptide segment 5979
Chemical synthesis of D-erythro-sphingosine-1-phosphate, and its inhibitory effect on cell motility
Multipurpose receptor ligands: -carboline cholecystokinin antagonists
Design and synthesis of novel 2',3'-dideoxy-4'-selenonucleosides as potential antiviral agents.
Synthetic medicinal chemistry of selected antimalarial natural products.
Design and synthesis of a beta-lactamase activated 5-fluorouracil prodrug.
Synthesis and promotion angiogenesis effect of chrysin derivatives coupled to NO donors.
5-Aryl-4-(5-substituted-2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone.
Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline.
Ceramides: branched alkyl chains in the sphingolipid siblings of diacylglycerol improve biological potency.
Synthesis and biological testing of thioalkane- and thioarene-spaced bis-beta-D-glucopyranosides.
Synthesis of novel substituted pyrazole-5-carbohydrazide hydrazone derivatives and discovery of a potent apoptosis inducer in A549 lung cancer cells.
Kinase domain mutations in cancer: implications for small molecule drug design strategies.
Design, synthesis, and structure-activity analysis of isoform-selective retinoic acid receptor beta ligands.
Naphthylisopropylamine and N-benzylamphetamine derivatives as monoamine oxidase inhibitors.
Structure-activity relationships of orotidine-5'-monophosphate decarboxylase inhibitors as anticancer agents.
Rigid analogs of camptothecin as DNA topoisomerase I inhibitors.
Metabotropic glutamate receptors: novel targets for drug development.
1-(Fluorobenzyl)-4-amino-1H-1,2,3-triazolo[4,5-c]pyridines: synthesis and anticonvulsant activity.
Three new cytochalasins produced by an endophytic fungus in the genus Rhinocladiella.
Locking the two ends of tetrapeptidic HTLV-I protease inhibitors inside the enzyme.
Spheciosterol sulfates, PKCzeta inhibitors from a philippine sponge Spheciospongia sp.
Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor.
Complexation of the anti-Trypanosoma cruzi drug benznidazole improves solubility and efficacy.
Effect of novel N-cyano-tetrahydro-pyridazine compounds, a class of cathepsin K inhibitors, on the bone resorptive activity of mature osteoclasts.
Novel aminopeptidase N inhibitors derived from 1,3,4-thiadiazole scaffold.
Is quantum mechanics necessary for predicting binding free energy?
T-type Ca2+ channel blockers suppress the growth of human cancer cells.
Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.
Progesterone receptor antagonists with a 3-phenylquinazoline-2,4-dione/2-phenylisoquinoline-1,3-dione skeleton.
Kadcoccilactones A-J, triterpenoids from Kadsura coccinea.
Identification of novel inhibitors of methionyl-tRNA synthetase (MetRS) by virtual screening.
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists.
Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids.
Synthesis and biological evaluation of combretastatin analogs as cell cycle inhibitors of the G1 to S transition in Saccharomyces cerevisiae.
Oblongifolins A-D, polyprenylated benzoylphloroglucinol derivatives from Garcinia oblongifolia.
Nitrogen-containing phorbol esters from Croton ciliatoglandulifer and their effects on cyclooxygenases-1 and -2.
Chromone derivatives from the filamentous fungus Lachnum sp. BCC 2424.
Vismiaphenones D-G, new prenylated benzophenones from Vismia cayennensis.
A new epidioxy sterol as an antifouling substance from a palauan marine sponge, lendenfeldia chondrodes
Cytotoxic isoprenylated flavans of Broussonetia kazinoki.
New alkaloids from the indopacific sponge Stylissa carteri.
New cytotoxic oxygenated fucosterols from the brown alga Turbinaria conoides.
Manaarenolides A-I, diterpenoids from the soft coral Sinularia manaarensis.
Photoactivated insecticidal thiophene derivatives from Xanthopappus subacaulis.
Oculatol, oculatolide, and A-nor sterols from the sponge Haliclona oculata.
Cytotoxic constituents from the formosan soft coral Clavularia inflata var. luzoniana.
Discovery, synthesis, and insecticidal activity of cycloaspeptide E.
Paratunamides A-D, oxindole alkaloids from Cinnamodendron axillare.
Triterpene saponins from clematis mandshurica.
Cytotoxic cis-fused bicyclic sesquiterpenoids from Jatropha neopauciflora.
Terpenoids and a diarylheptanoid from Zingiber ottensii.
Goniolactones A-F, six new styrylpyrone derivatives from the roots of Goniothalamus cheliensis.
Structure and absolute stereochemistry of hectochlorin, a potent stimulator of actin assembly.
Decipinin A and decipienolides A and B: new bioactive metabolites from the coprophilous fungus Podospora decipiens.
Cytotoxic sphingosine 4-sulfates from the sponge Spirastrella abata.
Naturally occurring cembranes from an Australian sarcophyton species.
Isotactic polymethoxydienes from the Philippines sponge Myriastra clavosa.
Three new modified limonoids from Khaya senegalensis.
Bryoanthrathiophene, a new antiangiogenic constituent from the bryozoan Watersipora subtorquata (d'Orbigny, 1852).
Coproverdine, a novel, cytotoxic marine alkaloid from a new zealand ascidian.
New marine diterpenoids from the Okinawan soft coral Clavularia koellikeri.
Pachyclavulariaenones D-G, new diterpenoids from the soft coral Pachyclavularia violacea.
New acetylenic acids from the marine sponge Stelletta species.
Placidenes C-F, novel alpha-pyrone propionates from the Mediterranean sacoglossan Placida dendritica.
Microbial hydroxylation of quadrone to 8a-hydroxyquadrone.
Maquiroside A, a new cytotoxic cardiac glycoside from Maquira calophylla.
Bioactive stilbenes of Scirpus maritimus.
Puupehenone, a cytotoxic metabolite from a deep water marine sponge, Stronglyophora hartmani.
Cytotoxic flavonols from Gutierrezia microcephala.
Constituents of Tritonia crocosmaeflora, II. Tricrozarin B, an antitumor naphthazarin derivative.
Antifungal activity of Trillium grandiflorum constituents.
Isolation of deoxyshikonin, an antidermatophytic principle from Lithospermum erythrorhizon cell cultures.
Inhibition of cow's milk xanthine oxidase by flavonoids.
Heyneanine hydroxyindolenine, a new indole alkaloid from Ervatamia coronaria var. plena.
[Cytotoxic and antibacterial substances from the ascidian Aplidium antillense]
10H-Phenothiazines: a new class of enzyme inhibitors for inflammatory diseases.
Synthesis, cytotoxicity and effects of some 1,2,4-triazole and 1,3,4-thiadiazole derivatives on immunocompetent cells.
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1).
A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode alpha-carbonic anhydrases.
Synthesis and evaluation of the antioxidant and anti-inflammatory activity of novel coumarin-3-aminoamides and their alpha-lipoic acid adducts.
Low molecular weight non-peptide mimics of omega-conotoxin GVIA.
Benzothiophene piperazine and piperidine urea inhibitors of fatty acid amide hydrolase (FAAH).
ent-Kaurane diterpenoids from Isodon pharicus.
Dapholdhamines A-D, alkaloids from Daphniphyllum oldhami.
Synthesis and evaluation of novel 7-azaindazolyl-indolyl-maleimide derivatives as antitumor agents and protein kinase C inhibitors.
Synthesis and structure-activity relationships of radicicol derivatives and WNT-5A expression inhibitory activity.
N-Substituted-2-alkyl- and 2-arylnorapomorphines: novel, highly active D2 agonists.
Synthesis and biological evaluation of novel 4-azaindolyl-indolyl-maleimides as glycogen synthase kinase-3beta (GSK-3beta) inhibitors.
Rearranged prenylated C6-C3 compounds and a highly oxygenated seco-prezizaane-type sesquiterpene from the stem bark of Illicium oligandrum.
Ionic interactions for substituted MCH1R inhibitors studied by pK(a) values.
Inhibition of the insulin-like growth factor-1 receptor (IGF1R) tyrosine kinase as a novel cancer therapy approach.
RmtC 16S rRNA methyltransferase in Australia.
Telithromycin and quinupristin-dalfopristin induce delayed death in Plasmodium falciparum.
Extended-spectrum beta-lactamases of the CTX-M type now in Switzerland.
Comparative antimalarial activities of six pairs of 1,2,4,5-tetraoxanes (peroxide dimers) and 1,2,4,5,7,8-hexaoxonanes (peroxide trimers).
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
Distribution of radioactivity in bone and related structures following administration of [14C]dalbavancin to New Zealand white rabbits.
Kojic acid-amino acid conjugates as tyrosinase inhibitors.
Identification of a cell-active non-peptide sirtuin inhibitor containing N-thioacetyl lysine.
Pyrazole NNRTIs 1: design and initial optimisation of a novel template.
A direct synthesis of 5,6-dihydroindolo[2,1-a]isoquinolines that exhibit immunosuppressive activity.
Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5).
Synthesis and anticancer activity of N-bis(trifluoromethyl)alkyl-N'-thiazolyl and N-bis(trifluoromethyl)alkyl-N'-benzothiazolyl ureas.
Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.
Synthesis and pharmacological evaluation of sulfamide-based analogues of anandamide.
Structure-guided development of selective TbcatB inhibitors.
Synthesis and biological evaluation of new 4-carboxyl quinoline derivatives as cyclooxygenase-2 inhibitors.
Search for new pharmacophores for antimalarial activity. Part III: synthesis and bioevaluation of new 6-thioureido-4-anilinoquinazolines.
Inhibitors of HIV-1 attachment. Part 3: A preliminary survey of the effect of structural variation of the benzamide moiety on antiviral activity.
4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors.
New Cephalotaxus Alkaloids from Cephalotaxus harringtonia var. drupacea
Makaluvic acids A and B: novel alkaloids from the marine sponge Zyzzya fuliginosus.
Chlorinated annonaceous acetogenins and their bioactivities.
Hippospongins AF: New Furanoterpenes from a Southern Australian Marine Sponge Hippospongia sp.
Callyspongins A and B: Novel Polyacetylene Sulfates from the Marine Sponge Callyspongia truncata That Inhibit Fertilization of Starfish Gametes
Fusaricide, a new cytotoxic N-hydroxypyridone from Fusarium sp.
Two 5-HT 1A Receptor-Interactive Tryptamine Derivatives from the Unripe Fruit of Evodia rutaecarpa
Four new cytotoxic germacranolides from Carpesium divaricatum.
Two new chymotrypsin inhibitors isolated from the Cyanobacterium Microcystis aeruginosa NIES-88.
Organoiodine (III)-mediated synthesis of 3-aryl/heteroaryl-5,7-dimethyl-1,2,4-triazolo[4,3-c]pyrimidines as antibacterial agents.
Gallium(III) complexes of 2-pyridineformamide thiosemicarbazones: cytotoxic activity against malignant glioblastoma.
Phenylpyrrole derivatives as neural and inducible nitric oxide synthase (nNOS and iNOS) inhibitors.
Synthesis, pharmacological evaluation and docking studies of new sulindac analogues.
Synthesis and biological evaluation of abietic acid derivatives.
New cyclopentane derivatives as inhibitors of steroid metabolizing enzymes AKR1C1 and AKR1C3.
Design, synthesis and evaluations of acridone derivatives using Candida albicans--search for MDR modulators led to the identification of an anti-candidiasis agent.
Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase.
Natural product inhibitors of protein-protein interactions mediated by Src-family SH2 domains.
Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.
Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors.
Virtual screening approach for the identification of new Rac1 inhibitors.
Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.
Synthesis and evaluation of estrogen agonism of diaryl 4,5-dihydroisoxazoles, 3-hydroxyketones, 3-methoxyketones, and 1,3-diketones: a compound set forming a 4D molecular library.
Duocarmycin-based prodrugs for cancer prodrug monotherapy.
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
Sultam thiourea inhibition of West Nile virus.
Antimalarial, antiviral, and antitoxoplasmosis norsesterterpene peroxide acids from the Red Sea sponge Diacarnus erythraeanus.
Polychlorinated acetamides from the cyanobacterium Microcoleus lyngbyaceus.
Two new constituents of Isodon excisus and their evaluation in an apoptosis inhibition assay.
Radiosumin B, an unusual dipeptide from the cyanobacterium Microcystis aeruginosa.
Dendocarbins A--N, new drimane sesquiterpenes from the nudibranch Dendrodoris carbunculosa.
Triterpene saponins from Tupidanthus calyptratus.
Chemical constituents from Lippia sidoides and cytotoxic activity.
New sesquiterpene hydroquinones from a Taiwanese marine sponge, Hippospongia metachromia.
Trichoflectin, a bioactive azaphilone from the ascomycete Trichopezizella nidulus.
Antibacterial activity of lonchocarpol A.
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.
Mollenines A and B: new dioxomorpholines from the ascostromata of Eupenicillium molle.
Synthesis and cytotoxic activity of pyranocoumarins of the seselin and xanthyletin series.
The characterization and structure-activity evaluation of toxic norditerpenoid alkaloids from two Delphinium species.
Antimalarial principles from Artemisia indica.
Growth-inhibitory activities of benzofuran and chromene derivatives toward Tenebrio molitor.
Synthesis and affinity to DNA of phenylbenzoimidazoles and benzoimidazo[1,2-c]quinazolines.
Phenylphenalenones from the Australian plant Haemodorum simplex.
In vitro and in vivo studies of 6,8-(diaryl)imidazo[1,2-a]pyrazin-3(7H)-ones as new antioxidants.
Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.
Discovery of N-[(1-aryl-1H-indazol-5-yl)methyl]amides derivatives as smoothened antagonists for inhibition of the hedgehog pathway.
Dopamine D3 receptor antagonists: the quest for a potentially selective PET ligand. Part one: lead identification.
Synthesis and structure-activity relationship of dicationic diaryl ethers as novel potent anti-MRSA and anti-VRE agents.
Highly tractable, sub-nanomolar non-steroidal glucocorticoid receptor agonists.
Synthesis of 4-thiophen-2'-yl-1,4-dihydropyridines as potentiators of the CFTR chloride channel.
Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists.
Interaction studies between human alpha-tocopherol transfer protein and nitric oxide donor tocopherol analogues with LDL-protective activity.
Synthesis and antitumor activity of novel 2',3'-dideoxy-2',3'-diethanethionucleosides bearing 1,2,3-triazole residues.
CD4 mimics targeting the mechanism of HIV entry.
Novel lead for potent inhibitors of breast cancer resistance protein (BCRP).
Highly selective and potent mu opioid ligands by unexpected substituent on morphine skeleton.
A novel chemotype of kinase inhibitors: Discovery of 3,4-ring fused 7-azaindoles and deazapurines as potent JAK2 inhibitors.
Gastroprotective flavonoid constituents from Oroxylum indicum Vent.
Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.
Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues.
Antioxidant and antibacterial studies of arylazopyrazoles and arylhydrazonopyrazolones containing coumarin moiety.
Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists.
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
4,4-Disubstituted cyclohexylamine based CCR5 chemokine receptor antagonists as anti-HIV-1 agents.
S1P receptor mediated activity of FTY720 phosphate mimics.
Bisleuconothine A, an eburnane-aspidosperma bisindole alkaloid from Leuconotis griffithii.
Selectively nonselective kinase inhibition: striking the right balance.
Isolation and biological evaluation of 8-epi-malyngamide C from the Floridian marine cyanobacterium Lyngbya majuscula.
Rigidified 2-aminopyrimidines as histamine H4 receptor antagonists: effects of substitution about the rigidifying ring.
Novel powerful water-soluble lipid immunoadjuvants inducing mouse dendritic cell maturation and B cell proliferation using TLR2 pathway.
Synthesis, antibacterial and antifungal activities of some carbazole derivatives.
Antimicrobial activity of long-chain (E)-3-alken-2-ones.
Transient receptor potential ankyrin 1 (TRPA1) channel as emerging target for novel analgesics and anti-inflammatory agents.
Analysis of the binding of mixed lineage leukemia 1 (MLL1) and histone 3 peptides to WD repeat domain 5 (WDR5) for the design of inhibitors of the MLL1-WDR5 interaction.
Structure-activity relationship for thiohydantoin androgen receptor antagonists for castration-resistant prostate cancer (CRPC).
"Viologen" dendrimers as antiviral agents: the effect of charge number and distance.
Optimisation of a pyrazole series of progesterone antagonists; Part 1.
Semisynthesis and pharmacological activities of thyroxine analogs: Development of new angiogenesis modulators.
Selective one-pot multicomponent synthesis and anti-tubercular evaluation of 5-(aryl/cyclohexylsulfanyl)-2-alkoxy-4,6-diarylnicotinonitriles.
Heterocycle-substituted proline dipeptides as potent VLA-4 antagonists.
Discovery, structure-activity relationships, pharmacokinetics, and efficacy of glucokinase activator (2R)-3-cyclopentyl-2-(4-methanesulfonylphenyl)-N-thiazol-2-yl-propionamide (RO0281675).
Stereochemical requirements for the mineralocorticoid receptor antagonist activity of dihydropyridines.
Structural and stereochemical requirements of the spiroketal group of hippuristanol for antiproliferative activity.
In vitro cytotoxic activity of isolated acridones alkaloids from Zanthoxylum leprieurii Guill. et Perr.
Identification of hits as matrix-2 protein inhibitors through the focused screening of a small primary amine library.
Discovery of 5-substituted-N-arylpyridazinones as inhibitors of p38 MAP kinase.
Structure-activity relationship of an ozonide carboxylic acid (OZ78) against Fasciola hepatica.
Antiproliferative activity of withanolides against human breast cancer cell lines.
Action of a pentacyclic triterpenoid, maslinic acid, against Toxoplasma gondii.
Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.
Inhibitors of prolyl oligopeptidases for the therapy of human diseases: defining diseases and inhibitors.
Synthesis, spectral characterization and bioassay of 3,3'-(1,4-phenylene)-bis[2-alkoxycarbonyl-alkyl)-2-thio-benzoxa-phosphinines].
Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone.
4-Substituted 4-(1H-1,2,3-triazol-1-yl)piperidine: novel C7 moieties of fluoroquinolones as antibacterial agents.
Truxillic acid derivatives act as peroxisome proliferator-activated receptor gamma activators.
New alkaloids from the papua new guinean sponge agelas nakamurai
Design and synthesis of cosalane, a novel anti-HIV agent
Potent inhibitors of neutral endopeptidase. 2-Biphenyl- methylglutaric acid amide derivatives
Synthesis of new maleimide derivatives of daunorubicin and biological activity of acid labile transferrin conjugates
Formation of the Michaelis complex without involvement of the prosthetic group dehydroalanine of histidine ammonialyase
Synthesis of novel taxol analogs and evaluation of their biological activities
Macrolide-type motilin receptor agonists: Acid-stable 12-O-methyl-8,9-anhydroerythromycin A 6,9-hemiacetals
Tripeptidyl pyridinium methyl ketones as potent active site inhibitors of thrombin
Structure/activity relationships among photosensitizers related to pheophorbides and bacteriopheophorbides
-lactam-recognizing enzymes exhibit different structural specificity in acyclic amide and ester substrates: a starting point in -lactamase evolution?
Identification and characterisation of an inhibitor of interleukin-8: a receptor based approach
Studies of the inactivation of general acyl-coa dehydrogenase by (1R)- and (1S)-(methylenecyclopropyl)acetyl-coa
Comparative molecular field analysis of benzopyran-4-carbothioamide potassium channel openers
Synthesis and preparation of an affinity chromatography column for the purification of cytosolic phospholipase A2
The chemical synthesis of large random peptide libraries and their use for the discovery of ligands for macromolecular acceptors
DNA cleavage by photoexcited diazoarenes
Syntheses and exploration of new biological activities in ethyl 6/7-substituted and 6, 7-disubstituted quinolin-4-one-3-carboxylates
Novel compound stimulates amylase induction in barley seeds
Enzymatic resolution of AMPA by use of -chymotrypsin
Synthesis and biological activities of new conformationally fixed analogues of ()-indolactam-V, the core structure of tumor-promoting teleocidins
Novel synthetic rotenoids with blocked B/C ring systems
Nonpeptide angiotensin II receptor antagonists: the discovery of DMP 581 and DMP 811
The synthesis and structure activity relationships of enantiomerically pure hydroxylated oxotremorine derivatives
The synthesis of a dipyrido[3,2-b:3,4-e][1,4]diazepinone: Convenient access to a C-ring isomer of the HIV-1 reverse transcriptase inhibitor nevirapine
Synthesis and in vitro cytotoxicity of (RS)-20-desethyl-20-substituted camptothecin analogues
Synthesis and evaluation of 4-5-dehydro-5-fluoroaristeromycins as S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitors
Synthesis and pharmacological evaluation of combined Thromboxane receptor antagonists/thromboxane synthase inhibitors: Pyridine-containing amino-prostanoids
A case study of combinatorial libraries: Endothelin receptor antagonist hexapeptides
Synthesis and anti-pseudomonal activity of new 2-isocephems with a dihydroxypyridone moiety at C-7
The chemical evolution of N,N-dimethyl-2-[5-(1,2,4-triazol-4-yl)-1H-indol-3-yl]ethylamine (L-741,604) and analogues: Potent and selective agonists for 5-HT1D receptors
Tetrazole-substituted ureas as inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT). A novel preparation of ureas from weakly nucleophilic amines
Novel frameworks for trifluoromethyl ketone and phosphonate tsa inhibitors of type II PLA2
Synthesis and evaluation of 3-deoxy-D-manno-2-octulosonate-8-phosphate (KDO8P) synthase inhibitors
The synthesis of N-aryl androsterone pyrazoles as aromatase inhibitors
Studies On uro'gen III synthase with modified bilanes
Synthesis of neoeudistomin analogsAs potential filaricides
Synthesis of potent 6-oxo and 9-fluoro-PGE1-derivatives and their biological properties
Modified triphosphates of carbocyclic nucleoside analogues: Synthesis, stability towards alkaline phosphatase and substrate properties for some DNA polymerases
1,1-Dicyano-2-substituted ethylenes: A new class of glucose uptake inhibitors in antifilarial chemotherapy
Synthesis and cardiotonic activity of 2,9-dihydro-6-(5-methyl-3-oxo-2,3,4,5-tetrahydropyridazin-6-yl)pyrazolo[4,3-b][1,4]benzoxazine
Synthesis and influenza neuraminidase inhibitory activity of aromatic analogues of sialic acid
Synthesis and pharmacological evaluation of the enantiomers of the dopamine autoreceptor agonist PD 135385
Inhibition of human immunodeficiency virus-1 protease by a C2-symmetrical phosphinic acid amide
Structure-activity relationships of sulfur-containing triazole antifungals
Synthesis of tetrazol-1-yl analogs of HMG-COA reductase inhibitor BMS180431 (formerly BMY21950)
Lipophilic bis-arylsulfonates as inhibitors of the CD4-gp120 interaction
Local constrained shifty pseudopeptides inhibitors of rasfarnesyl transferase
De novo design of nonpeptidic HIV-1 protease inhibitors: Incorporation of structural water.
New deoxynojirimycin derivatives as potent inhibitors of intestinal -glucohydrolases
Synthesis and HIV-1 inhibition of novel benzimidazole derivatives
-Glucan biosynthesis inhibitors isolated from fungi as hyphal malformation inducer
Muscarinic antagonist activity of 3-(5-alkoxy-oxazol-2-yl)-1,2,5,6-tetrahydropyridines.
Synthetic inhibitors of interleukin-6 I: 2,3,7,8-tetrahydro-4-aryl-1H-cyclopent [e] imidazo [1,2-a]- pyridin-5(6H)-one and related compounds
Synthesis and antitumor evaluation of 2-oxycarbonylpaclitaxels (paclitaxel-2-carbonates)
5-HT4receptor antagonists : oxazolo, oxazino and oxazepino[3,2-a]indole derivatives
The synthesis and antibacterial activity of 2-para-quarternary ammoniomethylphenyl-carbapenems.
5,7-Diphenyl-3-ureidohexahydroazepin-2-ones as Cholecystokinin-B receptor ligands
Synthesis and evaluation of the anticonvulsant activity of a series of 2-amino-1-phenyl-1-propanols derived from the metabolites of the antidepressant bupropion
NS 257 (1,2,3,6,7,8-hexahydro-3(hydroxyimino)-N,N,7-trimethyl-2-oxobenzo[2,1-b:3,4-c']dipyrrole-5-sulfonamide) is a potent, systemically active ampa receptor antagonist
Synthesis and antimicrobial activity of 5-thioabbeymycin: limitations of the iminothioether approach to carbinolamine-containing pyrrolobenzodiazepines
Bis-quinolinium cyclophanes: A novel class of potent blockers of the apamin-sensitive Ca2+-activated K+ channel
Linear amides as substance P antagonists
Structure-based design of novel calcineurin (PP2B) inhibitors
Semi-synthetic qualestatins: Squalene synthase inhibition and antifungal activity. The SAR of C6 and C7 modifications
C32-amino derivatives of the immunosuppressant ascomycin
A comparative SAR and computer modeling study of benzisothiazolone, mechanism-based inhibitors with porcine pancreatic and human leukocyte elastase
The preparation and utilization of paraherquamide-2-O-methyl imidate in the synthesis of 14-O-substituted paraherquamide derivatives
Difunctional enols of N-protected amino acids as low molecular weight and novel inhibitors of HIV-1 protease.
Synthesis and structure-activity relationships of novel THF 1-methylcarbapenems
Synthesis and x-ray structure of a potent superpositional analog of the enantiomeric forms of fluoxetine
Synthesis and inhibitory effects of bivalent sialyl lewis X analogs at preventing cell adhesion
Synthesis and biological activity of 3-alkyl- and 3-alkenyl-3-dephenyldocetaxels
Conformationally restricted 1,5-diarylpyrazoles are selective COX-2 inhibitors
Antiproliferative activity of haloosmocenium ions against human and murine cancer cell lines
Inhibitors of MMP-1: an examination of P1 C gem-disubstitution in the N-carboxyalkylamine and glutaramide carboxylate series
Stereoselectivity in the hydrolysis of synthetic esters by cultured cancer cells and normal tissue extracts of rat
Rollimembrin, a novel acetogenin inhibitor of mammalian mitochondrial complex I
Analogs of an endothelin antagonist RES-701-1: substitutions of C-terminal amino acid
Synthesis and PKC inhibitory activities of balanol analogs with a cyclopentane substructure
Inhibition of human leukocyte elastase. 5. Inhibition by 6-alkyl substituted penem benzyl esters.
Substituted 1,3,5-triazines as cholesteryl ester transfer protein inhibitors
RATIONAL DESIGN, SYNTHESIS, AND SERINE PROTEASE INHIBITORY ACTIVITY OF NOVEL P1-ARGININOYL HETEROCYCLES
Synthesis of phosphonate analogues of 1,3-bisphosphoglyceric acid and their binding to yeast phosphoglycerate kinase
Discovery of MK-0476, a potent and orally active leukotriene D4 receptor antagonist devoid of peroxisomal enxyme induction
Peptide mimics of glycylproline as inhibitors of prolidase
An efficient synthesis of short-chain sphingomyelin analogs and their susceptibility to hydrolysis catalyzed by sphingomyelinase
On the mechanism of activation of designed enediynes with selective cytotoxicity
Substituted piperidin-2-one biphenyltetrazoles as angiotensin II antagonists
Structure-directed discovery of an inhibitor of the binding of HIV GP120 to the CD4 receptor
Synthesis & characterization of N-amino-glyphosate as a potent analog inhibitor of E. coli EPSP synthase.
Synthesis and biological properties of quaternized N-methylation analogs of D-Arg-2-dermorphin tetrapeptide
Design, synthesis and SAR of RGD peptide hybrids as highly efficient inhibitors of platelet aggregation
Sulfobetaine zwitterionic inhibitors of squalene synthase
Synthesis, antimicrobial activity and binding properties of calix[4]arene based vancomycin mimics
A bioactive benzoindenone from Eichhornia crassipes solms
Novel 4-substituted pyridine derivatives: Practical derivatization and biological profiles of reversible inhibitors
6,7,8,9-tetrahydro-3-hydroxy-1H-1-benzazepine-2,5-diones via a diels-alder reaction:antagonists with a non-planar hydrophobic region for NMDA receptor glycine sites
Benzenepropanoic acids containing chromanone or naphthalenone moieties are potent and orally active leukotriene B4 antagonists
Anti-human immunodeficiency virus type-1 (HIV-1) and anti-hepatitis B virus (HBV) activities of (2,3-dideoxy-2-fluoro--L-threo-pentofuranosyl)nucleosides
7-aminoalkyl-2-amino-1,2,3,4-tetrahydro-2-naphthoic acids as inhibitors of tryptophan uptake
Phenyl-glycinol based NK1 receptor antagonists towards the minimum pharmacophore
Synthesis of new TNF- Inhibitors and their biological properties
Modifications of primaquine as antimalarials. 4. 5-Alkoxy derivatives of primaquine.
Nonsteroidal cardiotonics. 1. 2-Pyridyl-6,7-dihydro-3H,5H-pyrrolo[2,3-f]benzimidazol-6-ones, a novel class of cardiotonic agents.
Synthesis and biological evaluation of acyclic neplanocin analogues.
SAR of N-phenyl piperidine based oral integrin alpha5beta1 antagonists.
Triazole oxytocin antagonists: Identification of an aryloxyazetidine replacement for a biaryl substituent.
Sulfonylureido thiazoles as fructose-1,6-bisphosphatase inhibitors for the treatment of type-2 diabetes.
Synthesis and SAR of sulfonyl- and phosphoryl amidine compounds as anti-resorptive agents.
Synthesis and in vivo evaluation of bicyclic gababutins.
1-(3-Aryloxyaryl)benzimidazole sulfones are liver X receptor agonists.
Biaryl piperidines as potent and selective delta opioid receptor ligands.
Anti-human immunodeficiency virus activity and cytotoxicity of derivatized buckminsterfullerenes
Vasorelaxant activity of 2-substituted 6-nitro-2H-1-benzopyran-4-carbothioamide K+ channel openers
Studies on irreversible inhibition of serine proteases by -sulfonyloxyketone derivatives
Unusual stereochemical preferences of decahydroisoquinoline-3-cargoxylic acid competitive NMDA antagonists
Diphenylpyrazolidinone and benzodiazepine cholecystokinin antagonists: A case of convergent evolution in medicinal chemistry
Spiroepoxycyclohexadienone dimers: cytotoxic bisalkylating agents
The synthesis of aminobenzazepinones as anti-phenylalanine dipeptide mimics and their use in nep inhibition
Interaction of rigid polyamine analogues with the NMDA receptor complex from rat brain
The affinity of the excised binding domain of FK-506 for the immunophilin FKBP12.
Conformationally constrained analogues of diacylglycerol. 5. 2,5-Dideoxy-3-O-tetradecanoyl-D-galactono-1,4-lactone: A superior homologue of 3-O-tetradecanoyl-2-deoxy-L-ribonolactone with PK-C binding affinity.
Benzofuran based angiotensi II antagonists related to GR117289: Part II; amino acid amides
Avermectin B1-8,9-oxide: reactivity, bioactivity, and stereochemistry.
Substituted 6-alkyloxapenems: potent -lactamase inhibitors: synthesis and biological characterization
Inhibition of human leukocyte elastase. 7. Inhibition by 6-substituted penicillin amides.
The squalestatins: novel inhibitors of squalene synthase. The optimal C1 chain-length requirements.
Azido-functionalized thiourea analogues acting as efficient photoaffinity probes for the urea channel.
Synthesis of a peptidyl 2,2-difluoro-4-phenylbutyl ketone and its evaluation as an inhibitor of interleukin-1 converting enzyme.
Synthesis and in vitro acetylcholinesterase inhibitory activity of some 1-substituted analogues of velnacrine
Inhibition of cartilage breakdown by isothiazolones
Synthesis and mechanistic studies of a tetrazole-tethered cephalosporin-quinolone hybrid
Synthesis of 4(5)-imidazolyl allylamines and propargylamines as inhibitors of diamine oxidase
Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[1621, D-His16]
Synthesis and anticonvulsant activity of 3-arylamino-4-aryl-5-(N-4-chlorophenylthiocarbamido)-1,2,4-thiadiazoles
Biselectrostatic interaction with DNA as potential anti-turmor agents: novel 2,11-diamino-5,8-dithiaundecane derivatives
Enantioselective acetylation of primary amines by Cylindrocarpon radicicola
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties
New non-peptide angiotensin II receptor antagonists. 2: structure - activity relationship of a series of annelated 2(1H)-pyridinones
Synthesis and biological activities of fluorine-substituted ()-indolactam-V, the core structure of tumor promoter teleocidins
Conformationally constrained HIV-1 protease inhibitors
Novel water-solutle (7-(acylhydrazono)-formyl camptothecins as potent inhibitors of DNA topoisomerase I
Induction of endonucleolytic DNA fragmentation and apoptosis by the duocarmycins
3-Substituted 6-butyl-1,2-dihydropyridin-2-ones: A new series of potent nonpeptide angiotensin II receptor antagonists
p-Guanidinobenzoyl-[Hyp3, Thi5, D-Tic7, Oic8]bradykinin is almost completely devoid of the agonist effect of HOE140 on the endothelium-free femoral artery of sheep.
Novel cholecystokinin receptor ligands: Oxopiperazines derived from Boc-CCK-4
1,3-Oxazino[4,5-b]indole-2,4-(1H,9H)-diones and 5,6-dimethylpyrrolo-[2,3-d]-1,3-oxazin-2,4-(1H,7H)-diones as serine protease inhibitors
Quantitative structure-activity relationships study of endothelin-1 analogs
The squalestatins: novel inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C1-modified analogues.
Synthesis and antifungal activity of novel cationic pneumocandin B(o) derivatives.
Synthesis and structure activity relationships of cis- and trans-2,3,4,4a,9,9a-hexahydro-1H-indeno[2,1-c]pyridines for 5-HT receptor subtypes.
Glycylcyclines. 1. A new generation of potent antibacterial agents through modification of 9-aminotetracyclines.
Structure-activity relationships of new taxoids derived from 14 beta-hydroxy-10-deacetylbaccatin III.
Synthesis and delta-opioid receptor antagonist activity of a naltrindole analogue with a regioisomeric indole moiety.
Approaches toward selective inhibition of nitric oxide synthase.
Syntheses and anticholinesterase activity of tetrahydrobenzazepine carbamates.
Discovery of pyrazolyl propionyl cyclohexenamide derivatives as full agonists for the high affinity niacin receptor GPR109A.
Agonist/antagonist modulation in a series of 2-aryl benzimidazole H4 receptor ligands.
Analysis of kinase inhibitor selectivity using a thermodynamics-based partition index.
Substituted 2H-isoquinolin-1-one as potent Rho-Kinase inhibitors. Part 1: Hit-to-lead account.
Substituted 2H-isoquinolin-1-ones as potent Rho-kinase inhibitors: part 3, aryl substituted pyrrolidines.
Mapping the ATP-binding domain of DNA-dependent protein kinase (DNA-PK) with coumarin- and isocoumarin-derived inhibitors.
Synthesis and evaluation of new endomorphin-2 analogues containing (Z)-alpha,beta-didehydrophenylalanine (Delta(Z)Phe) residues.
New macrolactins from a marine Bacillus sp. Sc026.
Structure-activity relationship of polyisoprenyl benzophenones from Garcinia pyrifera on the tubulin/microtubule system.
Bioactive sesquiterpenes from the basidiomycete Resupinatus leightonii.
Microcyclamide, a cytotoxic cyclic hexapeptide from the cyanobacterium Microcystis aeruginosa.
Three new scalarane sesterterpenoids from the Okinawan sponge Hyrtios erectus.
Stilbene glycoside sulfates from Polygonum cuspidatum.
New cytotoxic sterol glycosides from the octocoral Carijoa (Telesto) riisei.
Cytotoxic prenyleudesmane diterpenes from the fruits of Dysoxylum kuskusense.
New marine cembrane-type diterpenoids from the Okinawan soft coral Clavularia koellikeri.
A new inhibitor of 5'-hydroxyaverantin dehydrogenase, an enzyme involved in aflatoxin biosynthesis, from Trichoderma hamatum.
Thirteen novel cycloartane-type triterpenes from Combretum quadrangulare.
Zygosporin D and two new cytochalasins produced by the fungus Metarrhizium anisopliae.
Cytotoxic oxygenated triterpenoid saponins from Symplocos chinensis.
Sulfated alkenes from the echinus Temnopleurus hardwickii.
Bioactive oligostilbenoids from the stem bark of Hopea exalata.
Design, synthesis, and structure-affinity relationship studies in NK1 receptor ligands based on azole-fused quinolinecarboxamide moieties.
Synthesis, binding properties and receptor docking of 4-halo-6-[2-(4-arylpiperazin-1-yl)ethyl]-1H-benzimidazoles, mixed ligands of D2 and 5-HT1A receptors.
Antifungal activity of chalcones: a mechanistic study using various yeast strains.
New taxane diterpenoids from the roots of Taxus mairei.
Niruriside, a new HIV REV/RRE binding inhibitor from Phyllanthus niruri.
Ferintoic Acids A and B, New Cyclic Hexapeptides from the Freshwater Cyanobacterium Microcystis aeruginosa
Mauritiamine, a New Antifouling Oroidin Dimer from the Marine Sponge Agelas mauritiana
Raocyclamides A and B, Novel Cyclic Hexapeptides Isolated from the Cyanobacterium Oscillatoria raoi
Sindurol and Nephthoside: New Tetraprenyltoluquinols from the Soft Coral Sinularia dura and Nephthea sp.
New Destruxins from the Entomopathogenic Fungus Aschersonia sp.
Cyclic peptides from higher plants. 24.1 yunnanin C, a novel cyclic heptapeptide from Stellaria yunnanensis.
Tetranortriterpenoids from Ruagea glabra
Structure and Plant Growth Regulatory Activity of New Diterpenes from Pterodon polygalaeflorus
Antiinflammatory C-glucosyl chromone from Aloe barbadensis.
Keenamide A, a bioactive cyclic peptide from the marine mollusk Pleurobranchus forskalii.
Antiplatelet flavonoids from seeds of Psoralea corylifolia.
Isolation of Polyhydroxysteroids from the Gorgonian Acabaria undulata
Cytotoxic Cembranoids from the Soft Corals Sinularia gibberosa and Sarcophyton trocheliophorum
Jineol, a Cytotoxic Alkaloid from the Centipede Scolopendra subspinipes
Hydroxycornexistin: A New Phytotoxin from Paecilomyces variotii
Bioactive Isoquinoline Quinone from an Undescribed Philippine Marine Sponge of the Genus Xestospongia
Tonkinecin, a novel bioactive annonaceous acetogenin from Uvaria tonkinesis.
Novel beta-methoxyacrylates of the 9-methoxystrobilurin and oudesmansin classes produced by the basidiomycete Favolaschia pustulosa.
A New Prenylated Flavone from Artocarpus champeden
Synthesis of 5-(3-Hydroxypropyl)-7-methoxy-2-(3-methoxy-4-hydroxyphenyl)-3- benzo[ b ]furancarbaldehyde, a Novel Adenosine A 1 Receptor Ligand from the Root of Salvia miltiorrhiza
N -(Indol-3-ylethyl)-2-hydroxy-3-methylpentanamide, a Novel Indole Derivative from Xenorhabdus nematophilus
Iridoid Molluscicidal Compounds from Apodytes dimidiata
Molluscicidal Triterpenoid Glycosides of Dialium guineense
Fulvinol, a New Long-Chain Diacetylenic Metabolite from the Sponge Reniera fulva
Isolation and structure of prorocentrolide B, a fast-acting toxin from Prorocentrum maculosum.
Serotonergic properties of spiroxatrine enantiomers.
Oral absorption of cephalosporin antibiotics. 2. Expanded structure-activity relationships of 7-(arylacetamido)-3-substituted cephalosporins.
4-N-hydroxy-L-2,4-diaminobutyric acid. A strong inhibitor of glutamine synthetase.
Acetohydroxamic acids as potent, selective, orally active 5-lipoxygenase inhibitors.
Renin inhibitors containing psi[CH2O] pseudopeptide inserts.
Flavins as potential antimalarials. 1. 10-(Halophenyl)-3-methylflavins.
Enantioselectivity of muscarinic antagonists. Isomeric 2-cyclohexyl-2-phenyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodides.
3-Phenoxypyridine 1-oxides as anticonvulsant agents.
Decomposition of N-(2-chloroethyl)-N-nitrosocarbamoyl amino acid amides.
Thienothiopyran-2-sulfonamides: novel topically active carbonic anhydrase inhibitors for the treatment of glaucoma.
Selective and enantiospecific acylation of kappa opioid receptors by (1S,2S)-trans-2-isothiocyanato-N-methyl-N-[2-(1-pyrrolidinyl) cyclohexy l] benzeneacetamide. Demonstration of kappa receptor heterogeneity.
Oxidation of neplanocin A to the corresponding 3'-keto derivative by S-adenosylhomocysteine hydrolase.
Synthesis and antitumor activity of ribavirin imidates. A new facile synthesis of ribavirin amidine (1-beta-D-ribofuranosyl-1,2,4-triazole-3-carboxamidine hydrochloride).
Synthesis of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones as potential antileukemic agents.
Potential cancer chemopreventive and cytotoxic agents from Pulicaria crispa.
Mollinedine, a New Alkaloid from Mollinedia costaricensis.
Inhibition of dopamine beta-hydroxylase by goitrin, a natural antithyroid compound.
Biosynthesis of staurosporine, 1. 1H- and 13C-NMR assignments.
Isolation and Bioactivity of 2-Aminoquinoline from Leucopaxillus albissimus.
Brianthein V, a New Cytotoxic and Antiviral Diterpene Isolated from Briareum asbestinum
Plant antimutagenic agents, 3. Coumarins.
1H-nmr analysis of herbimycins and dihydro-herbimycins.
Photodiode Array Detection and Structures of Griseolic Acid Analogues from Culture Broth
Studies of Swedish Marine Organisms, Part X. Biologically Active Compounds from the Marine Sponge Geodia baretti
Halleridone, a cytotoxic constituent from Cornus controversa.
Oxygenated Furanosesterterpene Tetronic Acids from a Sponge of the Genus Ircinia
Autooxidation Studies on the Marine Sesterterpene Tetronic Acid, Variabilin
The Chemistry of Taxol, a Clinically Useful Anticancer Agent
Enantiomeric Relationships and Anthelmintic Activity of Dysinin Derivatives from Dysidea Marine Sponges
Triterpenoids and Flavonoids from Hyptis albida
Minor Bioactive Polyacetylenes from Petrosia ficiformis
Furanoid lignans from Larrea tridentata.
Brominated Metabolites from the Sponge Aplysina (verongia) thiona
HIV-1 reverse transcriptase inhibitor design using artificial neural networks.
The stabilization of DNA topoisomerase II cleavable complex by mitonafide analogs
Synthesis of selective non-Ca(2+)-mobilizing inhibitors of D-myo-inositol 1,4,5-trisphosphate 5-phosphatase.
Application of the three-dimensional structures of protein target molecules in structure-based drug design.
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
Perhydrothiopyranopyrroles derivatives : A novel series of potent and selective nonpeptide NK1 antagonists.
EPSP synthase inhibitor design IV. New aromatic substrate analogs and symmetrical inhibitors containing novel 3-phosphate mimics.
Characterization of two taxol photoaffinity analogues bearing azide and benzophenone-related photoreactive substituents in the A-ring side chain.
3-Acrylamide-4-aryloxyindoles: synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists.
(1,2,3-Triazol-4-yl)benzenamines: synthesis and activity against VEGF receptors 1 and 2.
Synthesis and biological activity of anticoccidial agents: 2,3-diarylindoles.
3,4-Diamino-1,2,5-thiadiazole as potent and selective CXCR2 antagonists.
Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11beta-HSD1 inhibitors.
Iodine-catalyzed one-pot synthesis and antimalarial activity evaluation of symmetrically and asymmetrically substituted 3,6-diphenyl[1,2,4,5]tetraoxanes.
Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers.
Development of the renal glucose reabsorption inhibitors: a new mechanism for the pharmacotherapy of diabetes mellitus type 2.
5-Aminomethylbenzimidazoles as potent ITK antagonists.
Liver X receptor agonists with selectivity for LXRbeta; N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropionamides.
Structure-activity study of pentamidine analogues as antiprotozoal agents.
3-Hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-2-carboxylates--a new class of HIV-1 integrase inhibitors.
First asymmetric synthesis of CJ-14877 and its enantiomer and their interleukin-1beta inhibitory activities.
Synthesis and evaluation of myxochelin analogues as antimetastatic agents.
New isomalabaricane triterpenes from the marine sponge Stelletta globostellata that induce morphological changes in rat fibroblasts.
A new bioactive triene aldehyde from the marine sponge Leucetta microraphis.
Two new antimicrobial lysoplasmanylinositols from the marine sponge Theonella swinhoei.
Novel cytotoxic annonaceous acetogenins from Annona muricata.
Suberedamines A and B, new bromotyrosine alkaloids from a sponge Suberea species.
Phomoxanthones A and B, novel xanthone dimers from the endophytic fungus Phomopsis species.
Cytotoxic diacetylenes from the stony coral Montipora species.
Isolation and structure of korolkoside, a bis-iridoid glucoside from Lonicera korolkovii.
Pacovatinins A-C, new labdane diterpenoids from the seeds of Renealmia exaltata.
New guinea pig model of Cryptococcal meningitis.
Emergence of KPC-2 and KPC-3 in carbapenem-resistant Klebsiella pneumoniae strains in an Israeli hospital.
The many roles for fluorine in medicinal chemistry.
Cinnamoyl- and hydroxycinnamoyl amides of glaucine and their antioxidative and antiviral activities.
Design, synthesis, and antihepatocellular carcinoma activity of nitric oxide releasing derivatives of oleanolic acid.
The discovery of small molecule chemical probes of Bcl-X(L) and Mcl-1.
Refinement of histamine H3 ligands pharmacophore model leads to a new class of potent and selective naphthalene inverse agonists.
Design, synthesis, and biological evaluation of antiviral agents targeting flavivirus envelope proteins.
Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) in Gram-positive bacteria.
Novel terphenyls and 3,5-diaryl isoxazole derivatives endowed with growth supporting and antiapoptotic properties.
Synthesis of some novel imidazole-based dicationic carbazolophanes as potential antibacterials.
Investigation of the relative cellular permeability of DNA-binding pyrrole-imidazole polyamides.
Amide isosteres of oroidin: assessment of antibiofilm activity and C. elegans toxicity.
Arylpyrrolizines as inhibitors of microsomal prostaglandin E2 synthase-1 (mPGES-1) or as dual inhibitors of mPGES-1 and 5-lipoxygenase (5-LOX).
Synthesis of 4'-ester analogs of resveratrol and their evaluation in malignant melanoma and pancreatic cell lines.
Synthesis and structure-activity relationships of novel furazan-3,4-diamide analogs as potent anti-cancer agents.
Piperidine-based heterocyclic oxalyl amides as potent p38 alpha MAP kinase inhibitors.
Synthesis and biological evaluation of novel C5 halogen-functionalized S-DABO as potent HIV-1 non-nucleoside reverse transcriptase inhibitors.
In vitro TRPV1 activity of piperine derived amides.
Synthesis and biological evaluation of 1,4-diazepane derivatives as T-type calcium channel blockers.
Secondary metabolites from the roots of Litsea hypophaea and their antitubercular activity.
Role of hydrophobic substituents on the terminal nitrogen of histamine in receptor binding and agonist activity: development of an orally active histamine type 3 receptor agonist and evaluation of its antistress activity in mice.
Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides.
New pyrazolo[1,5a]pyrimidines as orally active inhibitors of Lck.
Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide.
Discovery of a series of indan carboxylic acid glycogen phosphorylase inhibitors.
Structure-activity relationship (SAR) investigations of tetrahydroquinolines as BKCa agonists.
Towards Gram-positive antivirulence drugs: new inhibitors of Streptococcus agalactiae Stk1.
N-(alpha-Hydroxyalkanoyl) derivatives of Leu-Val-Phe-OCH3 as inhibitors of renin.
Effect of magnesium lithospermate B on urinary prostaglandins in rats with renal failure.
New cytotoxic steroids from the Indian Ocean sponge Axinella cf. bidderi.
Structures of new sesquiterpenes and hepatoprotective constituents from the Egyptian herbal medicine Cyperus longus.
Cytotoxic sterols and saponins from the starfish Certonardoa semiregularis.
Antimicrobial chlorinated bibenzyls from the liverwort Riccardia marginata.
Phorbasterones A-D, cytotoxic nor-ring A steroids from the sponge Phorbas amaranthus.
Isolation and structure of gustastatin from the Brazilian nut tree Gustavia hexapetala.
New cytotoxic oleanane-type triterpenoids from the cones of Liquidamber styraciflua.
Cytotoxic furanosesterterpenes from a marine sponge Psammocinia sp.
Cytotoxic principles from the formosan milkweed, Asclepias curassavica.
Nematicidal epipolysulfanyldioxopiperazines from Gliocladium roseum.
Bis(bibenzyls) from liverworts inhibit lipopolysaccharide-induced inducible NOS in RAW 264.7 cells: a study of structure-activity relationships and molecular mechanism.
Discorhabdin W, the first dimeric discorhabdin.
Antineoplastic activity and cytotoxicity of flavones, isoflavones, and flavanones.
End-Product Regulation of Ergot Alkaloid Formation in Intact Cells and Protoplasts of Claviceps Species, Strain SD 58
Ipomopsin, a New Biscoumarin from Ipomopsis aggregata
Plant anticancer agents XXIX. Cleomiscosin A from Simaba multiflora, Soulamea soulameoides, and Matayba arborescens.
New secosteroids from a gorgonian of the genus Muricella.
Phycomysterols and other sterols from the fungus Phycomyces blakesleeanus.
Arugosin F: a new antifungal metabolite from the coprophilous fungus Ascodesmis sphaerospora.
Recent Biosynthetic Studies on Antibiotics
Alkaloids of Thalictrum XXX. Eleven Minor Alkaloids From Thalictrum rugosum
Alkaloids of Thalictrum XXXIV. Three New Alkaloids, Thalmirabine, Thalistine, and O-Methylthalibrine, and Others From Roots of Thalictrum minus Race B
Plant anticancer agents. X. Lignans from Juniperus phoenicea.
Argifin; efficient solid phase total synthesis and evaluation of analogues of acyclic peptide.
Design and structural analysis of novel pharmacophores for potent and selective peroxisome proliferator-activated receptor gamma agonists.
Synthesis and anti-hepatitis B virus activities of Matijing-Su derivatives.
N(G)-acylated imidazolylpropylguanidines as potent histamine H4 receptor agonists: selectivity by variation of the N(G)-substituent.
Synthesis and biological evaluation of novel conjugates of podophyllotoxin and 5-FU as antineoplastic agents.
Synthesis and in vitro evaluation of sulfonamide isatin Michael acceptors as small molecule inhibitors of caspase-6.
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 1.
Isoplatensimycin: Synthesis and biological evaluation.
Novel mannosyl derivatives of peptidoglycan monomer: Synthesis and biological evaluation of immunomodulatory properties.
Design of selective Cathepsin inhibitors.
Benzothiophene inhibitors of MK2. Part 1: structure-activity relationships, assessments of selectivity and cellular potency.
Design, synthesis, enzyme inhibition, and tumor cell growth inhibition of 2-anilinobenzamide derivatives as SIRT1 inhibitors.
Synthesis, biological evaluation, and metabolic stability of acrylamide derivatives as novel CCR3 antagonists.
Characterization of novel selective H1-antihistamines for clinical evaluation in the treatment of insomnia.
Pursuing aldose reductase inhibitors through in situ cross-docking and similarity-based virtual screening.
Indolobenzazepin-7-ones and 6-, 8-, and 9-membered ring derivatives as tubulin polymerization inhibitors: synthesis and structure--activity relationship studies.
In vitro antifungal susceptibilities of five species of sporothrix.
In vitro activities of doripenem and six comparator drugs against 423 aerobic and anaerobic bacterial isolates from infected diabetic foot wounds.
Synthesis and evaluation of alpha,alpha'-disubstituted phenylacetate derivatives for T-type calcium channel blockers.
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors.
Structure-activity relationship studies on vitamin D lactam derivatives as vitamin D receptor antagonist.
Synthesis and antiviral evaluation of some new pyrazole and fused pyrazolopyrimidine derivatives.
Sialyl alpha(2-->3) lactose clusters using carbosilane dendrimer core scaffolds as influenza hemagglutinin blockers.
Oxadiazole-carbonylaminothioureas as SIRT1 and SIRT2 inhibitors.
Achieving multi-isoform PI3K inhibition in a series of substituted 3,4-dihydro-2H-benzo[1,4]oxazines.
Blockade of glucocorticoid excess at the tissue level: inhibitors of 11beta-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes.
Efficient synthesis of (+/-)-parasitenone, a novel inhibitor of NF-kappaB.
Disubstituted pyrimidines as Lck inhibitors.
Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain.
Design and synthesis of novel substituted quinazoline derivatives as antileishmanial agents.
Synthesis of novel isoluminol probes and their use in rapid bacterial assays.
alpha-Tocopheryl succinate as a scaffold to develop potent inhibitors of breast cancer cell adhesion.
Synthesis and antiviral activity of HCV NS3/4A peptidomimetic boronic acid inhibitors.
Potent small molecule mouse CD22-inhibitors: exploring the interaction of the residue at C-2 of sialic acid scaffold.
Synthesis and antifungal activity of benzo[d]oxazole-4,7-diones.
Synthesis and antibacterial activity of 4,5,6,7-tetrahydro-thieno[3,2-c]pyridine quinolones.
A new 4-(2-methylquinolin-4-ylmethyl)phenyl P1' group for the beta-amino hydroxamic acid derived TACE inhibitors.
Modeling assisted rational design of novel, potent, and selective pyrrolopyrimidine DPP-4 inhibitors.
New syntheses of tetrazolylmethylphenylalanine and O-malonyltyrosine as pTyr mimetics for the design of STAT3 dimerization inhibitors.
Triterpene saponins from the roots of Clematis chinensis.
Two pyranocoumarins from the seeds of Calophyllum polyanthum.
Biscoumarin derivatives from Edgeworthia gardneri that inhibit the lyase activity of DNA polymerase beta.
Celogenamide A, a new cyclic peptide from the seeds of Celosia argentea.
Steroidal glycosides from the bulbs of Ornithogalum thyrsoides.
Blanchaquinone: a new anthraquinone from an Australian Streptomyces sp.
Phytochemical studies on Stemona burkillii prain: two new dihydrostemofoline alkaloids.
Asmarines I, J, and K and nosyberkol: four new compounds from the marine sponge Raspailia sp.
10-membered macrolides from the insect pathogenic fungus Cordyceps militaris BCC 2816.
Sesquiterpenes from the mycelial cultures of Dichomitus squalens.
6-Methoxylated and C-glycosyl flavonoids from Centaurea species.
Limonoids from the seeds of Melia azedarach.
Effects of p-Methoxycinnamaldehyde from Star Anise and Related Cinnamic Acid Derivatives on Velvetleaf Germination
Ficulinic acid A and B, two novel cytotoxic straight-chain acids from the sponge Ficulina ficus.
Antitumor agents, 79. Cytotoxic antileukemic alkaloids from Brucea antidysenterica.
Antineoplastic agents, 118. Isolation and structure of bryostatin 9.
Sesterterpenes from a common marine sponge, Hyrtios erecta.
Vasoactive substances from Saussurea lappa.
Novel HIV-inhibitory halistanol sulfates F-H from a marine sponge, Pseudoaxinissa digitata.
Uterotonic effect of Evodia rutaecarpa alkaloids.
Antineoplastic Agents. 67. Senecio fendleri Gray
Normaytansine, a new antileukemic ansa macrolide from Maytenus buchananii.
Isofraxidin, a cytotoxic coumarin from Micrandra elata (Euphorbiaceae).
Inhibition of Plant Growth by Phenethylamines and Tetrahydroisoquinolines
Soularubinone, a new antileukemic quassionoid from Soulamea tomentosa.
Catharanthus alkaloids. XXXIV. Catharanthamine, a new antitumor bisindole alkaloid from Catharanthus roseus.
Chemical composition and biological activity of the Tanzanian plant Ocimum suave.
Potential Anticancer Agents. XVIII. Constituents of Amyris pinnata
Some new decussine-type alkaloids from Strychnos decussata, Strychnos dale and Strychnos elaecocarpa.
Plant Anticancer Agents. XI. 2,6-Dimethoxybenzoquinone as a Cytotoxic Constituent of Tibouchina pulchra
Isoiguesterin, a new antileukemic bisnortriterpene from Salacia madagascariensis.
Inhibition of Mitochondrial Function in Termite Queen Ovary by Rabdosia Diterpenoids
Catharanthus alkaloids. XXXV. Isolation of leurosidine N'b-oxide from Catharanthus roseus.
Anticancer indole alkaloids of Rhazya stricta.
Chemical Constituents of Hyptis suaveolens. Part I. Spectral and Biological Studies on a Triterpene Acid
Recent Studies on Bioactive Compounds From Plants
Aporphine Alkaloids From Annona acuminata
Antineoplastic Agents 78. Isolation of Palystatins 1-3 From the Indian Ocean Palythoa liscia
Isolation and Structure of 14,15-Epoxyprieurianin From the South American Tree Guarea guidona
Microbial Transformations of Natural Antitumor Agents. 20. Glucosylation of Viridi-catumtoxin
New Dihydrochalcones and Flavanones From Uvaria Angolensis
Biologically active pyrrolizidine alkaloids from the true forget-me-not, Myosotis scorpioides.
Cytotoxic agent from Senecio anonymus wood.
Cytotoxic Flavones From Centaurea urvillei
Plant anticancer agents. XII. Isolation and structure elucidation of new cytotoxic quinones from Tabebuia cassinoides.
Normaytancyprine, A Minor Antileukemic Ansa Macrolide From Putterlickia verrucosa
Biological and phytochemical investigation of Clausena excavata.
Plant Anticancer Agents. XIII. Constituents of Austrocedrus chilensis
Novel drug resistance pattern associated with the mutations K70G and M184V in human immunodeficiency virus type 1 reverse transcriptase.
Increased susceptibility to colistin in hypermutable Pseudomonas aeruginosa strains from chronic respiratory infections.
Antimicrobial susceptibilities and clinical sources of Dialister species.
Increased macrolide resistance of Mycoplasma pneumoniae in pediatric patients with community-acquired pneumonia.
Human immunodeficiency virus types 1 and 2 exhibit comparable sensitivities to Zidovudine and other nucleoside analog inhibitors in vitro.
ent-Kaurane diterpenoids from Isodon scoparius.
Preparation and anti-HIV activity of N-3 amino substituted thymidine nucleoside analogs
Glyco-S-nitrosothiols, a novel class of no donor compounds
Decomposition of FK 409, a new vasodilator: Identification of nitric oxide as a metabolite
DHPMP: a novel group I specific metabotropic glutamate receptor agonist
N-(quinuclidin-3-YL)-1,8,-naphthalimides with 5-HT3 receptor antagonist and 5-HT4 receptor agonist properties
Inhibition of farnesyl protein transferase by new farnesyl phosphonate derivatives of phenylalanine
Design, synthesis and biological activity of some tetraamines related to methoctramine and 4-DAMP
elastase inhibitors containing conformationally restricted lactams as P3-P2 dipeptide replacements
Cholestane glycosides with potent cytostatic activities on various tumor cells from Ornithogalum saundersiae bulbs
Synthesis of new building blocks for peptide nucleic acids containing monomers with variations in the backbone
Design, synthesis and antiproliferative activity of methyl 4-Iodo-1--D-ribofuranosyl-pyrazole-3-carboxylate and related compounds
Synthesis and biological evaluation of 23-oxa-, 23-thia- and 23-oxa-24-oxo-1,25-dihydroxyvitamin D3
Synthesis of a piperidinomethylthiophene derivative as H2-antagonist with inhibitory activity against Helicobacter pylori
Inhibition of calpain by peptidyl heterocycles
A benzisothiazolone class of potent, selective mechanism-based inhibitors of human leukocyte elastase
New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors
Synthesis of novel ellipticine analogues and their inhibition of Moloney leukaemia reverse transcriptase
Structure-activity relationships of double-strand RGD peptides as GPIIb/IIIa receptor antogonists
Carboxyl-promoted enhancement of selectivity for the 3 adrenergic receptor. Negative charge of the sulfonic acid BMS-187413 introduces-3 binding selectivity
Fluorescent probes for 5-HT1A receptors: Synthesis and characterization of 5-methoxy-3-[n-propyl(4-n-aminobutyl)] amino-3,4-dihydro-2H-1-benzopyran derivatives
Preparation and activities of 4-epi and 4-deoxy-4-amino analogs derived from 9-deoxo-8a-aza-8a-homoerythromycin A
Synthesis of active metabolites of indole pyrrolothiazole paf antagonists
Inhibition of matrix metalloproteinases by P1 substituted N-carboxyalkyl dipeptides
Structure-based design of an inhibitor modeled at the substrate active site of aldose reductase
Design and synthesis of new potential photoaffinity labels for mammalian squalene epoxidase
Stereospecific synthesis of chiral acyclic analogues of guanosine
Attempts to introduce chemotherapeutic nucleotides into cells: studies on the anti-HIV agent FDT
Synthesis and antitubercular screening of imidazole derivatives.
Synthesis and in vitro anticancer activity of 2,4-azolidinedione-acetic acids derivatives.
A new synthesis of caged GABA compounds for studying GABAA receptors.
Synthesis and anti-tumor activities of some new pyridines and pyrazolo[1,5-a]pyrimidines.
Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1).
Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Peptidomimetic inhibitors of p21ras farnesyltransferase: Hydrophobic functionalization leads to disruption of p21ras membrane association in whole cells
Inhibitors of human leukocyte elastase. 3.1 inhibition by tetrahydrobenzisothiazolinylmethyl aryl carboxylates
Peptidyl epoxides as inhibitors of -chymotrypsin: Remarkable change from irreversible to reversible competitive inhibitor as a consequence of the improvement of binding affinity
Imidazole and triazole substituted ether phospholipids: potent antitumor agents
Synthesis and biology of the rigidified glutamate analogue, trans-2-carboxyazetidine-3-acetic acid (t-CAA)
Synthesis and biological activity of modified enediyne chemotypes
Imidazo[4,5-b]pyridine-based AT1 / AT2 angiotensin II receptor antagonists
Synthesis and potential anxiolytic activity of 4-amino-pyrido[2,3-b]indoles
Rational design and synthesis of a novel, selective class of thrombin inhibitors: P1-argininal derivatives incorporating P3P4 quaternary lactam dipeptide surrogates
Synthesis of homochiral potassium channel openers: role of the benzopyranyl 3-hydroxyl group in cromakalim and pyridine N-oxides in determining the biological activities of enantiomers
Novel oligodeoxyribonucleotides incorporating L-related isodeoxynucleosides: Solid phase synthesis, enzymology, and CD studies
Target directed enediyne prodrugs: hER and AhR degradation by a synthetic oxo-enediyne
Synthesis and pharmacological properties of BW315c and other inotropic 2-arylimidazo[1,2-a]pyrazines
Antiviral optically pure dioxolane purine nucleosides analogues
Synthesis and antiviral activity of alkylphosphonic acid derivatives of oxetanocin-A
Inhibition of human erythrocyte calpain I by novel quinolinecarboxamides
Rhombenone: farnesyl protein transferase inhibitor from the leaves of Hedera rhombea Bean
Development of L-689,065 - the prototype of a new class of potent 5-lipoxygenase inhibitors
6N-Cinnamoyl--naltrexamine and its p-nitro derivative. High efficacy -opioid agonists with weak antagonist actions
3-Pyridines as replacements for an isoxazole ring: The antirhinoviral activity of pyridine analogues related to disoxaril
Novel C-4 paclitaxel (Taxol) analogs: potent antitumor agents
N-Hydroxyglycine derivatives as novel inhibitors of squalene synthase
Synthesis and biological activity of a novel class of cephalosporins with a oxadiazolyl hydroxypyridone moiety at C-7
Quinazolinone Biphenyl Acylsulfonamides: A potent new class of angiotensin-II receptor antagonists
Synthesis and incorporation of 2-amino acid conjugated nucleotides into ribozymes
Muscarinic receptor probes based on amine congeners of pirenzepine and telenzepine
A novel series of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor
Bromobenzofurans : a new class of potent, non-peptide antagonists of angiotensin II
Structural requirements for biological activity of the marine alkaloid ascididemin
Structural influences of styryl-based inhibitors on epidermal growth factor receptor and p56lck tyrosine-specific protein kinases.
Dermorphin sequence with high -afinity by fixing the phe sidechain to trans at 1
Structure-activity-relationship pertaining to the north-west region of the kappa opioid agonist, U-50,488
Triply-convergent synthesis of two sets of homochiral cyclopent[a]indene carbacyclin analogs
Design, synthesis, and evaluation of orally active fibrinogen inhibitors
On the microbial biogeneration of (R) -jasmolactone
Indolocarbazoles.3. Synthesis of novel aza analogs of staurosporine and K 252a as PKC inhibitors.
Design, synthesis, and pharmacological evaluation of dual histamine H2 and gastrin receptor antagonists
Conversion of the phytoestrogen coumestrol into a selective estrogen receptor modulator (SERM) by attachment of an amine-containing sidechain
2-Deoxyadenylyl-(35)-isodideoxyadenosine, a unique dinucleotide: Synthesis, enzymology, and conformational studies
Inhibitors of leukotriene B4. Synthesis and sar of new -enaminoester open-chain analogues of zeneca ZD2138
Synthesis and biological evaluation of piperazinyl carbamates and ureas as fatty acid amide hydrolase (FAAH) and transient receptor potential (TRP) channel dual ligands.
Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.
Synthesis, stereochemistry and antimicrobial studies of novel oxime ethers of aza/diazabicycles.
Synthesis and biological evaluation of dehydroabietic acid derivatives.
Crotonkinensins A and B, diterpenoids from the Vietnamese medicinal plant Croton tonkinensis.
Lamiridosins, hepatitis C virus entry inhibitors from Lamium album.
Pyrrolidinones from the ascomycete fungus Albonectria rigidiuscula.
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
Phosphoinositide-3-kinase (PI3K) inhibitors: identification of new scaffolds using virtual screening.
Design and synthesis of substituted nicotinamides as inhibitors of soluble epoxide hydrolase.
Synthesis and biological activity of novel oxazolidinones.
Antitumor agents 269. Non-aromatic ring-A neotanshinlactone analog, TNO, as a new class of potent antitumor agents.
A facile synthesis and biological activity of novel tetrahydrobenzo[4',5']thieno[3',2':5,6]pyrido[4,3-d]pyrimidin-4(3H)-ones.
Discovery of pyrazol-3-ylamino pyrazines as novel JAK2 inhibitors.
COX, LOX and platelet aggregation inhibitory properties of Lauraceae neolignans.
Targeted delivery of paclitaxel to tumor cells: synthesis and in vitro evaluation.
Heterocyclic fused pyridone carboxylic acid M(1) positive allosteric modulators.
Identification of very potent inhibitor of human aminopeptidase N (CD13).
'Click chemistry' synthesis of a library of 1,2,3-triazole-substituted galactose derivatives and their evaluation against Trypanosoma cruzi and its cell surface trans-sialidase.
Discovery of tertiary sulfonamides as potent liver X receptor antagonists.
Amide-based inhibitors of p38alpha MAP kinase. Part 1: discovery of novel N-pyridyl amide lead molecules.
gamma-Lactams as glycinamide replacements in cyclohexane-based CC chemokine receptor 2 (CCR2) antagonists.
Tetrahydropyridine derivatives with inhibitory activity on the production of proinflammatory cytokines: part 2.
Swertifrancheside, an HIV-reverse transcriptase inhibitor and the first flavone-xanthone dimer, from Swertia franchetiana.
Polypropionates from the Mediterranean Mollusk Elysia timida
Insect Inhibitory Steroidal Saccharide Esters from Physalis peruviana
beta-Carbolines from the blue-green alga Dichothrix baueriana.
Further Chemical Studies of Mediterranean and Atlantic Hypselodoris Nudibranchs: A New Furanosesquiterpenoid from Hypsdodoris webbi
Biological activity of some coumarins from Sri Lankan Rutaceae.
Isolation of antirhinoviral sesquiterpenes from ginger (Zingiber officinale).
Synthesis and evaluation of alkoxy-phenylamides and alkoxy-phenylimidazoles as potent sphingosine-1-phosphate receptor subtype-1 agonists.
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of Cyclin D1-CDK4: synthesis, biological evaluation, and structure-activity relationships.
Anticancer and antimalarial efficacy and safety of artemisinin-derived trioxane dimers in rodents.
Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.
Studies on pyrrolopyrimidines as selective inhibitors of multidrug-resistance-associated protein in multidrug resistance.
Structure-activity study of the ORL1 antagonist Ac-Arg-D-Cha-Qaa-D-Arg-D-p-ClPhe-NH2.
2-aminothiazole-derived opioids. Bioisosteric replacement of phenols.
Orally bioavailable competitive CCR5 antagonists.
Sultam hydroxamates as novel matrix metalloproteinase inhibitors.
Vanilloid receptor TRPV1 antagonists as the next generation of painkillers. Are we putting the cart before the horse?
Triacylglycerols based on 2-(N-tert-butoxycarbonylamino)oleic acid are potent inhibitors of pancreatic lipase.
7-Alkoxy-4-phenylamino-3-quinolinecar-bonitriles as dual inhibitors of Src and Abl kinases.
A new lead compound for abscisic acid biosynthesis inhibitors targeting 9-cis-epoxycarotenoid dioxygenase.
In vitro SAR of (5-(2H)-isoxazolonyl) ureas, potent inhibitors of hormone-sensitive lipase.
Discovery of bicyclic thymidine analogues as selective and high-affinity inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.
Inhibition of HSV-1 protease by benzoxazinones
Morpholinoalkylindenes as antinociceptive agents: Novel cannabinoid receptor agonists
Synthesis, evaluation and Tc-99m complexation of a hydrazinonicotinyl conjugate of a GP IIb/IIIa antagonist cyclic peptide for the detection of deep vein thrombosis
Xanthene derived potent nonpeptidic inhibitors of recombinant human calpain I
3,4-diarylpyrazoles: Potent and selective inhibitors of cyclooxygenase-2
Balanced AT1 and AT2 angiotensin II antagonists. III. potent and orally active 5--ketosulfoxide imidazolyl biphenyl sulfonylureas
Synthesis and evaluation of pyrazolo[3,4-b]quinoline ribofuranosides and their derivatives as inhibitors of oncogenic Ras
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 7. pyridinylalkyl-substituted arylsulfonylamino arylalkanoic acids.
3-Acetoxy-2,2-bi-1H-indol as a novel inhibitor of ATP binding to DnaA, the protein initiating chromosomal replication in escherichia coli
Anti-pneumocystis activity of bis-amidoximes and bis-o-alkylamidoximes prodrugs
The synthesis of heterosubstituted benzimidazole derivatives with potent angiotensin II antagonist activity
Conformationally constrained analogues of DAG.7. Interaction of a medium-size -lactone with protein kinase C (PK-C)_
Characterization of the in vitro oxidative metabolites of the COX-2 selective inhibitor L-766,112
Oxa-prostanoid analogs. Identification of an orally effective, dual thromboxane receptor antagonist /thromboxane synthase inhibitor
Dihydropyrimidine calcium channel blockers 51: bicyclic dihydropyrimidines as potent mimics of dihydropyridines
UK-73,093: A non-peptide neurotensin receptor antagonist
Oxiranes with quinoline substitution : Stereoselective synthesis and antiviral activity
Biaryl substituted alkylboronate esters as thrombin inhibitors
Mapping the melatonin receptor. 1. the 5-methoxyl group of melatonin is not an essential requirement for biological activity
Rearrangement of unsymmetrical azetidinone disulfides to 2-(heterocyclylthiomethyl)penams, a synthetic approach to new -lactamase inhibitors
The synthesis and evaluation of diacylglycerol analogues as potential second-messenger antagonists
Modified thrombin receptor-agonist peptide ligands. Synthesis and conformational analysis of analogs of the N-terminal tripeptide region
Novel cyclohexyl amides as potent and selective D3 dopamine receptor ligands
Application of the trimethyl lock1 to Ganciclovir, a pro-prodrug with increased oral bioavailability
Biarylcarboxamide inhibitors of phosphodiesterase IV and tumor necrosis factor-
Synthesis of UB-165: A novel nicotinic ligand and anatoxin-a/epibatidine hybrid
A new structural analogue antagonist of peptido-leukotrienes. The discovery of bay x7195
Enantioselective reduction of ethyl 3-methyl-2-oxobutanoate by an enzymatic system from callus of catharanthus roseus
Artemisinin derivatives with 12-aniline substitution: Synthesis and antimalarial activity
An acid-cleavable linker stable at neutral pH that releases doxorubicin at lysosomal pH
Inhibitory activities of herpes simplex viruses type 1 and 2 and human cytomegalovirus by stereoisomers of 2-deoxy-3-oxa-5(E)-(2-bromovinyl)uridines and their 4-thio analogues.
Two novel amino acid derivatives containing side-chain thioamides for the synthesis of photoactivatable peptides
Non thiazolidinedione antihyperglycaemic agents. 1: -Heteroatom substituted -phenylpropanoic acids
Total synthesis of an optically active 8-carba-physostigmine analog: a potent acetylcholinesterase inhibitor
Design and synthesis of new hypocholesterolemic organosilanes with antioxidant properties
Simplified analogs of himbacine displaying potent binding affinity for muscarinic receptors
Pyridine and piperidine derivatives as inhibitors of dihydrodipicolinic acid synthase, a key enzyme in the diaminopimelate pathway to l-lysine
Nonpeptide glycoprotein IIb/IIIa inhibitors: 18. Indole alpha-sulfonamide acids are potent inhibitors of platelet aggregation
Benzopyran sulfoxide derivatives as New potassium channel activator
Stereoselective synthesis of novel analogues of 2-deoxy- and 2,3-dideoxynucleosides with potential antiviral activity
Synthesis of sialic acid-lipid conjugates and their neuritogenic effects on N1E.115 neuroblastoma cells
Arylacetamide kappa-selective opioid ligands
Biological evaluation of two potent inhibitors of Trypanosoma cruzi epimastigotes against the intracellular form of the parasite
Cephem sulfones as inactivators of human leukocyte elastase. II. Keto-enol tautomerish in cephem-4-ketones.
New TXA2/PGH2 receptor antagonists based on the carbacyclin skeleton
Diphenylmethyl ethers: synthesis and histamine H3-receptor antagonist in vitro and in vivo activity
Preparation and Properties of a fibrinogen receptor antagonist containing the Arg-Gly-Asp sequence and nitroxide radicals
Thionation of an antitumour cyclic pentapeptide, astin B, from Aster tataricus
Non-glycosidic/non-aminoalkyl-substituted indolocarbazoles as inhibitors of protein kinase C
Cyclic homopentapeptides 3. Synthetic modifications to the capreomycins and tuberactinomycins: Compounds with activity against methicillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci
Convergent syntheses and cytostatic properties of 2-chloro-2-deoxy-2-fluoroadenosine and its N7-isomer
Synthesis of cyclohexyl analogs of restricticin
Benzopyran-4-carboxamide K+ channel openers
Cytotoxic activity of neo-clerodane diterpenoids
Synthesis and antibacterial activity of some C-3-lactonyl substituted cephalosporins
New dipeptide isosteres useful for the inhibition of HIV-1 protease
The effect of pH on the solution structure of 1-pyrroline-2-carboxylic acid as revealed by NMR and electrospray mass spectroscopy.
Conformationally-restricted analogs of TXA2 antagonist SQ 33,961: Receptor binding conformation of the carboxyl sidechain
Aryl phosphate derivates of AZT inhibit HIV replication in cells where the nucleoside is poorly active
Design and synthesis of 10-oxo derivative of N-cyclopropylmethyl ()-6-acetylthiodihydro-normorphine, a potentially -selective opioid receptor ligand
Development of new non-peptide GPIIb/IIIa antagonists, NSL-95315 and NSL-95317, isosteres of NSL-95300
1,2-diaminobenzimidazoles : Selective inhibitors of nitric oxide synthase derived from aminoguanidine
Synthesis and inhibitory activity of optically active 2-benzyl-3-mercaptopropanoic acid against carboxypeptidase A
Synthesis and anti-HIV activity of dibenzylbutyrolactone lignans
Structure-activity relationship of novel tallimustine derivatives: synthesis and antitumor activity
Synthesis of new 3,4-disubstituted pyrrolidines as thromboxane A2/prostaglandin H2 (TP) receptor antagonists
Aromatic guanyl hydrazones: Synthesis, structural studies and in vitro activity against Trypanosoma cruzi
Palladium-catalyzed synthesis of C3-substituted 3-deoxymorphines.
7-Oxa[2.2.1]bicycloheptane-2,3-dicarboxylic acid derivatives as phosphatase inhibitors
THE ROLE OF ARGININE IN THE BINDING OF LTD4 ANTAGONISTS TO cysLT1 RECEPTORS OF GUINEA PIG LUNG
Synthesis of in vivo potent antimalarial 1,2,4-trioxanes
Probing the importance of the second chloroethyl arm of a benzoic acid mustard derivative of an imidazole-containing analogue of distamycin
6-Bromo-3-nitroflavone, a new high affinity benzodiazepine receptor agonist recognizes two populations of cerebral cortical binding sites
Probing the binding site of the penicillin side-chain based on the tipper-strominger hypothesis
Unsymmetrically substituted guanidines as potent histamine H3-receptor antagonists
2-Heterocyclic indole-3-sulfones as inhibitors of HIV-1 reverse transcriptase
Acidic phenols: a new class of potent nonpeptide angiotensin II receptor antagonists
Unusual cytotoxicities of 5-(acylethynyl)-1-(2-hydroxyethoxy)methyluracils
The discovery of novel openers of Ca2+-dependent large-conductance potassium channels: Pharmacophore search and physiological evaluation of flavonoids
A novel prodrug of an impermeant inhibitor of 3-deoxy-D-manno-2-octulosonate cytidylyltransferase has antibacterial activity.
Exploration of phenyl-spaced 2-amino-(5-9)-phosphonoalkanoic acids as competitive N-methyl-D-aspartic acid antagonists.
Retinobenzoic acids. 2. Structure-activity relationships of chalcone-4-carboxylic acids and flavone-4'-carboxylic acids.
Cyclohexane diester analogues of phorbol ester as potential activators of protein kinase C.
Synthesis and muscarinic activities of 1,2,4-thiadiazoles.
Hymenopsins A and B and a macrophorin analogue from a fungicolous Hymenopsis sp.
Surface plasmon resonance-based detection of ladder-shaped polyethers by inhibition detection method.
Isoprenylated chromone derivatives from the plant endophytic fungus Pestalotiopsis fici.
Unusual cellular uptake of cytotoxic 4-hydroxymethyl-3-aminoacridine.
New alpha-amino phosphonic acid derivatives of vinblastine: chemistry and antitumor activity.
Benzazepinone calcium channel blockers. 2. Structure-activity and drug metabolism studies leading to potent antihypertensive agents. Comparison with benzothiazepinones.
Novel naphthalenic ligands with high affinity for the melatonin receptor.
Novel sulfonamides as potential, systemically active antitumor agents.
Synthesis and antihistaminic activity of some thiazolidin-4-ones.
Omega-[(omega-arylalkyl)aryl]alkanoic acids: a new class of specific LTA4 hydrolase inhibitors.
Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
Novel cAMP PDE III inhibitors: 1,6-naphthyridin-2(1H)-ones.
Synthesis and properties of some peptide analogues of actinomycin D.
Benzyloxazolidine-2,4-diones as potent hypoglycemic agents.
Novel time-dependent inhibitors of human placental aromatase.
Synthesis and muscarinic cholinergic receptor affinities of 3-quinuclidinyl alpha-(alkoxyalkyl)-alpha-aryl-alpha-hydroxyacetates.
Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives.
Allosteric inhibitors of hepatitis C virus NS5B polymerase thumb domain site II: structure-based design and synthesis of new templates.
Recent advances in the identification of gamma-secretase inhibitors to clinically test the Abeta oligomer hypothesis of Alzheimer's disease.
Structure-activity relationships for substrate-based inhibitors of human complement factor B.
Structure--activity relationships of polymyxin antibiotics.
Selective p38alpha inhibitors clinically evaluated for the treatment of chronic inflammatory disorders.
Through the "gatekeeper door": exploiting the active kinase conformation.
Small molecule JNK (c-Jun N-terminal kinase) inhibitors.
Reduction of hERG inhibitory activity in the 4-piperidinyl urea series of H3 antagonists.
Identification of pyridazino[4,5-b]indolizines as selective PDE4B inhibitors.
Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffold.
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Novel N-substituted benzimidazole CXCR4 antagonists as potential anti-HIV agents.
A virtual screening hit reveals new possibilities for developing group III metabotropic glutamate receptor agonists.
Bioactive acridone alkaloids from Swinglea glutinosa.
Suillusin, a unique benzofuran from the mushroom Suillus granulatus.
New multiflorane-type triterpenoid acids from Sandoricum indicum.
Polyacetylene carboxylic acids from Mitrephora celebica.
New halogenated marine prostanoids with cytotoxic activity from the Okinawan soft coral Clavularia viridis.
Macharistol, a new cytotoxic cinnamylphenol from the stems of Machaerium aristulatum.
Cytotoxic polyacetylenic alcohols from the marine sponge Petrosia species.
Design and synthesis of a potent and selective peptidomimetic inhibitor of caspase-3.
Stereochemical analysis of (hydroxyethyl)urea peptidomimetic inhibitors of gamma-secretase.
Discovery of tetralin carboxamide growth hormone secretagogue receptor antagonists via scaffold manipulation.
Design, synthesis, and pharmacological characterization of novel, potent NMDA receptor antagonists.
Synthesis of benzoylpyrimidines as antagonists of the corticotropin-releasing factor-1 receptor.
Two novel immunosuppressive pregnane glycosides from the roots of Stephanotis mucronata.
Exploring alternative Zn-binding groups in the design of HDAC inhibitors: squaric acid, N-hydroxyurea, and oxazoline analogues of SAHA.
Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Synthesis and anti-tumor evaluation of new trisulfide derivatives.
A strategy for the design of selective RNA binding agents. Preparation and RRE RNA binding affinities of a neomycin-peptide nucleic acid heteroconjugate library.
8-(1-Naphthalen-2-yl-vinyl)-6,7,10-trioxaspiro (4.5) decane, a new 1,2,4-trioxane effective against rodent and simian malaria.
Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation.
Guiding farnesyltransferase inhibitors from an ECLiPS library to the catalytic zinc.
A QSAR model for in silico screening of MAO-A inhibitors. Prediction, synthesis, and biological assay of novel coumarins.
Application of fragment screening and fragment linking to the discovery of novel thrombin inhibitors.
Side-chain modified analogues of histaprodifen: asymmetric synthesis and histamine H1-receptor activity.
Synthesis and cytotoxic evaluation of new derivatives of the marine alkaloid variolin B.
Aromatic thiazole derivatives: structurally novel and selective serotonin-3 receptor antagonists.
Synthesis and antimicrobial and cytotoxic activities of pyrrole-containing analogues of trichostatin A.
High potency dipeptide sweeteners. 1. L-aspartyl-D-phenylglycine esters.
(S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: a putative 5-HT1A-receptor antagonist.
Quinolone antibacterial agents substituted at the 7-position with spiroamines. Synthesis and structure-activity relationships.
Inhibition of ornithine decarboxylase by the isomers of 1,4-dimethylputrescine.
Substituted 2-(aminomethyl)piperidines: a novel class of selective protein kinase C inhibitors.
Novel pyrrolo[2,3-d]pyrimidine antifolates: synthesis and antitumor activities.
Potential anticancer agents XXXII. Hydroquinone from Ipomopsis aggregata.
Trichothecenes, 1: The synthesis of 4-deoxyverrucarol from verrucarol and diacetoxyscirpenol.
Structure and conformation of two new dolabellane-based diterpenes from Dictyota sp.
Germination and Growth Inhibitory Sesquiterpenes from Iva axillaris Seeds
Lariciresinol derivatives from Turrea nilotica and Monechma ciliatum.
Biological Activities of Asterosaponins With Special Reference to Structure-Activity Relationships
Atractyloside, toxic compound from Wedelia glauca.
Hippamine, a Minor Alkaloid From Sternbergia lutea
Benzoxazolinone, 2,4-Dihydroxy-1,4-benzoxazin-3-one, and Its Glucoside from Acanthus mollis Seeds Inhibit Velvetleaf Germination and Growth
Dictyol H, a New Tricyclic Diterpenoid from the Brown Seaweed Dictyota dentata
Alkaloids and coumarins of Casimiroa edulis.
Constituents of Solanum dasyphyllum Fruit
Methyl -Orcinolcarboxylate and Depsides from Parmelia furfuracea
The Sesquiterpenes of Lactarius vellereus and Their Role in a Proposed Chemical Defense System
13-Deoxycarminomycin, a new biosynthetic anthracycline.
Cucurbitacin B and isocucurbitacin B: cytotoxic components of Helicteres isora.
Flavonoids from the Wood of Salix caprea as Inhibitors of Wood-Destroying Fungi
Effects of Sesquiterpene Lactones on Development of Aedes atropalpus and Relation to Partition Coefficient
Insect Antifeedant Activity of Four Prieurianin-Type Limonoids
Plant anticancer agents, XLI. Cardiac glycosides from Streblus asper.
Caparratriene, an active sesquiterpene hydrocarbon from Ocotea caparrapi.
Cytotoxic oxygenated desmosterols of the red alga Galaxaura marginata.
Amarogentin, a naturally occurring secoiridoid glycoside and a newly recognized inhibitor of topoisomerase I from Leishmania donovani.
Halicylindramides D and E, antifungal peptides from the marine sponge Halichondria cylindrata.
New Naphthalenyl Glucosides from the Roots of Juglans mandshurica
Efficient synthesis and biological evaluation of two modafinil analogues.
Cholecystokinin antagonists: (R)-tryptophan-based hybrid antagonists of high affinity and selectivity for CCK-A receptors.
The renewed potential for folate antagonists in contemporary cancer chemotherapy.
Hydrophobicity parameters for platinum complexes.
Synthesis and quantitative structure-activity relationship analysis of 2-(aryl or heteroaryl)quinolin-4-amines, a new class of anti-HIV-1 agents.
Trans-esterification reactions yield novel masked phosphate derivatives of the anti-cancer agent araC
Synthesis of substrate-based inhibitors of HMG CoA reductase (II).
Novel derivatives of pyridylbenzo[b]thiophene-2-carboxamides and benzo[b]thieno[2,3-c]naphthyridin-2-ones: minor structural variations provoke major differences of antitumor action mechanisms.
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part II).
Targeting the calcineurin pathway enhances ergosterol biosynthesis inhibitors against Trichophyton mentagrophytes in vitro and in a human skin infection model.
Application of phosphonyl carbanions to highly regioselective synthesis of some diazaphospholes and pyrazolinyl phosphonates.
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
Hansch analysis of veratric acid derivatives as antimicrobial agents.
Cytotoxic, antioxidant activities and structure activity relationship of some newly synthesized terpenoidal oxaliplatin analogs.
Discovery of benzothiazole derivatives as efficacious and enterocyte-specific MTP inhibitors.
Investigations of SCIO-469-like compounds for the inhibition of p38 MAP kinase.
Beta-peptides with improved affinity for hDM2 and hDMX.
[18F]FEAC and [18F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain.
Novel fatty acid synthase (FAS) inhibitors: design, synthesis, biological evaluation, and molecular docking studies.
Synthesis of protein tyrosine phosphatase 1B inhibitors: model validation and docking studies.
New axane and oppositane sesquiterpenes from Teclea nobilis.
Selective inhibition of porcine endogenous retrovirus replication in human cells by acyclic nucleoside phosphonates.
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.
Identification of NVP-TAE684, a potent, selective, and efficacious inhibitor of NPM-ALK.
Loss of huntingtin function complemented by small molecules acting as repressor element 1/neuron restrictive silencer element silencer modulators.
Molecular mechanism of action of monocyclam versus bicyclam non-peptide antagonists in the CXCR4 chemokine receptor.
Stelliferin riboside, a triterpene monosaccharide isolated from the Fijian sponge Geodia globostellifera.
Remarkable DNA binding affinity and potential anticancer activity of pyrrolo[2,1-c][1,4]benzodiazepine-naphthalimide conjugates linked through piperazine side-armed alkane spacers.
Prenylated dihydrochalcones from Boronia bipinnata that inhibit the malarial parasite enzyme target hemoglobinase II.
Aminoquinazolines as TRPV1 antagonists: modulation of drug-like properties through the exploration of 2-position substitution.
Discovery of piperidine carboxamide TRPV1 antagonists.
Synthesis, stereochemical identification, and selective inhibitory activity against human monoamine oxidase-B of 2-methylcyclohexylidene-(4-arylthiazol-2-yl)hydrazones.
New NSAIDs-NO hybrid molecules with antiproliferative properties on human prostatic cancer cell lines.
Structure-activity relationship studies of permeability modulating peptide AT-1002.
4-(1H-indazol-5-yl)-6-phenylpyrimidin-2(1H)-one analogs as potent CDC7 inhibitors.
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.
Total synthesis and biological evaluation of 22-hydroxyacuminatine.
Pharmacophore-based virtual screening: the discovery of novel methionyl-tRNA synthetase inhibitors.
Homobivalent quinazolinimines as novel nanomolar inhibitors of cholinesterases with dirigible selectivity toward butyrylcholinesterase.
Newly discovered orally active pure antiestrogens.
3-Aryl-4-hydroxyquinolin-2(1H)-one derivatives as type I fatty acid synthase inhibitors.
Small molecule inhibitors of IgE synthesis.
Synthesis of 3H-spiro[benzofuran-2,1'-cyclohexane] derivatives from naturally occurring filifolinol and their classical complement pathway inhibitory activity.
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Antiproliferative and apoptosis inducing properties of pyrano[3,2-c]pyridones accessible by a one-step multicomponent synthesis.
R-(-)-N-alkyl-11-hydroxy-10-hydroxymethyl- and 10-methyl-aporphines as 5-HT1A receptor ligands.
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists.
SAR and X-ray structures of enantiopure 1,2-cis-(1R,2S)-cyclopentyldiamine and cyclohexyldiamine derivatives as inhibitors of coagulation Factor Xa.
5-Arylidene-2,4-thiazolidinediones as inhibitors of protein tyrosine phosphatases.
Synthesis and evaluation of human T cell stimulating activity of an alpha-sulfatide analogue.
Synthesis and antiproliferative activity of clausine E, mukonine, and koenoline bioisosteres.
The synthesis of 18beta-glycyrrhetinic acid derivatives which have increased antiproliferative and apoptotic effects in leukemia cells.
Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN).
Isoflavonoid glycosides from the roots of Baphia bancoensis.
Sesquiterpenoids and phenylpropanoids from Chloranthus serratus.
Structural and mechanistic studies of mofegiline inhibition of recombinant human monoamine oxidase B.
5-(1-Acetoxyvinyl)-cycloSaligenyl-2',3'-dideoxy-2',3'- didehydrothymidine monophosphates, a second type of new, enzymatically activated cycloSaligenyl pronucleotides.
Identification of aquaporin 4 inhibitors using in vitro and in silico methods.
Synthesis of macrocyclic trypanosomal cysteine protease inhibitors.
Melanin synthesis inhibitors from Lespedeza cyrtobotrya.
Bioassay-guided isolation of xanthones and polycyclic prenylated acylphloroglucinols from Garcinia oblongifolia.
Cytotoxic spirostane-type saponins from the roots of Chlorophytum borivilianum.
Schisanwilsonenes A-C, anti-HBV Carotane sesquiterpenoids from the fruits of Schisandra wilsoniana.
Tetranortriterpenoids from the Leaves of Cipadessa cinerascens.
Quaternary ammonium N,N-dichloroamines as topical, antimicrobial agents.
Substrate based peptide aldehyde inhibits bacterial type I signal peptidase.
Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.
Triazinediones as prokineticin 1 receptor antagonists. Part 1: SAR, synthesis and biological evaluation.
Structure-activity relationships of diverse annonaceous acetogenins against human tumor cells.
Discovery of oxazolo[4,5-b]pyridines and related heterocyclic analogs as novel SIRT1 activators.
Optimisation of a series of potent, selective and orally bioavailable GlyT1 inhibitors.
Aziridine alkaloids as potential therapeutic agents.
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.
Synthesis, characterization, and anti-melanoma activity of tetra-O-substituted analogs of nordihydroguaiaretic acid.
Synthesis and biological evaluation of 1,2,4-trisubstituted imidazoles and 1,3,5-trisubstituted pyrazoles as inhibitors of transforming growth factor beta type 1 receptor (ALK5).
Novel and potent small-molecule urotensin II receptor agonists.
Synthesis, physicochemical properties and antimicrobial activity of some new benzimidazole derivatives.
Inhibition of human vascular NADPH oxidase by apocynin derived oligophenols.
Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening.
Nucleoside-amino acid conjugates: An alternative route to the design of ribonuclease A inhibitors.
Synthesis and evaluation of a novel 2-azabicyclo[2.2.2]octane class of long chain fatty acid elongase 6 (ELOVL6) inhibitors.
Synthesis and properties of nucleoside derivatives acylated by chemically stable 2-(trimethylsilyl)benzoyl group.
Synthesis and biological activities of thio-avarol derivatives.
Macaflavanones A-G, prenylated flavanones from the leaves of Macaranga tanarius.
Alkamides from the fruits of Piper longum and Piper nigrum displaying potent cell adhesion inhibition.
Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable.
Heme activates artemisinin more efficiently than hemin, inorganic iron, or hemoglobin.
Synthesis and cellular effects of cycloterpenals: cyclohexadienal-based activators of neurite outgrowth.
Reductive heme-dependent activation of the n-oxide prodrug AQ4N by nitric oxide synthase.
Cembrane diterpenes from the gorgonian Leptogorgia laxa.
Natural products chemistry and taxonomy of the marine cyanobacterium Blennothrix cantharidosmum.
Frajunolides E-K, briarane diterpenes from Junceella fragilis.
In silico screening of HIV-1 non-nucleoside reverse transcriptase and protease inhibitors.
8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
A bivalent ligand (KMN-21) antagonist for mu/kappa heterodimeric opioid receptors.
New small molecule inhibitors of hepatitis C virus.
Structural studies of pterin-based inhibitors of dihydropteroate synthase.
Dihydroxyphenylisoindoline amides as orally bioavailable inhibitors of the heat shock protein 90 (hsp90) molecular chaperone.
Structure-based design of pteridine reductase inhibitors targeting African sleeping sickness and the leishmaniases.
Structure-based design of TACE selective inhibitors: manipulations in the S1'-S3' pocket.
Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
Rapid synthesis of VX-745: p38 MAP kinase inhibition in Werner syndrome cells.
Membrane permeable esterase-activated fluorescent imaging probe.
Structure-activity relationships of 3,4-dihydro-1H-quinazolin-2-one derivatives as potential CDK5 inhibitors.
Aaptamines as sortase A inhibitors from the tropical sponge Aaptos aaptos.
1,2,4-benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity.
New Alkaloids from Haplophyllum tuberculatum
Structures of four new triterpenoid oligoglycosides: DS-penaustrosides A, B, C, and D from the sea cucumber Pentacta australis.
Nakahalene and Cytotoxic principles of Formosan Rhamnus Species
New Pentacyclic Compounds from the Okinawan Marine Sponge Xestospongia sapra
11-oxoaerothionin: a cytotoxic antitumor bromotyrosine-derived alkaloid from the Caribbean marine sponge Aplysina lacunosa.
Aflavarin and -Aflatrem: New Anti-Insectan Metabolites from the Sclerotia of Aspergillus flavus
Brominated polyacetylenic acids from the marine sponge Xestospongia muta: inhibitors of HIV protease.
Sarcochromenol sulfates A-C and sarcohydroquinone sulfates A-C, new natural products from the sponge Sarcotragus spinulosus.
Linear diterpenes from the Caribbean sponge Myrmekioderma styx.
Terpenoids and Alkaloids from Esenbeckia belizencis. Spontaneous Oxidation of Furoquinoline Alkaloids
Two new alkaloids from Xestospongia sp., a New Caledonian sponge.
Synthesis and antiprotozoal activities of simplified analogs of naphthylisoquinoline alkaloids.
Carbamate prodrugs of N-alkylfuramidines.
New stereoselective titanium reductive amination synthesis of 3-amino and polyaminosterol derivatives possessing antimicrobial activities.
SAR and QSAR studies: modelling of new DAPY derivatives.
Bioactive peroxides as potential therapeutic agents.
Synthesis of analogs of forodesine HCl, a human purine nucleoside phosphorylase inhibitor-Part I.
Synthesis and biological evaluation of penem inhibitors of bacterial signal peptidase.
Synthesis and evaluation of an acyl-chain unsaturated analog of the Th2 biasing, immunostimulatory glycolipid, OCH.
Identification of a beta3-peptide HIV fusion inhibitor with improved potency in live cells.
Synthesis, potency, and in vivo evaluation of 2-piperazin-1-ylquinoline analogues as dual serotonin reuptake inhibitors and serotonin 5-HT1A receptor antagonists.
Biologically active cannabinoids from high-potency Cannabis sativa.
(Nitrooxyacyloxy)methyl esters of aspirin as novel nitric oxide releasing aspirins.
Okundoperoxide, a bicyclic cyclofarnesylsesquiterpene endoperoxide from Scleria striatinux with antiplasmodial activity.
Tetrahydrofuran acetogenins from Laurencia glandulifera.
Dietary derived sesquiterpenes from Phyllodesmium lizardensis.
Evaluation of tea polyphenols as anti-HIV agents
Structure-activity relationships of anti-HIV-1 N-alkoxy- and N-allyloxy-benzimidazoles
Structural analogues of the michellamine anti-HIV agents. Importance of the tetrahydroisoquinoline rings for biological activity
Combretatroponeshybrids of combretastatin and colchicine. Synthesis and biochemical evaluation
3-Lithioquinuclidin-2-ene: A novel intermediate for the synthesis of muscarinic agonists and antagonists
Application of the multipin peptide synthesis technique for peptide receptor binding studies: Substance P as A model system
Synthesis of inhibitors of -1,3-fucosyltransferase
Potent -ketocarbonyl and boronic ester derived inhibitors of proteasome
Chloramphenicol: High dilution FT-IR evidence for an intramolecular hydrogen bond
Design, synthesis and X-ray crystallographic studies of novel FKBP-12 ligands
Pharmacological profile and chemical synthesis of SR 48968, a non-peptide antagonist of the neurokinin A (NK2) receptor
The synthesis and CCK receptor affinities of selected carboyxlic acid mimics of CI-988 - a potent and selective CCK-B antagonist
N,N-disubstituted benzopyran-4-(N-cyano)carboxamidines, cromakalim analogs with selective activity for guinea pig trachealis
Synthesis of new amide-linked N-hydroxyurea 5-lipoxygenase inhibitors by an intramolecular oxygen to nitrogen acyl transfer
The first protoberberine alkaloid analogue with in vivo antimalarial activity
Synthesis of (+)-biotin derivatives as HIV-1 protease inhibitors
Synthesis of thiophenol derivatives as inhibitors of human collagenase
One-step synthesis of radioiodinated biotin derivatives
Synthesis and -lactamase inhibition of anacardic acids and their analogues
Molecular design of novel PGI2 agonists without PG skeleton. II
A series of conformationally and sterically constrained analogs of N-phenyl-N-aralkylurea ACAT inhibitors
Novel 2,5-disubstituted-1H-pyrroles with high affinity for the dopamine D3 receptor
(E) and (Z)-3-Styrylpiperidines as sigma ligands
Double-headed molecules based on linear or angular psoralen and -methylene--butyrolactone: a search for non-phototoxic potential antiproliferative compounds
Phenyl pyrrolidine analogues as potent nicotinic acetylcholine receptor (nAChR) ligands
Synthesis and bronchospasmolytic properties of some pyridazinone derivatives
Enzymatic asymmetric synthesis of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid, a potent, selective and competitive NMDA antagonist
The prooligonucleotide approach. I: Esterase-mediated reversibility of dithymidine S-alkyl-phosphorothiolates to dithymidine phosphorothioates
The synthesis of 8,8-disubstituted tricyclic analogs of artemisinin
Synthesis and radioprotective effects of new phosphorothioate esters of WR-2721, WR-3689 and WR-151327
Silicon-mediated inactivation of semicarbazide-sensitive amine oxidase
Substituted N,N-diphenyl ureas as potent inhibitors of acyl-CoA:Cholesterol acyltransferase (ACAT)
Inhibition of interleukin-1 converting enzyme by N-Acyl-aspartic acid ketones
Spiro-piperidine non-peptide neurokinin-1 receptor antagonists
Solid phase synthesis of phosphinic acid endothelin converting enzyme inhibitors
Acyclic nucleoside triphosphate analogs as terminators in biocatalytic DNA replication
Novel peptidomimetics: inhibitors of substance P endopeptidase
Quaternised renzapride as a potent and selective 5-HT4 receptor agonist
PIPERIDINE CARBOXYLIC ACID DERIVATIVES AS SIALYL LEWIS X MIMETICS
Design, Synthesis and Pharmacology of Cannabimimetic Indoles
Polyhydroxylated 3-(N-phenyl) carbamoyl-2-iminochromene derivatives as potent inhibitors of tyrosine kinase p60c-src
Interphenylene phenyl oxazoles: novel, potent thromboxane receptor antagonists
Synthesis of the pyrimidine analog of 4,5,6,7-tetrahydroimidazo[4,5,1-jk][1,4]benzodiazepin-2(1H)one (TIBO) potential for HIV-1 inhibition
Pyrrolooctahydroisoquinolines as potent and selective opioid receptor ligands: SAR analysis and docking studies
(cis)-3-methyl-1,5-benzothiazepine-4-ones: potent analogs of the calcium channel blocker diltiazen
N-(1-phenyl-2-benzimidazolyl)-N-phenylurea derivatives as potent in hibitors of acylcoa:cholesterol acyltransferase (ACAT)
Dual metalloprotease inhibitors.v. Utilization of bicyclic azepinonethiazolidines and azepinonetetrahydrothiazines in constrained peptidomimetics of mercaptoacyl dipeptides
Asymmetric synthesis of enantiomerically pure 4-fluoroalkyl-2,3-dideoxy nucleosides
Synthesis and preliminary pharmacological evaluation of 2-benzyloxy substituted aryl ketones as 5-HT4 receptor antagonists
Probing the P3 pocket of stromelysin with piperazic acid analogs
Synthesis and evaluation of a -lactam-containing dipeptide analog as a protease inhibitor
Synthesis and biological evaluation of four stereoisomers of PDMP-analogue, N-(2-decylamino-3-hydroxy-3-phenylprop-1-yl)--valienamine, and related compounds
Targeting radiosensitizers to DNA by minor groove binding: nitroarenes based on netropsin and distamycin
A note of caution in the use of receptor binding assays to screen marine organisms: the action of halistanol trisulphate on adenosine receptors.
Configurational variants of hydroxyphenylkainoid: their potent depolarizing activities in the rat central nervous system
Novel inhibitors of influenza sialidases related to zanamivir. Heterocyclic replacements of the glycerol sidechain
Phenylpropanoids from Daphne feddei and their inhibitory activities against NO production.
Thiazolidinedione derivatives as PTP1B inhibitors with antihyperglycemic and antiobesity effects.
Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors.
A series of 1, 2-coupled indane dimers with mast cell stabilisation and smooth muscle relaxation properties.
Reversal of fluconazole resistance by sulfated sterols from the marine sponge Topsentia sp.
Oxygenated lignans from the fruits of Schisandra arisanensis.
Discovery and optimization of potent and selective functional antagonists of the human adenosine A2B receptor.
Gamma-lactones and ent-eudesmane sesquiterpenes from the endophytic fungus Eutypella sp. BCC 13199.
Alkaloids from the leaves of Daphniphyllum subverticillatum.
Function-oriented biosynthesis of beta-lactone proteasome inhibitors in Salinispora tropica.
Chrotacumines A-D, chromone alkaloids from Dysoxylum acutangulum.
Discovery and optimization of novel 4-[(aminocarbonyl)amino]-N-[4-(2-aminoethyl)phenyl]benzenesulfonamide ghrelin receptor antagonists.
Potent inhibitors of beta-tryptase and human leukocyte elastase based on the MCoTI-II scaffold.
Monoterpenoid indole alkaloids from Alstonia yunnanensis.
Synthesis and antitumor activities of 3-modified 2-methoxyestradiol analogs.
Cytotoxic neo-clerodane diterpenoid alkaloids from Scutellaria barbata.
Novel 3-arylideneindolin-2-ones as inhibitors of NAD+ -dependent histone deacetylases (sirtuins).
Synthesis and anticonvulsant activities of (R)-N-(4'-substituted)benzyl 2-acetamido-3-methoxypropionamides.
Design and synthesis of novel quinone inhibitors targeted to the redox function of apurinic/apyrimidinic endonuclease 1/redox enhancing factor-1 (Ape1/ref-1).
Pyridinylquinoxalines and pyridinylpyridopyrazines as lead compounds for novel p38 alpha mitogen-activated protein kinase inhibitors.
Cationic N-confused porphyrin derivative as a better molecule scaffold for G-quadruplex recognition.
Discovery of new SCH 39166 analogs as potent and selective dopamine D1 receptor antagonists.
Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
Practical and efficient synthesis of pyrano[3,2-c]pyridone, pyrano[4,3-b]pyran and their hybrids with nucleoside as potential antiviral and antileishmanial agents.
Synthesis and structure-activity relationship of substitutions at the C-1 position of Delta9-tetrahydrocannabinol.
Synthesis of 1-(D-glucopyranosyl)-1,2,3-triazoles and their evaluation as glycogen phosphorylase inhibitors.
New benzoxanthone derivatives as topoisomerase inhibitors and DNA cross-linkers.
Synthesis and anti-influenza virus activity of dihydrofuran-fused perhydrophenanthrenes with a benzyloxy-type side-chain.
Phenyltriazolinones as potent factor Xa inhibitors.
5-Modified-2'-dU and 2'-dC as mutagenic anti HIV-1 proliferation agents: synthesis and activity.
Toward the development of potent and selective bisubstrate inhibitors of protein arginine methyltransferases.
Oxazolomycins: natural product lead structures for novel antibacterials by click fragment conjugation.
Schiff base transition metal complexes as novel inhibitors of xanthine oxidase.
Kadsuracoccinic acids A-C, ring-A seco-lanostane triterpenes from Kadsura coccinea and their effects on embryonic cell division of Xenopus laevis.
Usimines A-C, bioactive usnic acid derivatives from the Antarctic lichen Stereocaulon alpinum.
Antimicrobial triterpenoids from Vladimiria muliensis.
Benzofused N-substituted cyclic enediynes: activation and DNA-cleavage potential.
Tetramic and tetronic acids: an update on new derivatives and biological aspects.
ent-Kaurane Diterpenoids from Isodon nervosus.
Recent developments of carbonic anhydrase inhibitors as potential anticancer drugs.
Glycosidic constituents of the tubers of Gymnadenia conopsea.
Complex sesquiterpenoids with tyrosinase inhibitory activity from the leaves of Chloranthus tianmushanensis.
Natural products as leads to potential drugs: an old process or the new hope for drug discovery?
Peptidomimetic growth hormone secretagogues: synthesis and biological activities of analogs varied at the indole nucleus of the prototypical spiropiperidine L-162,752
Novel 1,5-benzodiazepindione gastrin/CCKB antagonists
Inhibition of human rhinovirus 3C protease by homophthalimides
Synthesis and biological evaluation of an alkenyldiarylmethane (ADAM) which acts as a novel non-nucleoside HIV-1 reverse transcriptase inhibitor
Highly potent and selective inhibitors of endothelin converting enzyme
Synthesis and activity of enantiopure (S) (m-nitrobenzoyl) alanine, potent kynurenine-3-hydroxylase inhibitor
Structure activity studies on pseudo-symmetrical HIV-1 protease inhibitors
Application of hygromycin a structure activity relationships to the antibiotic A201A.
Synthesis of 7-substituted androstenediones by a 1,4-conjugate addition approach
Synthesis of 7-methoxy-2-(1,3-dithiolan-2-ylidene)cephem sulphones. A new series of human leukocyte elastase inhibitors
Stabilization of a prostaglandin tertiary allylic alcohol system by fluorine: synthesis, acid stability studies and pharmacology of a 16-fluoromethyl analog of SC-46275.
Novel 2-(2-furo[3,2-b]pyridinyl) pyrrolidines: potent neuronal nicotinic acetylcholine receptor ligands
DNA - gyrase inhibition and antibacterial activity of fluoro-quinolones: influence of the position of the fluorine(s).
Synthesis and structure-activity relationship of C-3 benzoyloxymethyl cephalosporins exhibiting anti-MRSA activities
(N-acyl-N-alkyl)glycyl borolysine analogs: A new class of potent thrombin inhibitors
17-hydroxywortmannin: A potent inhibitor of bone resorption and phosphatidylinositol-3-kinase
Discovery of selective dopamine D3 ligands: II. 2-[4-[3-(4-aryl-1-piperazinyl)propoxy]phenyl]benzimidazole partial agonists
A new class of dinucleotide analogues. The synthesis of 3-O-thymidylyl(5-deoxy-5-selene-thymidylyl)-Se-phosphoroselenolate, its O-methyl ester and methanephosphonate derivatives.
New 7-aryl analogues of anthracyclines: Synthesis and cytotoxic activity of ()-7-(3,4,5-trimethoxyphenyl)-7-deoxyidarubicinone
Conformationally constrained analogues of diacylglycerol. 6. Changes in PK-C binding affinity for 3-O-acyl-2-deoxy-L-ribonolactones bearing different acyl chains.
The design and synthesis of novel hydroxyproline inhibitors of HIV-1 proteinase
Characterization of the taxol structure-activity profile for the locus of the A-ring side chain
2-aminoalchohol immunosuppressants: Structure-activity relationships
Pseudopeptide CCK-4 analogues incorporating the [CH(CN)NH] peptide bond surrogate
Synthesis and structure-activity relationships of potent retinoid X receptor ligands
The conformation of cyclosporin a bound to cyclophilin is altered (once again) following binding to calcineurin: an analysis of receptor-ligand-receptor interactions
Identification and chemical synthesis of MDL 105,212, a non-peptide tachykinin antagonist with high affinity for NK1 and NK2 receptors
Nonpeptidic HIV protease inhibitors: 3-(S-benzyl substituted)-4-hydroxy-6-(phenyl substituted)-2H-pyran-2-one with an inverse mode of binding
The synthesis and anti-hiv activity of pyrimidine dioxolanyl nucleosides
Antileukaemic properties of 12-hydroxydaphnetoxin derivatives
Inhibition of human leukocyte elastase (HLE) by novel bicyclic -lactams
Acyliminothiadiazoline derivatives: New, highly potent, and orally active angiotensin II receptor antagonists
Synthesis of methyl -sialosides N-substituted with large alkanoyl groups, and investigation of their inhibition of agglutination of erythrocytes by influenza A virus
The discovery and synthesis of 2-biphenylcarbapenems active against methicillin resistant staphylococci
Synthesis and biological evaluation of new 5-HPETE analogs
Synthesis of potent -D-glucocerebrosidase inhibitors: N-alkyl--valienamines
Synthesis, insecticidal and anti-acetylcholinesterase activity of a new class of heterocyclic methanesulfonates
Design, synthesis, activity, and structure of a novel class of matrix metalloproteinase inhibitors containing a heterocyclic P2-P3 amide bond isostere
Structural and stereochemical requirements of time-dependent inactivators of the interleukin-1 converting enzyme
Synthesis of a novel series of 3-oxo-2,4-dioxobicyclo[3.2.1]octanes: additional evidence for two thromboxane receptor subtypes.
The structure of MK-571 (form I) at 170 K and conformational analysis by molecular modeling
Synthesis and biological evaluation of conformationally constrained bicyclic and tricyclic balanol analogues as inhibitors of protein kinase C
Synthesis and antitumor activity of novel distamycin derivatives
Synthesis and in vitro cytotoxicity of cis-dichloro[(2S,3R,4S)-2-aminomethyl-3,4-(O-isopropylidene)dihydroxy- or -3,4-dihydroxypyrrolidine]platinum(II)
Conformationally restricted inhibitors of the high affinity -glutamate transporter
Novel dithiocarbamate carbapenems1 with anti-MRSA activity
A general approach toward the design of inhibitors of serine proteinases: inhibition of human leukocyte elastase by substituted dihydrouracils
p-Nitrophenyl 1,5-dithio--l-fucopyranoside: a novel sulfur based fucosidase inhibitor
Inhibitory stereochemistry of N-chloroacetyl-N-hydroxyleucine methyl ester for thermolysin
Synthesis of C2-symmetrical polyhydroxyazepanes as inhibitors of glycosidases
Novel, extended transition state mimic in HIV-1 protease inhibitors with peripheral C-2-symmetry
Synthesis of 1-(2-aminopropyl)benzimidazoles, structurally related to the TIBO derivative R82150, with activity against human immunodeficiency virus
Synthesis of adamantane spiro sultones as potential antiviral agents
1,3-Dithian-2-ylidene and thiazolidin-2-ylidene derivatives as a novel class of antimycotic agents
Synthesis of rutaecarpine and cytotoxic analogues
Molecular modeling studies on 11-aminoethoxyphenyl and 7-aminoethoxyphenyl estradiols. evidence suggesting a common hydrophobic pocket in estrogen receptor
Synthesis and in vitro profile of 7-substituted quinoline chromanols as novel, non-acidic LTB4 antagonists
Hygromycin A: preparation of aminocyclitol analogs defining the minimum functionality required for biological activity
Topical antiinflammatory dehydroabietylamine derivatives. IV
Synthesis and biological evaluation of new arachidonic acid analogs
Antibody catalyzed hydrolysis of a phosphotriester
Synthesis and biological evaluation of flavonoids and related compounds as gastroprotective agents
Pentamidine congeners 1: Synthesis of Cis- and Trans-butamidine analogues as anti-Pneumocystis carinii pneumonia agents.
New cytostatic agents obtained by molecular topology
4-Substituted proline derivatives that inhibit angiotensin converting enzyme and neutral endopeptidase 24.11.
Nucleosides and nucleotides. 128. (2S)-2-deoxy-2-C-methyl-5-iodouridine (SMIU) as a novel potent anti-herpes virus agent
Synthesis and anti-HIV activity of 9-[(2R-5R)-2,5-dihydro-5-(phosphonomethoxy)-2-furanyl]-2,6-diaminopurine
7,10-Bis(2-mercapto-2-methyl)propyl-7,10-diazapalmitic acid: a novel, N2S2 ligand for technetium-99m
Design and syntheses of 4-acylaminopyridine derivatives: Novel high affinity choline uptake enhancers I
Synthesis and biological properties of carboranylaziridines bearing cascade polyols
Synthesis and neurobiological actions of pyrrolidine-2,3-dicarboxylic acids (PRDA). Conformationally restricted analogues of L-aspartate
Synthesis and structure-activity relationships of novel antiseptics
Synthesis of novel fluorescently labeled sphingomyelin derivatives useful for sphingomyelinase assay
Synthesis and antimalarial evaluation of 2,3,5-trioxabicyclo[2.2.2]octanes, models for the putative pharmacophore of qinghaosu (artemisinin)
Synthesis and SAR of diiodotyrosine-derived glycine-site N-methyl-D-aspartate receptor ligands
Alteration of Na+ permeability in human erythrocytes as studied by 23Na-NMR and inhibition of the kidney Na+,K+-ATPase activities with saponins: Interaction of Gleditsia saponins with human erythrocyte membranes
Novel, water-soluble phosphate derivatives of 2-ethoxy carbonylpaclitaxel as potential prodrugs of paclitaxel: Synthesis and antitumor evaluation
An efficient preparation of the potent and selective pseudopeptide thrombin inhibitor, inogatran
Linear sesterterpenes from the Caribbean sponge Thorecta horridus with inflammatory activity
1,25-Dihydroxyvitamin D3 Hybrid Analogs with Structural changes at both the A-ring and the C,D-ring side-chain. II
Topographical requirements for delta opioid ligands: The synthesis and biological properties of a cyclic analogue of deltorphin I
Structure-activity studies of nonmacrocyclic rapamycin derivatives
A novel series of 4-phenoxyquinolines: potent and highly selective inhibitors of PDGF receptor autophosphorylation
Novel 3-deoxy-3-descladinosyl-6-O-methyl erythromycin a analogues. Synthesis and in vitro activity
Synthesis and in vitro anti-HIV and antitumor activity of new 2-chloroethyl thiocarbamates
Inhibition of mevalonate 5-pyrophosphate decarboxylase by a proline-containing transition state analog
Alkyl ether derivatives of the FK-506 related, immunosuppressive macrolide L-683,742 (C31-O-desmethyl ascomycin)
Engineering of cyclic peptides with novel inhibiting properties to differentiate two serine proteases, chymotrypsin and subtilisin Carlsberg
The synthesis and identification of 4,6-diaminoquinoline derivatives as potent immunostimulants
A potent long-acting imidazole-5-acrylic acid angiotensin II AT-1 receptor antagonist
The effect of propargylic substitution on the activation and aromatization of enediynes
Res-701-1, synthesis and a reevaluation of its effects on the endothelin receptors
6-Carboxymethyl-2-azabicyclo[2.2.1]heptane enantiomers: muscarinic activities of rigid analogues of arecoline
A new rearranged cholestane glycoside from ornithogalum saundersiae bulbs exhibiting potent cytostatic activities on leukemia HL-60 and molt-4 cells
C5-piperazinyl-1,4-benzodiazepines, water-soluble, orally bioa vailable CCKB/gastrin receptor antagonists
Enzymatic synthesis of sialyl Lex and derivatives based on a recombinant fucosyltransferase
Boric acid effect ont he hydrolysis of 4-nitrophenyl 2,3-dihydroxybenzoate: mimic of borate inhibition of serine proteases
6-Phenyl-6-alkylamido-5,6-dihydro-2H-pyran-2-ones: novel HIV protease inhibitors
U-87947E, a protein quinolone antibacterial agent incorporating a bicyclo[1.1.1]pent-1-yl (BCP) subunit
Synthesis of partially non-peptidic neurotensin mimetics
Anthraquinones related to rhein inhibit glucose uptake into chondrocytes. A mechanism for anti-osteoarthritis drugs?
Structure-activity relationships study at the 3-N position of paclitaxel-part 1: Synthesis and biological evaluation of the 3-(t)-butylaminocarbonyloxy bearing paclitaxel analogs
Dual metalloprotease inhibitors. II. Effect of substitution and stereochemistry on benzazepinone based mercaptoacetyls
Synthesis and biological evaluation of a new series of dihydrofolate reductase inhibitors based on the 4-(2,6-diamino-5-pyrimidinyl)alkyl-L-glutamic acid structure
Tetraazaacenaphthene and tetraazaphenalene derivatives: A new class of hepatoprotectants: Part IV
Synthesis and biological activity of conformationally constrained 4a-phenanthreneamine derivatives as noncompetitive NMDA antagonists
1-Phenyl-[2H]-tetrahydropyridazin-3-one, A-53612, a selective orally active 5-lipoxygenase inhibitor
The prooligonucleotide approach. III: Synthesis and bioreversibility of a chimeric phosphorodithioate prooligonucleotide
Synthesis of conformationally constrained potential inhibitors of mammalian metalloproteinases
Novel benzimidazole-4-carboxylic acid derivatives as potent and selective 5-HT3 receptor ligands
A versatile synthesis of 2-methoxyestradiol, an endogenous metabolite of estradiol which inhibits tubulin polymerization by binding to the colchicine binding site
4-(3-furyl)-2-(4-methylpiperazino)pyrimidines: Potent 5-HT2A receptor antagonists
RP 73163: A bioavailable alkylsulphinyl-diphenylimidazole ACAT inhibitor
New orally active serine protease inhibitors.
New antihistamines: substituted piperazine and piperidine derivatives as novel H1-antagonists.
Novel angiotensin II receptor antagonists. Design, synthesis, and in vitro evaluation of dibenzo[a,d]cycloheptene and dibenzo[b,f]oxepin derivatives. Searching for bioisosteres of biphenylyltetrazole using a three-dimensional search technique.
Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells.
Synthesis and antimalarial activities of 12 beta-allyldeoxoartemisinin and its derivatives.
Evolution of a series of non-quinoline leukotriene D4 receptor antagonist; synthesis and sar of benzothiazoles and thiazoles substituted benzyl alcohols as potent LTD4 antagonists
4-Deoxy-4-aminoavermectins with potent broad spectrum antiparasitic activities
Syntheses of -, -monoglycosylceramides and four diastereomers of an -galactosylceramide
Alkoxy substituted benzisothiazolone (BIT) derivatives: potent inhibitors of human leukocyte elastase
()-1-Azabicyclo[2.2.1]heptan-3-one, O-(3-methyl-5-aryl-2-penten-4-ynyl) oximes: Potent muscarinic agonists
Synthesis and antiviral activity of phosphonate derivatives of enantiomeric dihydro-2H-pyranyl nucleosides
Preparation and in vitro activity of aryl ether derivatives of the FK-506 related immunosuppressive macrolides ascomycin and L-683,742
Isolation, structure determination and squalene synthase activity of L-731,120 and L-731,128, alkyl citrate analogs of zaragozic acids A and B
FPL 64176: The effect of the chain length separating the two aryl groups on calcium agonist activity
Phosphonates and phosphinates: novel leaving groups for benzisothiazolone inhibitors of human leukocyte elastase.
Vinyl sulfones as mechanism-based cysteine protease inhibitors.
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
1-Aminoindan-1,5-dicarboxylic acid: a novel antagonist at phospholipase C-linked metabotropic glutamate receptors.
Synthesis and bioactivity of photolabile sirolimus (rapamycin) analogs
Inhibition of interleukin-1 converting enzyme by N-acyl-aspartyl aryloxymethyl ketones
Growth inhibitory effect of naphthofuran and naphthofuranquinone derivatives on Trypanosoma cruzi epimastigotes
Methylenedioxyphenyl substituted compounds from Piper species as inhibitors of liver microsome-mediated aflatoxin B1-DNA binding in vitro
Symmetry-based HIV Protease inhibitors: rational design of 2-methylbenzamides as novel P2/P2 ligands
Hydroxylation at C-3 of doxorubicin alters the selected phenotype of cellular drug resistance
Annohexocin, a novel mono-THF acetogenin with six hydroxyls, from Annona muricata (Annonaceae)
Discovery of micromolar PDE IV inhibitors that exhibit much reduced affinity for the [3H]rolipram binding site: 3-norbornyloxy-4-methoxyphenylmethylene oxindoles
Cucurbitane-type triterpenoids from the African plant Momordica balsamina.
Xanthepinone, an antimicrobial polyketide from a soil fungus closely related to Phoma medicaginis.
The discovery and optimisation of benzazepine sulfonamide and sulfones as potent agonists of the motilin receptor.
Synthesis and biological evaluation of pyrrolopyridazine derivatives as novel HER-2 tyrosine kinase inhibitors.
Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.
Discovery of highly potent and selective type I B-Raf kinase inhibitors.
Synthesis of nucleoside analogues with a 1,5-anhydrohexitol moiety
Dual antagonists of platelet activating factor and histamine. 2. pyridine ring substitution of N-acetyl-4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)piperidines
Heterocyclic inhibitors of human leukocyte elastase: 3-Hydroxypyridazopyrimidine, 3-hydroxypyridopyrimidine and 3-hydroxyquinazoline-2,4-1H,3H0dione derivatives
Synthesis of pyrrolidine oxazoles as thromboxane A2/endoperoxide receptor antagonists
The stoichiometry of binding of flavin mononucleotide (FMN) hydroquinone to Escherichia coli chorismate synthase
Synthesis and antiflammatory activity of some 3-heterocycle-1,2-benzisothiazoles
A diazine heterocycle replaces a six-membered hydrogen-bonded array in the active site of scytalone dehydratase
Synthesis and antimalarial evaluation of 2,3,5-trioxabicyclo[2.2.3]nonane, a model for the putative pharmacophore of artemisinin
1-(hydroxyalkyl)-25-hydroxyvitamin D3 analogs of calcitriol. 2. Preliminary biological evaluation
Methoxylation of cocaine reduces binding affinity and produces compounds of differential binding and dopamine uptake inhibitory activity: discovery of a weak cocaine "antagonist".
Studies directed toward the design of orally active renin inhibitors. 1. Some factors influencing the absorption of small peptides.
Hydroxyurea derivatives as hypoglycemic agents.
Bicyclic thiazolidine lactam peptidomimetics of the dopamine receptor modulating peptide Pro-Leu-Gly-NH2.
A mechanism-based inactivation study of neutral endopeptidase 24.11.
A selective delta 1 opioid receptor agonist derived from oxymorphone. Evidence for separate recognition sites for delta 1 opioid receptor agonists and antagonists.
Design of potent non-peptide competitive antagonists of the human bradykinin B2 receptor.
Synthesis and antibacterial activity of a new series of tetracyclic pyridone carboxylic acids.
Oxindole N-Methyl-D-Aspartate (NMDA) antagonists
4-alkylamino-3-bromo-N-alkyl-1,8-naphthalimides: new photochemically activatable antiviral compounds
2'-(Trimethylammonio)ethyl 4-(hexadecyloxy)-3(S)-methoxybutanephosphonate: a novel potent antineoplastic agent.
Two new unsaturated fatty acid ethanolamides in brain that bind to the cannabinoid receptor.
Protonation of phosphoramide mustard and other phosphoramides.
Antibacterial activity of long-chain alcohols: the role of hydrophobic alkyl groups
New, potent anthelmintic and acaricidal agents: 4-deoxy-4-thio-substituted avermectin derivatives
Nonsteroidal inhibitors of human type I steroid 5-alpha-reductase.
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.
Lupane triterpenes and derivatives with antiviral activity.
DNA binding ligands targeting drug-resistant bacteria: structure, activity, and pharmacology.
Oxidosqualene cyclase inhibitors as antimicrobial agents.
Inclusion complexation and solubilization of paclitaxel by bridged bis(beta-cyclodextrin)s containing a tetraethylenepentaamino spacer.
Synthesis and in vitro study of novel Mannich bases as antibacterial agents.
Design and synthesis of nonpeptidal endothelin receptor antagonists based on the structure of a cyclic pentapeptide
in vivo potent antimalarial 1,2,4-trioxanes: Synthesis and activity of 8-(-arylvinyl)-6,7,10-trioxaspiro[4,5]decanes and 3-(-arylvinyl)-1,2,5-trioxaspiro[5,5]undecanes against Plasmodium berghei in mice
Enantioselective synthesis of inositols as intermediates for the preparation of deoxy-inositol phosphates from D-galactose
Novel open-ring analogues of N5,N10-methylenetetrahydrofolic acid with selective activity against brain tumor
5,6,7,8-Tetrahydroquinolones as antagonists at the glycine site of the NMDA receptor
2-Substituted penems with amino acid-related side chains: synthesis and antibacterial activity of a new series of beta-lactam antibiotics.
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.
Peptidyl aldehyde derivatives as potent and selective inhibitors of cathepsin L
Substrate specificity of farnesyl diphosphate synthase from Bacillus stearothermophilus
N-Methyl and N-cyclopropylmethyl-14,14-[dithiobis[(2-oxo-2,1-ethanediyl)imino]]bis(7,8-dihydro-5-methyl-morphinone) MET-TAMO and N-CPM-MET-TAMO: Synthesis and opioid binding properties
Protein kinase C inhibitory activities of balanol analogs bearing carboxylic acid replacements
Hydroxy-anthraquinones as antimalarial agents
Synthesis and porcine pancreatic elastase inhibitory evaluation of 6-(sulfonyl)oxy-and 6-chloropenicillanate sulfone esters and 3-(acyloxy)methyl-6-chloropenam sulfones
Synthesis and evaluation of nitro 5-deazaflavins as novel bioreductive antitumor agents
Synthesis and antibacterial activity of FR21818, a new, potent 1-methylcarbapenem
Aminodiol HIV protease inhibitors. 2. 1,1-Dimethyl-2-hydroxyethyl carbamate derivatives with enhanced potency
Inhibition of matrix metalloproteinases by N-carboxyalkyl peptides containing extended alkyl residues At P1'
Paclitaxel and docetaxel photoaffinity labels
Antitumor activities of -, -monogalactosylceramides and four diastereomers of an -galactosylceramide
4-Substituted analogues of idoxifene: Antiestrogens and calmodulin antagonists
Selective inhibition of the tyrosine kinase pp60src by analogs of 5,10-dihydropyrimido[4,5-b]quinolin-4(1H)-one
Pharmacological evaluation of UK-14,304 analogs at cloned human adrenergic receptors
C-Attached aminoalkylindoles: potent cannabinoid mimetics
Synthesis and biological activity of conformationally restricted tricyclic analogs of the hormone melatonin
Mechanism-based inactivation of serine proteases by dichlorocyclopropane fused lactone derivatives
4-cyanothiazolidides as very potent, stable inhibitors of dipeptidyl peptidase IV
Evaluation of furofuran as a P2 ligand for symmetry-based HIV protease inhibitors
Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif
Quantification of the extent of attenuation of the rate of turnover chemistry of the TEM-1 -lactamase by the -1R-hydroxyethyl group in substrates
Unsaturated thioacetic acids as novel mechanism-based inhibitors of peptidylglycine -hydroxylating monooxygenase
Mechanism-based inactivation of -chymotrypsin
Carboxylic acid bioisosteres of -linked dipeptide analogues of the folate-based thymidylate synthase (TS) inhibitor, 2-desamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583)
Cycloleonuripeptides A, B and C, three new proline-rich cyclic nonapeptides from Leonurus heterophyllus
Similarities and differences in the DNA binding/cleaving specificities and mechanisms of [SalenMn(III)]+ and [TMPPMn(III)]5+
Synthesis and antibacterial activity of new tropone-substituted phenyloxazolidinone antibacterial agents 2. Modification of the phenyl ring the potentiating effect of fluorine substitution on in vivo activity
Potential antitumor agents. 24. Synthesis and pharmacological behavior of imidazo[2,1-b]thiazole guanylhydrazones bearing at least one chlorine.
Approaches to short-acting neuromuscular blocking agents: nonsymmetrical bis-tetrahydroisoquinolinium mono- and diesters.
N-(substituted-phenyl) piperazines: antagonists with high binding and functional selectivity for dopamine D4 receptors
Structure-activity dependency of new bacterial tryptophanyl tRNA synthetase inhibitors
Substituted morpholine-2S-acetic acid derivatives: Sch 50911 and related compounds as novel GABAB antagonists
Synthesis of cephems bearing olefinic sulfoxide side chains as potential -lactamase inhibitors
Determination of the absolute configuration of the nonsteroidal contraceptive agent centchroman by X-ray crystallography on its N-methyl iodide salt
Synthesis and antitumor evaluation of paclitaxel phosphonooxymethyl ethers: a novel class of water soluble paclitaxel pro-drugs
Phosphonate-containing analogs of cholesteryl ester as novel inhibitors of cholesteryl ester transfer protein
()-SCH 57939: synthesis and pharmacological properties of a potent, metabolically stable cholesterol absorption inhibitor
Molecular design, chemical synthesis and biological studies of novel enediynes related to dynemicin a
Synthesis of water soluble prodrug of DMP323
Oximes: A new class of methoxytetrahydropyranyl inhibitors of leukotriene biosynthesis with high in vitro and in vivo potency
Syntheses of trans-3-substituted-CCG-IV analogs and their characterization to ionotropic glutamate receptors
Synthesis and biological activity of 4-azido- and 4-trifluoracetamido-3-chloro-3-deamino-4-deoxydaunorubicin
Epidermal growth factor receptor tyrosine kinase: Structure-activity relationships and antitumour activity of novel quinazolines
Use of CoMFA in validating the conformation used in designing 4-(1H-benzimidazole-2-carbonyl)piperidines with H1/NK1 receptor antagonist activity
Naphtho-fused azepines as potent growth hormone secretagogues
Synthesis and trypanocidal activity of the bis-carba analogue of pentamidine
3-(1H-indazol-3-ylmethyl)-1,5-benzodiazepines: CCK-A agonists that demonstrate oral activity as satiety agents.
Novel human histamine H(3) receptor antagonists.
Synthesis of aglycon analogues of sarmentosin and their bioactivity of lymphocyte proliferation.
Isolation and antimalarial activity of peroxydisulfate oxidation products of primaquine.
Aromatic farnesyl diphosphate analogues: vinyl triflate-mediated synthesis and preliminary enzymatic evaluation.
Scaffold hopping and optimization towards libraries of glycogen synthase kinase-3 inhibitors.
Antimalarial activities of ring-substituted bioimidazoles.
Discovery of non-zwitterionic GABA(A) receptor full agonists and a superagonist.
Structure-activity relationships of oxime neurokinin antagonists: oxime modifications.
Imidazo[5,1-f]triazin-4(3H)-ones, a new class of potent PDE 5 inhibitors.
Squaric acid derivatives as VLA-4 integrin antagonists.
N-Methylbenzanilide derivatives as a novel class of selective V(1A) receptor antagonists.
Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens.
Beta-aryl-succinic acid hydroxamates as dual inhibitors of matrix metalloproteinases and tumor necrosis factor alpha converting enzyme.
From imidazoles to pyrimidines: new inhibitors of cytokine release.
Synthesis and biological evaluation of 7,8,9,10-tetrahydroimidazo[1,2-c]pyrido[3,4-e]pyrimdin-5(6H)-ones as functionally selective ligands of the benzodiazepine receptor site on the GABA(A) receptor.
Synthesis and antimycobacterial activity of pyrazine and quinoxaline derivatives.
Correlation of the antibacterial activities of cationic peptide antibiotics and cationic steroid antibiotics.
Structural study of phenyl boronic acid derivatives as AmpC beta-lactamase inhibitors.
Synthesis, SAR and evaluation of [1,4']-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists.
Artoindonesianin C, a new xanthone derivative from Artocarpus teysmanii.
Chapecoderins A-C, new labdane-derived diterpenoids from Echinodorus macrophyllus.
Substituted indole-5-carboxamides and -acetamides as potent nonpeptide GnRH receptor antagonists.
Adamantylaminopyrimidines and -pyridines are potent inducers of tumor necrosis factor-alpha.
3-(Arylacetylamino)-N-methylbenzamides: a novel class of selective anti-Helicobacter pylori agents.
Synthesis and biological activity of novel macrocyclic antifungals: acylated conjugates of the ornithine moiety of the lipopeptidolactone FR901469.
Design and synthesis of matrix metalloproteinase inhibitors guided by molecular modeling. Picking the S(1) pocket using conformationally constrained inhibitors.
Design, synthesis, and evaluation of a long-acting, potent analogue of gonadotropin-releasing hormone.
2-(Anilinomethyl)imidazolines as alpha(1)-adrenoceptor agonists: the identification of alpha(1A) subtype selective 2'-carboxylic acid esters and amides.
Novel, lipophilic derivatives of 2,5-dideoxy-2,5-imino-D-mannitol (DMDP) are powerful beta-glucosidase inhibitors.
Synthesis and structural studies of aza analogues of functionalized amino acids: new anticonvulsant agents.
New anti-MRSA cephalosporins with a basic aminopyridine at the C-7 position.
Substituted acrylamides as factor Xa inhibitors: improving bioavailability by P1 modification.
Synthesis and hypoglycemic evaluation of substituted pyrazole-4-carboxylic acids.
4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo.
Design, synthesis, and evaluation of pharmacological properties of cinnamic derivatives as antiatherogenic agents.
A polyacetylene compound from herbal medicine regulates genes associated with thrombosis in endothelial cells.
Characterization of distamycin A binding to damaged DNA.
Trisubstituted 1,2,4-triazoles as ligands for the ghrelin receptor: on the significance of the orientation and substitution at position 3.
Novel cyanoguanidines with potent oral antitumour activity
1-Arylsulfonyl-3-(-hydroxybenzyl)-1H-pyrroles, a novel class of anti-HIV-1 reverse transcriptase inhibitors
Cytotoxicity of bis(phenylamidinium)furan alkyl derivatives in human tumour cell lines: Relation to DNA minor groove binding
Highly selective aldose reductase inhibitors. 3. Structural diversity of 3-(arylmethyl)-2,4,5-trioxoimidazolidine-1-acetic acids.
Synthesis and anti-HIV activity of novel N-1 side chain-modified analogs of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).
Bicyclo[2.2.1]heptane and 6,6-dimethylbicyclo[3.1.1]heptane derivatives: orally active, potent, and selective prostaglandin D2 receptor antagonists.
DIARYLETHER INHIBITORS OF FARNESYL-PROTEIN TRANSFERASE
3-Amino-1,2-benzisoxazoles: A new family of potent inhibitors of LTB4 binding to the human neutrophils
3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor
Design and synthesis of novel imidazole-substituted dipeptide amides as potent and selective inhibitors of Candida albicans myristoylCoA:protein N-myristoyltransferase and identification of related tripeptide inhibitors with mechanism-based antifungal activity.
N-Methyl-2-[4-(2-methylpropyl)phenyl]-3-(3-methoxy-5-methylpyrazin-2-ylsulfamoyl)benzamide; one of a class of novel benzenesulphonamides which are orally-active, ETA-selective endothelin antagonists
Two-ring DNA minor-groove binders consisting of readily available, di-substituted benzene derivatives
Synthesis and biological activity of a new anti-factor Xa pentasaccharide with a C-interglycosidic bond
Conformational preference of the 6-acetyl group in novel anticonvulsant trans 4S-benzamido-benzo[b]pyran-3R-ols
Benzothiazol-2-ylcarboxylic acids with diverse spacers: A novel class of potent, orally active aldose reductase inhibitors
Potent selective thienoxazinone inhibitors of herpes proteases
Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets
The synthesis and evaluation of the major metabolites of mazapertine
Synthesis of conformationally constrained analogues of BRL-32872. Determination of stereochemistry and related pharmacological properties
Synthesis and biological activity of artificial analogs of mycalamide A
Synthesis and receptor binding studies of quinolinic derivatives as melatonin receptor ligands
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
An aromatic moiety is not essential for pharmacophore binding to sigma binding sites: Synthesis of N-alkylazacycloheptane derivatives as potent sigma ligands
3D QSAR analysis of taxoids from Taxus cuspidata var. nana by comparative molecular field approach
Catalysis of the Kemp elimination by antibodies elicited against a cationic hapten
Sch 207278: a novel farnesyl protein transferase inhibitor from an unidentified fungus
Synthesis and biological evaluation of 14-alkoxymorphinans. 14.1 14-ethoxy-5-methyl substituted indolomorphinans with opioid receptor selectivity
The synthesis of (R)-1-(2-oxocyclopentyliden)-2-alkanols and the (S)-forms, and their bio-antimutagenic activity against UV-induced Escherichia coli WP2 B/r Trp
pH Dependence of the rate of DNA alkylation for (+)-duocarmycin SA and (+)-CCBI-TMI
ATP analogs with non-transferable groups in the position as inhibitors of glycerol kinase
Design and synthesis of dipeptidyl alpha',beta'-epoxy ketones, potent irreversible inhibitors of the cysteine protease cruzain.
New taxanes as highly efficient reversal agents for multidrug resistance in cancer cells.
Polycyclic aromatic compounds as anticancer agents: synthesis and biological evaluation of some chrysene derivatives.
Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model.
Selective chemical modifications of polymyxin B.
Tricyclic ureas: a new class of HIV-1 protease inhibitors.
Differential activity of rosiglitazone enantiomers at PPAR gamma.
Potent and selective inhibitors of the proteasome: dipeptidyl boronic acids.
Solid phase synthesis of benzylamine-derived sulfonamide library.
Orally active factor Xa inhibitors: 4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine derivatives.
Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C.
Design, synthesis and cytotoxic studies on the simplified oxy analog of eleutherobin.
Specific inhibition effects of N-pentafluorobenzyl-1-deoxynojirimycin on human CD4+ T cells.
Hydroxamic acid-based bisubstrate analog inhibitors of Ras farnesyl protein transferase.
Bis(31/31') ([CYS(31), Trp(32), Nva(34)] NPY-(31-36)): a specific NPY Y-1 receptor antagonist.
Synthesis and biological evaluation of1',2'-seconucleo-5'- phosphonates.
Neutral inhibitors of the serine protease factor Xa.
Antifungal activity of octyl gallate: structural criteria and mode of action.
First tricyclic oximino derivatives as 5-HT3 ligands.
Synthesis and antitumor evaluation of novel monoindolyl-4-trifluoromethylpyridines and bisindolyl-4-trifluoromethylpyridines.
Development of novel telomerase inhibitors based on a bisindole unit.
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase).
Current and novel approaches to the drug treatment of schizophrenia.
Synthesis and evaluation of caffeic acid amides as antioxidants.
Novel selective PDE4 inhibitors. 2. Synthesis and structure-activity relationships of 4-aryl-substituted cis-tetra- and cis-hexahydrophthalazinones.
Recent developments in the biology and medicinal chemistry of potassium channel modulators: update from a decade of progress.
Coumarins derivatives as dual inhibitors of acetylcholinesterase and monoamine oxidase.
Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
A new class of ibuprofen derivatives with reduced gastrotoxicity.
N,N-dibenzyl-N'-benzylidenehydrazines: potent competitive glucose-6-phosphatase catalytic enzyme inhibitors.
Discovery and parallel synthesis of a new class of cathepsin K inhibitors.
Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
Inhibition of carbonic anhydrase isozymes with benzene sulfonamides incorporating thio, sulfinyl and sulfonyl glycoside moieties.
Discovery and development of aurora kinase inhibitors as anticancer agents.
Ethyl 8-fluoro-6-(3-nitrophenyl)-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate as novel, highly potent, and safe antianxiety agent.
Cytotoxic calanquinone A from Calanthe arisanensis and its first total synthesis.
Epoxydons and a pyrone from the marine-derived fungus Nigrospora sp. PSU-F5.
Twenty-six years of anti-HIV drug discovery: where do we stand and where do we go?
Design and synthesis of a simplified inhibitor for XIAP-BIR3 domain.
Synthesis and biological evaluation of 2-amino-7,7-dimethyl 4-substituted-5-oxo-1-(3,4,5-trimethoxy)-1,4,5,6,7,8-hexahydro-quinoline-3-carbonitrile derivatives as potential cytotoxic agents.
chi-Conotoxin and tricyclic antidepressant interactions at the norepinephrine transporter define a new transporter model.
Structure activity relationships of quinoline-containing c-Met inhibitors.
Synthesis and evaluation of curcumin analogues as potential thioredoxin reductase inhibitors.
Design and synthesis of piperazine-indole p38 alpha MAP kinase inhibitors with improved pharmacokinetic profiles.
X-ray snapshot of the mechanism of inactivation of human neutrophil elastase by 1,2,5-thiadiazolidin-3-one 1,1-dioxide derivatives.
Design and synthesis of 2-pyridones as novel inhibitors of the Bacillus anthracis enoyl-ACP reductase.
Design, synthesis and evaluation of potent thymidylate synthase X inhibitors.
A refined pharmacophore model for HIV-1 integrase inhibitors: Optimization of potency in the 1H-benzylindole series.
Production of cytotoxic canthin-6-one alkaloids by Ailanthus altissima plant cell cultures.
New Type of Mono-tetrahydrofuran Ring Acetogenins from Goniothalamus donnaiensis
Rigidone, a sesquiterpene o-quinone from the gorgonian Pseudopterogorgia rigida.
Synthesis and biological evaluation of 2'-methyl taxoids derived from baccatin III and 14beta-OH-baccatin III 1,14-carbonate.
Inhibition of dipeptidyl peptidase-IV (DPP-IV) by atorvastatin.
Orally bioavailable prodrugs of a BCS class 2 molecule, an inhibitor of HIV-1 reverse transcriptase.
N-8-Substituted benztropinamine analogs as selective dopamine transporter ligands.
Triterpene, antioxidant, and antimicrobial compounds from Melissa officinalis.
Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer.
Brandisianins A-F, isoflavonoids isolated from Millettia brandisiana in a screening program for death-receptor expression enhancement activity.
Design, synthesis, and trypanocidal activity of new aminoadamantane derivatives.
Synthesis and anti-inflammatory activities of mono-carbonyl analogues of curcumin.
Nonsteroidal selective androgen receptor modulators (SARMs): dissociating the anabolic and androgenic activities of the androgen receptor for therapeutic benefit.
Improved peptide prodrugs of 5-ALA for PDT: rationalization of cellular accumulation and protoporphyrin IX production by direct determination of cellular prodrug uptake and prodrug metabolization.
Novel bisbenzamidines as potential drug candidates for the treatment of Pneumocystis carinii pneumonia.
Induction of G2/M cell cycle arrest and apoptosis by a benz[f]indole-4,9-dione analog in cultured human lung (A549) cancer cells.
General model for estimation of the inhibition of protein kinases using Monte Carlo simulations.
Synthesis and biological activity of 22-oxa CD-ring modified analogues of 1alpha,25-dihydroxyvitamin D3: spiro[5.5]undecane CF-ring analogues.
Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-disubstituted ureas.
Potent inhibition of checkpoint kinase activity by a hymenialdisine-derived indoloazepine.
QSAR analysis for heterocyclic antifungals.
Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Cyclea barbata.
Isolation and structure of the marine sponge cell growth inhibitory cyclic peptide phakellistatin 1.
Nickel(II) and cobalt(II) complexes of hydroxyl-substituted triazamacrocyclic ligand as potential antitumor agents.
Structure-activity relationships of untenone A and its derivatives for inhibition of DNA polymerases.
Potent imidazole and triazole CB1 receptor antagonists related to SR141716.
Synthesis of 5'-C-methyl-1',3'-dioxolan-4'-yl nucleosides.
Dipeptidyl aspartyl fluoromethylketones as potent caspase-3 inhibitors: SAR of the P2 amino acid.
Identification of novel potent bicyclic peptide deformylase inhibitors.
Design, synthesis and structure-activity relationships of new phosphinate inhibitors of MurD.
Synthesis and evaluation of a mechanism-based inhibitor of a 3-deoxy-D-arabino heptulosonate 7-phosphate synthase.
Unambiguous synthesis and prophylactic antimalarial activities of imidazolidinedione derivatives.
Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone.
Synthesis and antiviral evaluation of cis-substituted cyclohexenyl and cyclohexanyl nucleosides.
Synthesis and biological evaluation of methoxylated analogs of the newer generation taxoids IDN5109 and IDN5390.
Cassane furanoditerpenoids from the seed kernels of Caesalpinia bonduc from Thailand.
Psammaplysenes C and D, cytotoxic alkaloids from Psammoclemma sp.
Monoamine oxidase isoform-dependent tautomeric influence in the recognition of 3,5-diaryl pyrazole inhibitors.
Prospects for metabotropic glutamate 1 receptor antagonists in the treatment of neuropathic pain.
Tricyclic HIV integrase inhibitors: potent and orally bioavailable C5-aza analogs.
Synthesis and pharmacological evaluation of 1,3,4-oxadiazole bearing bis(heterocycle) derivatives as anti-inflammatory and analgesic agents.
Effect of the structure of adenosine mimic of bisubstrate-analog inhibitors on their activity towards basophilic protein kinases.
1,2-Diamines as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).
Discovery and SAR of 6-substituted-4-anilinoquinazolines as non-competitive antagonists of mGlu5.
Malevamides A-C, new depsipeptides from the marine cyanobacterium Symploca laete-viridis.
A cytotoxic sesquiterpene caffeate from the liverwort Bazzanianovae-zelandiae.
Polyhydroxylated sterols from the octocoral Dendronephthya gigantea.
Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent.
Evaluation of di-sansalvamide A derivatives: synthesis, structure-activity relationship, and mechanism of action.
Potent inhibitor scaffold against Trypanosoma cruzi trans-sialidase.
Structure-based drug design enables conversion of a DFG-in binding CSF-1R kinase inhibitor to a DFG-out binding mode.
Antileukemic activity of aminoparthenolide analogs.
Interdomain loop mutation Asp190Cys of the tetracycline efflux transporter TetA(B) decreases affinity for substrate.
Synthesis, antioxidant and DNA cleavage activities of novel indole derivatives.
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.
Synthesis and pharmacological evaluation of new methyloxiranylmethoxyxanthone analogues.
Synthesis and antibacterial activities of 6-O-methylerythromycin A 9-O-(3-aryl-2-propenyl) oxime ketolide, 2,3-enol ether, and alkylide analogues.
Synthesis and antibacterial activity of a novel series of acylides: 3-O-(3-pyridyl)acetylerythromycin A derivatives.
Dihydrofolate reductase mutant with exceptional resistance to methotrexate but not to trimetrexate.
Synthesis and GABA(A) receptor activity of a 6,19-oxido analogue of pregnanolone.
Synthesis and biological evaluation of 4-arylcoumarin analogues of combretastatins.
Design and synthesis of novel bioactive peptides and peptidomimetics.
Azolylchromans as a novel scaffold for anticonvulsant activity.
Synthesis and cytotoxic evaluation of combretafurans, potential scaffolds for dual-action antitumoral agents.
2,6-Quinolinyl derivatives as potent VLA-4 antagonists.
Synthesis of carbon-11 labeled sulfonanilide analogues as new potential PET agents for imaging of aromatase in breast cancer.
Tetrahydrobenzotriazines as a new class of nematocide.
Design and synthesis of conformationally constrained arginal thrombin inhibitors
Design and synthesis of the cartilage protective agent (CPA, Ro32-3555)
Discovery and structure-activity studies of a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors
Asymmetric synthesis of the sulfoxide metabolite of ON-579 by the kagan protocol
Oligopresentation of protease inhibitors with -cyclodextrin as template
Synthesis and biological activity of novel 3-trifluoromethyl taxoids
Development of the new potent non-peptide gpIIb/IIIa antagonist NSL-95301 by utilizing combinatorial technique
Anti-AIDS agents-XXVIII.1 Synthesis and Anti-HIV activity of methoxy substituted 3,4-Di-O-()-camphanoyl-(+)-cis-khellactone (DCK) analogues
Reversal of multidrug resistance (MDR) by aspidofractinine-type indole alkaloids.
Novel cytokine release inhibitors. Part II: Steroids.
Synthesis of anti-rheumatic agent epoxyquinomicin B.
C24 and C25 substituted marcfortine A derivatives.
Nonpeptide glycoprotein IIb/IIIa inhibitors: substituted quinazolinediones and quinazolinones as potent fibrinogen receptor antagonists.
Design and synthesis of a new type of non steroidal human aromatase inhibitors.
Novel imidazole derivatives with subtype-selective antimuscarinic activity (1).
Solid-phase synthesis of potential protein tyrosine phosphatase inhibitors via the Ugi four-component condensation.
Design and synthesis of new potent C2-symmetric HIV-1 protease inhibitors. Use of L-mannaric acid as a peptidomimetic scaffold.
Novel selective orally active CRTH2 antagonists for allergic inflammation developed from in silico derived hits.
Synthesis and antiviral activity of 5-substituted cytidine analogues: identification of a potent inhibitor of viral RNA-dependent RNA polymerases.
Synthesis, biological evaluation and molecular modelling of sulfonohydrazides as selective PI3K p110alpha inhibitors.
Synthesis and antibacterial activity of some new 2,3-dimethoxy-3-hydroxy-2-(1-phenyl-3-aryl-4-pyrazolyl)chromanones.
Bioactive terpenoids from Octocorallia, I. Bioactive diterpenoids: litophynols A and B from the mucus of the soft coral Litophyton sp.
Isolation of Spongosine and 2'-Deoxyspongosine from a Western Australian Sponge of the Order Hadromerida (Tethyidae)
Graminone B, a novel lignan with vasodilative activity from Imperata cylindrica.
Thorectandrols C, D, and E, new sesterterpenes from the marine sponge Thorectandra sp.
New labdene iterpenes from Eupatorium glutinosum.
Gloiosiphones A and B, Novel Metabolites from the Red Marine Alga Gloiosiphonia verticillaris
New benzo[5,6]pyrrolizino[1,2-b]quinolines as cytotoxic agents.
A novel series of piperidin-4-yl-1,3-dihydroindol-2-ones as agonist and antagonist ligands at the nociceptin receptor.
Per-6-substituted-per-6-deoxy beta-cyclodextrins inhibit the formation of beta-amyloid peptide derived soluble oligomers.
Design and semisynthesis of novel fredericamycin A derivatives with an improved antitumor profile.
Novel inhibitors of B-RAF based on a disubstituted pyrazine scaffold. Generation of a nanomolar lead.
A minimalist design approach to antimicrobial agents based on a thionin template.
Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors.
1,2,4-Oxadiazolidin-3,5-diones and 1,3,5-triazin-2,4,6-triones as cytosolic phospholipase A2alpha inhibitors.
Synthesis and anticonvulsant activity of new N-1',N-3'-disubstituted-2'H,3H,5'H-spiro-(2-benzofuran-1,4'-imidazolidine)-2',3,5'-triones.
Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins.
Thiosemicarbazones active against Clostridium difficile.
Synthesis and antimicrobial activities of 7-O-modified genistein derivatives.
Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7.
Design, synthesis and antiproliferative activity of two new heteroannelated (-)-muricatacin mimics.
Isoprenylated naphthoquinone dimers firmianones A, B, and C from Firmiana platanifolia.
KR025, a new cytotoxic compound from Myxococcus fulvus.
Non-peptidic alpha(v)beta3 antagonists containing indol-1-yl propionic acids.
Antifolate and antibacterial activities of 5-substituted 2,4-diaminoquinazolines.
Hemoglobin S antigelation agents based on 5-bromotryptophan with potential for sickle cell anemia.
Phosphoramidate peptide inhibitors of human skin fibroblast collagenase.
Synthesis and antimalarial activity of (+)-deoxoartemisinin.
Inhibitors of human leukocyte proteinase-3.
4-substituted thiophene- and furan-2-sulfonamides as topical carbonic anhydrase inhibitors.
Copyrine alkaloids: synthesis, spectroscopic characterization, and antimycotic/antimycobacterial activity of A- and B-ring-functionalized sampangines.
Cocaine receptor: biochemical characterization and structure-activity relationships of cocaine analogues at the dopamine transporter.
3-O-alkylascorbic acids as free radical quenchers. 3. Protective effect on coronary occlusion-reperfusion induced arrhythmias in anesthetized rats.
Structure-activity relationship studies of cocaine: replacement of the C-2 ester group by vinyl argues against H-bonding and provides an esterase-resistant, high-affinity cocaine analogue.
Synthesis and anticancer activity of chromone-based analogs of lavendustin A.
Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors.
Nonpeptidic and potent small-molecule inhibitors of cIAP-1/2 and XIAP proteins.
Synthesis of substituted thieno[2,3-d]pyrimidine-2,4-dithiones and their S-glycoside analogues as potential antiviral and antibacterial agents.
Design and synthesis of Hsp90 inhibitors: exploring the SAR of Sansalvamide A derivatives.
Synthesis, stereochemical separation, and biological evaluation of selective inhibitors of human MAO-B: 1-(4-arylthiazol-2-yl)-2-(3-methylcyclohexylidene)hydrazines.
Small-molecule inhibitors of NADPH oxidase 4.
In vivo efficacy of beta-cyclodextrin derivatives against anthrax lethal toxin.
Species distribution and in vitro antifungal susceptibility patterns of 75 clinical isolates of Fusarium spp. from northern Italy.
Mechanism of hepatitis C virus RNA polymerase inhibition with dihydroxypyrimidines.
Prenylated phenolics from Ganoderma fornicatum.
Cytotoxic cycloartane triterpene saponins from Actaea asiatica.
Crassolides A-F, cembranoids with a trans-fused lactone from the soft coral Sarcophyton crassocaule.
Design and synthesis of novel 2-pyridone peptidomimetic falcipain 2/3 inhibitors.
New Tetracyclic Sesterterpenes from Cydonia vulgaris
Indole Alkaloids of Haplophyton crooksii 1
Bioactive steroidal alkaloids from Solanum umbelliferum.
Design of new topoisomerase II inhibitors based upon a quinobenzoxazine self-assembly model.
Functionalized 1,3-teraryls as a new class of hepatoprotectants. Part V.
Antitumor agents. 181. Synthesis and biological evaluation of 6,7,2',3',4'-substituted-1,2,3,4-tetrahydro-2-phenyl-4-quinolones as a new class of antimitotic antitumor agents.
(-)-6-Chloro-2-[(1-furo[2, 3-c]pyridin-5-ylethyl)thio]-4-pyrimidinamine, PNU-142721, a new broad spectrum HIV-1 non-nucleoside reverse transcriptase inhibitor.
Development of new chromanol antagonists of leukotriene D4.
Unusual synthesis of new glycine antagonists via sequential aldol condensation-lactonization-elimination reaction.
DNA cleavage potency, cytotoxicity, and mechanism of action of a novel class of enediyne prodrugs.
SAR by MS: a ligand based technique for drug lead discovery against structured RNA targets.
Mazindol analogues as potential inhibitors of the cocaine binding site at the dopamine transporter.
Inhibition of the antibacterial target UDP-(3-O-acyl)-N-acetylglucosamine deacetylase (LpxC): isoxazoline zinc amidase inhibitors bearing diverse metal binding groups.
Bacteriopurpurinimides: highly stable and potent photosensitizers for photodynamic therapy.
Synthesis and antiaggregant properties of Stabilized analogues of polyunsaturated fatty acid metabolites.
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 1: 2-Pyridinylguanidines.
Design and synthesis of fluorinated RXR modulators.
Novel inhibitors of neuronal nitric oxide synthase with potent antioxidant properties.
Geraniol-derived 1,2,4-trioxanes with potent in-vivo antimalarial activity.
A novel metal-chelating inhibitor of protein farnesyltransferase.
N-arylaminonitriles as bioavailable peptidomimetic inhibitors of cathepsin B.
Array synthesis of novel lipodepsipeptide.
Design, synthesis, and SAR study of a series of N-alkyl-N'-[2-(aryloxy)-5-nitrobenzenesulfonyl]ureas and -cyanoguanidine as selective antagonists of the TPalpha and TPbeta isoforms of the human thromboxane A2 receptor.
Principal component analysis differentiates the receptor binding profiles of three antipsychotic drug candidates from current antipsychotic drugs.
Aminoalkoxybiphenylnitriles as histamine-3 receptor ligands.
Silanediol-based inhibitor of thermolysin.
Synthesis and evaluation of imidazo[1,5-a]pyrazines as corticotropin releasing hormone receptor ligands.
Enantio-dependent binding and transactivation of optically active phenylpropanoic acid derivatives at human peroxisome proliferator-activated receptor alpha.
Design and synthesis of dual inhibitors for matrix metalloproteinase and cathepsin.
Synthesis and biological evaluation of novel thio-substituted chromanes as high-affinity partial agonists for the estrogen receptor.
Novel cyclourethane-derived HIV protease inhibitors: a ring-closing olefin metathesis based strategy.
Synthesis and cytotoxicity of 3,4-diaryl-2(5H)-furanones.
Thalidomide and its analogues as cyclooxygenase inhibitors.
Structural approach of the mechanism of inhibition of alpha-chymotrypsin by coumarins.
Enantiospecific, selective cyclooxygenase-2 inhibitors.
The synthesis of substituted fluorenes as novel non-imidazole histamine h(3) inhibitors.
Anticholinesterase activity of compounds related to geneserine tautomers. N-Oxides and 1,2-oxazines.
Novel selective PDE4 inhibitors. 3. In vivo antiinflammatory activity of a new series of N-substituted cis-tetra- and cis-hexahydrophthalazinones.
Synthesis and characterization of a series of novel monoacylated ascorbic acid derivatives, 6-O-acyl-2-O-alpha-D-glucopyranosyl-L-ascorbic acids, as skin antioxidants.
Antifungal activity of artemisinin derivatives.
Cholinergic activity of acetylenic imidazoles and related compounds.
Synthesis and biological evaluation of a series of substituted N-alkoxyimides and -amides as potential atypical antipsychotic agents.
L-687,908, a potent hydroxyethylene-containing HIV protease inhibitor.
Design of novel porphyrin-binding peptides based on antibody CDR.
The cholesterol metabolite cholest-4-en-3-one and its 3-oxo derivatives suppress body weight gain, body fat accumulation and serum lipid concentration in mice.
Preparation of alpha-keto ester enol acetates as potential prodrugs of human neutrophil elastase inhibitors.
High-throughput synthesis and direct screening for the discovery of novel hydrolytic metal complexes.
Synthesis and modeling studies of a potent conformationally rigid muscarinic agonist: 1-azabicyclo[2.2.1]heptanespirofuranone.
Quantitative structure-activity relationships of 2, 4-diamino-5-(2-X-benzyl)pyrimidines versus bacterial and avian dihydrofolate reductase.
Syntheses of new isodethiaazacephems as potent antibacterial agents.
Hydroxyphthalocyanines as potential photodynamic agents for cancer therapy.
Isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds as hypoglycemic agents.
Potent inhibitors of the MAP kinase p38.
Immunophilins: beyond immunosuppression.
Acetamidine lysine derivative, N-(5(S)-amino-6,7-dihydroxyheptyl)ethanimidamide dihydrochloride: a highly selective inhibitor of human inducible nitric oxide synthase.
Molecular features associated with polyamine modulation of NMDA receptors.
A new antitumor agent: methyl sulfonium perchlorate of echinomycin.
Novel peptidyl phosphorus derivatives as inhibitors of human calpain I.
Stereoisomers of cyclic urea HIV-1 protease inhibitors: synthesis and binding affinities.
Optimization of 3-(phenylthio)quinolinium compounds against opportunistic fungal pathogens.
Homoflavonoid glucosides from Ophioglossum pedunculosum and their anti-HBV activity.
Identification and initial SAR of silybin: an Hsp90 inhibitor.
Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449).
Bioactive sesqui- and diterpenoids from the Argentine liverwort Porella chilensis.
Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells.
Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Targeting the c-Kit Promoter G-quadruplexes with 6-Substituted Indenoisoquinolines.
Phylogeny-guided isolation of ethyl tumonoate A from the marine cyanobacterium cf. Oscillatoria margaritifera.
Yojironins E-I, prenylated acylphloroglucinols from Hypericum yojiroanum.
Identification of a series of 4-[3-(quinolin-2-yl)-1,2,4-oxadiazol-5-yl]piperazinyl ureas as potent smoothened antagonist hedgehog pathway inhibitors.
Amine-constrained pyridazinone histamine H3 receptor antagonists.
A fast virtual screening approach to identify structurally diverse inhibitors of trypanothione reductase.
Synthesis and antiviral evaluation of -L-2'-deoxythreofuranosyl nucleosides.
Bioactive prenylogous cannabinoid from fiber hemp (Cannabis sativa).
N-Arylalkyl-2-azaadamantanes as cage-expanded polycarbocyclic sigma () receptor ligands.
Design and syntheses of melanocortin subtype-4 receptor agonists: evolution of the pyridazinone archetype.
Stereoselective synthesis of desloratadine derivatives as antagonist of histamine.
Homoisoflavonoids from the fibrous roots of Polygonatum odoratum with glucose uptake-stimulatory activity in 3T3-L1 adipocytes.
Discovery of anti-inflammatory clinical candidate E6201, inspired from resorcylic lactone LL-Z1640-2, III.
Bioactive triterpenoids from Salvia species.
2-Aminobenzophenones as a novel class of bradykinin B1 receptor antagonists.
Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs.
5'-O-dephosphorylated 2',5'-oligoadenylate (2-5A) with 8-methyladenosine at the 2'-terminus activates human RNase L.
In-vivo analgesic and anti-inflammatory activities of newly synthesized benzimidazole derivatives.
Highly oxygenated monoterpene acylglucosides from Spiraea cantoniensis.
A repurposing strategy identifies novel synergistic inhibitors of Plasmodium falciparum heat shock protein 90.
Imidazoacridin-6-ones as novel inhibitors of the quinone oxidoreductase NQO2.
Discovery and structural optimization of pyrazole derivatives as novel inhibitors of Cdc25B.
Amphimedosides, 3-alkylpyridine glycosides from a marine sponge Amphimedon sp.
Bohemamines from a marine-derived Streptomyces sp.
Ashwagandhanolide, a bioactive dimeric thiowithanolide isolated from the roots of Withania somnifera.
Xenofuranones A and B: phenylpyruvate dimers from Xenorhabdus szentirmaii.
Cactus Alkaloids. XXXIX. A Glucotetrahydroiosquinoline From the Mexican Cactus, Pterocereus gaumeri
Isolation of Diterpenoids of the Cladiellane Class from Gorgonians of the Genus Muricella
10-Epi-olguine from Rabdosia ternifolia.
Gloeolactone, a New Epoxy Lactone from a Blue-Green Alga
Cytotoxic polyacetylenes from the marine sponge Petrosia sp.
Stereoselective total synthesis of (3R,8S)-falcarindiol, a common polyacetylenic compound from umbellifers
A beta-carboline alkaloid from the soft coral lignopsis spongiosum
4-(2-Aminoethoxy)-N-(phenylsulfonyl)indoles as novel 5-HT6 receptor ligands.
Posaconazole enhances the activity of amphotericin B against Aspergillus hyphae in vitro.
Phenylglycine and phenylalanine derivatives as potent and selective HDAC1 inhibitors (SHI-1).
5-tert-butyl-N-pyrazol-4-yl-4,5,6,7-tetrahydrobenzo[d]isoxazole-3-carboxamide derivatives as novel potent inhibitors of Mycobacterium tuberculosis pantothenate synthetase: initiating a quest for new antitubercular drugs.
Neovibsanin F and its congeners, rearranged vibsane-type diterpenes from Viburnum suspensum.
New triterpenoid saponins from the sponge Melophlus isis.
Identification of 4-methyl-1,2,3,4,10,10a-hexahydropyrazino[1,2-a]indoles as 5-HT2C receptor agonists.
Discovery and SAR of biaryl piperidine MCH1 receptor antagonists through solid-phase encoded combinatorial synthesis.
Synthesis and antibacterial activity of alkyl derivatives of the glycopeptide antibiotic A40926 and their amides.
Hepatitis C virus NS3-4A serine protease inhibitors: use of a P2-P1 cyclopropyl alanine combination for improved potency.
Structure-activity relationship study to understand the estrogen receptor-dependent gene activation of aryl- and alkyl-substituted 1H-imidazoles.
Hyrtinadine A, a bis-indole alkaloid from a marine sponge.
Clavaminols A-F, novel cytotoxic 2-amino-3-alkanols from the ascidian Clavelina phlegraea.
Fluorinated dihydroquinolines as potent n-NOS inhibitors.
Synthesis and antiproliferative activity of 2-aryl-4-oxo-thiazolidin-3-yl-amides for prostate cancer.
2,3,4-Trimethyl-5,7-dihydroxy-2,3-dihydrobenzofuran, a novel antioxidant, from Penicillium citrinum F5.
Anti-inflammatory activity of two flavonoids from Tanacetum microphyllum.
Kulokekahilide-2, a cytotoxic depsipeptide from a cephalaspidean mollusk Philinopsis speciosa.
Inhibition of cytokine production by hymenialdisine derivatives.
Synthesis and antitumor activity of quinonoid derivatives of cannabinoids.
Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.
Parallel solution-phase synthesis of conformationally restricted congeners of pentamidine and evaluation of their antiplasmodial activities.
Benzoxazinones as PPARgamma agonists. 2. SAR of the amide substituent and in vivo results in a type 2 diabetes model.
Design and synthesis of heterocyclic malonyl-CoA decarboxylase inhibitors.
Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.
Beta- and gamma-di- and tripeptides as potential substrates for the oligopeptide transporter hPepT1.
Discovery of thienopyridines as Src-family selective Lck inhibitors.
Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARalpha/gamma dual agonists.
The Ichthyotoxic Principles of Zanthoxylum clava-herculis
Anthraquinones and a 10-Hydroxyanthrone from Phialophora alba
An antifungal polyacetylenic compound from the culture filtrate of the fungus Trametes pubescens.
A Sesquiterpene Quinone and Hydroquinone from the Southern Australian Marine Sponge, Thorecta choanoides
Selective optimization of side activities: another way for drug discovery.
Porphyrin-DNA cross-linking agent hybrids: chemical synthesis and biological studies.
Synthesis and antitubercular activity of 2-hydroxy-aminoalkyl derivatives of diaryloxy methano phenanthrenes.
Biaryls and heterobiaryls as alpha-glucosidase and protein tyrosine phosphatase inhibitors.
Synthesis and evaluation of azalanstat analogues as heme oxygenase inhibitors.
Isatin--thiosemicarbazones as potent herpes simplex virus inhibitors.
Antidotes to anthrax lethal factor intoxication. Part 2: structural modifications leading to improved in vivo efficacy.
Discovery of a piperazine urea based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor partial agonist.
Diphenylamine-based retinoid antagonists: regulation of RAR and RXR function depending on the N-substituent.
Synthesis of a new 4-aza-2,3-didehydropodophyllotoxin analogues as potent cytotoxic and antimitotic agents.
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
Inhibitory effects of Mannich bases of heterocyclic chalcones on NO production by activated RAW 264.7 macrophages and superoxide anion generation and elastase release by activated human neutrophils.
Synthesis and biological evaluation of orally active prodrugs of indomethacin.
Per-N-methylated analogues of an antitumor bicyclic hexapeptide RA-VII.
In vitro characterization of human peptide transporter hPEPT1 interactions and passive permeation studies of short cationic antimicrobial peptides.
Synthesis of novel 3-carboxamide-benzocoumarin derivatives as orally active antithrombotic agents.
Stereoselective synthesis of (RP)-8-substituted-N6-acylated and N6-alkylated adenosine-3',5'-cyclic phosphorothioic acids as cAMP antagonists.
Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: identification of the cycloalkylcarboxylic acids.
Evaluation of new chalcone derivatives as polyphenol oxidase inhibitors.
A small molecule that preferentially binds the closed conformation of Hsp90.
Cytotoxic and antiplatelet aggregation principles from Aglaia elliptifolia.
Tyromycic acids B-E, new lanostane triterpenoids from the mushroom Tyromyces fissilis.
New cytotoxic naphthopyrane derivatives from Adenaria floribunda.
Acaricidal activity of tonka bean extracts. Synthesis and structure-activity relationships of bioactive derivatives.
Synthesis, in vitro affinity, and efficacy of a bis 8-ethynyl-4H-imidazo[1,5a]- [1,4]benzodiazepine analogue, the first bivalent alpha5 subtype selective BzR/GABA(A) antagonist.
Kringle 5 peptide-albumin conjugates with anti-migratory activity.
Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.
4-Amino cyclohexylglycine analogues as potent dipeptidyl peptidase IV inhibitors.
Cycloalkyl[b][1,4]benzodiazepinoindoles are agonists at the human 5-HT2C receptor.
The effect of C2-fluoro group on the biological activity of DC-81 and its dimers.
Synthesis and evaluation of spirobenzazepines as potent vasopressin receptor antagonists.
Antibacterial activity of pyrrolopyridine-substituted oxazolidinones: synthesis and in vitro SAR of various C-5 acetamide replacements.
Modafinil enhances thalamocortical activity by increasing neuronal electrotonic coupling.
Dammarane triterpenoids from the roots of Gentiana rigescens.
9-(2-C-Cyano-2-deoxy-beta-D-arabino-pentofuranosyl)guanine, a potential antitumor agent against B-lymphoma infected with Kaposi's sarcoma-associated herpesvirus.
Potent and selective bicyclic lactam inhibitors of thrombin: Part 2: P1 modifications.
Synthesis and biological evaluation of two analogues of (S)-alpha-methyl-3-carboxyphenylalanine.
A potent, orally bioavailable benzazepinone growth hormone secretagogue.
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa.
The structure-based design and synthesis of selective inhibitors of Trypanosoma cruzi dihydrofolate reductase.
Synthesis and in vitro evaluation of 7-dialkylaminomethylbenzo[g]quinoxaline-5,10-diones.
Synthesis and evaluation of pyridazinylpiperazines as vanilloid receptor 1 antagonists.
Synthesis and biological evaluation of photoaffinity labeled fusidic acid analogues.
Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
Synthesis, in vitro inhibitory activity towards COX-2 and haemolytic activity of derivatives of esculentoside A.
8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes.
PDE5 inhibitors: An original access to novel potent arylated analogues of tadalafil.
Synthesis, activity, and pharmacophore development for isatin-beta-thiosemicarbazones with selective activity toward multidrug-resistant cells.
Analgesic narcotic antagonists. 4. 7-Methyl-N-(cycloalkylmethyl)-3-hydroxymorphinan-6-ones and -isomorphinan-6-ones.
Prostaglandin analogues possessing antinidatory effects. 2. Modification of the alpha chain.
Synthesis and antineoplastic activity of phenyl-substituted benzenesulfonylhydrazones of 2-pyridinecarboxyaldehyde 1-oxide.
Synthesis and antiinflammatory activity of some 2-(substituted-pyridinyl)benzimidazoles.
Pyrazolo[5,1-b]quinazolin-9-ones: a new series of antiallergic agents.
Antiinflammatory 5,6-dihydro-11-oxodibenz[b,e]azepine-3-acetic acids.
Synthesis and evaluation of some stable multisubstrate adducts as inhibitors of catechol O-methyltransferase.
Cell-specific ligands for selective drug delivery to tissues and organs.
Inhibition of antiassociation activity of translation initiation factor 3 by paromomycin.
Efficient inhibition of iron superoxide dismutase and of Trypanosoma cruzi growth by benzo[g]phthalazine derivatives functionalized with one or two imidazole rings.
Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists.
New antitumor imidazo[2,1-b]thiazole guanylhydrazones and analogues.
Rhodanine derivatives as novel inhibitors of PDE4.
NF-kappaB-inhibiting naphthopyrones from the Fijian echinoderm Comanthus parvicirrus.
Linezolid (ZYVOX), the first member of a completely new class of antibacterial agents for treatment of serious gram-positive infections.
A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol.
Prenylflavonoids and phloroglucinol derivatives from hops (Humulus lupulus).
Identification of 3-(acylamino)azepan-2-ones as stable broad-spectrum chemokine inhibitors resistant to metabolism in vivo.
Prostatic acid phosphatase in cloacal derivatives.
Lp-PLA2 inhibitory activities of fatty acid glycerols isolated from Saururus chinensis roots.
C-2 desmethyl seco-mevinic acids. Monocyclic HMG-CoA reductase inbibitors
Synthesis, antibacterial activities, and pharmacological properties of enantiomers of temafloxacin hydrochloride.
Thromboxane receptor antagonism combined with thromboxane synthase inhibition. 1. (+/-)-(3-pyridinylbicycloheptyl)alkanoic acids.
Peptide leukotrienes: current status of research.
Preparation of the geometric isomers of DDC, DDA, D4C and D4T as potential anti-HIV agents
Prevention of human leukocyte elastase-mediated lung damage by 3-alkyl-4-azetidinones
Monodeoxy-1,4:3,6-dianhydrohexitol nitrates
A concise synthesis of 12-(3'-hydroxy-n-propyl)-deoxoartemisinin
Phosphinic acid inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme a reductase
Preparation and evaluation of optically active 4,4-difluorothreonine as a potent novel antitumor material
Keto C-glycosides. a new class of antitumor compounds
Preparation and evaluation of some hydrophilic phenylacetyl-piperazines as peripherally selective -opioid receptor agonists
Synthesis and biological activity of a 5,6-substituted teleocidin
Stereoselective synthesis of hydroxylated bifenthrin isomers
Oral hypoglycemic agents. Pyrimido[1,2-a]indoles and related compounds.
Anti-HIV-I activity of linked lexitropsins.
Effects of inoculum, pH, and cations on the in vitro activity of fidaxomicin (OPT-80, PAR-101) against Clostridium difficile.
Mutant prevention concentrations of four carbapenems against gram-negative rods.
Characterization of CSP-1, a novel extended-spectrum beta-lactamase produced by a clinical isolate of Capnocytophaga sputigena.
The M230L nonnucleoside reverse transcriptase inhibitor resistance mutation in HIV-1 reverse transcriptase impairs enzymatic function and viral replicative capacity.
In vitro activity of telavancin against a contemporary worldwide collection of Staphylococcus aureus isolates.
Neopetrosiamine A, biologically active bis-piperidine alkaloid from the Caribbean sea sponge Neopetrosia proxima.
Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: selection of the scaffold.
Novel pyrrole- and 1,2,3-triazole-based 2,3-oxidosqualene cyclase inhibitors.
Optimization of N-benzyl-benzoxazol-2-ones as receptor antagonists of macrophage migration inhibitory factor (MIF).
Lupane triterpenoids from Maytenus species.
Elgonica-Dimers A and B, Two Potent Alcohol Metabolism Inhibitory Constituents of Aloe arborescens
A new P-glycoprotein inhibitor from the caper spurge (Euphorbia lathyris).
2,3,4-Tribromopyrrole from the Marine Polychaete Polyphysia crassa
The Effect of Aridanin Isolated from Tetrapleuratetraptera and Serotonin on the Isolated Gastrointestinal Tract Smooth Muscles of Biomphalaria glabrata and Uptake of Calcium
3'-Formyl-2',4',6'-trihydroxy-5'-methyldihydrochalcone, a Prospective New Agrochemical from Psidium acutangulum
Four Novel Diterpenoids: Clavirolides B, C, D, and E from the Chinese Soft Coral Clavularia viridis
The Structure of Clathrodin, a Novel Alkaloid Isolated from the Caribbean Sea Sponge Agelas clathrodes
Antimicrobial N-methylpyridinium salts related to the xestamines from the Caribbean sponge Calyx podatypa.
Cytotoxic norditerpene lactones from Ileostylus micranthus.
Inhibitory effect of tannic acid on gastric H+,K(+)-ATPase.
Synthesis and biological evaluation of antitumour-active betulin derivatives.
Discovery and SAR of small molecule PAR1 antagonists.
Novel 3-aminopyrazole inhibitors of MK-2 discovered by scaffold hopping strategy.
A small library of peptidomimetics to systematically vary and test the effects of X1 constraints
3-Amidinophenylalanine-based inhibitors of urokinase.
Dicationic 2-fluorenonylcarbapenems: potent anti-MRS agents with improved solubility and pharmacokinetic properties.
Synthesis and thromboxane A2 antagonistic activity activity of indane derivatives.
Reversal of P-glycoprotein mediated multidrug resistance by novel anthranilamide derivatives.
Isoquinoline-6-carboxamides as potent and selective anti-human cytomegalovirus (HCMV) inhibitors.
Synthesis and antitumor activity of novel thioester derivatives of leinamycin.
gamma-Aminobutyrate-A receptor modulation by 3-aryl-1-(arylsulfonyl)- 1,4,5,6-tetrahydropyridazines.
Imidazopyrimidines, potent inhibitors of p38 MAP kinase.
Unexpected inhibition of S-adenosyl-L-homocysteine hydrolase by a guanosine nucleoside.
Discovery of orally bioavailable NK1 receptor antagonists.
Synthesis and structure--activity relationships of aroylpyrrole alkylamide bradykinin (B2) antagonists.
Tripeptide probes for tripeptidyl protease I production via gene transfer.
Methoxylation of desazadesferrithiocin analogues: enhanced iron clearing efficiency.
1,3-dioxolane-based ligands as a novel class of alpha1-adrenoceptor antagonists.
Synthesis and biological evaluation of novel cyclosporin a analogues: potential soft drugs for the treatment of autoimmune diseases.
A new synthesis of cytoxazone and its diastereomers provides key initial SAR information.
Design and optimization of renin inhibitors: Orally bioavailable alkyl amines.
Discovery of 4-anilino-N-methylthieno[3,2-d]pyrimidines and 4-anilino-N-methylthieno[2,3-d]pyrimidines as potent apoptosis inducers.
Synthesis of 7 alpha- and 7 beta-spermidinylcholesterol, squalamine analogues.
Syntheses and activities of antioxidant derivatives of retinoic acids.
Sparsophenicol: a new synthetic hybrid antibiotic inhibiting ribosomal peptide synthesis.
Darmstoff analogues. 2. Ring and side-chain effects on smooth-muscle contraction.
Synthesis of N-(carbonylamino)-1,2,3,6-tetrahydropyridines with analgesic, antiinflammatory, and hyperglycemic activity.
Species- or isozyme-specific enzyme inhibitors. 4. Design of a two-site inhibitor of adenylate kinase with isozyme selectivity.
Beta-carbolines: synthesis and neurochemical and pharmacological actions on brain benzodiazepine receptors.
Retinoids at the threshold: their biological significance and therapeutic potential.
Synthesis, biological evaluation, and binding mode of novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles targeted at the HIV-1 reverse transcriptase.
Structure-based design and synthesis of 2-benzylidene-benzofuran-3-ones as flavopiridol mimics.
2-Amino-4-[3'-hydroxyphenyl]-4-hydroxybutanoic acid; a potent inhibitor of rat and recombinant human kynureninase.
Highly potent inhibitors of TNF-alpha production. Part 2: identification of drug candidates.
1H-Pyrazolo[3,4-b]pyridine inhibitors of cyclin-dependent kinases: highly potent 2,6-Difluorophenacyl analogues.
The imidazo[2,1-a]isoindole system. A new skeletal basis for antiplasmodial compounds.
Pyrrolo[2,3-h]quinolinones: synthesis and photochemotherapic activity.
Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists.
Identification of potent and novel small-molecule inhibitors of caspase-3.
Photoregulation of deacylation rate of acyl trypsin derived from photoresponsive inverse substrate.
Solid-phase synthesis of endothelin receptor antagonists.
Novel bicyclic furanopyrimidines with dual anti-VZV and -HCMV activity.
Phenothiazine and phenoxazine derivatives of nafazatrom. In vitro evaluation as 5-lipoxygenase and iron-dependent lipid peroxidation inhibitors.
Dual-acting thromboxane receptor antagonist/synthase inhibitors: heterocyclic variations
Phosphonoethylphenylalanine derivatives as novel antagonists of non-NMDA ionotropic glutamate receptors
Synthesis and pharmacological activity of rationally designed inhibitors of the leukotriene A4 hydrolase enzyme
Carbocyclic phosphonate analogs of 2,3-dideoxyadenosine-5-monophosphate as substrates of 5-phosphoribosyl-1-pyrophosphate (PRPP) synthetate
Substrate selectivity of imidazole-appended dimethyl--cyclodextrin
Use of transferred nuclear overhauser effects to determine the conformation of 1-(3,4-dichlorophenyl)-2-aminopropane when bound to the active site of phenylethanolamine N-methyltransferace (PNMT)
Synthesis of acid stable 5-o-fluoromethyl phosphonates of nucleosides. Evaluation as inhibitors of reverse transcriptase.
The design and biological evaluation of a series of 3-hydroxy-3-methylglutaryl coenzyme a (HMG-CoA) reductase inhibitors related to dihydromevinolin.
Synthesis and HIV activity of phosphonate isosteres of D4T monophosphate
Design and synthesis of novel ligands for the 5-HT3 and the 5-HT4 receptor
The role of arginine in interactions of microcystins with protein phosphatases 1 and 2a
DNA alkylation properties of the duocarmycins: (+)-duocarmycin A, epi-(+)-duocarmycin A, ent-()-duocarmycin A and epi,ent-()-duocarmycin A
Synthesis and biological activity of putative mono-hydroxylated metabolites of velnacrine
Synthesis of novel targeted pro-prodrugs of anthracyclines potentially activated by a monoclonal antibody galactosidase conjugate (part 1)
Discovery of dual activity molecules with thromboxane antagonist and thromboxane synthase inhibitory activity
Synthesis of a potent and selective non-peptide CCK-B/gastrin receptor antagonist tritiated ligand.
Backbone modified formyl-methionyl tripeptide chemoattractants
New potent angiotensin II receptor antagonists containing phenylthiophenes and phenylfurans in place of the biphenyl moiety.
Enhancement of binding of quaternary ammonium derivatives of chlorpromaxine to dopamine D-2 receptors by the addition of a H-bonding group
Synthesis and antitumor evaluation of water soluble taxol phosphates
Cyclic ether acetal platelet activating factor (PAF) receptor antagonists II: imidazo[4,5-c]pyridyl derivatives
Synthesis of N-Acetylhemiaminal metabolites of opc-21268, vasopressin V1 receptor antagonist
Synthesis and evaluation of 3-carboxymethyl steroids as inhibitors of human prostatic steroid 5-reductase
Synthesis and dopamine antagonist activity of 2-thioether derivatives of the ergoline ring system.
Intracellular delivery of bioactive AZT nucleotides by aryl phosphate derivatives of AZT.
Synthesis and evaluation of the antitumor activity of 4,5-diamino-substituted 1,2-benzoquinones.
Azaindole derivatives with high affinity for the dopamine D4 receptor: synthesis, ligand binding studies and comparison of molecular electrostatic potential maps.
Asymmetric synthesis of L-azetidine-2-carboxylic acid and 3-substituted congeners--conformationally constrained analogs of phenylalanine, naphthylalanine, and leucine.
A substrate combinatorial array for caspases.
Ring E analogs of methyllycaconitine (MLA) as novel nicotinic antagonists.
Synthesis of bisquinolines and their in vitro ability to produce methemoglobin in canine hemolysate.
On topography and functionality in the B-D rings of cephalostatin cytotoxins.
Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.
Highly potent inhibitors of the Grb2-SH2 domain.
Synthesis of novel analogues of the delta opioid ligand SNC-80 using AlCl3-promoted aminolysis.
Structure-activity relationship of small-sized HIV protease inhibitors containing allophenylnorstatine.
Cross-linking and sequence-specific alkylation of DNA by aziridinylquinones. 3. Effects of alkyl substituents.
New prenylflavones from the leaves of Epimedium saggitatum.
Antiplatelet arylnaphthalide lignans from Justicia procumbens.
Isolation of New Steroidal Hemiacetals from the Gorgonian Euplexaura anastomosans
New Terpenylated Dihydrochalcone Derivatives Isolated from Mitrella kentii
Insect Antifeedant Isoryanodane Diterpenes from Persea indica
The discovery of a structurally novel class of inhibitors of the type 1 glycine transporter.
Recent advances in the development of polyamine analogues as antitumor agents.
Antibacterial activities of aminoglycoside antibiotics-derived cationic amphiphiles. Polyol-modified neomycin B-, kanamycin A-, amikacin-, and neamine-based amphiphiles with potent broad spectrum antibacterial activity.
Synthesis and molecular modeling studies of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones as novel anti-filarial agents.
Conversion of ergolines to hexahydro- and octahydrobenzo[f]quinolines (depyrroloergolines).
Synthesis and biological activity of some 15-oxaestranes.
Conformationally restricted tricyclic antidepressants. 1. Octahydrodibenzazepinonaphthyridines as rigid imipramine analogues.
Potential Antitumor Agents: A Cytotoxic Cardenolide From Coronilla varia
Plant anticancer agents X. Isolation of camptothecin and 9-methoxycamptothecin from Ervatamia heyneana.
Celenamide E, a Tripeptide Alkaloid from the Patagonian Sponge Cliona chilensis
Aurilol, a Cytotoxic Bromotriterpene Isolated from the Sea Hare Dolabella auricularia
Sesquiterpenoids and plasmin-inhibitory flavonoids from Blumea balsamifera.
Structure-activity relationship of 2,4,5-trioxoimidazolidines as inhibitors of thymidine phosphorylase.
Discovery and SAR of spirochromane Akt inhibitors.
Synthesis and anticancer activities of some novel 2-(benzo[d]thiazol-2-yl)-8-substituted-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones.
Structure-based virtual screening approach to the discovery of phosphoinositide 3-kinase alpha inhibitors.
Substituted phenyl triazoles as selective inhibitors of 11-Hydroxysteroid Dehydrogenase Type 1.
Synthesis, cytotoxicity and topoisomerase inhibition properties of multifarious aminoalkylated indeno[1,2-c]isoquinolin-5,11-diones.
In vitro anticancer activity and evaluation of DNA duplex binding affinity of phenyl-substituted indoloquinolines.
Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents.
Peroxisome proliferator-activated receptor alpha/gamma dual agonists for the treatment of type 2 diabetes.
Efficient evaluation of binding free energy using continuum electrostatics solvation.
Configurationally restricted bismacrocyclic CXCR4 receptor antagonists.
Synthesis of 1-deoxy-1-hydroxymethyl- and 1-deoxy-1-epi-hydroxymethyl castanospermine as new potential immunomodulating agents.
Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists.
Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203).
Isolation of Isodrimenediol, a Possible Intermediate of Drimane Biosynthesis from Polyporus arcularius
Isolation and structure of leukotriene-A4 hydrolase inhibitor: 8(S)-amino-2(R)-methyl-7-oxononanoic acid produced by Streptomyces diastaticus.
Progress in the discovery of biosynthetic anticancer drugs.
New Oxygenated Cephalotaxus Alkaloids from Cephalotaxus harringtonia var. drupacea
Cytotoxic Degradation Product of Physostigmine
Hirtellanines A and B, a pair of isomeric isoflavonoid derivatives from Campylotropis hirtella and their immunosuppressive activities.
Synthesis and evaluation of 4-acyl-2-thiazolylhydrazone derivatives for anti-Toxoplasma efficacy in vitro.
Paecilosetin, a new bioactive fungal metabolite from a New Zealand isolate of Paecilomyces farinosus.
Cytotoxic activity of some natural and synthetic guaianolides.
Meroterpenes from the ascidian Aplidium aff. densum.
New Stemodane Diterpenes from Stemodia maritima
Anti-influenza virus effect of some propolis constituents and their analogues (esters of substituted cinnamic acids).
Isolation of the bioactive terpene 7-deacetoxy-olepupuane from the temperate marine sponge Dysidea sp.
Isolation of Latrunculin A, 6,7-Epoxylatrunculin A, Fijianolide A, and Euryfuran from a New Genus of the Family Thorectidae
4-(2-PYRTOYL)-5-phenylthiazoles as novel non-bicyclic reversible inhibitors of the gastric H+/K+-atpase
Synthesis of new potent leukotriene B4 antagonists and their biological properties. 2.
Synthesis and biological activities of truncated acridone: Structure-activity relationship studies of cytotoxic 5-hydroxy-4-quinolone
Unsaturated epoxy-C-glycosides. A new class of antitumor compounds with DNA cleavage properties.
Thiophenoxy peptides: A new class of HIV replication inhibitors
SAR of cocaine: further exploration of structural variations at the C-2 center provides compounds of subnanomolar binding potency
Determination of the active conformation of 6-amino--[(4-diphenylmethyl-1-piperazinyl)methyl-9H-purine]-9-ethanol: a positive inotropic agent
A prolyl endopeptidase-inhibiting benzofuran dimer from Polyozellus multiflex.
Nitric oxide inhibitory isopimarane-type diterpenes from Orthosiphon stamineus of Indonesia.
(Z)-sarcodictyin A, a new highly cytotoxic diterpenoid from the soft coral Bellonella albiflora.
Synthesis of 6-formyl-pyridine-2-carboxylate derivatives and their telomerase inhibitory activities.
Substituted 4-methylquinolines as a new class of anti-tuberculosis agents.
Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.
Two-carbon-elongated HIV-1 protease inhibitors with a tertiary-alcohol-containing transition-state mimic.
Potent inhibitors of the hedgehog signaling pathway.
Design, synthesis and preliminary pharmacological evaluation of new piperidine and piperazine derivatives as cognition-enhancers.
The translocator protein (18 kDa): central nervous system disease and drug design.
Effects of 5'-phosphate derivatives of 2-hexynyl adenosine and 2-phenylethynyl adenosine on responses of human platelets mediated by P2Y receptors.
Pyridinium-1-yl bisphosphonates are potent inhibitors of farnesyl diphosphate synthase and bone resorption.
Discovery of a new class of 4-anilinopyrimidines as potent c-Jun N-terminal kinase inhibitors: Synthesis and SAR studies.
Efficacy of tachyplesin III, colistin, and imipenem against a multiresistant Pseudomonas aeruginosa strain.
New terpenoids from Maytenus apurimacensis as MDR reversal agents in the parasite Leishmania.
New iodoreboxetine analogues for SPECT imaging of the noradrenaline transporter.
Design, synthesis and structure-activity relationship of simple bis-amides as potent inhibitors of GlyT1.
Identification of chemokine receptor CCR4 antagonist.
Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors.
Virtual screening for Raf-1 kinase inhibitors based on pharmacophore model of substituted ureas.
Evaluation of PMF scoring in docking weak ligands to the FK506 binding protein.
New 4-aminoquinoline Mannich base antimalarials. 1. Effect of an alkyl substituent in the 5'-position of the 4'-hydroxyanilino side chain.
Synthesis and biological activity of sulfonamide derivatives of epipodophyllotoxin.
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
A structure-guided approach to an orthogonal estrogen-receptor-based gene switch activated by ligands suitable for in vivo studies.
Conjugated indole-imidazole derivatives displaying cytotoxicity against multidrug resistant cancer cell lines.
Synthesis and anti-influenza activities of carboxyl alkoxyalkyl esters of 4-guanidino-Neu5Ac2en (zanamivir).
Development of oligoarginine-drug conjugates linked to new peptidic self-cleavable spacers toward effective intestinal absorption.
Inhibition of 15-lipoxygenase-catalysed oxygenation of arachidonic acid by substituted benzoic acids.
DNA threading bis(9-aminoacridine-4-carboxamides): effects of piperidine sidechains on DNA binding, cytotoxicity and cell cycle arrest.
Steroids and flavonoids from Physalis alkekengi var. franchetii and their inhibitory effects on nitric oxide production.
A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects.
Aurocitrin and related polyketide metabolites from the wood-decay fungus Hypocrea sp. BCC 14122.
Ring size effect in the PKC inhibitory activities of perhydroazepine analogs of balanol
Chemistry of Sponges, X. New Sesquiterpenes from a Marine Sponge of the Genus Eurypon
Two new brominated tyrosine derivatives from the sponge Druinella (= Psammaplysilla) purpurea.
Apotirucallane Triterpenes from Dysoxylum roseum
Synthesis of a novel lysophosphatidylcholine.
Synthesis and antifungal activity of new azole derivatives containing an oxathiane ring
Tetraazaacenaphthene, tetraazaphenalene and 1,3,4-thiadiazole derivatives as potential leishmanicides
Structures of new dammarane-type Triterpene Saponins from the flower buds of Panax notoginseng and hepatoprotective effects of principal Ginseng Saponins.
9,10-secosteroids, protein kinase inhibitors from the Chinese gorgonian Astrogorgia sp.
Design, synthesis, biophysical and biological studies of trisubstituted naphthalimides as G-quadruplex ligands.
Discovery of small molecules that enhance astrocyte differentiation in rat fetal neural stem cells.
Carbamates of 4'-demethyl-4-deoxypodophyllotoxin: synthesis, cytotoxicity and cell cycle effects.
Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator.
Bacterial production of the tunicate-derived antitumor cyclic depsipeptide didemnin B.
Synthesis and biological evaluation of arylated novobiocin analogs as Hsp90 inhibitors.
Dirlotapide as a model substrate to refine structure-based drug design strategies on CYP3A4-catalyzed metabolism.
Structure-activity relationships for naturally occurring coumarins as -secretase inhibitor.
Inhibition of noroviruses by piperazine derivatives.
In vitro activity of ceftaroline against 623 diverse strains of anaerobic bacteria.
New mutation in 23S rRNA gene associated with high level of azithromycin resistance in Neisseria gonorrhoeae.
In vitro activity of penem-1 in combination with beta-lactams against blaKPC-possessing Klebsiella pneumoniae isolates.
Novel FKS mutations associated with echinocandin resistance in Candida species.
Lack of a clinically relevant effect of an antacid on the pharmacokinetics of lersivirine.
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
Efflux pumps, OprD porin, AmpC beta-lactamase, and multiresistance in Pseudomonas aeruginosa isolates from cystic fibrosis patients.
Synthesis and pharmacological evaluation of novel 5-substituted-1-(phenylsulfonyl)-2-methylbenzimidazole derivatives as anti-inflammatory and analgesic agents.
Synthesis, characterization and antihypertensive activity of pyridazinone derivatives.
New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity.
Hyperatomarin, an antibacterial prenylated phloroglucinol from Hypericumatomarium ssp. degenii.
Two new quassinoids from Simaba multiflora fruits.
Isolation Of A Novel Cytotoxic Polyacetylene From A Traditional Anthelmintic Medicinal Plant, Minquartia guianensis
Inhibitory Substances from Myriophyllum brasiliense on Growth of Blue-Green Algae
New Chlorophyll-A-Related Compounds Isolated as Antioxidants from Marine Bivalves
Two bioactive pterocarpans from Erythrina burana.
Aminomethylpyridines as DPP-IV inhibitors.
Synthesis and nicotinic acetylcholine receptor binding affinities of 2- and 3-isoxazolyl-8-azabicyclo[3.2.1]octanes.
Biaryl amide glucagon receptor antagonists.
Respiratory syncytial virus inhibitors. Part 2: Benzimidazol-2-one derivatives.
Novel non-peptidic neuropeptide Y Y2 receptor antagonists.
Design and synthesis of novel small molecule N/OFQ receptor antagonists.
Design and synthesis of 8-octyl-benzolactam-V9, a selective activator for protein kinase C epsilon and eta.
HIV integrase inhibitors with nucleobase scaffolds: discovery of a highly potent anti-HIV agent.
A new chemical tool for exploring the physiological function of the PDE2 isozyme.
Substituted pyrrolidine-2,4-dicarboxylic acid amides as potent dipeptidyl peptidase IV inhibitors.
Suzuki-type Pd(0) coupling reactions in the synthesis of 2-arylpurines as Cdk inhibitors.
In vitro efficiency of new acridyl derivatives against Plasmodium falciparum.
Caffeoylglycolic and caffeoylamino acid derivatives, halfmers of L-chicoric acid, as new HIV-1 integrase inhibitors.
Phenylguanidines as selective nonpeptide melanocortin-5 receptor antagonists.
Tryptamine-based human beta3-adrenergic receptor agonists. Part 1: SAR studies of the 7-position of the indole ring.
Novel arylsulfoanilide-oxindole hybrid as an anticancer agent that inhibits translation initiation.
A novel antiproliferative agent, phenylpyridineylbutenol, isolated from Streptomyces sp.
Discovery of novel triazole-based opioid receptor antagonists.
Discovery of 3-arylpropionic acids as potent agonists of sphingosine-1-phosphate receptor-1 (S1P1) with high selectivity against all other known S1P receptor subtypes.
Pyrazole-based factor Xa inhibitors containing N-arylpiperidinyl P4 residues.
Identification, synthesis, and biological evaluation of novel pyrazoles as low molecular weight luteinizing hormone receptor agonists.
Structure-activity relationship studies of a new series of imidazo[2,1-f]purinones as potent and selective A(3) adenosine receptor antagonists.
Diarylimidazolyl oxadiazole and thiadiazole derivatives as cannabinoid CB1 receptor antagonists.
Notoamides F-K, prenylated indole alkaloids isolated from a marine-derived Aspergillus sp.
New derivatives of farnesylthiosalicylic acid (salirasib) for cancer treatment: farnesylthiosalicylamide inhibits tumor growth in nude mice models.
Syntheses and anti-depressant activity of 5-amino-1, 3, 4-thiadiazole-2-thiol imines and thiobenzyl derivatives.
Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library.
Studies on v-triazoles. 7. Antiallergic 9-oxo-1H,9H-benzopyrano[2,3-d]-v-triazoles.
11,12-secoprostaglandins. 6. Interphenylene analogues of acylhydroxyalkanoic acids and related compounds as renal vasodilators.
Antihypertensive agents: angiotensin converting enzyme inhibitors. 1-[3-(Acylthio)-3-aroylpropionyl]-L-prolines.
Some adenine and adenosine methylene-bridged estrogens.
1,3,7-Trimethylguanine from the Sponge Latrunculia brevis
Hepatoprotective activity of polyphenolic compounds from Cynara scolymus against CCl4 toxicity in isolated rat hepatocytes.
Plant antitumor agents, 26. Isolation, structure, and antitumor activity of alkaloids from Anopterus glandulosus.
Structure-activity relationships of 1,3,5-triazine-2,4,6-triones as human gonadotropin-releasing hormone receptor antagonists.
Synthesis of tripeptides as potent Yersinia protein tyrosine phosphatase inhibitors.
Identification of a potent non-hydroxamate histone deacetylase inhibitor by mechanism-based drug design.
Structure-activity relationships of novel piperazines as antagonists for the melanocortin-4 receptor.
Self-organizing maps for identification of new inhibitors of P-glycoprotein.
Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase.
Small molecule designed to target metal binding site in the alpha2I domain inhibits integrin function.
Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents.
Discovery and SAR of benzyl phenyl ethers as inhibitors of bacterial phenylalanyl-tRNA synthetase.
Preliminary evaluation of pharmacological properties of some xanthone derivatives.
Insecticidal anthranilic diamides: a new class of potent ryanodine receptor activators.
Synthesis, in vitro, and in vivo antibacterial activity of nocathiacin I thiol-Michael adducts.
Synthesis and anaerobic activity of novel 1-carba-1-dethiacephalosporins.
Mono- and bis(aminomethyl)phenylacetic acid esters as short-acting antiarrhythmic agents. 2.
Preparation of substituted N-phenyl-4-aryl-2-pyrimidinamines as mediator release inhibitors.
Inhibition of human leukocyte elastase. 6. Inhibition by 6-substituted penicillin esters.
Synthesis and biology of substituted 3-phenyl taxol analogues
Synthesis and evaluation of cytotoxic activity of novel arylsulfonylimidazolidinones
Conformationally constrained analogues of diacylglycerol (DAG). 3. Interaction of -alkyl--lactones with protein kinase C (PK-C)
Modelisation, Synthesis and Anti-HIV activities of N,N,N,N,N-pentakistetraazamacrocycles salts derivatives
Non-peptide itam mimics as ZAP-70 antagonists
Synthesis and in vitro anti-human immunodeficiency virus activity of artemisinin (qinghaosu)-related trioxanes
Inhibitors of glycolic acid oxidase. 4-substituted 2,4-dioxobutanoic acid derivatives.
Identification of magnolol and honokiol as anxiolytic agents in extracts of saiboku-to, an oriental herbal medicine.
Tyrosinase inhibitors from Bolivian medicinal plants.
Bioactive Prenylhydroquinone Sulfates and a Novel C 31 Furanoterpene Alcohol Sulfate from the Marine Sponge, Ircinia Sp.
Pseudoirroratin A, a new cytotoxic ent-kaurene diterpene from Isodon pseudo-irrorata.
Cytotoxic prenylflavanones from Taiwanese propolis.
Tumor-specific novel taxoid-monoclonal antibody conjugates.
1,3-dihydrobenzo[c]furan nucleoside analogues: additional studies of the thymine derivative.
Reaction of irofulven with zinc and acid.
Synthesis and inhibitory evaluation of cyclohexen-2-yl- and cyclohexyl-substituted phenols and quinones to endothelial cell and cancer cells.
Identification of retinoic acid receptor beta subtype specific agonists.
Quantitative structure-intestinal permeability relationship of benzamidine analogue thrombin inhibitor.
The Japanese toxicogenomics project: application of toxicogenomics.
Synthesis, characterization, and biological evaluation of novel diclofenac prodrugs.
Design and synthesis of imidazopyridine analogues as inhibitors of phosphoinositide 3-kinase signaling and angiogenesis.
Synthesis and anti-melanogenic activity of hydroxyphenyl benzyl ether analogues.
Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: new multimodal fluorinated and iodinated radiotracers.
Didemnidines A and B, indole spermidine alkaloids from the New Zealand ascidian Didemnum sp.
Effect of aromatic short-chain analogues of ceramide on axonal growth in hippocampal neurons.
Nucleosides and nucleotides. 185. Synthesis and biological activities of 4'alpha-C-branched-chain sugar pyrimidine nucleosides.
Combinatorial library of serine and cysteine protease inhibitors that interact with both the S and S' binding sites.
New natural sesquiterpenes as modulators of daunomycin resistance in a multidrug-resistant Leishmania tropica line.
A novel molecular design of thrombin receptor antagonist.
Fatty acid amide hydrolase substrate specificity.
Substituted 1,6-naphthyridines as human cytomegalovirus inhibitors: conformational requirements.
Synthesis of a potent aminocyclitol alpha-mannosidase inhibitor, 1L-(1,2,3,5/4)-5-amino-4-O-methyl-1,2,3,4-cyclopentanetetrol.
Novel arylpiperazines as selective alpha1-adrenergic receptor antagonists.
Corticotropin releasing factor (CRF) receptor modulators: progress and opportunities for new therapeutic agents.
Synthesis and structure-activity relationships of chiral allosteric modifiers of hemoglobin.
Expeditious synthesis and cytotoxic activity of new cyanoindolo[3,2-c]quinolines and benzimidazo[1,2-c]quinazolines.
Synthesis and characterization of a novel class of protein tyrosine phosphatase inhibitors.
Furan based cyclic oligopeptides selectively target G-quadruplex.
Site-activated multifunctional chelator with acetylcholinesterase and neuroprotective-neurorestorative moieties for Alzheimer's therapy.
Biologically active proteins from natural product extracts.
An extract of Tagetes lucida and its phenolic constituents as antioxidants.
Doxorubicin prodrug on the basis of tert-butyl cephalosporanate sulfones.
Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents.
Nucleic acid related compounds. 47. Synthesis and biological activities of pyrimidine and purine "acyclic" nucleoside analogues.
Adenosine deaminase inhibitors. Synthesis of deaza analogues of erythro-9-(2-hydroxy-3-nonyl)adenine.
(+/-)-4-Aryl-4,5-dihydro-3H-1,3-benzodiazepines. 3. 2-Phenyl and 2-amino analogues as potential antihypertensive agents.
Dopaminergic agonists: comparative actions of amine and sulfonium analogues of dopamine.
Racemic and optically active 1,3,3-trimethyl-4-phenyl-4-(propionyloxy)piperidine.
Folate antagonists. 21. Synthesis and antimalarial properties of 2,4-diamino-6-(benzylamino)pyrido[3,2-d]pyrimidines.
Synthesis of new polyoxin derivatives and their activity against chitin synthase from Candida albicans.
Compactin (ML-236B) and related compounds as potential cholesterol-lowering agents that inhibit HMG-CoA reductase.
Novel 1, 2, 4-oxadiazoles as potent and selective histamine H3 receptor antagonists
Crystal receptor models in medicinal chemistry: Application to the generation of highly potent potassium channel openers
Synthesis and protein kinase C inhibitory activities of indane analogs of balanol
Indole inhibitors of human nonpancreatic secretory phospholipase A2. 2. Indole-3-acetamides with additional functionality.
3-(2-Benzofuranyl)quinuclidin-2-ene derivatives: novel muscarinic antagonists.
D-Ring alkylamine derivatives of estradiol: effect on er-binding affinity and antiestrogenic activity
1-benzyl-3-thioaryl-2-carboxyindoles as potent non-peptide endothelin antagonists
Synthesis and evaluation of 2-(biphenylmethyl)glutaric acid amide derivatives as neutral endopeptidase inhibitors.
O-alkylcarboxylate oxime and N-hydroxyurea analogs of substituted indole leukotriene biosynthesis inhibitors
Design and synthesis of phosphinic acids that triply inhibit endothelin converting enzyme, angiotensin converting enzyme and neutral endopeptidase 24.11
Drupangtonine, a novel antileukemic alkaloid from Cephalotaxus harringtonia var. drupacea
Modelisation, synthesis and antiviral evaluation of new 2,3-disubstituted thiazolidinone nucleoside analogues
Synthesis and evaluation of amino acid ester prodrugs of penciclovir
Synthesis of azido derivatives of semotiadil, a novel 1,4-benzothiazine calcium antagonist, for photoaffinity probes of calcium channels
Synthesis and biological evaluation of 4-alkoxy substituted trinems. Part I
Synthesis and antibacterial activity of cephalosporins having hydroxamic acid at C-7 position
Studies on the active metabolite (DU-86) of KW-2189, a novel derivative of duocarmycin
Examination of the role of the duocarmycin SA methoxy substituents: Identification of the minimum, fully potent DNA binding subunit
Syntheses and biological evaluation of two new naproxen analogs
Phosphoramidate derivatives of 2,3-didehydro-2,3-dideoxyadenosine [d4A] have markedly improved anti-HIV potency and selectivity
Synthesis of new non-nucleoside inhibitors of HIV-1
Trifluoromethyl alcohol and ketone inhibitors of metallo--lactamases
Small peptide inhibitors of 47 mediated MAdCAM-1 adhesion to lymphocytes
Design and synthesis of novel 2,7-dialkyl substituted 5(S)-amino-4(S)-hydroxy-8-phenyl-octanecarboxamides as in vitro potent peptidomimetic inhibitors of human renin
Bisbenzamidine isoxazoline derivatives as factor Xa inhibitors
Rapid decomposition of peroxynitrite by manganese porphyrin-antioxidant redox couples
Inhibition of DNA topoisomerase II by azaelliptitoxins functionalized in the variable substituent domain.
Studies on selectin blocker. 3. Investigation of the carbohydrate ligand sialyl Lewis X recognition site of P-selectin.
The design and synthesis of kappa opioid ligands based on a binding model for kappa agonists
Structure-activity relationships from molecular similarity matrices.
Assessment of the biological value of the 11-hydroxy group of the azalides.
Structure-based design and pharmacological properties of potent selective and systemically active CCK-B peptidomimetics
Synthesis and antiviral activity of 5'-deoxypyrazofurin.
Tetrazole amino acids as competitive NMDA antagonists
Adenosine-2-monophosphate derivatives: Structural requirements as substrates for inositol monophosphatase
Synthesis and antihypertensive activity of KC-399, a benzopyran K+ channel opener with long duration of action and less tachycardia
Selective inactivation of monoamine oxidase B by aminoethyl 3-chlorobenzyl ether
Synthesis and antibacterial activity of (1R,5R,6R)-2-tert-butyl-6-(1-hydroxyethyl)oxapenem-3-carboxylic acid
The squalestatins: potent inhibitors of squalene synthase. The role of the tricarboxylic acid moiety.
1,3-dithianes with acid functionalities: potent inhibitors and candidate affinity probes for the gaba-gated chloride channel
Synthesis and sar study of novel CCK-B antagonists
(E) and (Z)5-fluoro olefin carbocyclic nucleosides: effect of olefin geometry on inhibition of s-adenosyl-l-homocysteine hydrolase
Semisynthetic modification of hygromycin A. 2. synthesis and antibacterial activity of aryl analogs.
The use of synthetic peptide combinatorial libraries for the determination of peptide ligands in radio-receptor assays: Opioid peptides
Synthesis of 1,3-diamino-2-hydroxypropane derivatives as pseudosymmetric HIV protease inhibitors
Novel derivatives at the C21 position of the FK-506 macrocycle
Evaluation of the intestinal permeability and hepatic handling of peptidomimetic analogs
Synthesis and vasorelaxant activity of N-imino-2-(benzopyran-4-yl)pyridine K+ channel openers
Taxol photoaffinity labels 2. Synthesis and biological evaluation of N-(4-azidobenzoyl)-N-debenzoyltaxol, N-(4-azido-2,3,5,6-tetrafluorobenzoyl)-N-debenzoyltaxol, and 7-(4-azido-2,3,5,6-tetrafluorobenzoyl)taxol
New neplanocin analogues. III. 6R-configuration is essential for the antiviral activity of 6-C-methyl-3-deazaneplanocin a's
EMD 61 753 as a favourable representative of structurally novel arylacetamido-type K opiate receptor agonists
Synthesis and DNA binding properties of a series of N to C linked and imidazole containing analogues of distamycin
N-chloromethyl quinuclidinium derivatives: A new class of irreversible ligands for 5-HT3 receptors.
Derivatives of D-penicillamine as potential antiarthritic agents
P1 aspartate-based peptide alpha-((2,6-dichlorobenzoyl)oxy)methyl ketones as potent time-dependent inhibitors of interleukin-1 beta-converting enzyme.
Synthesis of N-acetylglucosamine-modified ara-C and its effect on ovarian cancer cells.
Genetically evolved receptor models: a computational approach to construction of receptor models.
2,6-Disubstituted aryl carboxylic acids, leaving groups "par excellence" for benzisothiazolone inhibitors of human leukocyte elastase.
Synthesis and hypoglycemic effect of chrysin derivatives.
N-deacetyl-N-aminoacylthiocolchicine derivatives: synthesis and biological evaluation on MDR-positive and MDR-negative human cancer cell lines.
Novel antitumor 2-cyanoaziridine-1-carboxamides.
Tetrahydrobenzindoles: selective antagonists of the 5-HT7 receptor.
Acquisition of high-affinity, SH2-targeted ligands via a spatially focused library.
Novel inhibitors of carboxypeptidase G2 (CPG2): potential use in antibody-directed enzyme prodrug therapy.
Synthesis, calcium mobilizing, and physicochemical properties of D-chiro-inositol 1,3,4,6-tetrakisphosphate, a novel and potent ligand at the D-myo-inositol 1,4,5-trisphosphate receptor.
C32-O-phenalkyl ether derivatives of the immunosuppressant ascomycin: a tether length study.
P2-achiral, P'-extended alpha-ketoamide inhibitors of calpain I.
Novel phosphinic and phosphonic acid analogues of the anticonvulsant valproic acid.
Grayanane diterpenoids from the flowers of Rhododendron molle with cytotoxic activity against a Spodoptera frugiperda cell line.
Xanthone and sesquiterpene derivatives from the fruits of Garcinia scortechinii.
Eunicellin-based diterpenoids, australins A-D, isolated from the soft coral Cladiella australis.
Hyrtioerectines A-C, cytotoxic alkaloids from the red sea sponge hyrtioserectus.
Using jasplakinolide to turn on pathways that enable the isolation of new chaetoglobosins from Phomospis asparagi.
Dichotomins J and K, vasodilator cyclic peptides from Stellaria dichotoma.
New bioactive triterpenoids from Melia volkensii.
Study on cytotoxic oxygenated desmosterols isolated from the red alga Galaxaura marginata.
New steroidal alkaloids from Buxus longifolia.
New Diosgenin Glycosides from Costus afer
Insect Toxins from an Endophytic Fungus from Wintergreen
Pyrrolizidine Alkaloids from Senecio r oseus and Senecio h elodes
Bioactive iridoids and a new lignan from Allamanda cathartica and Himatanthus fallax from the Suriname rainforest.
Minor Bioactive Dihydrophenanthrenes from Juncus effusus
Chemistry of Fijian Plants. 13. 1 Floribundal, a Nonglycosidic Bisiridoid, and Six Novel Fatty Esters of -Amyrin from Scaevola floribunda
Preparation of 7-Alkoxylated Furanopyrones: Semisynthesis of ()-Etharvensin, a New Styryl-Lactone from Goniothalamus arvensis
Isolation and structure of the cytotoxic cycloheptapeptide phakellistatin 13.
Two New Bioactive Cyclic Peroxides from the Marine Sponge Plakortis angulospiculatus
Biological Activities of Avarol Derivatives, 1. Amino Derivatives
Diyne Enol Ethers of Glycerol from a New Zealand Sponge, Petrosia hebes
A New Brominated Diphenyl Ether from a Philippine Dysidea Species
Isolation and Structure Determination of Inostamycin, a Novel Inhibitor of Phosphatidylinositol Turnover
Peroxy Aliphatic Esters from the Sponge Plakortis lita
Antitumor agents, 115. Seselidiol, a new cytotoxic polyacetylene from Seseli mairei.
Elabunin, a New Cytotoxic Triterpene from an East African Medicinal Plant, Elaeodendron buchananii
New proazulene guaianolides from Thapsia villosa.
Norsesterterpenes from the North Adriatic Sponge Ircinia oros
New Polyhydroxy Sterols, Dysidamides, and a Dideoxyhexose from the Sponge Dysidea herbacea
Chemistry of Sponges, XI. 22-Deoxyvariabilin, a New Sesterterpene from the Sponge Thorecta sp.
Chemistry of Sponges, XII. A New Dihydric Phenol from the Sponge Fasciospongia sp.
Novel Bishomoscalarane Sesterterpenes from the Sponge Phyllospongia foliascens
New Sesquiterpenes from Xanthium catharticum
Additional bioactive heptenes from Melodorum fruticosum.
An Nmr Study of Four Benzophenanthridine Alkaloids
Anti-AIDS agents, 3. Inhibitory effects of colchicine derivatives on HIV replication in H9 lymphocyte cells.
Isolation and characterization of two antimicrobial agents from mace (Myristica fragrans).
Benzothienyloxy phenylpropanamines, novel dual inhibitors of serotonin and norepinephrine reuptake.
Expedited SAR study of an mGluR5 antagonists: generation of a focused library using a solution-phase Suzuki coupling methodology.
Design, synthesis, and biological evaluation of isoquinoline-1,3,4-trione derivatives as potent caspase-3 inhibitors.
Small, potent, and selective diaryl phosphonate inhibitors for urokinase-type plasminogen activator with in vivo antimetastatic properties.
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
Solid phase-assisted synthesis and screening of a small library of N-(4-hydroxyphenyl)retinamide (4-HPR) analogs.
Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials.
Synthesis of taxoids with improved cytotoxicity and solubility for use in tumor-specific delivery.
Novel synthesis of 3,4-diarylisoxazole analogues of valdecoxib: reversal cyclooxygenase-2 selectivity by sulfonamide group removal.
A novel series of cytotoxic iridoid glucosides derived from aucubin: design, synthesis and structure-activity relationships.
Design, synthesis and evaluation of mutual prodrug of 4-biphenylacetic acid and quercetin tetramethyl ether (BPA-QTME) as gastrosparing NSAID.
Novel benzimidazole-pyrimidine conjugates as potent antitumor agents.
Vitamin D receptor agonist/histone deacetylase inhibitor molecular hybrids.
Identification of new non-carboxylic acid containing inhibitors of aldose reductase.
Cytotoxic indole alkaloids from Melodinus tenuicaudatus.
Design and synthesis of 2,4-disubstituted polyhydroquinolines as prospective antihyperglycemic and lipid modulating agents.
Synthesis and HIV inhibition activity of 2',3'-dideoxy-3'-C-hydroxymethyl nucleosides.
Orally active squalene synthase inhibitors: bis((acyloxy)alkyl) prodrugs of the alpha-phosphonosulfonic acid moiety.
Synthesis, chromatographic resolution, and anti-human immunodeficiency virus activity of (+/-)-calanolide A and its enantiomers.
Synthesis and cyclic GMP phosphodiesterase inhibitory activity of a series of 6-phenylpyrazolo[3,4-d]pyrimidones.
Synthesis and identification of novel oxa-steroids as progesterone receptor antagonists.
Synthesis and antiparasitic evaluation of bis-2,5-[4-guanidinophenyl]thiophenes.
Cytotoxic xanthones from Psorospermum molluscum from the Madagascar rain forest.
Synthesis and evaluation of homodimeric GnRHR antagonists having a rigid bis-propargylated benzene core.
Polyacylated neohesperidosides from Geranium caespitosum: bacterial multidrug resistance pump inhibitors.
A new series of potent benzodiazepine gamma-secretase inhibitors.
Structure-activity relationship of (1-aryl-2-piperazinylethyl)piperazines: antagonists for the AGRP/melanocortin receptor binding.
Understanding the structure-activity relationship of the human ether-a-go-go-related gene cardiac K+ channel. A model for bad behavior.
Antimalarial drug quinacrine binds to C-terminal helix of cellular prion protein.
Conformationally defined retinoic acid analogues. 5. Large-scale synthesis and mammary cancer chemopreventive activity for (2E,4E,6Z,8E)-8-(3',4'-dihydro-1'(2'H)-naphthalen-1'-ylidene)-3,7-dimethyl-2,4,6-octatrienoic acid (9cUAB30).
Ascochlorin derivatives as ligands for nuclear hormone receptors.
Dihydroindenoisoquinolines function as prodrugs of indenoisoquinolines.
Control of hepatitis C: a medicinal chemistry perspective.
Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor.
Conformationally-restricted ligands for the histamine H1 receptor.
Convergent synthesis of ribonuclease L-active 2',5'-oligoadenylate-peptide nucleic acids.
Synthesis and in vitro antibacterial activity of 3-[N-methyl-N-(3-methyl-1,3-thiazolium-2-yl)aminolmethyl cephalosporin derivatives.
N-Terminal dipeptides of D(-)-penicillamine as sequestration agents for acetaldehyde.
S-Acyl-2-thioethyl aryl phosphotriester derivatives as mononucleotide prodrugs.
Activation of antibacterial prodrugs by peptide deformylase.
N1-Arylsulfonyl-N2-(1-aryl)ethyl-3-phenylpropane-1,2-diamines as novel calcimimetics acting on the calcium sensing receptor.
Bioactive components of Allamanda schottii.
New Briarane Stecholide Diterpenes from the Indonesian Gorgonian Briareum sp.
New pyrrole alkaloids from Solanum sodomaeum.
Recent natural products based drug development: a pharmaceutical industry perspective.
Tolyporphins J and K, two further porphinoid metabolites from the cyanobacterium Tolypothrix nodosa.
Aminomethylthiophene-2-carboxylic acids as dipeptide mimetic in new growth hormone secretagogues
Design of pyrrolo-1,4-benzoxazine derivatives as inhibitors of 5-lipoxygenase and PAF antagonists with anthihistaminic properties
Phenolic and triterpene glycosides from the stems of Ilex litseaefolia.
Cytotoxic polyprenylated xanthones from the resin of Garcinia hanburyi.
Bisphosphonate inhibition of a Plasmodium farnesyl diphosphate synthase and a general method for predicting cell-based activity from enzyme data.
Inhibition of aquaporin 4 by antiepileptic drugs.
Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity.
Identification of Hsp70 modulators through modeling of the substrate binding domain.
A cytotoxic and antifungal 1,4-naphthoquinone and related compounds from a New Zealand brown algae, Landsburgia quercifolia.
Aromatic Secondary Metabolites from the Sponge Tedania ignis
An antiviral sesquiterpene hydroquinone from the marine sponge Strongylophora hartmani.
Efficient Isolation of Glycosidase Inhibitory Stilbene Glycosides from Rheum palmatum
New Sterol Ester from a Deep Water Marine Sponge, Xestospongia sp.
An Unusual Sulfur-Containing Diketopiperazine from the Bermudian Sponge Tedania ignis
Chemical studies on Mexican plants used in traditional medicine, XXI. Ratibinolide II, a new sesquiterpene lactone from Ratibida latipalearis.
Toxins Produced by the Dogwood Anthracnose Fungus Discula sp.
Application of two-dimensional nmr spectroscopy in the structural determination of marine natural products. Isolation and total structural assignment of 4-deoxyasbestinin diterpenes from the Caribbean gorgonian Briareum asbestinum.
Methylpendolmycin, an indolactam from a Nocardiopsis sp.
A novel perlactone from the Caribbean sponge Plakortis angulospiculatus.
Isolation, NMR studies, and biological activities of onopordopicrin from Centaurea sonchifolia.
Four new bioactive polyhydroxylated sterols from the black coral Antipathes subpinnata.
Phytotoxins of Ascochyta hyalospora, Causal Agent of Lambsquarters Leaf Spot
Brominated beta-carbolines from the marine tunicate Eudistoma album.
An Epoxydon-Derived Ester from a Phoma sp. Pathogenic to Rhubarb
Synthesis and antifungal activities in vitro of novel pyrazino [2,1-a] isoquinolin derivatives.
Oxime carbamate--discovery of a series of novel FAAH inhibitors.
Anti-influenza diarylheptanoids from the bark of Alnus japonica.
Design, synthesis and biological evaluation of simplified analogues of the RNA polymerase inhibitor etnangien.
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.
Novel semisynthetic spin-labeled derivatives of podophyllotoxin with cytotoxic and antioxidative activity.
Synthesis, biological evaluation, and molecular modeling of berberine derivatives as potent acetylcholinesterase inhibitors.
1,2,4-Triacylpiperidine substance p antagonists: Separation of affinities for the NK-1 receptor and the L-type calcium channel
Structural modifications of 6-naphthalene-2-carboxylate retinoids
A cembranolide diterpene farnesyl protein transferase inhibitor from the marine soft coral Lobophytum cristagalli
Heterocyclic guanidines as calcium antagonists
Enzymatic fucosylations with purine-diphosphate-fucoses (PDP-Fucoses)
Dipeptide mimetics can substitute for the receptor activation domain resulting in highly potent analogues of hPTH(136)
Synthesis and biological evaluation of 4(5)-(6-methylpyridin-2-yl)imidazoles and -pyrazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Compounds from Acorus tatarinowii: determination of absolute configuration by quantum computations and cAMP regulation activity.
Design and synthesis of spirotryprostatin-inspired diketopiperazine systems from prolyl spirooxoindolethiazolidine derivatives.
Microbial transformations of the taxan ring of 10-DAB by some strains of the fungus Curvularia lunata: formation of the bis-abeotaxanes wallifoliol and 4-deacylwallifoliol.
Bacterial transferase MraY inhibitors: synthesis and biological evaluation.
New aryldithiolethione derivatives as potent histone deacetylase inhibitors.
Pyrrolopyrazinedione-based inhibitors of human hormone-sensitive lipase.
2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Synthesis and evaluation of ether and halogenated derivatives of mannopeptimycin glycopeptide antibiotics.
Cytotoxic constituents of roots of Chaerophyllum hirsutum.
New diterpenoids from the marine mangrove Bruguiera gymnorrhiza.
Antitumor agents, 81. Justicidin-A and diphyllin, two cytotoxic principles from Justicia procumbens.
8-Hydroxymanzamine A, a beta-carboline alkaloid from a sponge, Pachypellina sp.
Pentacyclic triterpenes derived from Maprounea africana are potent inhibitors of HIV-1 reverse transcriptase.
Structure-activity relationships of potent, selective inhibitors of neuronal nitric oxide synthase based on the 6-phenyl-2-aminopyridine structure.
Synthesis and monoamine transporter binding of 2-(diarylmethoxymethyl)-3 beta-aryltropane derivatives.
Development of a new type of allosteric modulator of muscarinic receptors: hybrids of the antagonist AF-DX 384 and the hexamethonio derivative W84.
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.
Synthesis of biotinylated photoaffinity probes based on arylsulfonamide gamma-secretase inhibitors.
Artemisinins inhibit Trypanosoma cruzi and Trypanosoma brucei rhodesiense in vitro growth.
In vitro inhibition of Streptococcus mutans biofilm formation on hydroxyapatite by subinhibitory concentrations of anthraquinones.
Synthesis and evaluation of quindoline derivatives as G-quadruplex inducing and stabilizing ligands and potential inhibitors of telomerase.
Retro hydrazino-azapeptoids as peptidomimetics of proteasome inhibitors.
A switch in enantiomer preference between mitochondrial F1F0-ATPase chemotypes.
Water soluble prodrug of a COX-2 selective inhibitor suitable for intravenous administration in models of cerebral ischemia.
Antiangiogenic activity of deoxoartemisinin derivatives on chorioallantoic membrane.
Arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 2: Optimization of P1 and N-aryl.
Structures of pahayokolides A and B, cyclic peptides from a Lyngbya sp.
Discovery of alogliptin: a potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV.
Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design.
Structural effects on the phosphorylation of 3-substituted 1-beta-D-ribofuranosyl-1,2,4-triazoles by human adenosine kinase.
Development of 6-benzyl substituted 4-aminocarbonyl-1,4-diazepane-2,5-diones as orally active human chymase inhibitors.
Synthesis and biodistribution of 8-iodo-11-(4-methylpiperazino)-5H-dibenzo[b,e][1,4]-diazepine: Iozapine.
Phenylpropanoic acid derivatives bearing a benzothiazole ring as PPARdelta-selective agonists.
NO-donors. Part 17: Synthesis and antimicrobial activity of novel ketoconazole-NO-donor hybrid compounds.
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor.
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Synthesis and pharmacological profile of two novel heterocyclic chromanols, CP-80,798 and CP-85,958, as potent LTD4 receptor antagonists
Synthesis of potent water-soluble tissue transglutaminase inhibitors.
New diterpenoids and the bioactivity of Erythrophleum fordii.
Synthetic strategies toward carbocyclic purine-pyrimidine hybrid nucleosides.
Linear TMC-95-based proteasome inhibitors.
Analysis of crucial structural requirements of 2-substituted pyrimido[4,5-b][1,5]oxazocines as NK(1) receptor antagonist by axially chiral derivatives.
Antiproliferative cardenolides of an Elaeodendron sp. from the Madagascar rain forest(1).
Synthesis and inhibitory activity of new benzimidazole derivatives against Burkitt's lymphoma promotion.
Towards erythropoietin mimicking small molecules.
Activity of Garenoxacin against Macrolide-Susceptible and -Resistant Mycoplasma pneumoniae.
Pyrimidine-based inhibitors of CaMKIIdelta.
Meclonazepam analogues as potential new antihelmintic agents.
Synthesis and anti-HIV activity of 4'-substituted 4'-thiothymidines: a new entry based on nucleophilic substitution of the 4'-acetoxy group.
A cytotoxic triterpene saponin from the root bark of Aralia dasyphylla.
Novel highly oxygenated bisabolane sesquiterpenes from Cremanthodium discoideum.
Identification of a novel class of androgen receptor antagonists based on the bicyclic-1H-isoindole-1,3(2H)-dione nucleus.
A non-crosslinking platinum-acridine hybrid agent shows enhanced cytotoxicity compared to clinical BCNU and cisplatin in glioblastoma cells.
Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors.
Structure-based design of novel Chk1 inhibitors: insights into hydrogen bonding and protein-ligand affinity.
Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelin
Antibacterial evaluation of novel N-Arylimino-1,2,3-dithiazoles and N-arylcyanothioformamides
Angiogenic factors: syntheses of 12(R)- and 12(S)-hydroxyeicosa-5(Z),8(Z),14(Z)-trienoic acid and their 14,15-dehydro analogs
A convenient degradation of polyoxin D to uracil polyoxin C: access to key intermediates and synthesis of antifungal -aminoacyl derivatives of UPOC
Benzofuran based non-peptide antagonists of angiotensin II related to GR117289: part IV; imidazopyridinylbenzofurans.
Novel pyridazino[4,5-b][1,5]oxazepines and -thiazepines as 5-HT1A receptor ligands
An SAR study for the non-peptide substance P receptor (NK1) antagonist, CP-96,345.
Structure-activity studies of N-cyano-3-pyridinecarboxamidines and their amide and thioamide congeners
Myo-inositol 1,4,6-trisphosphate: A new synthetic Ca2+-mobilising inositol phosphate
Phenalene metabolites from eichhornia crassipes
Synthesis and anticonvulsant properties of BW A78U structurally-related compounds
A novel bromopyrrole alkaloid from the sponge Agelas longissima with antiserotonergic activity
An ether-based peptide analog as c-AMP-dependent protein kinase inhibitor/substrate
Design, synthesis and biological activity of some 4-DAMP- related compounds
Novel inhibitors of influenza sialidase related to GG167 Synthesis of 4-amino and guanidino-4H-pyran-2-carboxylic acid-6-propylamides; selective inhibitors of influenza a virus sialidase
Cyclic urea HIV protease inhibitors containing alkynyl- and alkenyl-tethered heterocycles in the P2 region
Phosphonates and thiophosphonates as sulfate surrogates: synthesis of estrone 3-methylthiophosphonate, a potent inhibitor of estrone sulfatase
L-162,389: a potent orally active angiotensin II receptor antagonist with balanced affinity to both AT1 and AT2 receptor subtypes
Amselamine, a new selective histamine H2-receptor agonist
Inactivation of serine protease, -chymotrypsin by fluorinated phenylalanine analogues
Novel, selective mechanism-based inhibitors of the herpes proteases
Chemoselective thioacylation of amino acids. Preparation of the four monothiothymopentin analogs and their biological activity
Synthesis and biological activity of 5-[(2,5-dihydroxybenzyl)amino]salicylic acid analogs as inhibitors of EGF receptor-associated protein tyrosine kinase
Nuclear variations of quinuclidine substance P antagonists: 2-diphenylmethyl-1-azabicyclo[3.2.2]nonan-3-amines
N,N-6-bis-[2-(3,4-dihydroxybenzyl)pyrrolidinyl]hexane, a potent, selective, orally active dopamine analog with hypotensive and diuretic activity
Symmetry-based HIV protease inhibitors containing a hydroxy bis-urea isostere
Investigation of side-chain sar, formulation and injection site toleration of pyrazolo[3,4-f]quinoline derivatives: a potent series of in vivo active immunostimulants
Spiroketal glycomimetics: the synthesis of a conformationally restrained Sialyl Lewis X mimic
Regioselective synthesis of 3-aryl substituted pyrrolidines via palladium catalyzed arylation: pharmacological evaluation for central dopaminergic and serotonergic activity.
Novel A-ring cleaved analogs of oleanolic and ursolic acids which affect growth regulation in NRP.152 prostate cells
The use of a proline ring as a conformational restraint in CCK-B receptor dipeptoids.
Glucuronide prodrugs of hydroxy compounds for antibody directed enzyme prodrug therapy (ADEPT) : A phenol nitrogen mustard carbamate
Synthesis of 7-chloro-4-substituted aminoquinolines and their in vitro ability to produce methemoglobin in canine hemolysate
Short and unexpectedly potent difluorostatone type inhibitors of HIV-1 protease
Metabolism and structure activity data based drug design: discovery of () SCH 53079 an analog of the potent cholesterol absorption inhibitor () SCH 48461
Phenylamino-pyrimidine (PAP) derivatives: a new class of potent and highly selective PDGF-receptor autophosphorylation inhibitors
Novel polyamine derivatives as potent competitive inhibitors of Trypanosoma cruzi trypanothione reductase
Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor
Pyrazolo[3,4-d]pyrimidines; adenosine receptor selectivity
2-alkyl-4-ethyl-5-[6-methyl-6-(2H-tetrazol-5-yl)heptyloxy]phenol leukotriene B4 receptor antagonists
PD 165929 the first high affinity non-peptide neuromedin-B (NMB) receptor selective antagonist
Synthesis and serotonin-like activity of 2-amino-5,8-dimethoxy-6-methyl-1,2-dihydronaphthalene.
Puromycin analogues. Effect of aryl-substituted puromycin analogues on the ribosomal peptidyltransferase reaction.
Adrenoceptor blocking agents. Compounds related to metoprolol.
A novel connector linkage applicable in prodrug design.
Inhibition of bovine and rat liver dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(4-substituted-phenyl)-s-triazines.
Toxicity quantitative structure--activity relationships of colchicines.
Isomeric phenylthioimidazo[1,2-alpha]pyridines as anthelmintics.
1-(Naphthylalkyl)-1H-imidazole derivatives, a new class of anticonvulsant agents.
Synthesis and antineoplastic activity of mitosene analogues of the mitomycins.
Alkylating angiotensin II analogues: synthesis, analysis, and biological activity of angiotensin II analogues containing the nitrogen mustard melphalan in position 8.
Benzeneacetamide amines: structurally novel non-m mu opioids.
Double-head haptens. Synthesis of and experimentally induced contact sensitivity to substances containing two unrelated haptens, pyrocatechol and alpha-methylene-gamma-butyrolactone, in the same molecule.
Novel opiates and antagonists. 4. 7-Alkanoylhydromorphones.
Drug latentiation by gamma-glutamyl transpeptidase.
Synthesis and in vivo antitumor activity of potential 5-fluorouracil prodrugs.
Highly selective fluorescent analogue of the potent delta-opioid receptor antagonist Dmt-Tic.
Design and synthesis of dipeptidyl glutaminyl fluoromethyl ketones as potent severe acute respiratory syndrome coronovirus (SARS-CoV) inhibitors.
Derivatives of tramadol for increased duration of effect.
Substituted 4-hydroxyphenyl sulfonamides as pathway-selective estrogen receptor ligands.
Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities.
Synthesis and molecular modeling of a lisinopril-tryptophan analogue inhibitor of angiotensin I-converting enzyme.
Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.
An enantioselective synthesis and biobehavioral evaluation of 7-fluoro-3-(p-fluorophenyl)-2-propyltropanes.
1-Aminomethylisoquinoline-4-carboxylates as novel dipeptidylpeptidase IV inhibitors.
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors.
Synthesis and structure-activity relationships of 3-cyano-4-(phenoxyanilino)quinolines as MEK (MAPKK) inhibitors.
Fluoresceinated FKBP12 ligands for a high-throughput fluorescence polarization assay.
Design and synthesis of piperazine-based matrix metalloproteinase inhibitors.
Synthesis and biological activity of a novel 11a-homo (cyclohexyl) prostaglandin.
Synthesis and in vitro anti-mycobacterium activity of N-alkyl-1, 2-dihydro-2-thioxo-3-pyridinecarbothioamides. Preliminary toxicity and pharmacokinetic evaluation.
Synthesis, structure, and neuroprotective properties of novel imidazolyl nitrones.
Structure-based design and synthesis of a potent matrix metalloproteinase-13 inhibitor based on a pyrrolidinone scaffold.
Neuroleptic activity of chiral trans-hexahydro-gamma-carbolines.
Antibacterial activity of phosphono dipeptides related to alafosfalin.
Selective monoamine oxidase inhibitors. 4. 4-Aminophenethylamine derivatives with neuron-selective action.
5-HT1 and 5-HT2 binding characteristics of 1-(2,5-dimethoxy-4-bromophenyl)-2-aminopropane analogues.
Synthesis and biological evaluation of irreversible inhibitors of aldose reductase.
Bimorphinans as highly selective, potent kappa opioid receptor antagonists.
5-fluoro- and 8-fluorotrimetoquinol: selective beta 2-adrenoceptor agonists.
2-[(3-Pyridinylmethyl)thio]pyrimidine derivatives: new bronchosecretolytic agents.
Synthesis of 5-beta-D-ribofuranosylnicotinamide and its N-methyl derivative. The isosteric and isoelectronic analogues of nicotinamide nucleoside.
gem-Diphosphonate and gem-phosphonate-phosphate compounds with specific high density lipoprotein inducing activity.
Preparation and antileukemic screening of some new 6'-deoxyhexopyranosyladenine nucleosides.
Assessment of structural requirements for the monoamine oxidase-B-catalyzed oxidation of 1,4-disubstituted-1,2,3,6-tetrahydropyridine derivatives related to the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine.
Metal-chelating inhibitors of a zinc finger protein HIV-EP1. Remarkable potentiation of inhibitory activity by introduction of SH groups.
Mechanism-based inhibition of L-pipecolate oxidase by 4,5-dehydro-L-pipecolic acid.
Synthesis of furo[2,3-c]pyran--D-thymidine
Z1046, a novel peripheral dopaminergic agent
Synthesis and biological activities of camphor-based non-peptide growth hormone secretagogues
Inhibitory potency of lithocholic acid analogs and other bile acids on glucuronosyltransferase activity in a colon cancer cell line
The identification of cyclooxygenase-1 inhibitors from 4-thiazolidinone combinatorial libraries
A comparative study of the solvolysis reactivity, regioselectivity, and stereochemistry of the duocarmycin a and sa alkylation subunits
Azonia derivatives of the -carboline system. A new class of DNA intercalators
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
Design and synthesis of bisubstrate analogues for 3-hydroxy-3-methyl-glutaryl coenzyme a reductase
Quantitative structure-activity relationships for the in vitro antimycobacterial activity of pyrazinoic acid esters.
3-Benzyloxy-2-phenylpiperidine NK1 antagonists: the influence of alpha methyl substitution
Novel 2,3-dihydrobenzofuran-2-carboxylic acids: highly potent and subtype-selective PPARalpha agonists with potent hypolipidemic activity.
Furanyl-1,3-thiazol-2-yl and benzoxazol-5-yl acetic acid derivatives: novel classes of heparanase inhibitor.
A new orally active insulin-mimetic vanadyl complex: bis(pyrrolidine-N-carbodithioato)oxovanadium (IV).
Structural requirements for respiratory inhibition by rotenoids; is an intact B/C ring system essential?
Anti-HIV activity of N-(2,3-dihalogenopropyl)- and N-allyl-glycine containing pentapeptides.
Tetrahydroisoquinoline derivatives with AT2-specific angiotensin II reception binding inhibitory activity
Five-membered heterocyclic amines as potential anti-rheumatoid arthritis agents.
Pyrazolo[1,5-a]pyridines and pyrazolo[1,5-b]pyridazines as 5ht3-antagonists
Synthesis of a photoaffinity taxol analogue and its use in labeling tubulin.
1,4-substituted indoles: a potent and selective class of angiostensin II receptor antagonists
Development of tetrazole bioisosteres in angiotensin II antagonists
Synthesis of coumarins as subtype-selective inhibitors of monoamine oxidase
(6-oxo-3-pyridazinyl)-benzimidazoles as potent angiotensin II receptor antagonists
Conformationally constrained analogues of dag .8. Changes in PK-C binding affinity produced by isosteric groups of the 3-O-acyl function in 2-deoxy-L-ribonolactones
A congener study of zileuton reveals interesting effects on glucuronidation rates
The role of peptide bond in chemotactic for-met-leu-phe-ome focused by depsipeptide analogs
Cycloheptimidazole based angiotensin II receptor antagonists. 4,5,6,7-tetrahydro-8-carboxymethylidene cycloheptimidazoles
Dual metalloprotease inhibitors. I. constrained peptidomimetics of mercaptoacyl dipeptides
The squalestatins: Potent inhibitors of squalene synthase, 3-hydroxymethyl derivatives.
Enantioselective synthesis of the optical isomers of broad-spectrum orally active antifungal azoles, Sch 42538 and Sch 45012
Synthesis of novel monocyclic squalestatin analogues as potential inhibitors of squalene synthase
Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease
Beneficial replacement of the P1 phenylalanine side chain in HIV-1 protease inhibitors of the difluorostatone type
Novel conformationally restricted aromatic piperidines as selective sigma receptor ligands
Selective inhibitors of protein kinase C in a model of graft-vs-host disease
Discovery of nonpeptide potent conformationally restricted angiotensin II receptor antagonists
Potent and selective inhibitors of gelatinase-a 1. hydroxamic acid derivatives
Synthesis and biological evaluation of a library containing potentially 1600 amides / esters. A strategy for rapid compound generation and screening.
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: heterocyclic bioisosteres for the urea group in DuP 128
Synthesis of chromophoric dipeptides as substrates for papain
Aryl-fused sphingolipids as novel PKC inhibitors with topical antiinflammatory activity
Isosteric replacement of the indole nucleus by benzothiophene in a series of pyrido[2,3-b]indoles with potential anxiolytic activity
Synthesis of novel 20-oxo-pregnacalciferol analogs with binding affinity to the progesterone receptor
A general method for synthesis of ether phospholipids with -linolenic acid and their properties
Discovery and optimization of indole pyrrolothiazole paf antagonists
1,5-Benzodiazepines as CCK-B antagonists. Effect of halogen substitution at the benzo-fused ring on potency and selectivity
Synthesis and biological activity of a series of 4-aryl substituted benz[b]azepines: Antagonists at the strychnine-insensitive glycine site
Synthesis and biological activities of new fluorinated abscisic acid
Hydroxamate inhibitors of human gelatinase B (92 kDa)
Synthesis of 2,3-dideoxy-3,4-dihydroxymethyl substituted pyrimidine nucleoside analogues
Molecular design of novel PGI2 agonists without PG skeleton. III
Octahydro-1,2,3,4,4a,5,11,11a-pyrido[3,4-c][1,5]benzoxazepines: conformationally restricted fentanyl analogs
Synthesis and antiviral activity of rigid acyclonucleotide analogs
New orally active serine protease inhibitors: structural requirements for their good oral activity.
(+)-cis-4,5,7a,8,9,10,11,11a-octahydro-7H-10-methylindolo[1,7- bc][2,6]-naphthyridine: a 5-HT2C/2B receptor antagonist with low 5-HT2A receptor affinity.
Design and syntheses of potent and selective dipeptide inhibitors of Candida albicans myristoyl-CoA:protein N-myristoyltransferase.
Synthesis, pharmacologic activity, and structure-activity relationships of a series of propafenone-related modulators of multidrug resistance.
Structure-activity relationships of unsaturated analogues of valproic acid.
Synthesis and biological activity of enantiomers of a conformationally restricted muscarone analog
Isoniazid-related copper(II) and nickel(II) complexes with antimycobacterial in vitro activity. Part 9.
Design, synthesis, and structure-activity relationship studies of ATP analogues as DNA gyrase inhibitors.
SAR studies of 2-o-substituted-benzoyl- and 2-alkanoyl-cyclohexane-1,3-diones as inhibitors of 4-hydroxyphenylpyruvate dioxygenase.
Synthesis and biological evaluation of 2-fluoro-8-azaadenosine and related compounds.
Synthesis and pharmacological activity of 6-[(E)-2-(2,6,6-trimethyl-1-cyclohexen-1-yl)ethen-1-yl]- and 6-(1,2,3,4-tetrahydro-1,1,4,4-tetramethyl-6-naphthyl)-2-naphthalenecarboxylic acids.
Khellin analogues. 1. General topological requirements for lipid-altering activity in furochromones.
Novel bromopyrrole alkaloids from the sponge Agelas dispar.
Structure and antimicrobial activity of diterpenes from the roots of Plectranthus hereroensis.
The antiallergic activities of synthetic acrophylline and acrophyllidine.
Additional dolabellane diterpenes from the Caribbean gorgonian octocoral Eunicea laciniata.
Crystal Structure of Sandaracopimaric Acid, a Lipoxygenase Inhibitor from Juniperus phoenicea
4-Dehydroecdysterone, a new ecdysteroid from the zoanthid Parazoanthus sp.
A new cytotoxic dihydroxy sterol from the soft coral Alcyonium patagonicum.
The 1994 Japan-U.S. Seminar on Bioorganic Marine Chemistry, Meeting Report
Cyathocaline, an Azafluorenone Alkaloid from Cyathocalyx zeylanica
Bipolal: anti-microalgal compound isolated as a candidate for marine antifouling produced by Bipolaris sp. F5206.
Studies on the inhibitory effects of caffeoylquinic acids on monocyte migration and superoxide ion production.
Further Structural Studies on the Petroformynes
Isolation of Novel Beauvericin Analogues from the Fungus Beauveria bassiana
A novel phorbol ester from Excoecaria agallocha.
Methyl ethers of podophyllotoxin-related cyclolignans.
Mycalolides D and E, new cytotoxic macrolides from a collection of the stony coral Tubastrea faulkneri.
Uprolides D-G, 2. A rare family of 4,7-oxa-bridged cembranolides from the Caribbean gorgonian Eunicea mammosa.
Secondary Mold Metabolites, Part 49. Isolation, Structural Elucidation, and Biomimetic Synthesis of Trametol, a New 1-Arylpropane-1,2-diol Produced by the Fungus Trametes sp.
A Short Enantioselective Synthesis of a Biologically Active Compound from Persea americana
Bioactive Constituents from the Flower Buds and Peduncles of Lindera megaphylla
Sulfated Polyprenylhydroquinones from the Sponge Ircinia spinosula
Salmahyrtisol A, a novel cytotoxic sesterterpene from the Red Sea sponge Hyrtios erecta.
Juncenolide A, a new briarane from the Taiwanese Gorgonian Junceella juncea.
Flavonoids from Ulex airensis and Ulex europaeus ssp. europaeus.
S(R)-podolactone D, a new sulfoxide-containing norditerpene dilactone from Podocarpus macrophyllus var. maki.
3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors.
Unprecedented sugar-dependent in vivo antitumor activity of carbohydrate-pendant cis-diamminedichloroplatinum(II) complexes.
Synthesis and biological evaluation of L- and D-configurations of 2',3'-dideoxy-4'-C-methyl-3'-oxacytidine analogues.
LY294002-geldanamycin heterodimers as selective inhibitors of the PI3K and PI3K-related family.
Synthesis and biological evaluation of simplified mycothiazole analogues.
Synthesis and biological activity of (+)-hedychilactone A and its analogs from (+)-sclareolide.
Synthesis and antifungal activity of 6-arylamino-phthalazine-5,8-diones and 6,7-bis(arylthio)-phthalazine-5,8-diones.
Design and synthesis of novel heterobiaryl amides as metabotropic glutamate receptor subtype 5 antagonists.
Discovery of innovative small molecule therapeutics.
Codrugs linking L-dopa and sulfur-containing antioxidants: new pharmacological tools against Parkinson's disease.
Discovery of novel hydroxamates as highly potent tumor necrosis factor-alpha converting enzyme inhibitors. Part II: optimization of the S3' pocket.
Design and evaluation of a potential mutagen for Hepatitis C virus.
Synthesis and SAR of aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Optimization of triaryl bis-sulfones as cannabinoid-2 receptor ligands.
Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I.
Antimicrobial activity of rationally designed amino terminal modified peptides.
4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Phenolic constituents of Amorpha fruticosa that inhibit NF-kappaB activation and related gene expression.
Discovery and development of fatty acid amide hydrolase (FAAH) inhibitors.
A novel photoaffinity label for the dopamine transporter based on N-substituted 3-[bis(4-fluorophenyl)methoxy]tropane
Synthesis of thiophenes and thieno[3,2-c]pyran-4-ones as antileishmanial and antifungal agents
Synthesis and biological evaluation of non-polyene analogs of amphotericin B
Discovery of imidazo[1,2-c]pyrimidin-5(6H)-one heterosubstituted nucleoside analogues with potent activity against human hepatitis B virus in vitro
The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity
Synthesis and antiproliferative activity of 2-O-allyl-1--D-arabinofuranosyl-uracil, -cytosine and -adenine
Peptidyl -keto thiazole as potent thrombin inhibitors
Antitumor agents. 1771. Design, syntheses, and biological evaluation of novel etoposide analogs bearing pyrrolecarboxamidino group as DNA topoisomerase II inhibitors
A new series of selective COX-2 inhibitors: 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles
INVESTIGATION OF BIOISOSTERS OF THE GROWTH HORMONE SECRETAGOGUE L-692,429.
Design, synthesis and biological evaluation of 1,3-diaminopropanes: a new class of polyamine analogs as leishmanicidal agents
Synthesis and cytotoxicity of 5-deazaflavins containing o- and p-quinone moieties
Design and synthesis of novel nonpeptide CCK-B receptor antagonists
New non peptidic C5a receptor antagonists
Bioactivatable derivatives of 8-substituted cAMP-analogues
ECD peptides inhibit in vitro fertilization in mice
Synthesis and inhibitory effect of a sialyl lewis X-acrylamide homopolymer at preventing cell adhesion
Structure-activity studies of aryl-spaced decahydroisoquinoline-3-carboxylic acid ampa receptor antagonists
Further evidence for a dopamine reuptake pharmacophore. The effect of N-methylation on Threo-methylphenidate and its analogs
Synthesis and antitumor evaluation of new thiazolo[5,4-b]quinoline derivatives.
Discovery of HIV-1 integrase inhibitors by pharmacophore searching.
Inhibition of human telomerase by a G-quadruplex-interactive compound.
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists.
Synthesis and structure-activity relationships of potent thrombin inhibitors: piperazides of 3-amidinophenylalanine.
Potent and selective 1,2,3-trisubstituted indole NPY Y-1 antagonists.
Additional New Maytansinoids from Trewia nudiflora: 10-Epitrewiasine and Nortrewiasine
New sesquiterpene hydroquinones from a Taiwanese marine sponge Polyfibrospongia australis.
Identification of "latent hits" in compound screening collections.
A second-generation 99m technetium single photon emission computed tomography agent that provides in vivo images of the dopamine transporter in primate brain.
Synthesis and in vitro efficacy of acid-sensitive poly(ethylene glycol) paclitaxel conjugates.
Aryl piperazine melanocortin MC4 receptor agonists.
Synthesis of a prodrug designed to release multiple inhibitors of the epidermal growth factor receptor tyrosine kinase and an alkylating agent: a novel tumor targeting concept.
Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists.
Amino functionalized novel cholic acid derivatives induce HIV-1 replication and syncytia formation in T cells.
First dual M3 antagonists-PDE4 inhibitors: synthesis and SAR of 4,6-diaminopyrimidine derivatives.
Design, synthesis and biological evaluation of 3-amino-3-phenylpropionamide derivatives as novel mu opioid receptor ligands.
1,3-Diarylcycloalkanopyrazoles and diphenyl hydrazides as selective inhibitors of cyclooxygenase-2.
Non-depolarizing neuromuscular blocking activity of bisquaternary amino di- and tripeptide derivatives.
A novel class of potent 3-isoxazolol GABA(A) antagonists: design, synthesis, and pharmacology.
Hydroxamic acid derivatives as potent peptide deformylase inhibitors and antibacterial agents.
Heteroarylmethoxyphenylalkoxyiminoalkylcarboxylic acids as leukotriene biosynthesis inhibitors.
Synthesis and In vitro binding affinities of 1-azabicyclic compounds as muscarinic ligands.
Novel 5-vinyl pyrimidine nucleosides with potent anti-hepatitis B virus activity.
Discovery and evaluation of piperidinyl carboxylic acid derivatives as potent alpha(4)beta(1) integrin antagonists.
Two novel cytotoxic and antimicrobial triterpenoids from Pseudolarix kaempferi.
Biflavonoids as novel antituberculosis agents.
Effect of zinc ion on the inhibition of carboxypeptidase A by imidazole-bearing substrate analogues.
Discovery of potent and selective phenylalanine derived CCR3 receptor antagonists. Part 2.
Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13.
Bioorganic synthesis of end-capped anti-HIV peptides by simultaneous cyanocysteine-mediated cleavages of recombinant proteins.
Synthesis, reactivity and biological evaluation of novel halogenated tripentones.
Plasmid-encoded ACC-4, an extended-spectrum cephalosporinase variant from Escherichia coli.
Lathyrane diterpenes from Euphorbia lathyris as modulators of multidrug resistance and their crystal structures.
New briaranes from the Taiwanese gorgonian Junceella juncea.
A new phytotoxic nonenolide from Phoma herbarum.
Continuing studies on the cyanobacterium Lyngbya sp.: isolation and structure determination of 15-norlyngbyapeptin A and lyngbyabellin D.
Synthesis and characterization of novel phenylindoles as potential probes for imaging of -amyloid plaques in the brain.
Synthesis and anti breast cancer activity of biphenyl based chalcones.
Discovery of potent and orally active tricyclic-based FBPase inhibitors.
Discovery of orally available spirodiketopiperazine-based CCR5 antagonists.
Synthesis and antiproliferative evaluation of certain iminonaphtho[2,3-b]furan derivatives.
Heat shock protein 70 (hsp70) as an emerging drug target.
Evolution of poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. From concept to clinic.
Unexpected reaction of 2-alkylsulfanylimidazoles to imidazol-2-ones: pyridinylimidazol-2-ones as novel potent p38alpha mitogen-activated protein kinase inhibitors.
Synthesis and characterization of in vitro and in vivo profiles of hydroxybupropion analogues: aids to smoking cessation.
Cytotoxicity of artesunic acid homo- and heterodimer molecules toward sensitive and multidrug-resistant CCRF-CEM leukemia cells.
Triterpene saponins from Clematis chinensis and their potential anti-inflammatory activity.
Isopropylidene substitution increases activity and selectivity of biphenylmethylene 4-pyridine type CYP17 inhibitors.
Symbiopolyol, a VCAM-1 inhibitor from a symbiotic dinoflagellate of the jellyfish Mastigias papua.
The endocannabinoid system: drug targets, lead compounds, and potential therapeutic applications.
Synthesis and biological activity of glycosyl-1H-1,2,3-triazoles.
2-Substituted N-aryl piperazines as novel triple reuptake inhibitors for the treatment of depression.
Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors.
Synthesis and biological evaluation of indolyl chalcones as antitumor agents.
Novel coumarin derivatives as potential antidyslipidemic agents.
Montmorillonite K-10 catalyzed cyclization of N-ethoxycarbonyl-N'-arylguanidines: access to pyrimido[4,5-c]carbazole and pyrimido[5,4-b]indole derivatives.
Inhibitors for expression of IgE receptor on human mast cell from Puerariae Flos.
Broad spectrum alkynyl inhibitors of T315I Bcr-Abl.
Synthesis of two marine farnesylacetones that dilate the basilar arteries of rabbits.
Structure-based design and synthesis of pyrrole derivatives as MEK inhibitors.
Structure-based optimization of potent PDK1 inhibitors.
Epsilon substituted lysinol derivatives as HIV-1 protease inhibitors.
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials.
New 6-amino-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines and [1,2,4]triazolo[3,4-b] [1,3,4]thiadiazin-6-ones: synthesis, characterization and antibacterial activity evaluation.
Design, synthesis and antiproliferative activity of styryl lactones related to (+)-goniofufurone.
Synthesis of some N-alkyl substituted urea derivatives as antibacterial and antifungal agents.
Synthesis and antitumor activity of new shikonin glycosides.
Multiple toxin production in the cyanobacterium microcystis: isolation of the toxic protease inhibitor cyanopeptolin 1020.
Synthesis of antimicrobial 2,9,10-trisubstituted-6-oxo-7,12-dihydro-chromeno[3,4-b]quinoxalines.
Binding mode and affinity studies of DNA-binding agents using topoisomerase I DNA unwinding assay.
Endomorphin-1 analogs with enhanced metabolic stability and systemic analgesic activity: design, synthesis, and pharmacological characterization.
Novel and versatile methodology for synthesis of cyclic imides and evaluation of their cytotoxic, DNA binding, apoptotic inducing activities and molecular modeling study.
Antineoplastic agents. 511. Direct phosphorylation of phenpanstatin and pancratistatin.
Dihydrolindbladiones, three new naphthoquinone pigments from a myxomycete Lindbladia tubulina.
Constituents of the stem bark of Pongamia pinnata with the potential to induce quinone reductase.
Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.
New analogue of arenastatin A, a potent cytotoxic spongean depsipeptide, with anti-tumor activity.
Efficient synthesis and structure-activity relationship of honokiol, a neurotrophic biphenyl-type neolignan.
Potent androgen antagonists based on carborane as a hydrophobic core structure.
Androstene-3,5-dienes as ER-beta selective SERMs.
Versatile templates for the development of novel kinase inhibitors: Discovery of novel CDK inhibitors.
2D QSAR studies on thyroid hormone receptor ligands.
High confidence predictions of drug-drug interactions: predicting affinities for cytochrome P450 2C9 with multiple computational methods.
Discovery of new inhibitors of D-alanine:D-alanine ligase by structure-based virtual screening.
3-(3-Aryloxyaryl)imidazo[1,2-a]pyridine sulfones as liver X receptor agonists.
Imidazolinones as nonpeptide angiotensin II receptor antagonists
Retro-Inverso Tripeptide Renin Inhibitors
A selective matrix metalloprotease 12 inhibitor for potential treatment of chronic obstructive pulmonary disease (COPD): discovery of (S)-2-(8-(methoxycarbonylamino)dibenzo[b,d]furan-3-sulfonamido)-3-methylbutanoic acid (MMP408).
1,8-Naphthyridine-3-carboxamide derivatives with anticancer and anti-inflammatory activity.
Synthesis, antimalarial evaluation and molecular modeling studies of hydroxyethylpiperazines, potential aspartyl protease inhibitors, part 2.
7,7-Dimethylaporphine alkaloids from the stem of Guatteriopsis friesiana.
Synthesis and pharmacological evaluation of (2-oxaadamant-1-yl)amines.
Selective, potent PPARgamma agonists with cyclopentenone core structure.
Molecular probes of DNA bulges: functional assay and spectroscopic analysis.
Novel 1H-(benzimidazol-2-yl)-1H-pyridin-2-one inhibitors of insulin-like growth factor I (IGF-1R) kinase.
Novel pyrazole derivatives as potent inhibitors of type II topoisomerases. Part 1: synthesis and preliminary SAR analysis.
Discovery and optimization of a series of quinazolinone-derived antagonists of CXCR3.
Antiproliferative cassane diterpenoids of Cordyla madagascariensis ssp. madagascariensis from the Madagascar rainforest.
Prodrugs of phosphates and phosphonates.
A different molecular mechanism underlying antimicrobial and hemolytic actions of temporins A and L.
Synthesis and evaluation of novel aromatic substrates and competitive inhibitors of GABA aminotransferase.
Design and campaign synthesis of piperidine- and thiazole-based histone deacetylase inhibitors.
Opioids and efflux transporters. Part 2: P-glycoprotein substrate activity of 3- and 6-substituted morphine analogs.
Trigoxyphins A-G: diterpenes from Trigonostemon xyphophylloides.
Bioactive xanthones from the stems of Cratoxylum formosum ssp. pruniflorum.
Synthesis and study of anti-inflammatory activity of some novel cyclophane amides.
Directed molecular screening for RecA ATPase inhibitors.
Structure-based design of flavonoid compounds as a new class of small-molecule inhibitors of the anti-apoptotic Bcl-2 proteins.
Mechanism-based thrombin inhibitors: design, synthesis, and molecular docking of a new selective 2-oxo-2H-1-benzopyran derivative.
Synthesis and biological activity of novel nonsteroidal progesterone receptor antagonists based on cyclocymopol monomethyl ether.
Homo-N-nucleosides: Incorporation into oligonucleotides and antiviral activity
Design and synthesis of ring-constrained boropeptide thrombin inhibitors
Squalene synthase inhibitors: isosteric replacements of the farnesyl chain of benzyl farnesyl amine
Conformationally restricted TRH analogs: a probe for the pyroglutamate region.
Synthesis and antibacterial activity of 4- and 8-methoxy trinems
Synthesis and radical scavenging activity of 3,3-dialkyl-3,4-dihydro-isoquinoline 2-oxides
Inhibition of protein phosphatase 2A by cantharidin analogues
Diastereoselective synthesis of trans-2-(1-triphenylmethyl-1H-imidazol-4-yl)cyclopropanecarboxylic acids: key intermediates for the preparation of potent and chiral histamine H3 receptor agents
Synthesis of 4-trifluoromethylsteroids: A novel class of steroid 5-reductase inhibitors
trans N-Methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] cycloprop-2-ene-1-carboxamides: Novel lipophilic kappa opioid agonists
A boronated benzamide as melanoma-seeking agent
Synthesis of a pyrimido[4,5-b]azepine analog of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF)
Design and biological evaluation of a series of thiophene-based 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors
SAR for MHC class II binding tetrapeptides: Correlation with potential binding site
INCORPORATION OF CONFORMATIONALLY CONSTRAINED PHENYLALANINE DERIVATIVES TIC, SIC, HIC AND NIC INTO A CHOLECYSTOKININ-B/GASTRIN RECEPTOR ANTAGONIST
Sulfonopeptide inhibitors of leukocyte adhesion
Synthesis and evaluation of dual action cephalosporins as elastase inhibitors
An exceptionally potent analog of sandramycin
The SAR of UK-78,282: A novel blocker of human T cell Kv1.3 potassium channels
Structure-based design of novel, dipeptide ligands targeting the pp60Src SH2 domain
D4 dopamine receptor-selective compounds from the Chinese plant Phoebe chekiangensis
Synthesis and in vitro evaluation of two progressive series of bifunctional polyhydroxybenzamide catechol-O-methyltransferase inhibitors.
Ras farnesyltransferase: a new therapeutic target.
Synthesis and antimalarial activity in vitro and in vivo of a new ferrocene-chloroquine analogue.
Benzo[c]quinoliziniums: A new family of inhibitors for protein kinase CK II
The design and synthesis of orally active short duration spiroindane growth hormone secretagogues
Exceptionally potent antispermatogenic compounds from 8-halogenation of (4aRS,5SR,9bRS)-hexahydroindeno-[1,2-c]pyridines.
Synthesis and hepatoprotective effects of soyasapogenol B derivatives
A CHROMOGENIC SUBSTRATE FOR THE CONTINUOUS ASSAY OF MAMMALIAN PHOSPHOINOSITIDE-SPECIFIC PHOSPHOLIPASE C
Search for surrogates: A study of endothelin receptor antagonist structure activity relationships
Pyridazinones with a pendant acylsulfonamide moiety as endothelin receptor antagonists
Repromicin derivatives with potent antibacterial activity against Pasteurella multocida.
Synthesis and biological activities of (R)-5,6-dihydro-N,N-dimethyl-4H-imidazo[4,5,1-ij]quinolin-5-amine and its metabolites.
Constrained analogues of 2-nor cyclic nucleoside monophosphates
Potent novel nonsteroidal androgen antagonists with a phthalimide skeleton
Design and synthesis of a novel class of thrombin inhibitors incorporating heterocyclic dipeptide surrogates
Synthesis and antitumor activity of novel cyclopropapyrroloindole(CPI) derivatives bearing methoxycarbonyl and trifluoromethyl groups
Molecular modeling of the interaction of trypanocide guanyl hydrazones with B-DNA
Novel 5-amino-6-methylquinolone antibacterials: A new class of non-6-fluoroquinolones
Benzoylphenoxy analogs of isoprenoid diphosphates as photoactivatable substrates for bacterial prenyltransferases
2-Aryloxycarbonylthiophene-3-sulfonamides: Highly potent and etA selective endothelin receptor antagonists
Synthesis and hypolipidemic activity of novel 2-(4-(2-substituted aminothiazole-4-yl) phenoxy) acetic acid derivatives.
Synthesis and GABAA receptor activity of A-homo analogues of neuroactive steroids.
Synthesis of novel peptidomimetics as inhibitors of protozoan cysteine proteases falcipain-2 and rhodesain.
Drimane Sesquiterpene Lactones from Peniophora polygonia
Novel tryptophan dioxygenase inhibitors and combined tryptophan dioxygenase/5-HT reuptake inhibitors
3-Hydroxy-19-nor-17-pregna-1,3,5(10)-triene-21,17-carbolactone as inhibitor of 17-hydroxysteroid dehydrogenase type 2
Potential anxiolytic agents. 2. Improvement of oral efficacy for the pyrido[1,2-a]benzimidazole (PBI) class of GABA-A receptor modulators
Chemical and enzymatic synthesis of high-affinity selectin ligands
MALONIC ACID DERIVATIVES AS SIALYL LEWIS X MIMETICS
Lack of stereospecificity in the binding of the P2 amino acid of ritonavir to HIV protease
New Oligosaccharidic Crown Ethers as Potential Drug-Targetting Vectors: Synthesis & Biological Evaluation
Probing the S-1 subsite selectivity of an industrial alkaline protease in anhydrous t-butanol
Acetylcholinesterase inhibition by tacrine analogues
A rationale for the design and synthesis of m1 selective muscarinic agonists.
Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists
New reagents for controlled release of nitric oxide. Structure-stability relationships
Apigenin-7-O--D-glucopyranoside, an anti-HIV principle from Kummerowia striata
Potent, non-peptidic oxytocin receptor antagonists from a natural source
N-(Aminoalkyl)imide antineoplastic agents. Synthesis and biological activity.
Scalarane-type bishomosester terpenes from the sponge Phyllospongia foliascens.
Isolation of 9-Dihydro-13-acetylbaccatin III from Taxus canadensis
Two Benzylated Dihydroflavonols from Cudrania tricuspidata
Isolation and characterization of cytotoxic and antibacterial tetrasaccharide glycosides from Ipomoea stans.
Bruceanols G and H cytotoxic quassinoids from Brucea antidysenterica.
Bioactive natural products from a sclerotium-colonizing isolate of Humicola fuscoatra.
Structures and Total Synthesis of 2-Aminoimidazoles from a Notodoris Nudibranch
Dragonamides C and D, linear lipopeptides from the marine cyanobacterium brown Lyngbya polychroa.
4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity.
Benzanilides with spasmolytic activity: chemistry, pharmacology, and SAR.
Lycoparins A-C, new alkaloids from Lycopodium casuarinoides inhibiting acetylcholinesterase.
Synthesis and neuraminidase inhibition studies of 4-azido, amino, and acetamido substituted sialosides
Inhibition of human cytomegalovirus protease by benzoxazinones and evidence of antiviral activity in cell culture
Preparation and in vitro activities of naphthyl and indolyl ether derivatives of the FK-506 related immunosuppressive macrolide ascomycin
Glycosyl derivatives of NK2 tachykinin receptor antagonists
Synthesis and immunoregulating activity of vitamin D analogues bearing pregnane side chains
Endothelin eceptor Ligands. Multiple D-Amino acid replacement net approach
Excitatory amino acids: 6-phosphonomethyltetrahydro-4-pyrimidinecarboxylic acids and their acyclic analogues are competitive N-methyl-D-aspartic acid receptor antagonists.
Benzopyran potassium channel activators related to cromakalim - amide replacements at position 4.
Synthesis and biological activity of C-6 modified derivatives of the glucosidase inhibitor 1-deoxynojirimycin.
Phosphate derivatives of d4T as inhibitors of HIV
Evaluation of heterocyclic acid equivalents as tetrazole replacements in imidazopyridine-based nonpeptide angiotensin II receptor antagonists
Enzymatic synthesis and antiviral ativity of 2-deoxy-2-fluoro-ribavirin
Silyl ethers of cycloheptene, novel proton pump inhibitors obtained during the total synthesis of the scopadulcic acids
Structure-activity studies of 5-substituted pyridopyrimidines as adenosine kinase inhibitors.
Discovery of novel Myc-Max heterodimer disruptors with a three-dimensional pharmacophore model.
Topological polar surface area defines substrate transport by multidrug resistance associated protein 1 (MRP1/ABCC1).
Substrate optimization for monitoring cathepsin C activity in live cells.
3-(2-Aminoethyl)pyridine analogs as alpha4beta2 nicotinic cholinergic receptor ligands.
Discovery of potent orally active thrombin receptor (protease activated receptor 1) antagonists as novel antithrombotic agents.
Angiotensin-converting enzyme inhibitors. 2. Perhydroazepin-2-one derivatives.
Amine peroxides as potential antimalarials.
Deaminoteicoplanin and its derivatives. Synthesis, antibacterial activity, and binding strength to Ac-D-Ala-D-Ala.
Potential antitumor agents. 57. 2-Phenylquinoline-8-carboxamides as "minimal" DNA-intercalating antitumor agents with in vivo solid tumor activity.
Benzodiazepine receptor binding activity of 6,9-disubstituted purines.
Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.
Potential tumor or organ-imaging agents. 30. Radioiodinated phospholipid ethers.
A multisubstrate adduct inhibitor of a purine biosynthetic enzyme with a picomolar dissociation constant.
4'-[(4-Piperidyl)carbonyl]methanesulfonanilides as potent, selective, bioavailable class III antiarrhythmic agents.
Angiotensin-converting enzyme inhibitors. 9. Novel [[N-(1-carboxy-3-phenylpropyl)amino]acyl]glycine derivatives with diuretic activity.
Chalcones: a new class of antimitotic agents.
Extension of a redox-based chemical delivery system to alpha, beta-unsaturated ketones.
Design and synthesis of benzoic acid derivatives as influenza neuraminidase inhibitors using structure-based drug design.
Kutznerides 1-4, depsipeptides from the actinomycete Kutzneria sp. 744 inhabiting mycorrhizal roots of Picea abies seedlings.
A new sesquiterpene as an antifouling substance from a palauan marine sponge, dysidea herbacea
Bisabolane sesquiterpenes from the roots of Ligularia cymbulifera.
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
Synthesis and biological evaluation of polysulfated oligosaccharide glycosides as inhibitors of angiogenesis and tumor growth.
In silico search for multi-target anti-inflammatories in Chinese herbs and formulas.
Chemical biology studies on norrisolide.
Diaryl piperidines as CB1 receptor antagonists.
2-aminoimidazole amino acids as inhibitors of the binuclear manganese metalloenzyme human arginase I.
Cyclopeptide Smac mimetics as antagonists of IAP proteins.
Antimalarial bromotyrosine derivatives from the Australian marine sponge Hyattella sp.
Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase.
Aurantoside C, a new tetramic acid glycoside from the sponge Homophymia conferta.
Synthesis and anti-mycobacterial activity of novel amino alcohol derivatives.
Structure-activity relationships in nucleotide oligomerization domain 1 (Nod1) agonistic -glutamyldiaminopimelic acid derivatives.
Claurailas A-D, cytotoxic carbazole alkaloids from the roots of Clausena harmandiana.
1,2,3-triazole analogs of combretastatin A-4 as potential microtubule-binding agents.
Substituted biaryl pyrazoles as sodium channel blockers.
Dialkylaminoalkyl derivatives of bicyclic compounds with antiplasmodial activity.
A new series of macrolide derivatives with 4''-O-saccharide substituents.
Structure-activity relationship study of glaziovianin A against cell cycle progression and spindle formation of HeLa S3 cells.
N,O-diacyl-4-benzoyl-N-phenylhydroxylamines as photoinduced DNA cleaving agents.
Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
Effects of structure on inhibitory activity in a series of mechanism-based inhibitors of human neutrophil elastase.
Topsentinols, 24-isopropyl steroids from the marine sponge Topsentia sp.
Antioxidant flavone glycosides from the leaves of Fargesia robusta.
Terpioside B, a difucosyl GSL from the marine sponge Terpios sp. is a potent inhibitor of NO release.
Morphinans and isoquinolines: acetylcholinesterase inhibition, pharmacophore modeling, and interaction with opioid receptors.
2-phenyl-1-[4-(2-piperidine-1-yl-ethoxy)benzyl]-1H-benzimidazoles as ligands for the estrogen receptor: synthesis and pharmacological evaluation.
Inhibiting gene expression at transcription start sites in chromosomal DNA with antigene RNAs.
Bradykinin B1 receptor antagonists as potential therapeutic agents for pain.
Elucidation of the topography of the thapsigargin binding site in the sarco-endoplasmic calcium ATPase.
Synthesis and biological evaluation of 3-alkyl-dihydrotetrabenazine derivatives as vesicular monoamine transporter-2 (VMAT2) ligands.
Fungal metabolite of naftazone inhibits nitrite production by activated murine macrophages
Synthesis and antibacterial activity of 2-functionalized-vinyl 1-methylcarbapenems and related compounds
Benzoxepin and benzothiepin derivatives as potent, orally active inhibitors of 5-lipoxygenase
Synthesis of avermectin B1-4,4a-oxide: a precursor of potent anthelmintic agents
Synthesis of racemic 2-phosphonomethyl-1,3-dioxolane nucleoside analogues as potential antiviral agents
S-(2-oxopentadecyl)-CoA, a nonhydrolyzable analogue of myristoyl-CoA, is a potent inhibitor of myristoyl-CoA:protein N-myristoyltransferase.
Plant antimutagenic agents, 1. General bioassay and isolation procedures.
Isolation of a New Indole Alkaloid, Pendolmycin, from Nocardiopsis
Starfish Saponins, Part 43. Structures of Two New Sulfated Steroidal Fucofuranosides (Imbricatosides A and B) and Six New Polyhydroxysteroids from the Starfish Dermasterias imbricata
Chemistry of Sponges, VII. 11,19-Dideoxyfistularin 3 and 11-Hydroxyaerothionin, Bromotyrosine Derivatives from Pseudoceratina durissima
Isotsaokoin, an antifungal agent from Amomum tsao-ko.
Cytotoxic triterpenoids from Acridocarpus vivy from the Madagascar rain forest.
Botcinins A, B, C, and D, metabolites produced by Botrytis cinerea, and their antifungal activity against Magnaporthe grisea, a pathogen of rice blast disease.
Studies of the Thymelaeaceae II. Antineoplastic principles of Gnidia kraussiana.
Inhibition of cAMP-phosphodiesterase by biflavones of Ginkgo biloba in rat adipose tissue.
Antifeedant Diterpenes For the Gypsy Moth Larvae From Kalmia latifolia: Isolation and Characterization of Ten Grayanoids
Abietane and C20-norabietane diterpenes from the stem bark of Fraxinus sieboldiana and their biological activities.
Synthesis of azafluorenone antimicrobial agents.
Abyssomicin I, a modified polycyclic polyketide from Streptomyces sp. CHI39.
Izumiphenazines A-C: isolation and structure elucidation of phenazine derivatives from Streptomyces sp. IFM 11204.
Pyridone and tetramic acid alkaloids from the spider pathogenic fungus Torrubiella sp. BCC 2165.
Molecular modeling studies on imidazo[4,5-b]pyridine derivatives as Aurora A kinase inhibitors using 3D-QSAR and docking approaches.
Novel 4-aryl-pyrido[1,2-c]pyrimidines with dual SSRI and 5-HT(1A) activity. part 3.
Prediction of drug intestinal absorption by new linear and non-linear QSPR.
Microwave supported synthesis of some novel 1,3-diarylpyrazino[1,2-a]benzimidazole derivatives and investigation of their anticancer activities.
Design, synthesis and SAR of a series of 1,3,5-trisubstituted benzenes as thrombin inhibitors.
6-amino-4-(pyrimidin-4-yl)pyridones: novel glycogen synthase kinase-3 inhibitors.
3-amido-4-anilinocinnolines as a novel class of CSF-1R inhibitor.
3,5-diarylazoles as novel and selective inhibitors of protein kinase D.
Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity.
Discovery of N-methyl-1-(1-phenylcyclohexyl)methanamine, a novel triple serotonin, norepinephrine, and dopamine reuptake inhibitor.
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Thienopyrrole acetic acids as antagonists of the CRTH2 receptor.
Organelle-selective energy transfer: a fluorescent indicator of intracellular environment.
Novel dihydrothieno[2,3-e]indazole derivatives as IB kinase inhibitors.
5-oxo-15-HETE: total synthesis and bioactivity.
Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.
Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators.
Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series.
Antibacterial activities of imidazolium, pyrrolidinium and piperidinium salts.
Synthesis and in vitro anti-HSV-1 activity of a novel Hsp90 inhibitor BJ-B11.
Tetrahydroquinolin-3-yl carbamate glucocorticoid receptor agonists with reduced PEPCK activation.
CD22-antagonists with nanomolar potency: the synergistic effect of hydrophobic groups at C-2 and C-9 of sialic acid scaffold.
Design, synthesis and docking study of 5-amino substituted indeno[1,2-c]isoquinolines as novel topoisomerase I inhibitors.
Synthesis and biochemical evaluation of a range of (4-substituted phenyl)sulfonate derivatives of 4-hydroxybenzyl imidazole-based compounds as potent inhibitors of 17alpha-hydroxylase/17,20-lyase (P45017alpha) derived from rat testicular microsomes.
Baculiferins A-O, O-sulfated pyrrole alkaloids with anti-HIV-1 activity, from the Chinese marine sponge Iotrochota baculifera.
Casarett and Doull's Toxicology The Basic Science of Poisons, 7th edition
Identification, structural properties and chelating capacity of miltipolone as a broad-spectrum inhibitor to cancer cells.
Development of 2,4-diaminopyrimidine derivatives as novel SNSR4 antagonists.
Small-molecule probe using dual signals to monitor leucine aminopeptidase activity.
Synthesis and anti-inflammatory activity of ent-kaurene derivatives.
Discovery of indole alkaloids with cannabinoid CB1 receptor antagonistic activity.
3,5-Disubstituted-indole-7-carboxamides: the discovery of a novel series of potent, selective inhibitors of IKK-.
Design and synthesis of several small-size HTLV-I protease inhibitors with different hydrophilicity profiles.
Stachylines A-D from the sponge-derived fungus Stachylidium sp.
Tirucallane triterpenoids from Cornus walteri.
Cytochrome P450 3A4 inhibitory constituents of the wood of Taxus yunnanensis.
Structure-based design, synthesis and preliminary anti-inflammatory activity of bolinaquinone analogues.
Synthesis and biological activity of 7H-benzo[4,5]indolo[2,3-b]-quinoxaline derivatives.
Biological evaluation of novel benzisoxazole derivatives as PPAR agonists.
TRPV1 modulators: structure-activity relationships using a rational combinatorial approach.
Imidazolone-amide bridges and their effects on tubulin polymerization in cis-locked vinylogous combretastatin-A4 analogues: synthesis and biological evaluation.
Synthesis and Biological Evaluation of Muraymycin Analogues Active against Anti-Drug-Resistant Bacteria.
Identification and synthesis of N'-(2-oxoindolin-3-ylidene)hydrazide derivatives against c-Met kinase.
Asymmetric synthesis and biological evaluations of (+)- and (-)-6-dimethoxymethyl-1,4-dihydropyridine-3-carboxylic acid derivatives blocking N-type calcium channels.
The identification of new metallo--lactamase inhibitor leads from fragment-based screening.
Novel, potent, and orally bioavailable phosphinic acid inhibitors of the hepatitis C virus NS3 protease.
Structure-based lead identification of ATP-competitive MK2 inhibitors.
Efficacy switching SAR of mGluR5 allosteric modulators: highly potent positive and negative modulators from one chemotype.
3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors.
Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria.
Selective labeling and monitoring pH changes of lysosomes in living cells with fluorogenic pH sensors.
Tryptamine derivatives as novel non-nucleosidic inhibitors against hepatitis B virus.
Synthesis and evaluation of 1-(1H-indol-3-yl)ethanamine derivatives as new antibacterial agents.
Synthesis of 5-thiodidehydropyranylcytosine derivatives as potential anti-HIV agents.
Efficient radiosynthesis of 2-[(18)f]fluoroadenosine: a new route to 2-[(18)f]fluoropurine nucleosides.
Synthesis and characterisation of a novel tubulin-directed DO3A-colchicine conjugate with potential theranostic features.
Design, synthesis of symmetrical bivalent mimetics of annonaceous acetogenins and their cytotoxicities.
Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies.
Regulation of mprF in daptomycin-nonsusceptible Staphylococcus aureus strains.
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
Colorimetric high-throughput screen for detection of heme crystallization inhibitors.
Activity of temocillin against KPC-producing Klebsiella pneumoniae and Escherichia coli.
Bacteriostatic and bactericidal activities of tigecycline against Coxiella burnetii and comparison with those of six other antibiotics.
Antibiotic susceptibility of Waddlia chondrophila in Acanthamoeba castellanii amoebae.
Impact of human serum albumin on oritavancin in vitro activity against enterococci.
Inhibition of a prolyl hydroxylase domain (PHD) by substrate analog peptides.
Synthesis of antitrypanosomal 1,2-dioxane derivatives based on a natural product scaffold.
Synthesis and evaluation of bidentate ligands designed to interact with PDZ domains.
Synthesis and biological evaluation of naphthyl phenyl ethers (NPEs) as novel nonnucleoside HIV-1 reverse transcriptase inhibitors.
Development of potent B-RafV600E inhibitors containing an arylsulfonamide headgroup.
Benzothiazole-based N-(phenylsulfonyl)amides as a novel family of PPAR antagonists.
Synthesis and SAR of new pyrazolo[4,3-h]quinazoline-3-carboxamide derivatives as potent and selective MPS1 kinase inhibitors.
New isoprenylated flavonoids and adipogenesis-promoting constituents from Morus notabilis.
Opioid 1 receptor antagonist 7-benzylidenenaltrexone as an effective resistance reverser for chloroquine-resistant Plasmodium chabaudi.
Identification of a New Series of STAT3 Inhibitors by Virtual Screening.
Antiproliferative and differentiating activities of a novel series of histone deacetylase inhibitors.
From taxuspine x to structurally simplified taxanes with remarkable p-glycoprotein inhibitory activity.
Cerep in vitro phospholipidosis assay data
Synthesis and antimicrobial properties of some new thiazolyl coumarin derivatives.
Synthesis and biological evaluation of 1,9-disubstituted -carbolines as potent DNA intercalating and cytotoxic agents.
Synthesis, pharmacological evaluation and docking studies of coumarin derivatives.
Pantolactams as androgen receptor antagonists for the topical suppression of sebum production.
Tricyclic thiazolopyrazole derivatives as metabotropic glutamate receptor 4 positive allosteric modulators.
New aporphinoid 5-HT2A and 1A antagonists via structural manipulations of nantenine.
Discovery of (+)-N-(3-aminopropyl)-N-[1-(5-benzyl-3-methyl-4-oxo-[1,2]thiazolo[5,4-d]pyrimidin-6-yl)-2-methylpropyl]-4-methylbenzamide (AZD4877), a kinesin spindle protein inhibitor and potential anticancer agent.
Synthesis of 4-triazole-podophyllotoxin derivatives by azide-alkyne cycloaddition and biological evaluation as potential antitumor agents.
Arylamides hybrids of two high-affinity 2 receptor ligands as tools for the development of PET radiotracers.
Synthesis and anti-microbial activity of some 1- substituted amino-4,6-dimethyl-2-oxo-pyridine-3-carbonitrile derivatives.
CNS and antimalarial activity of synthetic meridianin and psammopemmin analogs.
Novel peptide-specific quantitative structure-activity relationship (QSAR) analysis applied to collagen IV peptides with antiangiogenic activity.
Synthesis and biological activity of novel tiliroside derivants.
4-anilinoquinoline triazines: a novel class of hybrid antimalarial agents.
Stereoselective first total synthesis, confirmation of the absolute configuration and bioevaluation of botryolide-E.
Synthesis and preliminary evaluation of curcumin analogues as cytotoxic agents.
Synthesis and anticoagulant activity of a new series of 1,4-dihydropyridine derivatives.
Synthesis and antitumor activity of novel ribonucleosides with C-5 OH replaced by a diaminopyrimidinyl group.
Influence of pKa on the biotransformation of indene H1-antihistamines by CYP2D6.
Synthesis and antitubercular evaluation of novel substituted aryl and thiophenyl tethered dihydro-6H-quinolin-5-ones.
Pyridylmethylthio derivatives as VEGF inhibitors: part 2.
Analysis of -amino alcohols as inhibitors of the potential anti-tubercular target N-acetyltransferase.
Potent radiosensitizing agents: 5-methylselenyl- and 5-phenylselenyl-methyl-2'-deoxyuridine.
Benzyl benzoates: New phlorizin analogs as mushroom tyrosinase inhibitors.
Synthesis and pharmacological evaluation of the individual stereoisomers of 3-[methyl(1,2,3,4-tetrahydro-2-naphthalenyl)amino]-1-indanone, a potent mast cell stabilising agent.
Efficient synthesis and biological evaluation of 1,3-benzenedicarbonyl dithioureas.
Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group.
Edible Myrciaria vexator fruits: bioactive phenolics for potential COPD therapy.
NOSH-Aspirin: A Novel Nitric Oxide-Hydrogen Sulfide-Releasing Hybrid: A New Class of Anti-inflammatory Pharmaceuticals.
Neo-clerodane diterpenes from Salvia herbacea.
Cytotoxic and antivascular 1-methyl-4-(3-fluoro-4-methoxyphenyl)-5-(halophenyl)-imidazoles.
Synthesis and biological activity of new bispyridinium salts of 4,4'-bispyridyl-5,5'-perfluoroalkyl-2,2'-bisoxazoles.
Bioactive dammarane-type saponins from Operculina turpethum.
Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases.
Synthesis of novel cinnamanilides as potential immunosuppressive agents.
Arylcyanoacrylamides as inhibitors of the Dengue and West Nile virus proteases.
Bioactive myrsinol diterpenoids from the roots of Euphorbia prolifera.
3,5-Disubstituted-thiazolidine-2,4-dione analogs as anticancer agents: design, synthesis and biological characterization.
New N-methylpiperazinyl derivatives of bicyclic antiprotozoal compounds.
Synthesis, biological evaluation and molecular docking studies of resveratrol derivatives possessing curcumin moiety as potent antitubulin agents.
On a possible neutral charge state for the catalytic dyad in -secretase when bound to hydroxyethylene transition state analogue inhibitors.
Cyclic ether-containing macrolactins, antimicrobial 24-membered isomeric macrolactones from a marine Bacillus sp.
Synthesis and inhibitory activity of thymidine analogues targeting Mycobacterium tuberculosis thymidine monophosphate kinase.
Synthesis of quinolinomorphinan-4-ol derivatives as opioid receptor agonists.
Plasmid-mediated 16S rRNA methylases in aminoglycoside-resistant Enterobacteriaceae isolates in Shanghai, China.
Detection of the pandemic O25-ST131 human virulent Escherichia coli CTX-M-15-producing clone harboring the qnrB2 and aac(6')-Ib-cr genes in a dog.
Simple but powerful: phenanthroline-based small molecules for cellular imaging and cancer screening.
Cytotoxic diterpenoid quinonemethides from the roots of Pygmacopremna herbacea.
Discovery and synthesis of a new class of opioid ligand having a 3-azabicyclo[3.1.0]hexane core. An example of a 'magic methyl' giving a 35-fold improvement in binding.
Synthesis of novel alkyltriazole tagged pyrido[2,3-d]pyrimidine derivatives and their anticancer activity.
Synthesis and antimicrobial evaluation of new benzofuran derivatives.
Identification of 2-oxatriazines as highly potent pan-PI3K/mTOR dual inhibitors.
Synthesis, in vitro and in vivo preliminary evaluation of anti-angiogenic properties of some pyrroloazaflavones.
The characterization of a novel V1b antagonist lead series.
Cardenolides of Leptadenia madagascariensis from the Madagascar dry forest.
Structure and cytotoxicity of diterpenoids from Isodon eriocalyx.
Terpenoids from the aerial parts of Parasenecio deltophylla.
Highly brominated antimicrobial metabolites from a marine Pseudoalteromonas sp.
Synthesis and optimization of novel 4,4-disubstituted cyclohexylbenzamide derivatives as potent 11-HSD1 inhibitors.
Discovery of isoindoline and tetrahydroisoquinoline derivatives as potent, selective PPAR agonists.
Synthesis of novel 5-amino-thiazolo[4,5-d]pyrimidines as E. coli and S. aureus SecA inhibitors.
Synthesis and biological activity of novel 5'-arylamino-nucleosides by microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction.
Topical anti-inflammatory activity of boropinic acid and its natural and semi-synthetic derivatives.
A novel screening model for the molecular drug for diabetes and obesity based on tyrosine phosphatase Shp2.
Overcoming hERG activity in the discovery of a series of 4-azetidinyl-1-aryl-cyclohexanes as CCR2 antagonists.
Synthesis and antioxidant activity of oxazolyl/thiazolylsulfonylmethyl pyrazoles and isoxazoles.
Novel dihydropyrimidines as a potential new class of antitubercular agents.
Expanding the diversity of allosteric bcr-abl inhibitors.
Exploration of piperidine-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-Phenyl derivatives with broad potency against resistant mutant viruses.
A novel arylethynyltriazole acyclonucleoside inhibits proliferation of drug-resistant pancreatic cancer cells.
Validated predictive QSAR modeling of N-aryl-oxazolidinone-5-carboxamides for anti-HIV protease activity.
Thienopyrimidines as 3-adrenoceptor agonists: hit-to-lead optimization.
Bottromycin derivatives: efficient chemical modifications of the ester moiety and evaluation of anti-MRSA and anti-VRE activities.
Synthesis and evaluation of selected key methyl ether derivatives of vancomycin aglycon.
Novel variant of the qnrB gene, qnrB12, in Citrobacter werkmanii.
Induction of L1 and L2 beta-lactamases of Stenotrophomonas maltophilia.
Fluoroquinolone-resistant mutants of Burkholderia cepacia.
Bobel-24 activity against Cryptosporidium parvum in cell culture and in a SCID mouse model.
Mechanisms of resistance to daptomycin in Enterococcus faecium.
Relationship between antibiotic use and incidence of MexXY-OprM overproducers among clinical isolates of Pseudomonas aeruginosa.
Subacute toxicity of colistin methanesulfonate in rats: comparison of various intravenous dosage regimens.
Microdialysis study of imipenem distribution in the peritoneal fluid of rats with experimental acute pancreatitis.
Selection for high-level telithromycin resistance in Staphylococcus aureus yields mutants resulting from an rplB-to-rplV gene conversion-like event.
Escherichia coli isolate coproducing 16S rRNA Methylase and CTX-M-type extended-spectrum beta-lactamase isolated from an outpatient in the United States.
Desmethyl Macrolides: Synthesis and Evaluation of 4,10-Didesmethyl Telithromycin.
Pyrido[3,4-e]-1,2,4-triazines and related heterocycles as potential antifungal agents.
Umuhengerin, a new antimicrobially active flavonoid from Lantana trifolia.
Searching for Bioactive Compounds: Various Strategies
Flavonoids and benzene derivatives from the flowers and fruit of Tetrapanax papyriferus.
Isolation of translactone-containing triterpenes with thrombin inhibitory activities from the leaves of Lantana camara.
Isolation of a new potential antitumor compound from Wedelia asperrima.
Cytotoxic triterpenoid glycosides from the roots of Gordonia chrysandra.
Activity of new penems against defined MRSA strains
Syntheses of homoserine phosphate analogs as potential inhibitors of bacterial threonine synthase
High-affinity FKBP-12 ligands derived from (R)-()-carvone. Synthesis and evaluation of FK506 pyranose ring replacements
The inhibition of C5a receptor binding by analogs of L-156,602, a cyclic hexadepsipeptide antibiotic
Enantiomerically pure synthesis and antiviral evaluation of [(2S, 3S)-bis(hydroxymethyl)azetidin-1-yl] purine nucleosides: Analogs of oxetanocin-A
Rational design of substituted diarylureas: a scaffold for binding to G-quadruplex motifs.
Derivatives of 1,4-bis(3-hydroxycarbonyl-4-hydroxyl)styrylbenzene as PTP1B inhibitors with hypoglycemic activity.
()-Phenylahistin: A new mammalian cell cycle inhibitor produced by aspergillus ustus
The stereochemical requirements of the novel -opioid selective dipeptide antagonist TMT-Tic
A study of 3-amino-N-hydroxypropanesulfonamide derivatives as potential GABAB agonists and their fragmentation to 3-aminopropanesulfinic acid
The conformation-dependent lipophilicity of morphine glucuronides as calculated from their molecular lipophilicity potential
Technetium-99m-labeled HOE 140: a potential bradykinin B2 receptor imaging agent.
Synthesis and pharmacological activity of conformationally restricted, acetylenic retinoid analogs
Synthesis and biological evaluation of both enantiomers of L-761,000 as inhibitors of cyclooxygenase 1 and 2
5-Aminomethyl-1H-benzimidazoles as orally active inhibitors of inducible T-cell kinase (Itk).
Cobalt-alkyne complexes with imidazoline ligands as estrogenic carriers: synthesis and pharmacological investigations.
Synthesis of a series of novel dihydroartemisinin derivatives containing a substituted chalcone with greater cytotoxic effects in leukemia cells.
Synthesis, antifungal, haemolytic and cytotoxic activities of a series of bis(alkylpyridinium)alkanes.
Potent non-6-fluoro-substituted quinolone antibacterials: synthesis and biological activity.
Caracasanamide, a novel hypotensive agent from Verbesina caracasana
Pyridine Carboxamides: Potent Palm Site Inhibitors of HCV NS5B Polymerase.
Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.
Synthesis of 4'-Ethynyl-2'-deoxy-4'-thioribonucleosides and Discovery of a Highly Potent and Less Toxic NRTI.
Design and synthesis of benzenesulfonamide derivatives as potent anti-influenza hemagglutinin inhibitors.
Design and synthesis of novel 5-phenyl-N-piperidine ethanone containing 4,5-dihydropyrazole derivatives as potential antitumor agents.
Growth inhibition and mechanism of action of p-dodecylaminophenol against refractory human pancreatic cancer and cholangiocarcinoma.
Prevalence of fosfomycin resistance among CTX-M-producing Escherichia coli clinical isolates in Japan and identification of novel plasmid-mediated fosfomycin-modifying enzymes.
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
Prophylactic activity of intramuscular peramivir in mice infected with a recombinant influenza A/WSN/33 (H1N1) virus containing the H274Y neuraminidase mutation.
Novel chromosome-encoded CTX-M-78 beta-lactamase from a Kluyvera georgiana clinical isolate as a putative origin of CTX-M-25 subgroup.
Hirsutalins A-H, eunicellin-based diterpenoids from the soft coral Cladiella hirsuta.
Biological evaluation of donor-acceptor aminonaphthoquinones as antitumor agents.
Developing dual functional allosteric modulators of GABA(A) receptors.
SAR studies of gymnasterkoreayne derivatives with cancer chemopreventive activities.
Structure-based design, synthesis, and pharmacological evaluation of 3-(aminoalkyl)-5-fluoroindoles as myeloperoxidase inhibitors.
The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: the second clinical candidate having a shorter and favorable human half-life.
Synthesis of (S)-(+)-decursin and its analogues as potent inhibitors of melanin formation in B16 murine melanoma cells.
Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity.
Antimicrobial, antitumor and 5-reductase inhibitor activities of some hydrazonoyl substituted pyrimidinones.
Antiarrhythmic, serotonin antagonist and antianxiety activities of novel substituted thiophene derivatives synthesized from 2-amino-4,5,6,7-tetrahydro-N-phenylbenzo[b]thiophene-3-carboxamide.
A journey from benzanilides to dithiobenzanilides: Synthesis of selective spasmolytic compounds.
Potent and selective thiophene urea-templated inhibitors of S6K.
Quinazolinones as -secretase modulators.
Psammaplysin H, a new antimalarial bromotyrosine alkaloid from a marine sponge of the genus Pseudoceratina.
Biological study of a somatostatin mimetic based on the 1-deoxynojrimycin scaffold.
Discovery of fused 5,6-bicyclic heterocycles as -secretase modulators.
8-Aza-7,9-dideazaxanthine acyclic nucleoside phosphonate inhibitors of thymidine phosphorylase.
Effects of Tetracyclic and Pentacyclic Triterpenoids on Growth of Phytophthora cactorum
Development of colistin-dependent Acinetobacter baumannii-Acinetobacter calcoaceticus complex.
Synthesis and biological activity of J-104,118, a novel, potent inhibitor of squalene synthase
Nonpeptide GPIIB/IIIA inhibitors. 16. Thieno[2,3-b]thiophene -sulfonamides are potent inhibitors of platelet aggregation
Imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates as dual inhibitors of acetylcholinesterase and monoamine oxidase
Imetit and N-methyl derivatives. The transition from potent agonist to antagonist at histamine H3 receptors.1
Synthesis of ()-6-(3-aminopropyloxy)methyl-4-demethoxy-6, 7-dideoxy-daunomycinone, a new dna intercalator related to anthracyclines
Taxol structure-activity relationships: synthesis and biological evaluation of taxol analogs modified at C-7
1-Naphthylmethylphosphonic acid derivatives as osteoclastic acid phosphatase inhibitors
Design and synthesis of new taxol-containing aminophosphates as protaxols
An efficient synthesis and biological activities of 19-nor-17-hydroxy-17-trifluoromethyl-4-estren-3-one and its analogs
Synthesis and anti HIV-1 activity of new thiadiazepindioxides
J-104,123, a novel and orally-active inhibitor of squalene synthase: Stereoselective synthesis and cholesterol lowering effects in dogs
6-Substituted Quinazolinone Angiotensin II Receptor Antagonists
Synthesis and nti-tubulin activity of aza-combretastatins
Synthesis and bioactivity of new antineoplastic terpenylquinones
Design and synthesis of HIV protease inhibitors. Variations of the carboxy terminus of the HIV protease inhibitor L-682,679.
Antimicrobial principles from in vitro tissue culture of Peganum harmala.
Rollinone, a new cytotoxic acetogenin from Rollinia papilionella.
Antineoplastic agents, 105. Zephyranthes grandiflora.
The Identification of a Major Phytotoxic Component from Alternaria macrospora as -Dehydrocurvularin
New Furostanol Glycosides from Asparagus plumosus Leaves
Degradation of Lycorine by Pseudomonas Species Strain ITM 311
Novel Zaragozic Acids from Leptodontidium elatius
Vasculyne, a new cytotoxic acetylenic alcohol from the marine sponge Cribrochalina vasculum.
Irreversible inhibition of dihydrodipicolinate synthase by 4-oxo-heptenedioic acid analogues.
Synthesis and structure-activity relationships of 2-amino-1-aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents.
Antagonists of the P2X(7) receptor. From lead identification to drug development.
Antinociceptive effects of 14-membered cyclopeptide alkaloids.
Dendrimers ended by non-symmetrical azadiphosphonate groups: synthesis and immunological properties.
Synthesis of novel nitric oxide (NO)-releasing esters of timolol.
Induction of L1 and L2 beta-lactamase production in Stenotrophomonas maltophilia is dependent on an AmpR-type regulator.
Killing of Neisseria gonorrhoeae, Streptococcus agalactiae (group B streptococcus), Haemophilus ducreyi, and vaginal Lactobacillus by 3-O-octyl-sn-glycerol.
Four new cytotoxic oligosaccharidic derivatives of 12-oleanene from Lysimachia heterogenea Klatt.
Pyrazoline bearing benzimidazoles: search for anticancer agent.
Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.
Discovery of a new and efficient small molecule for neuronal differentiation from mesenchymal stem cell.
Benzo[e]isoindole-1,3-diones as potential inhibitors of glycogen synthase kinase-3 (GSK-3). Synthesis, kinase inhibitory activity, zebrafish phenotype, and modeling of binding mode.
Cytotoxic 3,4-seco-cycloartane triterpenes from the exudate of Gardenia tubifera.
Synthesis and antioxidant properties of enone core based dendrimers with carbazole as surface group.
Antioxidant and antiviral activities of silybin fatty acid conjugates.
Chemical constituents from the leaves and stems of Schisandra rubriflora.
Synthesis of azaisoflavones and their inhibitory activities of NO production in activated microglia.
N-Arylmethyl substituted iminoribitol derivatives as inhibitors of a purine specific nucleoside hydrolase.
Synthesis and cytotoxicity of aurilide analogs.
Synthesis and characterization of environment-sensitive fluorescent ligands for human 5-HT1A receptors with 1-arylpiperazine structure.
Synthesis and antitumor evaluation of 8-phenylaminopyrimido[4,5-c]isoquinolinequinones.
Rational design of potent GSK3beta inhibitors with selectivity for Cdk1 and Cdk2.
Emerging targets in osteoporosis disease modification.
Synthesis of aminoquinazoline derivatives and their antiproliferative activities against melanoma cell line.
Use of the anionic dye carboxy-2',7'-dichlorofluorescein for sensitive flow cytometric detection of multidrug resistance-associated protein activity.
Structural determinants of P-glycoprotein-mediated transport of glucocorticoids.
Synthesis of an analogue of tabtoxinine as a potential inhibitor of D-alanine:D-alanine ligase (ADP forming).
A novel solution-stable, water-soluble prodrug type for drugs containing a hydroxyl or an NH-acidic group.
6-Alkyl-N,N-disubstituted-2-pyridinamines as anticonvulsant agents.
Synthesis and antitubercular activity of N-(2-naphthyl)glycine hydrazide analogues.
Synthesis and anticonvulsant activity of 1-phenylcyclohexylamine analogues.
Water-soluble renin inhibitors: design of a subnanomolar inhibitor with a prolonged duration of action.
Inhibitors of cholesterol biosynthesis. 2. 1,3,5-trisubstituted [2-(tetrahydro-4-hydroxy-2-oxopyran-6-yl)ethyl]pyrazoles.
Hypolipidemic activity of rifamycin derivatives.
Novel 5-HT3 antagonists. Isoquinolinones and 3-aryl-2-pyridones.
Novel caffeic acid derivatives: extremely potent inhibitors of 12-lipoxygenase.
Studies on the macrocyclic part of the trichothecene satratoxin: partial synthesis and structure-activity relationship
Structure-activity relationships of monocyclic endothelin analogs
Design, synthesis and cytotoxic evaluation of keto-C-glycoside fatty acid conjugates.
Optical isomers of the H1 antihistamine terfenadine: synthesis and activity
The synthesis and reactivity of ,-acetylenic and allenic sulfoxides and sulfones of dehydroepiandrosterone and their reactions with 1-butanethiol and glucose-6-phosphate dehydrogenase
Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors.
The synthesis of a conformationally rigid calcium channel blocker
Design & synthesis of a novel EPSP synthase inhibitor based on its ternary complex with shikimate-3-phosphate and glyphosate
The synthesis of conformationally-restricted diacyl glycerol analogues
Azaheteroaromatic ethers as carbonyl bioisosteres. Synthesis and evaluation of a novel class of 5-HT3 receptor antagonists
Synthesis and biological activity of carbocyclic derivatives of the potent antiviral agent 9-[2-(phosphonomethoxy)ethyl]guanine (PMEG)
Substituted Benzamides with Conformationally Restricted Side Chains. 3. Azabicyclo[x.y.0] derivatives as gastric prokinetic agents.
N1-sterically hindered 2H-imidazol-2-one angiotensin II receptor antagonists: The conversion of surmountable antagonists to insurmountable antagonists
EPSP synthase inhibitor design II. The importance of the 3-phosphate group for ligand binding at the shikimate-3-phosphate site & the identification of 3-malonate ethers as novel 3-phosphate mimics.
Synthesis and biological evaluation of some 25,26-epoxy-1,24-dihydroxyvitamin D3 analogues
Thiol and hydroxamic acid containing inhibitors of endothelin converting enzyme
2-substituted penems, new candidates for cephalosporinase inhibitors
Synthesis and biological activity of 2-desamino and 4-deoxy analogs of 5,10-dideazatetrahydrofolic acid (DDATHF)
4-Aryltetrahydropyridines as selective ligands
()-7-deazaaristeromycin lacking the hydroxymethyl substituent
Biological diversity from a structurally diverse library: systematically scanning conformational space using a pyranose scaffold.
QSAR study of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2 using LS-SVM and GRNN based on principal components.
Novel 6,12-disubstituted chrysene as potent anticancer agent: synthesis, in vitro and in vivo study.
E-2-[3-(3,4-dichlorophenyl)-1-oxo-2-propenyl]-3-methylquinoxaline-1,4-dioxide: a lead antitubercular agent which alters mitochondrial respiration in rat liver.
Rose Bengal analogs and vesicular glutamate transporters (VGLUTs).
Potent and fully noncompetitive peptidomimetic inhibitor of multidrug resistance P-glycoprotein.
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors.
Synthesis and evaluation of original amidoximes as antileishmanial agents.
Design and preparation of sterol mimetics as potential antiparasitics.
In vitro comparison of the efficacies of natamycin and silver nitrate against ocular fungi.
In vitro activity of Isavuconazole against Aspergillus species and zygomycetes according to the methodology of the European Committee on Antimicrobial Susceptibility Testing.
Accelerated metabolism of voriconazole and its partial reversal by cimetidine.
Interactions between triazoles and amphotericin B in treatment of disseminated murine infection by Fusarium oxysporum.
Functional characterization of the sigmaB-dependent yabJ-spoVG operon in Staphylococcus aureus: role in methicillin and glycopeptide resistance.
Further identification of CTX-M-2 extended-spectrum beta-lactamase in Pseudomonas aeruginosa.
3-Alkylpyridinium alkaloids from the Pacific sponge Haliclona sp.
Anti-allergy agents. 3. Angular tricyclic ether derivatives of the 1,8-naphthyridin-2(1H)-one ring system
Synthesis and biological activity of some 3-acryloxymethyl cephalosporins
Peptide-binding antibiotics: A solid-phase assay for screening libraries of vancomycin mimics for selective d-Ala-d-Ala binding
Phosphonamidates and phosphonamidate esters as HIV-1 protease inhibitors
Rational design of potent carboxylic acid based bisubstrate inhibitors of ras farnesyl protein transferase
7,11-Disubstituted estrogens: Probes for the shape of the ligand binding pocket in the estrogen receptor
Nonpeptide HIV protease inhibitors designed to replace a bound water
Novel 4,5,6,7-tetrahydrobenzothiazole dopamine agonists display very low stereoselectivity in their interaction with dopamine receptors.
-cyano-substituted analogoues of decarboxylated S-adenosylmethionine as enzyme activated, irreversible inhibitors of S-adenosylmethionine decarboxylase
Synthesis and biological evaluation of novel 2-vinyl carbapenems. Remarkable DHP-1 stability of 1-substituted analogs
Activated ketones as potent reversible inhibitors of interleukin-I converting enzyme
Preparation of neurotensin analogs with a novel pro-tyr replacement
Derivatives of 5-amidine indole as inhibitors of thrombin catalytic activity
Optically active fluorinated cyclobutane nucleoside analogs with potent anti-herpes activity
Quinoline-substituted dihydroindoles as cysLT1 (LTD4 receptor) antagonists
Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors.
Crystal structure of Bacillus anthracis dihydrofolate reductase with the dihydrophthalazine-based trimethoprim derivative RAB1 provides a structural explanation of potency and selectivity.
Gene Context and DNA rearrangements in the carbapenemase locus of division II strains of Bacteroides fragilis.
Simultaneous determination of voriconazole and posaconazole concentrations in human plasma by high-performance liquid chromatography.
CMY-29 and CMY-30, two novel plasmid-mediated AmpC beta-lactamases.
Lon protease is essential for paradoxical survival of Escherichia coli exposed to high concentrations of quinolone.
Prospective open-label study of the administration of two-percent voriconazole eye drops.
Daptomycin rapidly penetrates a Staphylococcus epidermidis biofilm.
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
A balancing act: efflux/influx in mycobacterial drug resistance.
In vitro activities of telavancin and vancomycin against biofilm-producing Staphylococcus aureus, S. epidermidis, and Enterococcus faecalis strains.
Molecular basis and phenotype of methicillin resistance in Staphylococcus aureus and insights into new beta-lactams that meet the challenge.
Efficacy of triazoles in a murine disseminated infection by Candida krusei.
Characterization of ermA in macrolide-susceptible strains of methicillin-resistant Staphylococcus aureus.
Lack of antimicrobial activity by the antiretroviral drug nevirapine against common bacterial pathogens.
H-NS modulates multidrug resistance of Salmonella enterica serovar Typhimurium by repressing multidrug efflux genes acrEF.
Nukacin ISK-1, a bacteriostatic lantibiotic.
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
Synthesis and evaluation of novel chloropyrrole molecules designed by molecular hybridization of common pharmacophores as potential antimicrobial agents.
Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.
Synthesis, antiviral activity and cytotoxicity evaluation of Schiff bases of some 2-phenyl quinazoline-4(3)H-ones.
3D-QSAR pharmacophore modeling and in silico screening of new Bcl-xl inhibitors.
Anticancer activity of N-bis(trifluoromethyl)alkyl-N'-(polychlorophenyl) and N'-(1,2,4-triazolyl) ureas.
New octahydroquinazoline derivatives: synthesis and hypotensive activity.
Design, synthesis and inhibitory effect of pentapeptidyl chloromethyl ketones on proteinase K.
Discovery and synthesis of 6,7,8,9-tetrahydro-5H-pyrimido-[4,5-d]azepines as novel TRPV1 antagonists.
Tetrahydrocarboline analogs as MCH-1 antagonists.
Identification of potent ITK inhibitors through focused compound library design including structural information.
Pyrazole derivatives from azines of substituted phenacyl aryl/cyclohexyl sulfides and their antimycobacterial activity.
N-substituted pyrrolidines and tetrahydrofurans as novel AMPAR positive modulators.
Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity.
Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2.
Design and synthesis of threading intercalators to target DNA.
The discovery of new spirocyclic muscarinic M3 antagonists.
Synthesis, molecular modeling and biological evaluation of guanidine derivatives as novel antitubulin agents.
Allosteric modulation of the dopamine D2 receptor by Pro-Leu-Gly-NH2 peptidomimetics constrained in either a polyproline II helix or a type II beta-turn conformation.
Rs-100235: A high affinity 5-HT4 receptor antagonist
Pulmonary versus systemic delivery of antibiotics: comparison of vancomycin dispositions in the isolated rat lung.
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists.
New furanoflavanoids, intestinal alpha-glucosidase inhibitory and free-radical (DPPH) scavenging, activity from antihyperglycemic root extract of Derris indica (Lam.).
Synthesis of D-3-deoxy-3-phosphonomethyl-myo-inositol and its dimethyl ester - compounds of use in studying the ptdins-3-kinase signalling pathway
New analogues of N-(2-aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the most potent monoamine oxidase-B inactivators.
Anticonvulsant sugar sulfamates. Potent cyclic sulfate and cyclic sulfite analogues of topiramate
Pharmacology of (2R, 4R, 5S)-2-amino-4,5-(1,2-cyclohexyl)-7-phosphonoheptanoic acid (NPC 17742); a selective, systemically active, competitive NMDA antagonist
The total synthesis of fukiic acid, an HIV-1 integrase inhibitor.
Synthesis and antitumor activity studies of some new fused 1,2,4-triazole derivatives carrying 2,4-dichloro-5-fluorophenyl moiety.
Application of Huisgen (3+2) cycloaddition reaction: synthesis of 1-(2,3-dihydrobenzofuran-2-yl-methyl [1,2,3]-triazoles and their antitubercular evaluations.
Leuconicines A-G and (-)-eburnamaline, biologically active strychnan and eburnan alkaloids from Leuconotis.
Inhibition of stromelysin-1 (MMP-3) by peptidyl phosphinic acids
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing two heterocyclic head groups
Structure-based design of nonpeptidic HIV protease inhibitors from a cyclooctylpyranone lead structure.
WEHI/Eskitis Trypanosoma b. brucei screening data
Discovery of s-nitrosoglutathione reductase inhibitors: potential agents for the treatment of asthma and other inflammatory diseases.
Nicotinic acids: liver-targeted SCD inhibitors with preclinical anti-diabetic efficacy.
Design and synthesis of 6,6-fused heterocyclic amides as raf kinase inhibitors.
Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Design, Synthesis, and Antitumor Activity of 4-Halocolchicines and Their Pro-drugs Activated by Cathepsin B.
Novel dendrimeric lipopeptides with antifungal activity.
Synthesis and preliminary antibacterial evaluation of Linezolid-like 1,2,4-oxadiazole derivatives.
Binding of faropenem and other beta-lactam agents to penicillin-binding proteins of pneumococci with various beta-lactam susceptibilities.
Part 3: Design and synthesis of proline-derived 2 ligands.
Actin depolymerizing effect of trisoxazole-containing macrolides.
Synthesis and antimycobacterial activity of 5-formylaminopyrimidines; analogs of antibacterial purines.
Synthesis and antitumor activity of novel pyrido[2,3-d][1,2,4]triazolo[4,3-a]pyrimidin-5-one derivatives.
Synthesis, spectroscopic characterization and antiproliferative evaluation in vitro of novel Schiff bases related to benzimidazoles.
Design, synthesis and insulin-sensitizing activity of indomethacin and diclofenac derivatives.
Development of Fluorescent Ligands for the Human 5-HT1A Receptor.
Lead optimization of 4-imidazolylflavans: new promising aromatase inhibitors.
Synthesis and antiproliferative evaluation of 23-hydroxybetulinic acid derivatives.
Daphnane-type diterpenoids from Trigonostemon howii.
Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.
Discovery of selective PDE4B inhibitors.
Discovery of diphenylmethane analogs as anti-bovine diarrhea viral agents.
Unexpected binding orientation of bulky-B-ring anti-androgens and implications for future drug targets.
Novel 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2)-curcumin, kojic acid, quercetin, and baicalein conjugates as HIV agents.
Synthesis of 2-aziridinyl phosphonates by modified Gabriel-Cromwell reaction and their antibacterial activities.
Chisomicines A-C, limonoids from Chisocheton ceramicus.
A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor.
Substituted N-aryl-6-pyrimidinones: a new class of potent, selective, and orally active p38 MAP kinase inhibitors.
Pharmacokinetics and ex vivo pharmacodynamic antimalarial activity of dihydroartemisinin-piperaquine in patients with uncomplicated falciparum malaria in Vietnam.
Synergistic interaction between silver nanoparticles and membrane-permeabilizing antimicrobial peptides.
Emergence of extended-spectrum beta-lactamase PER-1 in Proteus vulgaris and Providencia stuartii isolates from Algiers, Algeria.
Mosaic penicillin-binding protein 2 in Neisseria gonorrhoeae isolates collected in 2008 in San Francisco, California.
Overexpression of the naturally occurring blaOXA-51 gene in Acinetobacter baumannii mediated by novel insertion sequence ISAba9.
Efficient clearance of Aspergillus fumigatus in murine lungs by an ultrashort antimicrobial lipopeptide, palmitoyl-lys-ala-DAla-lys.
Novel mutation in 23S rRNA that confers low-level resistance to clarithromycin in Helicobacter pylori.
Discovery of novel imidazo[1,2-a]pyridines as inhibitors of the insulin-like growth factor-1 receptor tyrosine kinase.
Design, synthesis and biological evaluation of 2'-deoxy-2',2'-difluoro-5-halouridine phosphoramidate ProTides.
Discovery of novel c-Met kinase inhibitors bearing a thieno[2,3-d]pyrimidine or furo[2,3-d]pyrimidine scaffold.
Inhibition of monoamine oxidase by C5-substituted phthalimide analogues.
Structure-activity relationships of C-17-substituted estratriene-3-O-sulfamates as anticancer agents.
The discovery and development of inhibitors of fatty acid amide hydrolase (FAAH).
The 2010 Philip S. Portoghese Medicinal Chemistry Lectureship: addressing the "core issue" in the design of estrogen receptor ligands.
Synthesis and cytotoxicity of the depsipeptides analogues of callipeltin B.
Synthesis of new pyrazole derivatives and their anticancer evaluation.
Asperaculin A, a sesquiterpenoid from a marine-derived fungus, Aspergillus aculeatus.
Vicenin-2, a potential anti-inflammatory constituent of Urtica circularis.
Synthesis and evaluation of mansonone F derivatives as topoisomerase inhibitors.
Discovery of potent, metabolically stable purine CRF-1 antagonists with differentiated binding kinetic profiles.
Identification of novel BRAF kinase inhibitors with structure-based virtual screening.
Synthesis and study of a series of 3-arylcoumarins as potent and selective monoamine oxidase B inhibitors.
Benzofurans from Styrax agrestis as acetylcholinesterase inhibitors: structure-activity relationships and molecular modeling studies.
Efficient conversion of a nonselective norepinephrin reuptake inhibitor into a dual muscarinic antagonist-2-agonist for the treatment of chronic obstructive pulmonary disease.
In vivo anti-inflammatory and antioxidant properties of ellagitannin metabolite urolithin A.
Discovery and kinetic evaluation of 6-substituted 4-benzylthio-1,3,5-triazin-2(1H)-ones as inhibitors of cathepsin B.
Synthesis, biological evaluation and molecular docking studies of 1,3,4-thiadiazole derivatives containing 1,4-benzodioxan as potential antitumor agents.
Fuscoside E: a strong anti-inflammatory diterpene from Caribbean octocoral Eunicea fusca.
Antiplasmodial and antiproliferative pseudoguaianolides of Athroisma proteiforme from the Madagascar Dry Forest.
Hydrazidomycins, cytotoxic alkylhydrazides from Streptomycesatratus.
Diastereoselective synthesis and bioactivity of long-chain anti-2-amino-3-alkanols.
Antimalarial activity of imidazo[2,1-a]isoindol-5-ol derivatives and related compounds.
A compound isolated from Schisandra chinensis induces apoptosis.
Design, synthesis, and testing of potential antisickling agents. 3. Ethacrynic acid.
Synthesis and beta-adrenergic blocking activity of new aliphatic and alicyclic oxime ethers.
Difluorostatine- and difluorostatone-containing peptides as potent and specific renin inhibitors.
Selective thromboxane synthetase inhibitors. 3. 1H-imidazol-1-yl-substituted benzo[b]furan-, benzo[b]thiophene-, and indole-2- and -3-carboxylic acids.
Synthesis of 6-substituted beta-carbolines that behave as benzodiazepine receptor antagonists or inverse agonists.
Synthesis and biological activity of 5-(2,2-difluorovinyl)-2'-deoxyuridine.
Antimalarial activity of 2-(substituted amino)-4,6-bis(trichloromethyl)-1,3,5-triazines and N-(chlorophenyl)-N'-[4-(substituted amino)-6-(trichloromethyl)-1,3,5-triazin-2-yl]guanidines.
Novel type of potential anticancer agents derived from chrysophanol and emodin. Some structure-activity relationship studies.
Arylformamidines with antinociceptive properties.
Semi-rigid tripeptide agonists of melanocortin receptors.
Antitubercular activity of alpha,omega-diaminoalkanes, H2N(CH2)nNH2.
Synthesis and evaluation of alpha-halogenated analogues of 3-(acetylhydroxyamino)propylphosphonic acid (FR900098) as antimalarials.
Chemistry of sponges. 19. Novel bioactive metabolites from Hamigera tarangaensis.
Haterumaimides F-I, four new cytotoxic diterpene alkaloids from an ascidian Lissoclinum species.
Synthesis and anticancer activity of novel amide derivatives of non-acetal deoxoartemisinin.
The development and validation of a novel virtual screening cascade protocol to identify potential serotonin 5-HT(7)R antagonists.
Studies of the synthesis of all stereoisomers of MG-132 proteasome inhibitors in the tumor targeting approach.
Structure and biosynthesis of norneolambertellin produced by Lambertella sp. 1346.
N-heterocyclic derived M1 positive allosteric modulators.
Evaluation of NTF1836 as an inhibitor of the mycothiol biosynthetic enzyme MshC in growing and non-replicating Mycobacterium tuberculosis.
Studies on the synthesis and antibacterial activity of 3,6-disubstituted 1,2,4-triazolo[3,4-b]1,3,4-thiadiazoles.
Design, synthesis and biological evaluation of cycloalkyl arylpyrimidines (CAPYs) as HIV-1 NNRTIs.
Aza vinyl sulfones: synthesis and evaluation as antiplasmodial agents.
N4-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.
Cytotoxic triterpenoid saponins from Lysimachia clethroides.
1,2,4-Triazole D-ribose derivatives: design, synthesis and antitumoral evaluation.
Isoxazoles incorporated N-substituted decahydroquinolines: a precursor to the next generation antimicrobial drug.
Farinamycin, a quinazoline from Streptomyces griseus.
Cyclopeptide Alkaloids from Ziziphus apetala.
New 5-benzylidenethiazolidin-4-one inhibitors of bacterial MurD ligase: design, synthesis, crystal structures, and biological evaluation.
Emodin inhibits migration and invasion of DLD-1 (PRL-3) cells via inhibition of PRL-3 phosphatase activity.
Inhibitory constituents of Nardostachys chinensis on nitric oxide production in RAW 264.7 macrophages.
5-HT2c receptor selectivity and structure-activity relationship of N-methyl-N-(1-methylpiperidin-4-yl)benzenesulfonamide analogs.
Facile synthesis of 1,2,3-triazole analogs of SGLT2 inhibitors by 'click chemistry'.
Minutissamides A-D, antiproliferative cyclic decapeptides from the cultured cyanobacterium Anabaena minutissima.
Synthesis and evaluation of biotinylated sansalvamide A analogs and their modulation of Hsp90.
Xylarenones C-E from an endophytic fungus isolated from Alibertia macrophylla.
Synthesis and inhibitory activity of sialic acid derivatives targeted at viral sialate-O-acetylesterases.
A PIM2 analogue suppresses allergic airway disease.
Lyconadins D and E, and complanadine E, new Lycopodium alkaloids from Lycopodium complanatum.
Inhibition of secreted phospholipases A2 by 2-oxoamides based on -amino acids: Synthesis, in vitro evaluation and molecular docking calculations.
Synthesis and SAR of novel CXCR4 antagonists that are potent inhibitors of T tropic (X4) HIV-1 replication.
Novel 9a,11-bridged azalides: One-pot synthesis of N'-substituted 2-imino-1,3-oxazolidines condensed to an azalide aglycone.
Receptor activity and conformational analysis of 5'-halogenated resiniferatoxin analogs as TRPV1 ligands.
Glycosylated nordihydroguaiaretic acids as anti-cancer agents.
Synthesis and SAR study of diphenylbutylpiperidines as cell autophagy inducers.
Facile synthesis and biological evaluation of 3,3-diphenylpropanoyl piperazines as T-type calcium channel blockers.
In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors.
Vasorelaxant effect of flavonoids through calmodulin inhibition: Ex vivo, in vitro, and in silico approaches.
Discovery of novel and orally active FXR agonists for the potential treatment of dyslipidemia & diabetes.
A pulse at the heart of targeted therapy.
Ligand-directed tosyl chemistry for protein labeling in vivo.
Identification of the toxic trigger in mushroom poisoning.
Augmented photoswitching modulates immune signaling.
Absorption, pharmacokinetics, and safety of triclosan after dermal administration.
Efficacy of posaconazole in a murine disseminated infection by Candida tropicalis.
First isolation of the blaOXA-23 carbapenemase gene from an environmental Acinetobacter baumannii isolate.
Hydrolysis and inhibition profiles of beta-lactamases from molecular classes A to D with doripenem, imipenem, and meropenem.
In vitro potency of CXA-101, a novel cephalosporin, against Pseudomonas aeruginosa displaying various resistance phenotypes, including multidrug resistance.
Activity and toxicity of farnesol towards Candida albicans are dependent on growth conditions.
Triclosan resistance of Pseudomonas aeruginosa PAO1 is due to FabV, a triclosan-resistant enoyl-acyl carrier protein reductase.
Bortezomib inhibits hepatitis B virus replication in transgenic mice.
Chemical reprogramming of Caenorhabditis elegans germ cell fate.
Chemical phylogenetics of histone deacetylases.
alpha-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) antagonists: from bench to bedside.
Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.
Proanthocyanidins from the leaves of Machilus philippinensis.
Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
Exploring aigialomycin d and its analogues as protein kinase inhibitors for cancer targets.
Melodinines M-U, cytotoxic alkaloids from Melodinus suaveolens.
Pharmacokinetic study of the hepatobiliary transport of indomethacin.
Inhibition of the CYP3A4-mediated metabolism and P-glycoprotein-mediated transport of the HIV-1 protease inhibitor saquinavir by grapefruit juice components.
Increased sensitivity to vincristine of MDR cells by the leukotriene D4 receptor antagonist, ONO-1078.
Human P-glycoprotein transports cortisol, aldosterone, and dexamethasone, but not progesterone.
PSC833, cyclosporin A, and dexniguldipine effects on cellular calcein retention and inhibition of the multidrug resistance pump in human leukemic lymphoblasts.
Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs.
Multispecific amphipathic substrate transport by an organic anion transporter of human liver.
Major role of organic anion transporter 3 in the transport of indoxyl sulfate in the kidney.
Effect of levothyroxine administration on intestinal P-glycoprotein expression: consequences for drug disposition.
Carrier-mediated hepatic uptake of peptidic endothelin antagonists in rats.
Solvent-free, microwave assisted synthesis of polyhalo heterocyclic ketene aminals as novel anti-cancer agents.
Antitubercular potential of some semisynthetic analogues of phytol.
Probing a catalytic antibody active site using spin-labelled haptens
Substituted O6-benzylguanine derivatives and their inactivation of human O6-alkylguanine-DNA alkyltransferase.
The use of oxadiazole and triazole substituted naphthyridines as HIV-1 integrase inhibitors. Part 1: Establishing the pharmacophore.
Virtual ligand screening of -glucosidase: Identification of a novel potent noncarbohydrate mimetic inhibitor.
Synthesis and antibacterial activity of C-12 pyrazolinyl spiro ketolides.
2-Azetidinone--a new profile of various pharmacological activities.
Identification of the spiro(oxindole-3,3'-thiazolidine)-based derivatives as potential p53 activity modulators.
In vitro activities of tigecycline against clinical isolates of Aeromonas, Vibrio, and Salmonella species in Taiwan.
Antimalarial activity of a new stilbene glycoside from Parthenocissus tricuspidata in mice.
Efficacy of ciprofloxacin and moxifloxacin against Nocardia brasiliensis in vitro and in an experimental model of actinomycetoma in BALB/c mice.
Codetection of blaOXA-23-like gene (blaOXA-133) and blaOXA-58 in Acinetobacter radioresistens: report from the SENTRY antimicrobial surveillance program.
Impact of inoculum size and heterogeneous vancomycin-intermediate Staphylococcus aureus (hVISA) on vancomycin activity and emergence of VISA in an in vitro pharmacodynamic model.
Antileishmanial activity of 1,3,4-thiadiazolium-2-aminide in mice infected with Leishmania amazonensis.
Statistical model to evaluate in vivo activities of antimalarial drugs in a Plasmodium cynomolgi-macaque model for Plasmodium vivax malaria.
A 6-aminoquinolone compound, WC5, with potent and selective anti-human cytomegalovirus activity.
Activity of levofloxacin alone and in combination with a DnaK inhibitor against gram-negative rods, including levofloxacin-resistant strains.
Klebsiella pneumoniae OmpA confers resistance to antimicrobial peptides.
IncA/C plasmid-mediated florfenicol resistance in the catfish pathogen Edwardsiella ictaluri.
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
Methicillin-resistant and -susceptible Staphylococcus aureus strains of clonal lineages ST398 and ST9 from swine carry the multidrug resistance gene cfr.
Design of novel N-phenylnicotinamides as selective cyclooxygenase-1 inhibitors.
Microwave assisted one-pot synthesis of highly potent novel isoniazid analogues.
Potent inhibitors of hepatitis C core dimerization as new leads for anti-hepatitis C agents.
Synthesis and study of 2-amino-7-bromofluorenes modified with nitroxides and their precursors as dual anti-amyloid and antioxidant active compounds.
Evaluation of dihydropyrimidin-(2H)-one analogues and rhodanine derivatives as tyrosinase inhibitors.
Synthesis of Arabino glycosyl triazoles as potential inhibitors of mycobacterial cell wall biosynthesis.
Synthesis, cytotoxic activity, and mechanism of action of furo[2,3-c]acridin-6-one and benzo[b]furo[3,2-h]acridin-6-one analogues of psorospermin and acronycine.
Asperelines A-F, peptaibols from the marine-derived fungus Trichoderma asperellum.
Fitness cost and impaired survival in penicillin-resistant Streptococcus gordonii isolates selected in the laboratory.
Design, synthesis, and antifungal activity of triazole and benzotriazole derivatives.
Inhibition of ribonuclease A by nucleoside-dibasic acid conjugates.
Tedanol: a potent anti-inflammatory ent-pimarane diterpene from the Caribbean Sponge Tedania ignis.
Combretastatin-like chalcones as inhibitors of microtubule polymerisation. Part 2: Structure-based discovery of alpha-aryl chalcones.
The preparation of novel dopamine analogues via palladium catalysed cyclisation reactions
Refinement of a molecular model of angiotensin II (AII) employed in the discovery of potent nonpeptide antagonists
Synthesis and evaluation of ligands for D2-like receptors: the role of common pharmacophoric groups.
Design, synthesis and AChE inhibitory activity of indanone and aurone derivatives.
Substrate specificity and inhibitory study of human airway trypsin-like protease.
Discovery of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amine aurora kinase inhibitors.
Malyngamides O and P from the sea hare Stylocheilus longicauda.
Cytotoxic cembrenolides and steroids from the formosan soft coral Sarcophyton crassocaule.
Antiproliferative triterpene saponins from Trevesia palmata.
Two novel cyclic peptides with antifungal activity from the cyanobacterium Tolypothrix byssoidea (EAWAG 195).
Lipid-conjugated oligonucleotides via "click chemistry" efficiently inhibit hepatitis C virus translation.
Discovery of 5-[[4-[(2,3-dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methyl-benzenesulfonamide (Pazopanib), a novel and potent vascular endothelial growth factor receptor inhibitor.
mu-Opioid/5-HT4 dual pharmacologically active agents-efforts towards an effective opioid analgesic with less GI and respiratory side effects (Part I).
Discovery of disubstituted phenanthrene imidazoles as potent, selective and orally active mPGES-1 inhibitors.
Evaluation of substituted 6-arylquinazolin-4-amines as potent and selective inhibitors of cdc2-like kinases (Clk).
Conformationally-restricted amino acid analogues bearing a distal sulfonic acid show selective inhibition of system x(c)(-) over the vesicular glutamate transporter.
Papyriferic acid derivatives as reversal agents of multidrug resistance in cancer cells.
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Synthetic pseudopterosin analogues: A novel class of antiinflammatory drug candidates.
Potent and selective 5-LO inhibitor bearing benzothiophene pharmacophore: discovery of MK-5286.
Synthesis and evaluation of novel monosubstituted sulfonylurea derivatives as antituberculosis agents.
Design and synthesis of 8-substituted benzamido-phenylxanthine derivatives as MAO-B inhibitors.
Synthesis and interaction with midkine of biotinylated chondroitin sulfate tetrasaccharides.
Discovery of INCB3284, a Potent, Selective, and Orally Bioavailable hCCR2 Antagonist.
Hypoxylonols C-F, benzo[j]fluoranthenes from Hypoxylon truncatum.
Novel synthesis and biological evaluation of enigmols as therapeutic agents for treating prostate cancer.
Design, synthesis and evaluation of telomerase inhibitory, hTERT repressing, and anti-proliferation activities of symmetrical 1,8-disubstituted amidoanthraquinones.
Fluorinated F508-CFTR correctors and potentiators for PET imaging.
Chromophenazines from the terrestrial Streptomyces sp. Ank 315.
Bacterial biofilm formation inhibitory activity revealed for plant derived natural compounds.
Discovery of CS-0777: A Potent, Selective, and Orally Active S1P1 Agonist.
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
Novel morpholine ketone analogs as potent histamine H3 receptor inverse agonists with wake activity.
Prostaglandin analogues possessing antinidatory effects. 1. Modification of the omega chain.
5-Tetrazolecarboxamides and their salts: new orally active antiallergy agents.
31P NMR kinetic studies of the intra- and intermolecular alkylation chemistry of phosphoramide mustard and cognate N-phosphorylated derivatives of N,N-bis(2-chloroethyl)amine.
A specific inhibitor of IgE-antibody formation: n-pentyl beta-D-fructopyranoside.
Adenosine receptors: targets for future drugs.
Adriamycin analogues. Preparation of 9,10-anhydrodaunorubicin, 9,10-anhydroadriamycin, and some related compounds.
Design of potent and selective antagonists of the vasopressor responses to arginine-vasopressin.
Angiotensin converting enzyme inhibitors: 1-glutarylindoline-2-carboxylic acids derivatives.
2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines.
Synthesis and antibacterial activities of new (alpha-hydrazinobenzyl)cephalosporins.
In vitro activities of tigecycline, minocycline, and colistin-tigecycline combination against multi- and pandrug-resistant clinical isolates of Acinetobacter baumannii group.
Antimicrobial activities of jadomycin B and structurally related analogues.
Naturally occurring Class A ss-lactamases from the Burkholderia cepacia complex.
New composite genetic element of the Tn916 family with dual macrolide resistance genes in a Streptococcus pneumoniae isolate belonging to clonal complex 271.
Synthesis and anti-mycobacterial evaluation of some pyrazine-2-carboxylic acid hydrazide derivatives.
Synthesis and antitumor activities of novel 1,4-disubstituted phthalazine derivatives.
A novel aryl-hydrazide from the marine lichen Lichina pygmaea: isolation, synthesis of derivatives, and cytotoxicity assays.
Synthesis of polyhalo acridones as pH-sensitive fluorescence probes.
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
4-(3-Trifluoromethylphenyl)-pyrimidine-2-carbonitrile as cathepsin S inhibitors: N3, not N1 is critically important.
Design and synthesis of 4-[3,5-dioxo-11-oxa-4,9-diazatricyclo[5.3.1.0(2,6)]undec-4-yl]-2-trifluoromethyl-benzonitriles as androgen receptor antagonists.
Synthesis and in vitro evaluation of N-alkyl-3-hydroxy-3-(2-imino-3-methyl-5-oxoimidazolidin-4-yl)indolin-2-one analogs as potential anticancer agents.
beta-Secretase (BACE-1) inhibitory effect of biflavonoids.
Derivatives of tetrahydroisoquinoline: synthesis and initial evaluation of novel non-peptide antagonists of the alpha(IIb)beta(3)-integrin.
Smoothened antagonists for hair inhibition.
Improvement of both plasmepsin inhibitory activity and antimalarial activity by 2-aminoethylamino substitution.
3-D-QSAR and docking studies on the neuronal choline transporter.
Discovery of 4-azaindoles as novel inhibitors of c-Met kinase.
Ingol and ingenol diterpenes from the aerial parts of Euphorbia royleana and their antiangiogenic activities.
Synthetic resveratrol aliphatic acid inhibits TLR2-mediated apoptosis and an involvement of Akt/GSK3beta pathway.
Guide to Receptors and Channels (GRAC), 4th Edition.
Mutations in three distinct loci cause resistance to peptide deformylase inhibitors in Bacillus subtilis.
Efficacy of piperacillin combined with the Penem beta-lactamase inhibitor BLI-489 in murine models of systemic infection.
Effect of beta-1,6-glucan inhibitors on the invasion process of Candida albicans: potential mechanism of their in vivo efficacy.
Human immunodeficiency virus type 1 recombinant reverse transcriptase enzymes containing the G190A and Y181C resistance mutations remain sensitive to etravirine.
Carbapenem-resistant KPC-2-producing Escherichia coli in a Tel Aviv Medical Center, 2005 to 2008.
Raltegravir penetration in seminal plasma of healthy volunteers.
OXA-24 carbapenemase gene flanked by XerC/XerD-like recombination sites in different plasmids from different Acinetobacter species isolated during a nosocomial outbreak.
Steady-state intrapulmonary pharmacokinetics and pharmacodynamics of posaconazole in lung transplant recipients.
Serum and cerebrospinal fluid levels of colistin in pediatric patients.
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
Short cationic antimicrobial peptides interact with ATP.
Rapid and sensitive liquid chromatography/mass spectrometry assay for caspofungin in human aqueous humor.
Discovery of novel osthole derivatives as potential anti-breast cancer treatment.
Discovery of novel quinolinone adenosine A2B antagonists.
Design, synthesis, and biological evaluation of novel N--carboline arylsulfonamides as anticancer agents.
Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.
Design and synthesis of harzialactone analogues: promising anticancer agents.
Pyridylmethylthio derivatives as VEGF inhibitors. Part 1.
Two new cytotoxic labdane diterpenes from the rhizomes of Hedychium coronarium.
Exploring 7-Nicotinic Receptor Ligand Diversity by Scaffold Enumeration from the Chemical Universe Database GDB.
Facile synthesis of a fluorescent cyclosporin a analogue to study cyclophilin 40 and cyclophilin 18 ligands.
Aminoindazole PDK1 Inhibitors: A Case Study in Fragment-Based Drug Discovery.
A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis.
Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway.
Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity.
Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy.
Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR.
Discovery of N-Aryl Piperazines as Selective mGlu(5) Potentiators with Efficacy in a Rodent Model Predictive of Anti-Psychotic Activity.
Modification at the Lipophilic Domain of RXR Agonists Differentially Influences Activation of RXR Heterodimers.
Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues.
Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors.
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
Distinct mode of interaction of a novel ketolide antibiotic that displays enhanced antimicrobial activity.
Resistance to colistin in Acinetobacter baumannii associated with mutations in the PmrAB two-component system.
Candida albicans and Staphylococcus aureus form polymicrobial biofilms: effects on antimicrobial resistance.
Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.
Bicyclic heteroaryl inhibitors of stearoyl-CoA desaturase: from systemic to liver-targeting inhibitors.
Labdane diterpenes from the aerial parts of Curcuma comosa enhance fetal hemoglobin production in an erythroid cell line.
Lack of an effect of antibiotic treatment on prolonged detection of chlamydial DNA in murine genital tract infection.
Antioxidant 2-phenylbenzofurans and a coumestan from Lespedeza virgata.
2-phenyl-4-piperazinylbenzimidazoles: orally active inhibitors of the gonadotropin releasing hormone (GnRH) receptor.
Discovery of new binding elements in DPP-4 inhibition and their applications in novel DPP-4 inhibitor design.
Discovery of AMG 853, a CRTH2 and DP Dual Antagonist.
New losartan-hydrocaffeic acid hybrids as antihypertensive-antioxidant dual drugs: Ester, amide and amine linkers.
Discovery of substituted biphenyl oxazolidinone inhibitors of cholesteryl ester transfer protein.
Discovery of a Potent Pyrazolopyridine Series of -Secretase Modulators.
JBIR-94 and JBIR-125, antioxidative phenolic compounds from Streptomyces sp. R56-07.
Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists.
Pyrazolo[1,5-a]pyridines as p38 kinase inhibitors.
Imidazopyridines as selective CYP3A4 inhibitors.
Design and synthesis of estrogen receptor degradation inducer based on a protein knockdown strategy.
The human bile salt export pump: characterization of substrate specificity and identification of inhibitors.
Cytotoxic and multidrug resistance reversal activity of a vegetable, 'Anastasia Red', a variety of sweet pepper.
Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).
Bumetanide is not transported by the Ntcp or by the oatp: evidence for a third organic anion transporter in rat liver cells.
Characterization of the mouse bile salt export pump overexpressed in the baculovirus system.
Discovery of novel alpha7 nicotinic receptor antagonists.
Exploration of a new series of CCR5 antagonists: multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.
Antibacterial activity of ultrashort cationic lipo-beta-peptides.
Avian Aspergillus fumigatus strains resistant to both itraconazole and voriconazole.
Tetracyclines modulate protease-activated receptor 2-mediated proinflammatory reactions in epidermal keratinocytes.
Benzoxazinones as potent positive allosteric AMPA receptor modulators: part I.
Total synthesis of largazole and analogues: HDAC inhibition, antiproliferative activity and metabolic stability.
New class azaphilone produced by a marine fish-derived Chaetomium globosum. The stereochemistry and biological activities.
Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase.
Synthesis and antimicrobial activity of some novel dicationic sulphonophanes.
Efficient synthesis of 3-O-thia-cPA and preliminary analysis of its biological activity toward autotaxin.
Lignans and neolignans from Sinocalamus affinis and their absolute configurations.
Modulation of the activity of histone acetyltransferases by long chain alkylidenemalonates (LoCAMs).
KSRP/FUBP2 Is a Binding Protein of GO-Y086, a Cytotoxic Curcumin Analogue.
Pyrrolo[2,3-c]azepine derivatives: a new class of potent protein tyrosine phosphatase 1B inhibitors.
Novel agmatine and agmatine-like peptidomimetic inhibitors of the West Nile virus NS2B/NS3 serine protease.
Synthesis and antimicrobial activities of hexahydroimidazo[1,5-a]pyridinium bromides with varying benzyl substituents.
In vivo efficacy of anidulafungin against mature Candida albicans biofilms in a novel rat model of catheter-associated Candidiasis.
Cationic amphiphiles, a new generation of antimicrobials inspired by the natural antimicrobial peptide scaffold.
Design of novel and potent cPLA2 inhibitors containing an -methyl-2-ketothiazole as a metabolically stable serine trap.
Enediol mimics as inhibitors of the D-arabinose 5-phosphate isomerase (KdsD) from Francisella tularensis.
An inhibitor-like binding mode of a carbonic anhydrase activator within the active site of isoform II.
Synthesis and biological evaluation of benzyl styrylsulfonyl derivatives as potent anticancer mitotic inhibitors.
Discovery of histone deacetylase 8 selective inhibitors.
Design and synthesis of N-phenylacetyl (sulfonyl) 4,5-dihydropyrazole derivatives as potential antitumor agents.
Design and synthesis of substituted N-(1,3-diphenyl-1H-pyrazol-5-yl)benzamides as positive allosteric modulators of the metabotropic glutamate receptor subtype 5.
Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.
A new class of -carboline alkaloid-peptide conjugates with therapeutic efficacy in acute limb ischemia/reperfusion injury.
Synthesis, cytotoxicity, metabolic stability and pharmacokinetic evaluation of fluorinated docetaxel analogs.
The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties.
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents.
Improvement of the synthesis and pharmacokinetic properties of chromenotriazolopyrimidine MDM2-p53 protein-protein inhibitors.
Semisynthesis of triptolide analogues: effect of -lactone and C-14 substituents on cytotoxic activities.
Conformationally constrained farnesoid X receptor (FXR) agonists: alternative replacements of the stilbene.
Benzotriazinone and benzopyrimidinone derivatives as potent positive allosteric AMPA receptor modulators.
Screening and optimization of specific chemical series against human African Trypanosomiasis (HAT)
A new bactericidal lead structure for the protection of materials.
Ptilomycalin A inhibits laccase and melanization in Cryptococcus neoformans.
Copper(II) chloride mediated synthesis and DNA photocleavage activity of 1-aryl/heteroaryl-4-substituted-1,2,4-triazolo[4,3-a]quinoxalines.
Anti-inflammatory amino acid derivatives from the ascidian Herdmania momus.
Microbial transformations of diosgenin by the white-rot basidiomycete Coriolus versicolor.
Molecular wipes: application to epidemic keratoconjuctivitis.
Tricyclic aminopyrimidine histamine H4 receptor antagonists.
Synthesis and anticonvulsant properties of new acetamide derivatives of phthalimide, and its saturated cyclohexane and norbornene analogs.
Halogen substituents on the aromatic moiety of the tetracaine scaffold improve potency of cyclic nucleotide-gated channel block.
Discovery and synthesis of novel substituted benzocoumarins as orally active lipid modulating agents.
1-Azaaurones derived from the naturally occurring aurones as potential antimalarial drugs.
Design and synthesis of 2-phenylimidazo[1,2-a]pyridines as a novel class of melatonin receptor ligands.
Anti-inflammatory endiandric acid analogues from the roots of Beilschmiedia tsangii.
Design and synthesis of (+)-discodermolide-paclitaxel hybrids leading to enhanced biological activity.
Exploring Left-Hand-Side substitutions in the benzoxazinone series of 4-amino-piperidine bacterial type IIa topoisomerase inhibitors.
Synthesis and antioxygenic activities of seabuckthorn flavone-3-ols and analogs.
Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease.
Tritoniopsins A-D, cladiellane-based diterpenes from the South China Sea nudibranch Tritoniopsis elegans and its prey Cladiella krempfi.
Isolation and characterization of aphidicolin and chlamydosporol derivatives from Tolypocladium inflatum.
Indolin-2-one p38 inhibitors II: Lead optimisation.
Current status and research strategies in tuberculosis drug development.
Piperidine-based renin inhibitors: upper chain optimization.
Discovery of a series of potent, orally active ,-disubstituted piperidine NK(1) antagonists.
Synthesis and biological evaluation of indolyl glyoxylamides as a new class of antileishmanial agents.
Discovery of the inhibitors of tumor necrosis factor alpha with structure-based virtual screening.
Rational design of novel pyrrolidine derivatives as orally active neurokinin-3 receptor antagonists.
Synthesis and antifungal activity of benzofuran-5-ols.
Discovery of orally bioavailable imidazo[1,2-a]pyrazine-based Aurora kinase inhibitors.
Search for antifungal compounds from the wood of durable tropical trees.
A Bisindole Alkaloid with Hedgehog Signal Inhibitory Activity from the Myxomycete Perichaena chrysosperma.
Design, synthesis and antifungal evaluation of 1-(2-(2,4-difluorophenyl)-2-hydroxy-3-(1H-1,2,4-triazol-1-yl)propyl)-1H-1,2,4-triazol-5(4H)-one.
Dual IGF-1R/SRC inhibitors based on a N'-aroyl-2-(1H-indol-3-yl)-2-oxoacetohydrazide structure.
Identification of pentacyclic triterpenes derivatives as potent inhibitors against glycogen phosphorylase based on 3D-QSAR studies.
Efficient synthesis, structural characterization and anti-microbial activity of chiral aryl boronate esters of 1,2-O-isopropylidene--D-xylofuranose.
Benzodihydrofurans from Cyperus teneriffae.
Synthesis, radiofluorination and pharmacological evaluation of a fluoromethyl spirocyclic PET tracer for central 1 receptors and comparison with fluoroalkyl homologs.
Synthesis of novel histamine H4 receptor antagonists.
Synthesis, characterization and activity of new phosphonate dipeptides as potential inhibitors of VanX.
Towards a modern definition of vitamin E-evidence for a quinone hypothesis.
Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.
Synthesis of new 5,6-dihydrobenzo[h]quinazoline 2,4-diamino substituted and antiplatelet/antiphlogistic activities evaluation.
Thiazolides as novel antiviral agents. 2. Inhibition of hepatitis C virus replication.
Quinolone derivatives containing strained spirocycle as orally active glycogen synthase kinase 3 (GSK-3) inhibitors for type 2 diabetics.
Novel potent 2,5-pyrrolidinedione peptidomimetics as aminopeptidase N inhibitors. Design, synthesis and activity evaluation.
Synthesis and in vitro evaluation of novel pro-drugs for the treatment of nephropathic cystinosis.
Bioactive neo-clerodane diterpenoids from the whole plants of Ajuga ciliata Bunge.
Quinoline-4-methyl esters as human nonpancreatic secretory phospholipase A2 inhibitors.
Seco-eremophiladiolides and eremophilane glucosides from Pittocaulon velatum.
Regioselective synthesis of water-soluble monophosphate derivatives of combretastatin A-1.
Antifungal susceptibility profile of human-pathogenic species of Lichtheimia.
Mutant selection window and characterization of allelic diversity for ciprofloxacin-resistant mutants of Rhodococcus equi.
Role of Fks1p and matrix glucan in Candida albicans biofilm resistance to an echinocandin, pyrimidine, and polyene.
Antimicrobial activity of CHIR-090, an inhibitor of lipopolysaccharide biosynthesis, against the Burkholderia cepacia complex.
N-acetylcysteine-mediated modulation of bacterial antibiotic susceptibility.
The GABA(A) receptor as a target for photochromic molecules.
Synthesis, biological assay in vitro and molecular docking studies of new imidazopyrazinone derivatives as potential dipeptidyl peptidase IV inhibitors.
Synthesis and antimicrobial studies of thiazolotriazinones.
Synthesis and antituberculosis activity of some new pyridazine derivatives. Part II.
Synthesis and biological evaluation of some 1,3,4-oxadiazole derivatives.
Synthesis and antitumor activity of novel 6-aryl and 6-alkylpyrazolo[3,4-d]pyrimidin-4-one derivatives.
Synthesis and biological evaluation of 2-phenylthiazole-4-carboxamide derivatives as anticancer agents.
Concise synthesis of 5,6-dihydrovaltrate leading to enhanced Rev-export inhibitory congener.
Dual inhibitors of inosine monophosphate dehydrogenase and histone deacetylase based on a cinnamic hydroxamic acid core structure.
Limonoids from the leaves of Cipadessa baccifera.
Novel antifungal agents: triazolopyridines as inhibitors of beta-1,6-glucan synthesis.
Flavonoids in the poisonous plant Oxytropis falcata.
Computer-aided optimization of phosphinic inhibitors of bacterial ureases.
Crystal structure-based selective targeting of the pyridoxal 5'-phosphate dependent enzyme kynurenine aminotransferase II for cognitive enhancement.
Synthesis and structure-activity relationships of novel 8a-aza-8a-homoerythromycin A ketolides.
Glucosylated deferiprone and its brain uptake: implications for developing glucosylated hydroxypyridinone analogues intended to cross the blood-brain barrier.
Polyacetylenes from the roots of Polyalthia debilis.
Affinity of doripenem and comparators to penicillin-binding proteins in Escherichia coli and Pseudomonas aeruginosa.
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
In vivo therapeutic effect of gatifloxacin on BALB/c mice infected with Nocardia brasiliensis.
Efficacy of SPK-843, a novel polyene antifungal, in a murine model of systemic cryptococcosis.
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
Biochemical characterization of SHV-55, an extended-spectrum class A beta-lactamase from Klebsiella pneumoniae.
Efficacy of benzoxazinorifamycins in a mouse model of Chlamydia pneumoniae lung infection.
Susceptibility testing of anidulafungin and voriconazole alone and in combination against conidia and hyphae of Aspergillus spp. under hypoxic conditions.
Antistreptococcal activity of AR-709 compared to that of other agents.
Factor Xa inhibitors: next-generation antithrombotic agents.
Synthesis, SAR, and atropisomerism of imidazolopyrimidine DPP4 inhibitors.
Peripheral but crucial: a hydrophobic pocket (Tyr(706), Leu(337), and Met(336)) for potent and selective inhibition of neuronal nitric oxide synthase.
Metallocene catalyzed synthesis of fungistatic vicinal aminoalcohols under solvent free conditions.
Biologically active biotin derivatives of schweinfurthin F.
Synthesis and evaluation of benzoxazole derivatives as 5-lipoxygenase inhibitors.
Berberine derivatives, with substituted amino groups linked at the 9-position, as inhibitors of acetylcholinesterase/butyrylcholinesterase.
New pyridazinone derivatives with vasorelaxant and platelet antiaggregatory activities.
Tailored -methylene--butyrolactones and their effects on growth suppression in pancreatic carcinoma cells.
Synthesis and evaluation of bivalent, peptidomimetic antagonists of the v3 integrins.
Cell permeability as a parameter for lead generation in the protein Tyrosine kinase inhibition field.
Acid dissociation constant, a potential physicochemical factor in the inhibition of the enzyme estrone sulfatase (ES).
Genomics of Drug Sensitity in Cancer screening data, Wellcome Trust Sanger Institute
Molecular basis of inverse agonism in a G protein-coupled receptor.
Metabolic installation of thiols into sialic acid modulates adhesion and stem cell biology.
Diarylquinolines target subunit c of mycobacterial ATP synthase.
Small-molecule activation of neuronal cell fate.
Indole RSK inhibitors. Part 1: discovery and initial SAR.
New benzimidazole derivatives as antiplasmodial agents and plasmepsin inhibitors: synthesis and analysis of structure-activity relationships.
New inhibitors of dihydroorotate dehydrogenase (DHODH) based on the 4-hydroxy-1,2,5-oxadiazol-3-yl (hydroxyfurazanyl) scaffold.
CMY-31 and CMY-36 cephalosporinases encoded by ColE1-like plasmids.
Bronchopulmonary disposition of micafungin in healthy adult volunteers.
Contribution of vraSR and graSR point mutations to vancomycin resistance in vancomycin-intermediate Staphylococcus aureus.
Activity of anidulafungin in a murine model of Candida krusei infection: evaluation of mortality and disease burden by quantitative tissue cultures and measurement of serum (1,3)-beta-D-glucan levels.
Inhibitory and bactericidal activities of daptomycin, vancomycin, and teicoplanin against methicillin-resistant Staphylococcus aureus isolates collected from 1985 to 2007.
A small-molecule dengue virus entry inhibitor.
Susceptibility of gram-negative pathogens isolated from patients with complicated intra-abdominal infections in the United States, 2007-2008: results of the Study for Monitoring Antimicrobial Resistance Trends (SMART).
Endocannabinoids inhibit the growth of free-living amoebae.
Synthesis and biological evaluation of N-substituted-3,5-diphenyl-2-pyrazoline derivatives as cyclooxygenase (COX-2) inhibitors.
Solomonsterols A and B from Theonella swinhoei. The first example of C-24 and C-23 sulfated sterols from a marine source endowed with a PXR agonistic activity.
Development of potent and opioid agonists with high lipophilicity.
Pipecolic acid derivatives as small-molecule inhibitors of the Legionella MIP protein.
Synthesis and antimalarial assessment of a new series of orally active amino-functionalized spiro 1,2,4-trioxanes.
Nicotinic acid adenine dinucleotide phosphate analogues containing substituted nicotinic acid: effect of modification on Ca(2+) release.
Synthesis and evaluation of pyrazolone compounds as SARS-coronavirus 3C-like protease inhibitors.
Indazolylpyrazolopyrimidine as highly potent B-Raf inhibitors with in vivo activity.
Design and synthesis of acetamido tri- and tetra-hydroxyazepanes: potent and selective beta-N-acetylhexosaminidase inhibitors.
Synthesis and in vivo evaluation of 3-substituted gababutins.
Synthesis and anticancer activities of ageladine A and structural analogs.
Synthesis and antiviral activity of 3-substituted imidazo[1,2-a]pyridines.
Atropisomeric small molecule Bcl-2 ligands: determination of bioactive conformation.
[2-(4-Phenyl-4-piperidinyl)ethyl]amine based CCR5 antagonists: derivatizations at the N-terminal of the piperidine ring.
Synthesis of casimiroin and optimization of its quinone reductase 2 and aromatase inhibitory activities.
7-Sulfonamido-3-benzazepines as potent and selective 5-HT2C receptor agonists: hit-to-lead optimization.
Identification of a metabolically stable triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor with antimalarial activity in mice.
Fundamental relationships between structure, reactivity, and biological activity for the duocarmycins and CC-1065.
Synthesis of new acridines and hydrazones derived from cyclic beta-diketone for cytotoxic and antiviral evaluation.
Rapid assessment of a novel series of selective CB(2) agonists using parallel synthesis protocols: A Lipophilic Efficiency (LipE) analysis.
1,4-Benzodiazepin-2-one derived neurokinin-1 receptor antagonists
2-[4-(o-methoxyphenyl)piperazin-1-ylmethyl]-1,3-dioxoperhydroimidazo[1,5-a]pyridine as a new selective 5-HT1A receptor ligand
K-13 and of4949: Evaluation of key partial structures and pharmacophore delineation
Synthesis and opioid binding properties of 2-chloroacrylamido derivatives of 7,8-dihydromorphinans
Antiinflammatory -benzeneethanamines. III
Inactivation of HIV-1 protease by a tripeptidyl epoxide
Synthesis and evaluation of a thio analogue of duocarmycin SA.
Structurally diverse limonoids from the fruits of Swietenia mahagoni.
Differential antibiotic susceptibility of Mycobacterium abscessus variants in biofilms and macrophages compared to that of planktonic bacteria.
Cytotoxic and novel compounds from Solanum indicum.
Sequoiatones C-f, constituents of the redwood endophyte Aspergillus parasiticus.
New Xenia diterpenoids from the Indonesian soft coral Xenia sp.
Potent D-peptide inhibitors of HIV-1 entry.
Zwitterionic uracil derivatives as potent GnRH receptor antagonists with improved pharmaceutical properties.
Synthesis of somatostatin analogues containing C-terminal adamantane and their antiproliferative properties.
Insulin-releasing activity of a series of phenylalanine derivatives.
9-Arylpurines as a novel class of enterovirus inhibitors.
Synthesis and opioid receptor binding affinities of 2-substituted and 3-aminomorphinans: ligands for mu, kappa, and delta opioid receptors.
Highly suppressing wild-type HIV-1 and Y181C mutant HIV-1 strains by 10-chloromethyl-11-demethyl-12-oxo-calanolide A with druggable profile.
Synthesis of bisboron compounds and their strong inhibitory activity on store-operated calcium entry.
Regioselective one-pot synthesis and anti-proliferative and apoptotic effects of some novel tetrazolo[1,5-a]pyrimidine derivatives.
3D-QSAR studies on quinazoline antifolate thymidylate synthase inhibitors by CoMFA and CoMSIA models.
Synthesis of novel benzocoumarin derivatives as lipid lowering agents.
Phloroglucinol glycosides from the fresh fruits of Eucalyptus maideni.
Identification of novel monoamine oxidase B inhibitors by structure-based virtual screening.
Design and synthesis of HCV agents with sequential triple inhibitory potentials.
Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.
Discovery of cannabinoid-1 receptor antagonists by virtual screening.
Discovery of substituted benzyl tetrazoles as histamine H3 receptor antagonists.
Design, synthesis, and evaluation of quinazoline T cell proliferation inhibitors.
Unnatural enantiomer of chaetocin shows strong apoptosis-inducing activity through caspase-8/caspase-3 activation.
Synthesis, activity, and pharmacokinetic properties of a series of conformationally-restricted thiourea analogs as novel hepatitis C virus inhibitors.
Penta-substituted benzimidazoles as potent antagonists of the calcium-sensing receptor (CaSR-antagonists).
1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists.
SHAFTS: a hybrid approach for 3D molecular similarity calculation. 2. Prospective case study in the discovery of diverse p90 ribosomal S6 protein kinase 2 inhibitors to suppress cell migration.
Scalarane sesterterpenes from the sponge Hyatella sp.
Evaluation of superior BACE1 cleavage sequences containing unnatural amino acids.
Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.
Identification of inhibitors that block vaccinia virus infection by targeting the DNA synthesis processivity factor D4.
Flavonoids with an oligopolysulfated moiety: a new class of anticoagulant agents.
First Selective CYP11B1 Inhibitors for the Treatment of Cortisol-Dependent Diseases.
A Opioid Pharmacophore Becomes a Spinally Selective - Agonist When Modified with a Basic Extender Arm.
Study of kaempferol glycoside as an insulin mimic reveals glycon to be the key active structure.
Kinase inhibition by deoxy analogues of the resorcylic lactone L-783277.
Identification of potent and selective glucosylceramide synthase inhibitors from a library of N-alkylated iminosugars.
N-3 Hydroxylation of Pyrimidine-2,4-diones Yields Dual Inhibitors of HIV Reverse Transcriptase and Integrase.
Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS.
Development of Selective LH Receptor Agonists by Heterodimerization with a FSH Receptor Antagonist.
Sulfonate-containing thiiranes as selective gelatinase inhibitors.
Discovery of AMG 369, a Thiazolo[5,4-b]pyridine Agonist of S1P1 and S1P5.
Erythromycin- and chloramphenicol-induced ribosomal assembly defects are secondary effects of protein synthesis inhibition.
CraA, a major facilitator superfamily efflux pump associated with chloramphenicol resistance in Acinetobacter baumannii.
Emerging Klebsiella pneumoniae isolates coproducing KPC-2 and VIM-1 carbapenemases.
Identification of the aminoglycoside resistance determinants armA and rmtC among non-Typhi Salmonella isolates from humans in the United States.
Antimalarial activity of tigecycline, a novel glycylcycline antibiotic.
In vitro activities of trioxaquines against Schistosoma mansoni.
Emergence of Klebsiella pneumoniae ST258 with KPC-2 in Poland.
Efficacy of albaconazole against Candida albicans in a vaginitis model.
In vivo antibacterial activity of vertilmicin, a new aminoglycoside antibiotic.
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
Nosocomial spread of colistin-only-sensitive sequence type 235 Pseudomonas aeruginosa isolates producing the extended-spectrum beta-lactamases GES-1 and GES-5 in Spain.
In vitro activity of a new quinoline derivative, ER-2, against clinical isolates of Mycoplasma pneumoniae and Mycoplasma hominis.
In vivo activity of a novel anti-methicillin-resistant Staphylococcus aureus cephalosporin, ceftaroline, against vancomycin-susceptible and -resistant Enterococcus faecalis strains in a rabbit endocarditis model: a comparative study with linezolid and vancomycin.
Novel N-substituted 4-hydrazino piperidine derivative as a dipeptidyl peptidase IV inhibitor.
8-(Dicyclopropylmethyl)-1,3-dipropylxanthine: a potent and selective adenosine A1 antagonist with renal protective and diuretic activities.
Tolerance of benznidazole in treatment of Chagas' disease in adults.
In vitro activities of several antimicrobial agents against recently isolated and genotyped Chlamydia trachomatis urogenital serovars D through K.
Convergent evolution-guided design of antimicrobial peptides derived from influenza A virus hemagglutinin.
Evaluation of quinazoline analogues as glucocerebrosidase inhibitors with chaperone activity.
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Melampomagnolide B: a new antileukemic sesquiterpene.
Novel Cyclic Phosphinic Acids as GABAC Receptor Antagonists: Design, Synthesis, and Pharmacology.
Synthesis and Evaluation of Fluorinated Aporphines: Potential Positron Emission Tomography Ligands for D2 Receptors
Synthesis and in Vitro and in Vivo Evaluation of Phosphoinositide-3-kinase Inhibitors.
Discovery of MK-5046, a Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Structure-Activity Relationships at the Monoamine Transporters for a Novel Series of Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide) Analogues.
Activation of Neuropeptide FF Receptors by Kisspeptin Receptor Ligands.
Discovery of PSI-353661, a Novel Purine Nucleotide Prodrug for the Treatment of HCV Infection.
TSPO 18 kDa (PBR) Targeted Photosensitizers for Cancer Imaging (PET) and PDT.
Discovery of novel cyanamide-based inhibitors of cathepsin C.
Benzimidazoles as Potent and Orally Active mGlu5 Receptor Antagonists with an Improved PK Profile.
Novel 3-aryl indoles as progesterone receptor antagonists for uterine fibroids.
Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1).
Discovery of MK-1220: A Macrocyclic Inhibitor of Hepatitis C Virus NS3/4A Protease with Improved Preclinical Plasma Exposure.
Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist.
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.
Discovery of a potent nicotinic Acid receptor agonist for the treatment of dyslipidemia.
Synthesis and antibacterial activity of a novel class of 15-membered macrolide antibiotics, "11a-azalides".
Synthesis and SAR of Thiazolylmethylphenyl Glucoside as Novel C-Aryl Glucoside SGLT2 Inhibitors.
Structure guided development of potent reversibly binding penicillin binding protein inhibitors.
Inhibitors of HCV NS5A: From Iminothiazolidinones to Symmetrical Stilbenes.
Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone.
Hybrid dual aromatase-steroid sulfatase inhibitors with exquisite picomolar inhibitory activity.
Novel, Broad Spectrum Anti-Cancer Agents Containing the Tricyclic 5:7:5-Fused Diimidazodiazepine Ring System.
In vitro activities of linezolid against clinical isolates of Mycobacterium tuberculosis complex isolated in Taiwan over 10 years.
Inducible resistance of fish bacterial pathogens to the antimicrobial peptide cecropin B.
Coprevalence of plasmid-mediated quinolone resistance determinants QepA, Qnr, and AAC(6')-Ib-cr among 16S rRNA methylase RmtB-producing Escherichia coli isolates from pigs.
Origin and molecular evolution of the determinant of methicillin resistance in staphylococci.
Frequency of spontaneous resistance to fosfomycin combined with different antibiotics in Pseudomonas aeruginosa.
Characteristics and dissemination of mosaic penicillin-binding protein 2-harboring multidrug-resistant Neisseria gonorrhoeae isolates with reduced cephalosporin susceptibility in northern Taiwan.
A mecA-negative strain of methicillin-resistant Staphylococcus aureus with high-level -lactam resistance contains mutations in three genes.
Emergence of metallo--lactamase NDM-1-producing multidrug-resistant Escherichia coli in Australia.
Interplay between drug efflux and antioxidants in Escherichia coli resistance to antibiotics.
Inhibition of bacterial multidrug resistance by celecoxib, a cyclooxygenase-2 inhibitor.
Extremely drug-resistant Citrobacter freundii isolate producing NDM-1 and other carbapenemases identified in a patient returning from India.
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
Interaction potential of etravirine with drug transporters assessed in vitro.
Nardosinane sesquiterpenoids from the Formosan soft coral Lemnalia flava.
Thiazolidione derivatives as novel antibiofilm agents: design, synthesis, biological evaluation, and structure-activity relationships.
Flavonoids from eight tropical plant species that inhibit the multidrug resistance transporter ABCG2.
Tripeptide motifs in biology: targets for peptidomimetic design.
Dinoxin B, a withanolide from Datura inoxia leaves with specific cytotoxic activities.
Bendigoles D-F, bioactive sterols from the marine sponge-derived Actinomadura sp. SBMs009.
Ethionamide boosters: synthesis, biological activity, and structure-activity relationships of a series of 1,2,4-oxadiazole EthR inhibitors.
Design, synthesis and in vitro antimicrobial evaluation of novel Imidazo[1,2-a]pyridine and imidazo[2,1-b][1,3]benzothiazole motifs.
Synthesis of 4-carbamoyl epipodophyllotoxins as potential antitumour agents.
Two-step synthesis of novel, bioactive derivatives of the ubiquitous cofactor nicotinamide adenine dinucleotide (NAD).
Identification and characterization of novel inhibitors of mPTPB, an essential virulent phosphatase from Mycobacterium tuberculosis.
Cytotoxic triterpenoids from the stems of Microtropis japonica.
Monoterpenoid indole alkaloids from Gardneria ovata.
An efficient preparation of N-alkyl-2-benzazepine derivatives and investigation of their biological activity.
Toluidinesulfonamide hypoxia-induced factor 1 inhibitors: alleviating drug-drug interactions through use of PubChem data and comparative molecular field analysis guided synthesis.
Design and synthesis of 3-alkyl-2-aryl-1,3-thiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
Concise synthesis and CDK/GSK inhibitory activity of the missing 9-azapaullones.
Thiazolylmethyl ortho-substituted phenyl glucoside library as novel C-aryl glucoside SGLT2 inhibitors.
Microwave-assisted synthesis, crystal structure of pyrazolo[1,5-a]pyrazin-4(5H)-ones and their selective effects on lung cancer cells.
1,5-Disubstituted indole derivatives as selective human neuronal nitric oxide synthase inhibitors.
9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.
Synthesis and in vitro activity of novel 1,2,4-triazolo[4,3-a]pyrimidine oxazolidinone antibacterial agents. Part II.
In vitro activities of piperaquine, lumefantrine, and dihydroartemisinin in Kenyan Plasmodium falciparum isolates and polymorphisms in pfcrt and pfmdr1.
Postantibiotic effect of ceftaroline against gram-positive organisms.
Susceptibilities of 23 Desulfovibrio isolates from humans.
Extended-spectrum cephalosporinase in Acinetobacter baumannii.
Development of daptomycin nonsusceptibility with heterogeneous vancomycin-intermediate resistance and oxacillin susceptibility in methicillin-resistant Staphylococcus aureus during high-dose daptomycin treatment.
Easy strategy to protect antimicrobial peptides from fast degradation in serum.
Clinical outcomes by methicillin-resistant Staphylococcus aureus staphylococcal cassette chromosome mec type: isolates recovered from a phase IV clinical trial of linezolid and vancomycin for complicated skin and skin structure infections.
In vitro antimicrobial activity and mutant prevention concentration of colistin against Acinetobacter baumannii.
Synthesis and activities of naphthalimide azoles as a new type of antibacterial and antifungal agents.
New 2-thioether-substituted apomorphines as potent and selective dopamine D2 receptor agonists.
Azaphilones from the endophyte Chaetomium globosum.
Structure and cytotoxicity of diterpenoids from Isodon adenolomus.
Synthesis of novel vitamin K2 analogues with modification at the -terminal position and their biological evaluation as potent steroid and xenobiotic receptor (SXR) agonists.
Development of endocannabinoid-based chemical probes for the study of cannabinoid receptors.
Protuboxepins A and B and protubonines A and B from the marine-derived fungus Aspergillus sp. SF-5044.
Progress in structure based drug design for G protein-coupled receptors.
Synthesis and docking studies on styryl chromones exhibiting cytotoxicity in human breast cancer cell line.
Discovery of omecamtiv mecarbil the first, selective, small molecule activator of cardiac Myosin.
A broad spectrum anticancer nucleoside with selective toxicity against human colon cells in vitro.
Identification of a new series of non-peptidic NK3 receptor antagonists.
Semisynthetic analogues of the marine cembranoid sarcophine as prostate and breast cancer migration inhibitors.
Synthesis and antidepressant-like activity evaluation of sulphonamides and sulphonyl-hydrazones.
The synthesized novel fluorinated compound (LJJ-10) induces death receptor- and mitochondria-dependent apoptotic cell death in the human osteogenic sarcoma U-2 OS cells.
Selectivity of kinase inhibitor fragments.
Specific inhibitions of annonaceous acetogenins on class II 3-hydroxy-3-methylglutaryl coenzyme A reductase from Streptococcus pneumoniae.
Hippocampal and cortical neuronal growth mediated by the small molecule natural product clovanemagnolol.
C5'-Alkyl Substitution Effects on Digitoxigenin -l-Glycoside Cancer Cytotoxicity.
6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.
Development of a highly selective fluorescence probe for alkaline phosphatase.
3-benzhydryl-4-piperidones as novel neurokinin-1 receptor antagonists and their efficient synthesis.
Synthesis and antiplasmodial activity of bicyclic dioxanes as simplified dihydroplakortin analogues.
Dimerization of piceatannol by Momordica charantia peroxidase and -glucosidase inhibitory activity of the biotransformation products.
Synthesis and evaluation of dual site inhibitors of 3-deoxy-D-arabino-heptulosonate 7-phosphate synthase.
New PDE4 inhibitors based on pharmacophoric similarity between papaverine and tofisopam.
Preliminary finding on a new calcium channel entry blocker chemotype: 5,6-diamino-4-hydroxy-2-mercaptopyrimidine derivatives.
Fragment based discovery of a novel and selective PI3 kinase inhibitor.
Combining symmetry elements results in potent naphthyridinone (NTD) HIV-1 integrase inhibitors.
Identification of pyrido[1,2-]pyrimidine-4-ones as new molecules improving the transcriptional functions of estrogen-related receptor .
Comparative studies on interactions of baicalein, baicalin and scutellarin with lysozyme.
Daedalols A-C, fungal-derived BACE1 inhibitors.
Synthesis and evaluation of novel N-fluoropyridyl derivatives of tropane as potential PET imaging agents for the dopamine transporter.
New imidazo[2,1-b]thiazole derivatives: synthesis, in vitro anticancer evaluation, and in silico studies.
Amine-alkyl derivatives of hydantoin: new tool to combat resistant bacteria.
Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists.
Synthesis, in vivo occupancy, and radiolabeling of potent phosphodiesterase subtype-10 inhibitors as candidates for positron emission tomography imaging.
Radiosynthesis of three [11C]ureido-substituted benzenesulfonamides as PET probes for carbonic anhydrase IX in tumors.
Synthesis and biological profile of new 1,2,3,4-tetrahydroisoquinolines as selective carbonic anhydrase inhibitors.
Diversity-oriented synthesis: exploring the intersections between chemistry and biology.
Synthesis and kinetic testing of new inhibitors for a metallo--lactamase from Klebsiella pneumonia and Pseudomonas aeruginosa.
Indolin-2-one p38 inhibitors III: bioisosteric amide replacement.
Synthesis of 9-substituted 2,3,4,9-tetrahydro-1H-carbazole derivatives and evaluation of their anti-prion activity in TSE-infected cells.
Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 1: perhydropyrrole[1,2-a]pyrazines.
Synthesis and antimycobacterial evaluation of 3a,4-dihydro-3H-indeno [1,2-c] pyrazole-2-carboxamide analogues.
Discovery of spiropiperidine-based potent and selective Orexin-2 receptor antagonists.
Design and synthesis of a library of chemokine antagonists.
Discovery of a novel potent GABA(B) receptor agonist.
A fluorescent probe for GM1 gangliosidosis related -galactosidase: N-(dansylamino)hexylaminocarbonylpentyl-1,5-dideoxy-1,5-imino-D-galactitol.
Continued exploration of biphenylsulfonamide scaffold as a platform for aggrecanase-1 inhibition.
Structural requirement of phenylthiourea analogs for their inhibitory activity of melanogenesis and tyrosinase.
Design, synthesis, and SAR studies of novel polycyclic acids as potent and selective inhibitors of human 11-hydroxysteroid dehydrogenase type 1 (11-HSD-1).
The antiplasmodial activity of norcantharidin analogs.
Polyamide amino acids trimers as TAR RNA ligands and anti-HIV agents.
Toward the development of innovative bifunctional agents to induce differentiation and to promote apoptosis in leukemia: clinical candidates and perspectives.
Chalcone HTMC causes in vitro selective cytotoxicity, cell-cycle G1 phase arrest through p53-dependent pathway in human lung adenocarcinoma A549 cells, and in vivo tumor growth suppression.
Catharanthine C16 substituent effects on the biomimetic coupling with vindoline: preparation and evaluation of a key series of vinblastine analogues.
Indazole derivatives as novel bradykinin B1 receptor antagonists.
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Discovery of 4-anilinofuro[2,3-b]quinoline derivatives as selective and orally active compounds against non-small-cell lung cancers.
Pyrazolopyridazine alpha-2-delta-1 ligands for the treatment of neuropathic pain.
Cytotoxic steroidal alkaloids from Kibatalia laurifolia.
Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP.
An optimized immunoaffinity fluorescent method for natural product target elucidation.
Concise synthesis and antiangiogenic activity of artemisinin-glycolipid hybrids on chorioallantoic membranes.
Design, synthesis and evaluation of polar head group containing 2-keto-oxazole inhibitors of FAAH.
LDV peptidomimetics equipped with biotinylated spacer-arms: synthesis and biological evaluation on CCRF-CEM cell line.
Synthesis and biological evaluation of molecular probes based on the 9-methylstreptimidone derivative DTCM-glutarimide.
Conjugation of spermine enhances cellular uptake of the stapled peptide-based inhibitors of p53-Mdm2 interaction.
Cytotoxic withanolide constituents of Physalis longifolia.
Chromenones as potent bradykinin B1 antagonists.
Fused thiophene derivatives as MEK inhibitors.
Structure-based design of PDK1 inhibitors.
Discovery of bacterial NAD+-dependent DNA ligase inhibitors: improvements in clearance of adenosine series.
Cytotoxic potential of novel 6,7-dimethoxyquinazolines.
Synthesis and biological evaluation of some novel N-aryl-1,4-dihydropyridines as potential antitubercular agents.
Chromomycin SA analogs from a marine-derived Streptomyces sp.
A synthetic antimicrobial peptidomimetic (LTX 109): stereochemical impact on membrane disruption.
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
Reduced Candida glabrata susceptibility secondary to an FKS1 mutation developed during candidemia treatment.
Comparison of the essential cellular functions of the two murA genes of Bacillus anthracis.
Apoptosis induced by aminoglycosides in LLC-PK1 Cells: comparative study of neomycin, gentamicin, amikacin, and isepamicin using electroporation.
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
Alteration of GyrA amino acid required for ciprofloxacin resistance in Klebsiella pneumoniae isolates in China.
Plasmid-mediated QnrS2 determinant from a clinical Aeromonas veronii isolate.
Plasmid-mediated qnrB2 and carbapenemase gene bla(KPC-2) carried on the same plasmid in carbapenem-resistant ciprofloxacin-susceptible Enterobacter cloacae isolates.
Cell-penetrating peptide TP10 shows broad-spectrum activity against both Plasmodium falciparum and Trypanosoma brucei brucei.
Activities of ceftobiprole, linezolid, vancomycin, and daptomycin against community-associated and hospital-associated methicillin-resistant Staphylococcus aureus.
Mechanism and fitness costs of PR-39 resistance in Salmonella enterica serovar Typhimurium LT2.
Kinetic characterization of VIM-7, a divergent member of the VIM metallo-beta-lactamase family.
Small-molecule regulation of zebrafish gene expression.
Identification and mechanistic characterization of low-molecular-weight inhibitors for HuR.
Mechanisms, biology and inhibitors of deubiquitinating enzymes.
Panel of prototypical raltegravir-resistant infectious molecular clones in a novel integrase-deleted cloning vector.
Combined ramR mutation and presence of a Tn1721-associated tet(A) variant in a clinical isolate of Salmonella enterica serovar Hadar resistant to tigecycline.
In vitro activity of CEM-101, a new fluoroketolide antibiotic, against Chlamydia trachomatis and Chlamydia (Chlamydophila) pneumoniae.
High prevalence of ST131 isolates producing CTX-M-15 and CTX-M-14 among extended-spectrum-beta-lactamase-producing Escherichia coli isolates from Canada.
Evaluation of new thiazolide/thiadiazolide derivatives reveals nitro group-independent efficacy against in vitro development of Cryptosporidium parvum.
In vitro sensitivities of Plasmodium falciparum to different antimalarial drugs in Uganda.
GES-13, a beta-lactamase variant possessing Lys-104 and Asn-170 in Pseudomonas aeruginosa.
Design, synthesis and evaluation of (E)-alpha-benzylthio chalcones as novel inhibitors of BCR-ABL kinase.
Synthesis and evaluation of graveoline and graveolinine derivatives with potent anti-angiogenesis activities.
N'-[(5-chloro-3-methyl-1-phenyl-1H-pyrazol-4-yl)methylene] 2/4-substituted hydrazides: synthesis and anticonvulsant activity.
Design, synthesis, and structure-activity relationship studies of N-arylsulfonyl morpholines as -secretase inhibitors.
Syntheses of fluorescent imidazoquinoline conjugates as probes of Toll-like receptor 7.
Substituted pyrazoles as novel sEH antagonist: investigation of key binding interactions within the catalytic domain.
Triazolyl tryptoline derivatives as -secretase inhibitors.
Macrolide antibiotic-mediated downregulation of MexAB-OprM efflux pump expression in Pseudomonas aeruginosa.
Development of caspofungin resistance following prolonged therapy for invasive candidiasis secondary to Candida glabrata infection.
Metronidazole lacks antibacterial activity in guinea pigs infected with Mycobacterium tuberculosis.
Fluoroquinolone enhances the mutation frequency for meropenem-selected carbapenem resistance in Pseudomonas aeruginosa, but use of the high-potency drug doripenem inhibits mutant formation.
Characterization of TolC efflux pump proteins from Pasteurella multocida.
Effect of therapeutic chemical agents in vitro and on experimental meningoencephalitis due to Naegleria fowleri.
Interspecies recombination occurs frequently in quinolone resistance-determining regions of clinical isolates of Streptococcus pyogenes.
Inhibition of Toxoplasma gondii by indirubin and tryptanthrin analogs.
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
Synthesis and biological evaluation of vitamin K derivatives as angiogenesis inhibitor.
Synthesis, biological evaluation, and docking studies of novel heterocyclic diaryl compounds as selective COX-2 inhibitors.
Allicin and derivates are cysteine protease inhibitors with antiparasitic activity.
[3-azabicyclo[3.1.0]hex-1-yl]phenyl-benzenesulfonamides as selective dopamine D3 antagonists.
Discovery of a novel class of aldol-derived 1,2,3-triazoles: potent and selective inhibitors of human cytochrome P450 19A1 (aromatase).
Synthesis and antifungal evaluation of pyrido[1,2-a]indole-1,4-diones and benzo[f]pyrido[1,2-a]indole-6,11-diones.
Design and synthesis of potent carboxylic acid DGAT1 inhibitors with high cell permeability.
Cytotoxic and antimalarial azaphilones from Chaetomium longirostre.
Identification of novel, exosite-binding matrix metalloproteinase-13 inhibitor scaffolds.
aza-Flavanones as potent cross-species microRNA inhibitors that arrest cell cycle.
Semisynthetic neoboutomellerone derivatives as ubiquitin-proteasome pathway inhibitors.
A specific protein disorder catalyzer of HIV-1 Nef.
Nodularin-Har: a new nodularin from Nodularia.
Suberosols A-D, four new sesquiterpenes with beta-caryophyllene skeletons from a Taiwanese gorgonian coral Subergorgia suberosa.
Tasiamide, a cytotoxic peptide from the marine cyanobacterium Symploca sp.
Ravenic acid, a new tetramic acid isolated from a cultured microfungus, Penicillium sp.
Novel terpenoids from the formosan soft coral Cespitularia hypotentaculata.
Antitumor agents, 93. Bruceanol C, a new cytotoxic quassinoid from Brucea antidysenterica.
Additional biologically active constituents of the Chinese tallow tree (Sapium sebiferum).
Daucane sesquiterpenes from Ferula hermonis.
A new photosystem II electron transfer inhibitor from Sorghum bicolor.
Five new polyacetylenes from a sponge of the genus petrosia
2,4,5- triarylimidazole inhibitors of IL-1 biosynthesis
Design of dual acting anticonvulsant-antimuscarinic succinimide and hydantoin derivatives
Potent, selective, water-soluble benzodiazepine-based CCKB receptor antagonists that contain lipophilic carboxylate surrogates
Heterocyclic analogs of the benzolactam nucleus of the non-peptidic growth hormone secretagogue L-692,429
Kinetics of thermal [1,7a]-sigmatropic shift of hexafluoro vitamin D3 and vitamin D3 derivatives. Evaluation of conformations of the A ring affected by 1-OH and 3-OH groups.
Synthesis of -hydroxy statine through a facially selective osmylation of a chiral -amido crotonate
Synthesis of a chemiluminescent probe useful for the purification of steroid 5-reductase
Selective cyclooxygenase inhibitors: Novel 4-spiro 1,2-diarylcyclopentenes are potent and orally active cox-2 inhibitors
Anti-human immunodeficiency virus type 1 activities of antimicrobial peptides derived from human and bovine cathelicidins.
Microbiological and genotypic analysis of methicillin-resistant Staphylococcus aureus bacteremia.
Plasmid-encoded carbapenem-hydrolyzing beta-lactamase OXA-48 in an imipenem-susceptible Klebsiella pneumoniae strain from Belgium.
Trioxaquines and heme-artemisinin adducts inhibit the in vitro formation of hemozoin better than chloroquine.
Lowering of 5-nitroimidazole's mutagenicity: towards optimal antiparasitic pharmacophore.
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus.
Tricyclic HIV integrase inhibitors V. SAR studies on the benzyl moiety.
Anthranilamide-based N,N-dialkylbenzamidines as potent and orally bioavailable factor Xa inhibitors: P4 SAR.
Modified low molecular weight cyclic peptides as mimetics of BDNF with improved potency, proteolytic stability and transmembrane passage in vitro.
Brain-penetrating 2-aminobenzimidazole H(1)-antihistamines for the treatment of insomnia.
Design, synthesis and hypolipidemic activity of novel 2-(naphthalen-2-yloxy)propionic acid derivatives as desmethyl fibrate analogs.
Cytotoxic and anti-inflammatory cembranoids from the soft coral Lobophytum crassum.
Preliminary SAR analysis of novel antiproliferative N(6),5'-bis-ureidoadenosine derivatives.
Synthesis and activity in enhancing long-term potentiation (LTP) of clausenamide stereoisomers.
3-Hydroxyisoquinolines as inhibitors of HCV NS5b RNA-dependent RNA polymerase.
Ganomycins A and B, new antimicrobial farnesyl hydroquinones from the basidiomycete Ganoderma pfeifferi.
Bioactive compounds from Combretum erythrophyllum.
Synthesis and antiproliferative activities of ottelione a analogues.
Synthesis and structure-activity relationships of tri-substituted thiazoles as RAGE antagonists for the treatment of Alzheimer's disease.
CJ-1639: A Potent and Highly Selective Dopamine D3 Receptor Full Agonist.
Synthesis, characterization and biological studies of diosgenyl analogues.
Fluorescent derivatives of AC-42 to probe bitopic orthosteric/allosteric binding mechanisms on muscarinic M1 receptors.
Small Molecule Ligands For Active Targeting Of TrkC-expressing Tumor Cells.
SAR Development of Lysine-Based Irreversible Inhibitors of Transglutaminase 2 for Huntington's Disease.
Tuning the activity of a short arg-trp antimicrobial Peptide by lipidation of a C- or N-terminal lysine side-chain.
Preparation of N-(Hetero)cyclyl Benzamides as Inhibitors of the Activity of Complex III of the Mitochondrial Electron Transport Chain: Patent Highlight.
Sesquiterpenoids from Atractylodes macrocephala act as farnesoid X receptor and progesterone receptor modulators.
Phenolic compounds from Caesalpinia sappan heartwood and their anti-inflammatory activity.
Synthesis and antibacterial activity of new fluoroquinolones containing a cis- or trans-cyclohexane moiety.
Prodrugs of a CXC Chemokine-12 (CXCL12) Neutraligand Prevent Inflammatory Reactions in an Asthma Model in Vivo.
Synthesis and biological evaluation of novel spin labeled 18-glycyrrhetinic acid derivatives.
Peptides and Pseudopeptides as SIRT6 Deacetylation Inhibitors.
Evaluation of [(11)C]N-Methyl Lansoprazole as a Radiopharmaceutical for PET Imaging of Tau Neurofibrillary Tangles.
Linear and cyclic dipeptides with antimalarial activity.
Atom-based enumeration: new eribulin analogues with low susceptibility to P-glycoprotein-mediated drug efflux.
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Structure Activity Relationship Study of the Cleistriosides and Cleistetrosides for Antibacterial/Anticancer Activity.
Nitric oxide donor doxorubicins accumulate into Doxorubicin-resistant human colon cancer cells inducing cytotoxicity.
Brominated aromatic furanones and related esters from the ascidian Synoicum sp.
Antioxidant glucosylated caffeoylquinic acid derivatives in the invasive tropical soda apple, Solanum viarum.
Riccardin C derivatives as anti-MRSA agents: structure-activity relationship of a series of hydroxylated bis(bibenzyl)s.
Discovery of a 4-Azetidinyl-1-thiazoyl-cyclohexane CCR2 Antagonist as a Development Candidate.
4-Phenyl tetrahydroisoquinolines as dual norepinephrine and dopamine reuptake inhibitors.
Target-Activated Prodrugs (TAPs) for the Autoregulated Inhibition of MMP12.
Pharmaceutical composition comprising indole compound for treatment of diseases associated with oxidative stress: patent highlight.
Desmethyl Macrolides: Synthesis and Evaluation of 4,8-Didesmethyl Telithromycin.
Syntheses and biological evaluation of novel 2alpha-substituted 1alpha,25-dihydroxyvitamin D3 analogues.
Highly potent and selective inhibition of varicella-zoster virus by bicyclic furopyrimidine nucleosides bearing an aryl side chain.
Design, synthesis, and antimicrobial activity of 6-O-substituted ketolides active against resistant respiratory tract pathogens.
Solution structure of iron(III)-anthracycline complexes.
Synthesis and anti-tubulin activity of a 3'-(4-azidophenyl)-3'-dephenylpaclitaxel photoaffinity probe.
Evaluation of antitumor properties of novel saframycin analogs in vitro and in vivo.
(+)-Curcuphenol and (+)-Curcudiol, Sesquiterpene Phenols from Shallow and Deep Water Collections of the Marine Sponge Didiscus flavus
Lipopolyamines incorporating the tetraamine spermine, bound to an alkyl chain, sequester bacterial lipopolysaccharide.
Discovery of an orally bioavailable alkyl oxadiazole beta3 adrenergic receptor agonist.
Cyclic peptides from a Ruegeria strain of bacteria associated with the sponge Suberites domuncula.
Relationship of structure of bridged (2,6-dimethyl-4-pyridinyl)quinolones to mammalian topoisomerase II inhibition
New 1-aryl-4-(biarylmethylene)piperazines as potential atypical antipsychotics sharing dopamine D(2)-receptor and serotonin 5-HT(1A)-receptor affinities.
The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists.
An orally bioavailable positive allosteric modulator of the mGlu4 receptor with efficacy in an animal model of motor dysfunction.
Comparative in vitro susceptibilities of human mycoplasmas and ureaplasmas to a new investigational ketolide, CEM-101.
Functional expression of the canalicular bile salt export pump of human liver.
Characterization of uremic toxin transport by organic anion transporters in the kidney.
Mitochondria-targeting drug oligomycin blocked P-glycoprotein activity and triggered apoptosis in doxorubicin-resistant HepG2 cells.
Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture.
Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.
Synthesis of marine-derived 3-alkylpyridinium alkaloids with potent antiprotozoal activity.
Molecular Insights into Human Monoamine Oxidase B Inhibition by the Glitazone Anti-Diabetes Drugs.
Identification of small-molecule inhibitors of the steroidogenic acute regulatory protein (STARD1) by structure-based design.
Tubulin binding, protein-bound conformation in solution, and antimitotic cellular profiling of noscapine and its derivatives.
Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.
Use of libraries to access new chemical space: applications to CRTH2.
Copper-Free Click for PET: Rapid 1,3-Dipolar Cycloadditions with a Fluorine-18 Cyclooctyne.
Structural basis of selective inhibition of human tankyrases.
Receptor-ligand interaction-based virtual screening for novel Eg5/kinesin spindle protein inhibitors.
Pyrrole-Based Antitubulin Agents: Two Distinct Binding Modalities are Predicted for C-2 Analogs in the Colchicine Site.
An improved microwave assisted one-pot synthesis, and biological investigations of some novel aryldiazenyl chromeno fused pyrrolidines.
Synthesis and characterization of 2'-C-Me branched C-nucleosides as HCV polymerase inhibitors.
Coumarin-trioxane hybrids: synthesis and evaluation as a new class of antimalarial scaffolds.
Disubstituted piperidines as potent orexin (hypocretin) receptor antagonists.
Identification of novel adenosine A(2A) receptor antagonists by virtual screening.
Reexamining hydroxamate inhibitors of botulinum neurotoxin serotype A: extending towards the -exosite.
Discovery of a Potent Retinoid X Receptor Antagonist Structurally Closely Related to RXR Agonist NEt-3IB.
Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening.
Syntheses and biological studies of novel spiropiperazinyl oxazolidinone antibacterial agents using a spirocyclic diene derived acylnitroso Diels-Alder reaction.
Synthesis and SAR of tetrahydroisoquinolines as Rev-erb agonists.
Proposed Bioactive Conformations of Opiorphin, an Endogenous Dual APN/NEP Inhibitor.
Synthesis and SAR of selective small molecule neuropeptide Y Y2 receptor antagonists.
Biological evaluation of new largazole analogues: alteration of macrocyclic scaffold with click chemistry.
Novel 2-aminobenzamides as potential orally active antithrombotic agents.
Insulin-like growth factor-1 receptor inhibitors: a potential cancer treatment: patent highlight.
3D-QSAR Assisted Design, Synthesis and Evaluation of Novobiocin Analogues.
Azepines and piperidines with dual norepinephrine dopamine uptake inhibition and antidepressant activity.
L-Aminoacyl-triazine derivatives are isoform-selective PI3K inhibitors that target non-conserved Asp862 of PI3K
Treatment of Obesity and Related Disorders with Acetyl-CoA Carboxylase Inhibitors.
Discovery of a Series of Thiazole Derivatives as Novel Inhibitors of Metastatic Cancer Cell Migration and Invasion.
Imidazopyridine-Based Fatty Acid Synthase Inhibitors That Show Anti-HCV Activity and in Vivo Target Modulation.
Near native binding of a fluorescent serotonin conjugate to serotonin type 3 receptors.
TRPV4 Antagonists: Potential Treatment for Congestive Heart Failure, Bladder Dysfunctions, and Pain.
Irreversible inhibitors of cysteine proteases.
Antimalarial and Structural Studies of Pyridine-containing Inhibitors of 1-Deoxyxylulose-5-phosphate Reductoisomerase.
Cyclic analogs of galanin and neuropeptide Y by hydrocarbon stapling.
High-Throughput Selectivity Assays for Small-Molecule Inhibitors of -Catenin/T-Cell Factor Protein-Protein Interactions.
Synthesis and Anti-inflammatory Evaluation of Novel Benzimidazole and Imidazopyridine Derivatives.
Discovery of (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid and congeners as highly potent inhibitors of human arginases I and II for treatment of myocardial reperfusion injury.
Azaindole-Based Inhibitors of Cdc7 Kinase: Impact of the Pre-DFG Residue, Val 195.
Novel Amino-Nicotinamide Derivatives as Modulators of KCNQ2/3 Potassium Channels.
Discovery of O-Alkylamino Tethered Niclosamide Derivatives as Potent and Orally Bioavailable Anticancer Agents.
Bodilisant-a novel fluorescent, highly affine histamine h3 receptor ligand.
Modulators of the GPR119 Receptor for the Treatment of Metabolic Syndrome.
Acetylcholinesterase immobilized capillary reactors-tandem mass spectrometry: an on-flow tool for ligand screening.
Bioactive polyhydroxylated steroids from the Hainan soft coral Sinularia depressa Tixier-Durivault.
Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor r1530 for the treatment of solid tumors.
Improving the affinity of SL0101 for RSK using structure-based design.
Identification of acidic heterocycle-substituted 1H-pyrazolo[3,4-b]pyridines as soluble guanylate cyclase stimulators.
Development of opioid receptor antagonists.
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions.
[3a,4]-Dihydropyrazolo[1,5a]pyrimidines: Novel, Potent, and Selective Phosphatidylinositol-3-kinase Inhibitors.
Discovery of a Highly Selective, Brain-Penetrant Aminopyrazole LRRK2 Inhibitor.
Selective inhibition of glycosyltransferases by bivalent imidazolium salts.
Metabolites of the pyrimidine amine preladenant as adenosine a2a receptor antagonists.
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
Structure-Based Approach for the Discovery of Pyrrolo[3,2-d]pyrimidine-Based EGFR T790M/L858R Mutant Inhibitors.
Structural permutation of potent cytotoxin, polytheonamide B: discovery of cytotoxic Peptide with altered activity.
Novel small molecule protein arginine deiminase 4 (PAD4) inhibitors.
The role of the acidity of N-heteroaryl sulfonamides as inhibitors of bcl-2 family protein-protein interactions.
Optimization of a Novel Series of TRPV4 Antagonists with In Vivo Activity in a Model of Pulmonary Edema.
Inhibition of Ebola Virus Infection: Identification of Niemann-Pick C1 as the Target by Optimization of a Chemical Probe.
The C-terminus of Botulinum A Protease Has Profound and Unanticipated Kinetic Consequences Upon the Catalytic Cleft.
Spleen Tyrosine Kinase Inhibitors (SYK) as Potential Treatment for Autoimmune and Inflammatory Disorders: Patent Highlight.
Structure-guided design of selective inhibitors of neuronal nitric oxide synthase.
Discovery of Indenopyrazoles as a New Class of Hypoxia Inducible Factor (HIF)-1 Inhibitors.
New potent calcimimetics: I. Discovery of a series of novel trisubstituted ureas.
Cytotoxicity and modulation of cancer-related signaling by (Z)- and (E)-3,4,3',5'-tetramethoxystilbene isolated from Eugenia rigida.
Bifunctional inhibition of HIV-1 reverse transcriptase: a first step in designing a bifunctional triphosphate.
Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents.
Design, synthesis and insulin-sensitising effects of novel PTP1B inhibitors.
Design, synthesis and biological evaluation of novel imidazo[4,5-c]pyridinecarboxamide derivatives as PARP-1 inhibitors.
Triazolopyridazine LRRK2 kinase inhibitors.
Quinic acid derivatives from Pimpinella brachycarpa exert anti-neuroinflammatory activity in lipopolysaccharide-induced microglia.
Synthesis and biological evaluation of pyridazine derivatives as novel HIV-1 NNRTIs.
Synthesis and evaluation of an imidazole derivative-fluorescein conjugate.
Design, synthesis and SAR of novel glucokinase activators.
A potent bivalent Smac mimetic (SM-1200) achieving rapid, complete, and durable tumor regression in mice.
Design, synthesis, and molecular modelling of pyridazinone and phthalazinone derivatives as protein kinases inhibitors.
Design, synthesis and antithrombotic evaluation of novel dabigatran prodrugs containing methyl ferulate.
6-Oxo and 6-thio purine analogs as antimycobacterial agents.
Synthesis and biological evaluation of substituted imidazoquinoline derivatives as mPGES-1 inhibitors.
Development of an in situ mouse brain perfusion model and its application to mdr1a P-glycoprotein-deficient mice.
Substrate specificity of sinusoidal bile acid and organic anion uptake systems in rat and human liver.
Role of breast cancer resistance protein in the bioavailability and fetal penetration of topotecan.
The interaction of n-tetraalkylammonium compounds with a human organic cation transporter, hOCT1.
Proton-coupled oligopeptide transport by rat renal cortical brush border membrane vesicles: a functional analysis using ACE inhibitors to determine the isoform of the transporter.
Expression and localization of organic cation/carnitine transporter OCTN2 in Caco-2 cells.
Acceleration of MRP-associated efflux of rhodamine 123 by genistein and related compounds.
Modulation of digoxin transport across Caco-2 cell monolayers by citrus fruit juices: lime, lemon, grapefruit, and pummelo.
Molecular identification of the corticosterone-sensitive extraneuronal catecholamine transporter.
Kinetic analysis of hepatobiliary transport of organic anions in Eisai hyperbilirubinemic mutant rats.
5'-Amino acid esters of antiviral nucleosides, acyclovir, and AZT are absorbed by the intestinal PEPT1 peptide transporter.
Computer-aided design, synthesis and biological assay of p-methylsulfonamido phenylethylamine analogues.
Synthesis and study of a new adenine-acridine tandem, inhibitor of exonuclease III.
Computational studies on HIV-1 protease inhibitors: influence of calculated inhibitor-enzyme binding affinities on the statistical quality of 3D-QSAR CoMFA models.
Identification of novel inhibitors of urokinase via NMR-based screening.
S-Adenosylhomocysteine hydrolase of the protozoan parasite Trichomonas vaginalis: potent inhibitory activity of 9-(2-deoxy-2-fluoro-,D-arabinofuranosyl)adenine.
A domino Knoevenagel hetero-Diels-Alder reaction for the synthesis of polycyclic chromene derivatives and evaluation of their cytotoxicity.
Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.
3-Arylcoumarin derivatives manifest anti-proliferative activity through Hsp90 inhibition.
Discovery of BMS-846372, a Potent and Orally Active Human CGRP Receptor Antagonist for the Treatment of Migraine.
Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization.
Thermodynamic Investigation of Inhibitor Binding to 1-Deoxy-D-Xylulose-5-Phosphate Reductoisomerase.
Lasionectrin, a naphthopyrone from a Lasionectria sp.
Synthesis of benzo-annulated tryptanthrins and their biological properties.
Design, synthesis and antibacterial activities of a series of new 2-oxaisocephems.
The -Amyloid Hypothesis in Alzheimer's Disease: Seeing Is Believing.
Tandem synthesis and in vitro antiplasmodial evaluation of new naphtho[2,1-d]thiazole derivatives.
Identification of a novel serum and glucocorticoid regulated kinase-1 (SGK1) ligand from virtual screening.
Sequences in the HSP90 promoter form G-quadruplex structures with selectivity for disubstituted phenyl bis-oxazole derivatives.
USP Dictionary of USAN and International Names (2010 edition) and USAN registrations 2007-date
Novel inhibitors of nitric oxide synthase with antioxidant properties.
A facile 'click' approach to novel 15-triazolyl-5-androstane derivatives, and an evaluation of their antiproliferative activities in vitro.
Ethionamide boosters. 2. Combining bioisosteric replacement and structure-based drug design to solve pharmacokinetic issues in a series of potent 1,2,4-oxadiazole EthR inhibitors.
Natural Product Based 6-Hydroxy-2,3,4,6-tetrahydropyrrolo[1,2-a]pyrimidinium Scaffold as A New Antifungal Template.
Structure-activity relationship studies of SYA 013, a homopiperazine analog of haloperidol.
Discovery of 4''-ether linked azithromycin-quinolone hybrid series: influence of the central linker on the antibacterial activity.
High-affinity fluorescent ligands for the 5-HT(3) receptor.
Combination Therapy: JAK PI3K/mTOR. A Novel Approach for Cancer Treatment.
The 2'-Trifluoromethyl Analogue of Indomethacin Is a Potent and Selective COX-2 Inhibitor.
Multivalent presentation of a hydrolytically stable GM(3) lactone mimetic as modulator of melanoma cells motility and adhesion.
New Promising Compounds with in Vitro Nanomolar Activity against Trypanosoma cruzi.
Novel thiazolobenzodiazepines as inhibitors of histamine h3 receptor.
2-(1H-Pyrazol-4-yl)acetic acids as CRTh2 antagonists.
Discovery of a potent, dual serotonin and norepinephrine reuptake inhibitor.
7-Phenyl-imidazoquinolin-4(5H)-one derivatives as selective and orally available mPGES-1 inhibitors.
Selective Inhibitors of Fibroblast Activation Protein (FAP) with a (4-Quinolinoyl)-glycyl-2-cyanopyrrolidine Scaffold.
Discovery of MK-3168: A PET Tracer for Imaging Brain Fatty Acid Amide Hydrolase.
Therapeutic and pharmacokinetic characterizations of an anti-amyloidogenic bis-styrylbenzene derivative for Alzheimer's disease treatment.
Negative allosteric modulators of metabotropic glutamate receptor subtype.
Antiviral alkaloids produced by the mangrove-derived fungus Cladosporium sp. PJX-41.
Evaluation of 2'--fluorine modified nucleoside phosphonates as potential inhibitors of HCV polymerase.
Crystallographic Investigation and Selective Inhibition of Mutant Isocitrate Dehydrogenase.
Bioactive dimeric carbazole alkaloids from Murraya koenigii.
Bioactive dibenzocyclooctadiene lignans from the stems of Schisandra neglecta.
Recent advances in malaria drug discovery.
Dihydrooxazines As Inhibitors of BACE-1 or BACE-2.
SAR Based Optimization of a 4-Quinoline Carboxylic Acid Analog with Potent Anti-Viral Activity.
Imidazopyrazine Derivatives As Inhibitors of mTOR.
3-Hydroxyquinolin-2(1H)-ones As Inhibitors of Influenza A Endonuclease.
Selective inhibition of bacterial and human topoisomerases by N-arylacyl O-sulfonated aminoglycoside derivatives.
Discovery of 2-((1H-benzo[d]imidazol-1-yl)methyl)-4H-pyrido[1,2-a]pyrimidin-4-ones as novel PKM2 activators.
Synthesis and biological evaluation of novel tamoxifen analogues.
Synthesis and in vitro evaluation of glycosyl derivatives of luteinizing hormone-releasing hormone (LHRH).
Anticancer effects of a novel class rosin-derivatives with different mechanisms.
Bioactive terpenoids from the fruits of Aphanamixis grandifolia.
Carbonic anhydrase inhibitors. Benzenesulfonamides incorporating cyanoacrylamide moieties strongly inhibit Saccharomyces cerevisiae -carbonic anhydrase.
Synthesis and antitumor activities of naturally occurring oleanolic acid triterpenoid saponins and their derivatives.
An analysis of the synthetic tryptamines AMT and 5-MeO-DALT: emerging 'Novel Psychoactive Drugs'.
New azole antagonists with high affinity for the P2Y(1) receptor.
Green synthesis of tetrahydropyrimidine analogues and evaluation of their antimicrobial activity.
Solid phase synthesis and biological evaluation of probestin as an angiogenesis inhibitor.
Enmein-type diterpenoid analogs from natural kaurene-type oridonin: Synthesis and their antitumor biological evaluation.
Rational design, synthesis and QSAR study of vasorelaxant active 3-pyridinecarbonitriles incorporating 1H-benzimidazol-2-yl function.
Identification of M. tuberculosis thioredoxin reductase inhibitors based on high-throughput docking using constraints.
Design, synthesis and structure activity relationships of spirocyclic compounds as potent CCR1 antagonists.
New nitric oxide donating 1,2,4-triazole/oxime hybrids: synthesis, investigation of anti-inflammatory, ulceroginic liability and antiproliferative activities.
Synthesis and characterization of 123I-CMICE-013: a potential SPECT myocardial perfusion imaging agent.
Discovery of TAK-960: an orally available small molecule inhibitor of polo-like kinase 1 (PLK1).
Stapled peptide-based membrane fusion inhibitors of hepatitis C virus.
N-Benzyloxycarbonyl-S-(2,4-dinitrophenyl)glutathione dibutyl diester is inhibitory to melarsoprol resistant cell lines overexpressing the T. bruceiMRPA transporter.
Nicotinamide N-oxides as CXCR2 antagonists.
Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383.
Synthesis and biological evaluation of a sialyl Lewis X mimic with significantly improved E-selectin inhibition.
Synthesis and HIV-1 integrase inhibitory activities of catechol and bis-catechol derivatives.
Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists.
Structure-activity relationships for a series of thiobenzamide influenza fusion inhibitors derived from 1,3,3-trimethyl-5-hydroxy-cyclohexylmethylamine.
Synthesis of more potent analogues of the acetylcholinesterase inhibitor, huperzine B.
Meiosis activating sterols derived from diosgenin.
Multisubstrate analogue inhibitors of glucosamine-6-phosphate synthase from Candida albicans.
4D-QSAR analysis of a set of propofol analogues: mapping binding sites for an anesthetic phenol on the GABA(A) receptor.
Dicarboxylic acid bis(L-prolyl-pyrrolidine) amides as prolyl oligopeptidase inhibitors.
In vivo active antimalarial isonitriles.
Molecular characterization of human and rat organic anion transporter OATP-D.
Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin.
Circumvention of tumor multidrug resistance by a new annonaceous acetogenin: atemoyacin-B.
Sequence analysis and functional characterization of the 5'-flanking region of the rat multidrug resistance protein 2 (mrp2) gene.
Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?
Pharmacokinetic and prognostic significance of intestinal MDR1 expression in recipients of living-donor liver transplantation.
Expression of recombinant human multidrug resistance P-glycoprotein in insect cells confers decreased accumulation of technetium-99m-sestamibi.
Pyrazolopyridine Inhibitors of B-Raf(V600E). Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors.
7,8-dichloro-1-oxo--carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.
A scaffold hopping approach to identify novel monoamine oxidase B inhibitors.
Near infrared active heptacyanine dyes with unique cancer-imaging and cytotoxic properties.
Indomethacin Analogues that Enhance Doxorubicin Cytotoxicity in Multidrug Resistant Cells without Cox Inhibitory Activity.
Synthesis, anti-HBV activity and renal cell toxicity evaluation of mixed phosphonate prodrugs of adefovir.
Synthesis and evaluation of debromohymenialdisine-derived Chk2 inhibitors.
Influence of various central moieties on the hypolipidemic properties of long hydrocarbon chain diols and diacids.
DNA binding affinity of bisguanidine and bis(2-aminoimidazoline) derivatives with in vivo antitrypanosomal activity.
Synthesis of 3-(1H-benzimidazol-2-yl)-5-isoquinolin-4-ylpyrazolo[1,2-b]pyridine, a potent cyclin dependent kinase 1 (CDK1) inhibitor.
07H239-A, a new cytotoxic eremophilane sesquiterpene from the marine-derived Xylariaceous fungus LL-07H239.
The design, synthesis, and biological evaluation of potent receptor tyrosine kinase inhibitors.
Radiosynthesis and in vivo tumor uptake of 2-deoxy-2-[(18)F]fluoro-myo-inositol.
Exploration of the SAR of anti-invasive chalcones: synthesis and biological evaluation of conformationally restricted analogues.
Synthesis and biological evaluation of cyanoguanidine derivatives of loratadine.
Laxiflorolides A and B, epimeric bishomoditerpene lactones from Isodon eriocalyx.
Identification of new snake venom metalloproteinase inhibitors using compound screening and rational Peptide design.
Rational Design, Synthesis, and SAR of a Novel Thiazolopyrimidinone Series of Selective PI3K-beta Inhibitors.
Bicyclic Cyclohexenones as Inhibitors of NF-B Signaling.
Novel racemic tetrahydrocurcuminoid dihydropyrimidinone analogues as potent acetylcholinesterase inhibitors.
New trifluoromethyl quinolone derivatives: synthesis and investigation of antimicrobial properties.
Structure-based design of HSPA5 inhibitors: from peptide to small molecule inhibitors.
Discovery, synthesis, selectivity modulation and DMPK characterization of 5-azaspiro[2.4]heptanes as potent orexin receptor antagonists.
Identification of novel SIRT3 inhibitor scaffolds by virtual screening.
Synthesis and evaluation of Janus type nucleosides as potential HCV NS5B polymerase inhibitors.
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.
Conformationally restricted homotryptamines. Part 6: indole-5-cycloalkyl methylamines as selective serotonin reuptake inhibitors.
Ligand based approach to L-type calcium channel by imidazo[2,1-b]thiazole-1,4-dihydropyridines: from heart activity to brain affinity.
Design, synthesis, and biological evaluation of novel histone deacetylase 1 inhibitors through click chemistry.
Chemotherapy of leishmaniasis. Part XII: design, synthesis and bioevaluation of novel triazole integrated phenyl heteroterpenoids as antileishmanial agents.
Synthesis, cytotoxicity and topoisomerase II inhibitory activity of lomefloxacin derivatives.
Synthesis and preliminary biological evaluation of a compound library of triazolylcyclitols.
Synthesis and SAR of potent and selective tetrahydropyrazinoisoquinolinone 5-HT(2C) receptor agonists.
Design, synthesis and evaluation of inhibitor of apoptosis protein (IAP) antagonists that are highly selective for the BIR2 domain of XIAP.
Synthesis and antitumor activity of novel 3,4-diaryl squaric acid analogs.
Synthesis of some novel chalcones, flavanones and flavones and evaluation of their anti-inflammatory activity.
tert-Butyl 1,5-bis(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)-1,5-dioxopentan-2-ylcarbamate urea/thiourea derivatives as potent H+/K(+)-ATPase inhibitors.
Discovery of novel indolinone-based, potent, selective and brain penetrant inhibitors of LRRK2.
The identification of novel p38 isoform selective kinase inhibitors having an unprecedented p38 binding mode.
3-Aryl-3-arylmethoxyazetidines. A new class of high affinity ligands for monoamine transporters.
Discovery of novel P2 substituted 4-biaryl proline inhibitors of hepatitis C virus NS3 serine protease.
Synthesis and antiprotozoal activity of novel 2-{[2-(1H-imidazol-1-yl)ethyl]sulfanyl}-1H-benzimidazole derivatives.
Discovery and structure-activity relationships of ent-Kaurene diterpenoids as potent and selective 11-HSD1 inhibitors: potential impact in diabetes.
2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.
Development of polyamine transport ligands with improved metabolic stability and selectivity against specific human cancers.
Inhibition of rhodesain as a novel therapeutic modality for human African trypanosomiasis.
Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development.
Reversible inhibition of human acetylcholinesterase by methoxypyridinium species.
Expression of the bile salt export pump is maintained after chronic cholestasis in the rat.
Impact of Mrp2 on the biliary excretion and intestinal absorption of furosemide, probenecid, and methotrexate using Eisai hyperbilirubinemic rats.
Difloxacin reverses multidrug resistance in HL-60/AR cells that overexpress the multidrug resistance-related protein (MRP) gene.
Altered pharmacokinetics of vinblastine in Mdr1a P-glycoprotein-deficient Mice.
P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in rats.
Chelerythrine stimulates GSH transport by rat Mrp2 (Abcc2) expressed in canine kidney cells.
Cloning of the mouse and human solute carrier 22a3 (Slc22a3/SLC22A3) identifies a conserved cluster of three organic cation transporters on mouse chromosome 17 and human 6q26-q27.
Quantitative analysis of breast cancer resistance protein and cellular resistance to flavopiridol in acute leukemia patients.
Effect of organic isothiocyanates on the P-glycoprotein- and MRP1-mediated transport of daunomycin and vinblastine.
P-glycoprotein mediates profound resistance to bisantrene.
Successful bridging from a peptide to a non peptide antagonist at the human tachykinin NK-2 receptor.
Designing analogues of mini atrial natriuretic peptide based on structural analysis by NMR and restrained molecular dynamics.
Structure-activity study of novel tricyclic benzazepine arginine vasopressin antagonists.
Effect of catechol derivatives on cell growth and lipoxygenase activity.
beta-alanine dipeptides as MC4R agonists.
A novel N-terminal cyclic dynorphin A analogue cyclo(N,5)[Trp(3),Trp(4),Glu(5)] dynorphin A-(1-11)NH(2) that lacks the basic N-terminus.
Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.
Nocathiacin analogs: Synthesis and antibacterial activity of novel water-soluble amides.
Repenins A-D, four new antioxidative coumarinolignoids from Duranta repens Linn.
Synthesis and biological evaluation of ester prodrugs of Benzafibrate as orally active hypolipidemic agents.
2-Substituted 4,5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo--lactamases.
Novel 4-aminoquinoline-pyrimidine based hybrids with improved in vitro and in vivo antimalarial activity.
Targeting the liver stage of malaria parasites: a yet unmet goal.
An efficient one-pot synthesis and photoinduced DNA cleavage studies of 2-chloro-3-(5-aryl-4,5-dihydroisoxazol-3-yl)quinolines.
Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation.
An investigation into the structure-activity relationships associated with the systematic modification of the (2)-adrenoceptor agonist indacaterol.
UDP made a highly promising stable, potent, and selective P2Y6-receptor agonist upon introduction of a boranophosphate moiety.
Synthesis and anticonvulsant activity of new N-Mannich bases derived from 3-(2-fluorophenyl)- and 3-(2-bromophenyl)-pyrrolidine-2,5-diones. Part II.
Synthesis and structure-activity relationships of pyrazolo[1,5-a]pyridine derivatives: potent and orally active antagonists of corticotropin-releasing factor 1 receptor.
Synthesis and Agonistic Activity at the GPR35 of 5,6-Dihydroxyindole-2-carboxylic Acid Analogues.
"True" antiandrogens-selective non-ligand-binding pocket disruptors of androgen receptor-coactivator interactions: novel tools for prostate cancer.
Design and synthesis of potent, selective inhibitors of matriptase.
Small molecule suppression of carbapenem resistance in NDM-1 producing Klebsiella pneumoniae.
Metabotropic glutamate receptor 5 negative allosteric modulators as novel tools for in vivo investigation.
Optimized 5-membered heterocycle-linked pterins for the inhibition of Ricin Toxin A.
Thiazoline peptides and a tris-phenethyl urea from Didemnum molle with anti-HIV activity.
Design and synthesis of gambogic acid analogs as potent cytotoxic and anti-inflammatory agents.
The rat canalicular conjugate export pump (Mrp2) is down-regulated in intrahepatic and obstructive cholestasis.
HMG-CoA reductase inhibitors (statins) characterized as direct inhibitors of P-glycoprotein.
Methadone inhibits rhodamine123 transport in Caco-2 cells.
Structure-activity relationship data for chemical series of agonists of the motilin receptor (Supplementary Bioactivity Data for publication CHEMBL1141008)
6'-Methyl-5'-homoaristeromycin: a structural variation of the anti-orthopox virus candidate 5'-homoaristeromycin.
Benzimidazole-2-one: a novel anchoring principle for antagonizing p53-Mdm2.
Synthesis and evaluation of novel orally active p53-MDM2 interaction inhibitors.
Heterocyclic modification of a novel bicyclo[3.1.0]hexane NPY1 receptor antagonist.
Synthesis of kojic acid derivatives as secondary binding site probes of D-amino acid oxidase.
Inhibition of soluble epoxide hydrolase by fulvestrant and sulfoxides.
Synthesis and neuroprotective effect of E-3,4-dihydroxy styryl aralkyl ketones derivatives against oxidative stress and inflammation.
An effective prodrug strategy to selectively enhance ocular exposure of a cannabinoid receptor (CB1/2) agonist.
Optimization of ligand and lipophilic efficiency to identify an in vivo active furano-pyrimidine Aurora kinase inhibitor.
The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.
Synthesis and anticancer activity of 2,4-disubstituted furo[3,2-b]indole derivatives.
Structure optimization of 2-benzamidobenzoic acids as PqsD inhibitors for Pseudomonas aeruginosa infections and elucidation of binding mode by SPR, STD NMR, and molecular docking.
Effect of ring-constrained phenylpropyloxyethylamines on sigma receptors.
BACE Inhibitors: Potential Treatment of Alzheimer's Disease, Dementia, and Related Neurodegenerative Disorders (A): 5,6-Dihydroimidazo[1,2-a]pyrazin-8-yl-amine Derivatives: Patent Highlight.
Prostaglandin e2 synthase-1 inhibitors as potential treatment for osteoarthritis: patent highlight.
Macrocyclic Hedgehog Pathway Inhibitors: Optimization of Cellular Activity and Mode of Action Studies.
Cyclopropyl-spiro-piperidines Useful as Sodium Channel Blockers: Patent Highlight.
Remarkable potential of the -aminophosphonate/phosphinate structural motif in medicinal chemistry.
Irreversible 4-Aminopiperidine Transglutaminase 2 Inhibitors for Huntington's Disease.
Bromodomains: are readers right for epigenetic therapy?
Design, synthesis and biological evaluation of new peptide-based ureas and thioureas as potential antagonists of the thrombin receptor PAR1.
Novel and selective inhibitors of histone deacetylase: patent highlight.
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS A Reduction.
Novel indolethylbenzamides for the treatment of tauopathies: patent highlight.
Discovery of a new molecular probe ML228: an activator of the hypoxia inducible factor (HIF) pathway.
Compounds and Their Use as BACE Inhibitors: Patent Highlight.
Neuroprotective Tri- and Tetracyclic BChE Inhibitors Releasing Reversible Inhibitors upon Carbamate Transfer.
Zizimauritic acids A-C, three novel nortriterpenes from Ziziphus mauritiana.
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor.
Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist.
Discovery of Disubstituted Imidazo[4,5-b]pyridines and Purines as Potent TrkA Inhibitors.
BACE-Inhibitors: Potential Treatment of Alzheimer Disease, Dementia, and Related Neurodegenerative Diseases. C. Spiro-Heterocyclic Derivatives: Patent Highlight.
Discovery of 2-Alkyl-1-arylsulfonylprolinamides as 11-Hydroxysteroid Dehydrogenase Type 1 Inhibitors.
Imidazo[1,2-a]pyridines: orally active positive allosteric modulators of the metabotropic glutamate 2 receptor.
Initial Optimization of a New Series of -Secretase Modulators Derived from a Triterpene Glycoside.
Novel Benzoisoxazole as Partial Agonist of the 5-HT4 Receptor: Patent Highlight.
Benzenesulfonyl and Benzenesulfonamide as Modulators of the 5-HT6 Receptor: Patent Highlight.
The Synthesis and Antimicrobial Activity of Heterocyclic Derivatives of Totarol.
5-Amino-oxazepine and 5-Amino-thiazepine Compounds as -Secretase Antagonists and Methods of Use: Patent Highlight.
Symmetric kv1.5 blockers discovered by focused screening.
Lipidated peptidomimetics with improved antimicrobial activity.
Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.
Elaiomycins D-F, antimicrobial and cytotoxic azoxides from Streptomyces sp. strain HKI0708.
Pyrrolo[2,3-b]quinoxalines as inhibitors of firefly luciferase: their Cu-mediated synthesis and evaluation as false positives in a reporter gene assay.
Quinolinyl Pyrimidines: Potent Inhibitors of NDH-2 as a Novel Class of Anti-TB Agents.
Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.
Substrate-Selective Inhibition of Cyclooxygenase-2: Development and Evaluation of Achiral Profen Probes.
Tuned-Affinity Bivalent Ligands for the Characterization of Opioid Receptor Heteromers.
Short-acting T-type calcium channel antagonists significantly modify sleep architecture in rodents.
Anthraquinones from a marine-derived Streptomyces spinoverrucosus.
Novel compounds for the treatment of neurodegenerative diseases: patent highlight.
From in Silico Discovery to intra-Cellular Activity: Targeting JNK-Protein Interactions with Small Molecules.
Novel Quinolinones as Activators of AMP Activated Protein Kinase: Patent Highlight.
Synthesis, anticancer activities and molecular modeling studies of novel indole retinoid derivatives.
Hepatitis C virus protease inhibitors: patent highlight.
Discovery of a novel chemotype of tyrosine kinase inhibitors by fragment-based docking and molecular dynamics.
Synthesis and SAR of 1-hydroxy-1H-benzo[d]imidazol-2(3H)-ones as Inhibitors of D-Amino Acid Oxidase.
Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus.
Synthesis and antioxidant activity of 1,3,4-oxadiazole tagged thieno[2,3-d]pyrimidine derivatives.
Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Cytotoxic oxoisoaporphine alkaloids from Menispermum dauricum.
The identification and optimization of 2,4-diketobutyric acids as flap endonuclease 1 inhibitors.
Probing binding requirements of type I and type II isoforms of inosine monophosphate dehydrogenase with adenine-modified nicotinamide adenine dinucleotide analogues.
Novel nucleotide triphosphates as potent P2Y2 agonists with enhanced stability over UTP.
A novel small-molecule inhibitor of the avian influenza H5N1 virus determined through computational screening against the neuraminidase.
Interactions of curcumin with the PfATP6 model and the implications for its antimalarial mechanism.
Discovery of a Potent HIV Integrase Inhibitor that Leads to a Prodrug with Significant anti-HIV Activity.
Potent CXCR4 antagonists containing amidine type Peptide bond isosteres.
The effects of aminoguanidine on retinopathy in STZ-induced diabetic rats.
Synthesis and biological evaluation of novel (E) stilbene-based antitumor agents.
Benzothiazoles: search for anticancer agents.
Synthesis and antitumor activity of formononetin nitrogen mustard derivatives.
Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.
Discovery and optimization of 2,4-diaminoquinazoline derivatives as a new class of potent dengue virus inhibitors.
Synthesis and antitumor activity of novel quinazoline derivatives containing thiosemicarbazide moiety.
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.
Discovery of a potent inhibitor of anaplastic lymphoma kinase with in vivo antitumor activity.
Evaluation of synthetic acridones and 4-quinolinones as potent inhibitors of cathepsins L and V.
Potent antiviral HIV-1 protease inhibitor GRL-02031 adapts to the structures of drug resistant mutants with its P1'-pyrrolidinone ring.
Regioselective synthesis and antimicrobial studies of ester linked 1,4-disubstituted 1,2,3-bistriazoles.
Expanded Utility of the -Glucuronide Linker: ADCs That Deliver Phenolic Cytotoxic Agents.
Optimization of the Central Core of Indolinone-Acetic Acid-Based CRTH2 (DP2) Receptor Antagonists.
Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs.
Identification of lactate as a driving force for prostanoid transport by prostaglandin transporter PGT.
pH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: implications for drug-drug interactions.
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
Isolation of a family of organic anion transporters from human liver and kidney.
Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein.
Cyclosporin A treatment induces overexpression of P-glycoprotein in the kidney and other tissues.
Biliary excretion of glycyrrhizin in rats: kinetic basis for multiplicity in bile canalicular transport of organic anions.
Ligand Promiscuity between the Efflux Pumps Human P-Glycoprotein and S. aureus NorA.
Pyrazolo[4,3-c][1,2]benzothiazines 5,5-dioxide: a promising new class of Staphylococcus aureus NorA efflux pump inhibitors.
Trigoflavidols A-C, degraded diterpenoids with antimicrobial activity, from Trigonostemon flavidus.
Iotrochamides A and B, antitrypanosomal compounds from the Australian marine sponge Iotrochota sp.
N-Pyridyl and Pyrimidine Benzamides as KCNQ2/Q3 Potassium Channel Openers for the Treatment of Epilepsy.
Potent inhibition of norovirus 3CL protease by peptidyl -ketoamides and -ketoheterocycles.
The macrocycle of leinamycin imparts hydrolytic stability to the thiol-sensing 1,2-dithiolan-3-one 1-oxide unit of the natural product.
Lipo--AApeptides as a new class of potent and broad-spectrum antimicrobial agents.
Discovery of a Novel Class of Bicyclo[3.1.0]hexanylpiperazines as Noncompetitive Neuropeptide Y Y1 Antagonists.
Synthesis and antidepressant activity of arylalkanol-piperidine derivatives as triple reuptake inhibitors.
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye.
Semi-synthesis and bio-evaluation of polybrominated diphenyl ethers from the sponge Dysidea herbacea.
Synthesis and in vitro cytostatic activity of 1,2- and 1,3-diacylglycerophosphates of clofarabine.
Design and synthesis of 2-phenyl-1,4-dioxa-spiro[4.5]deca-6,9-dien-8-ones as potential anticancer agents starting from cytotoxic spiromamakone A.
Synthesis, biological activity and molecular modeling studies on 1H-benzimidazole derivatives as acetylcholinesterase inhibitors.
Design and synthesis of novel series of 5-HT6 receptor ligands having indole, a central aromatic core and 1-amino-4 methyl piperazine as a positive ionizable group.
Synthesis and bioevaluation of novel 4-aminoquinoline-tetrazole derivatives as potent antimalarial agents.
In search of potent and selective inhibitors of neuronal nitric oxide synthase with more simple structures.
Design and synthesis of novel 1,25-dihydroxyvitamin D3 analogues having a spiro-oxetane fused at the C2 position in the A-ring.
Neuroactive diol and acyloin metabolites from cone snail-associated bacteria.
Histone Deacetylase 4 (HDAC4) Inhibitors: A Promising Treatment for Huntington's Disease.
Design, synthesis, and in vitro hMAO-B inhibitory evaluation of some 1-methyl-3,5-diphenyl-4,5-dihydro-1H-pyrazoles.
Herbimycins D-F, ansamycin analogues from Streptomyces sp. RM-7-15.
Assay platform for clinically relevant metallo--lactamases.
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
Highly potent and selective nonsteroidal dual inhibitors of CYP17/CYP11B2 for the treatment of prostate cancer to reduce risks of cardiovascular diseases.
Synthesis and broad spectrum antiviral evaluation of bis(POM) prodrugs of novel acyclic nucleosides.
Synthesis, antileishmanial activity and structure-activity relationship of 1-N-X-phenyl-3-N'-Y-phenyl-benzamidines.
Synthesis and biological evaluation of flavones and benzoflavones as inhibitors of BCRP/ABCG2.
Substrate-like water soluble lipase inhibitors from Filipendula kamtschatica.
Identification of an Adamantyl Azaquinolone JNK Selective Inhibitor.
Inhibitors of LRRK2 as Treatment for Parkinson's Disease: Patent Highlight.
An ultrahigh affinity d-peptide antagonist Of MDM2.
Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists.
Total Syntheses and Cytotoxicity of (R)- and (S)-Boehmeriasin A.
Enhanced ROS production and cell death through combined photo- and sono-activation of conventional photosensitising drugs.
Substituted pyridines as sodium channel blockers: patent highlight.
JBIR-129 and -139, cytotoxic 34-membered polyol macrolides of microbial origin.
Combatting Drug-Resistant Bacteria with Gyrase and Topoisomerase IV Inhibitors: Patent Highlight.
Synthesis and Biological Evaluation of a Biotinylated Paclitaxel With an Extra-Long Chain Spacer Arm.
BACE Inhibitors: Potential Treatment of Alzheimer's Disease, Dementia, and Related Neurodegenerative Disorders (B): 3-Amino-4-fluoro-1H-isoindol Derivatives: Patent Highlight.
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of -Secretase.
Discovery and development of 7 nicotinic acetylcholine receptor modulators.
Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP.
Design, Synthesis, and Anti-leukemic Activity of Stereochemically Defined Constrained Analogs of FTY720 (Gilenya).
Discovery of 2 Adrenergic Receptor Ligands Using Biosensor Fragment Screening of Tagged Wild-Type Receptor.
Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.
Identification of 1-[4-Benzyloxyphenyl)-but-3-enyl]-1H-azoles as New Class of Antitubercular and Antimicrobial Agents.
Insights into soluble guanylyl cyclase activation derived from improved heme-mimetics.
Synthesis of amino-hydroxy-benzocycloheptenones as potent, selective, non-peptidic dinuclear zinc metalloaminopeptidase inhibitors.
Arylthioamides as H2S Donors: l-Cysteine-Activated Releasing Properties and Vascular Effects in Vitro and in Vivo.
5-Deazaflavin derivatives as inhibitors of p53 ubiquitination by HDM2.
Anti-proliferative activity of hydnocarpin, a natural lignan, is associated with the suppression of Wnt/-catenin signaling pathway in colon cancer cells.
Anabaseine analogues as modulators of nicotinic acetylcholine receptor.
Novel carvedilol analogues that suppress store-overload-induced Ca2+ release.
A structurally simplified analogue of geldanamycin exhibits neuroprotective activity.
Potent Vinblastine C20' Ureas Displaying Additionally Improved Activity Against a Vinblastine-Resistant Cancer Cell Line.
Largazole Arrests Cell Cycle at G1 Phase and Triggers Proteasomal Degradation of E2F1 in Lung Cancer Cells.
Synthesis and structure-activity relationship studies of novel dihydropyridones as androgen receptor modulators.
Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.
Fragment-based identification of a locus in the Sec7 domain of Arno for the design of protein-protein interaction inhibitors.
Synthesis and biological evaluation of direct thrombin inhibitors bearing 4-(piperidin-1-yl)pyridine at the P1 position with potent anticoagulant activity.
An epoxyisoprostane is a major regulator of endothelial cell function.
Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
Synthesis and in vitro evaluation of a novel radioligand for v3 integrin receptor imaging: [18F]FPPA-c(RGDfK).
Synthesis and biological evaluation of novel acylhydrazone derivatives as potential antitumor agents.
Discovery of pyrazolo[1,5-a]pyrimidine-based Pim inhibitors: a template-based approach.
Thiazolidinone-peptide hybrids as dengue virus protease inhibitors with antiviral activity in cell culture.
A SAR study on a series of synthetic lipophilic chalcones as inhibitor of transcription factor NF-B.
Design, synthesis, and in vitro activity of novel 2'-O-substituted 15-membered azalides.
Fragment-based discovery of hydroxy-indazole-carboxamides as novel small molecule inhibitors of Hsp90.
A novel class of small-molecule caspase-3 inhibitors prepared by multicomponent reactions.
The impact of ionization States of matrix metalloproteinase inhibitors on docking-based inhibitor design.
Quinolizidinone carboxylic acids as CNS penetrant, selective m1 allosteric muscarinic receptor modulators.
Design and synthesis of new (E)-cinnamic N-acylhydrazones as potent antitrypanosomal agents.
Metabolism-based synthesis, biologic evaluation and SARs analysis of O-methylated analogs of quercetin as thrombin inhibitors.
Disubstituted Bis-THF Moieties as New P2 Ligands in Nonpeptidal HIV-1 Protease Inhibitors.
New quinoline-5,8-dione and hydroxynaphthoquinone derivatives inhibit a chloroquine resistant Plasmodium falciparum strain.
Synthesis and Biochemical Testing of 3-(Carboxyphenylethyl)imidazo[2,1-f][1,2,4]triazines as Inhibitors of AMP Deaminase.
Coordinate induction by antioxidants of UDP-glucuronosyltransferase UGT1A6 and the apical conjugate export pump MRP2 (multidrug resistance protein 2) in Caco-2 cells.
Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin.
Cisplatin induces renal expression of P-glycoprotein and canalicular multispecific organic anion transporter.
Transport of drugs across the hepatic sinusoidal membrane: sinusoidal drug influx and efflux in the liver.
Effects of ursodeoxycholic and cholic acid feeding on hepatocellular transporter expression in mouse liver.
NOpiates: Novel Dual Action Neuronal Nitric Oxide Synthase Inhibitors with -Opioid Agonist Activity.
A-ring dihalogenation increases the cellular activity of combretastatin-templated tetrazoles.
Molecular Docking and in Vitro Antileishmanial Evaluation of Chromene-2-thione Analogues.
Discovery of 1,3-Diaminobenzenes as Selective Inhibitors of Platelet Activation at the PAR1 Receptor.
Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein.
Inhibitors for Bacterial Cell-Wall Recycling.
Natural products as a gold mine for selective matrix metalloproteinases inhibitors.
Synthesis of pacidamycin analogues via an Ugi-multicomponent reaction.
Synthesis and evaluation of a set of para-substituted 4-phenylpiperidines and 4-phenylpiperazines as monoamine oxidase (MAO) inhibitors.
Hydrophobic Interactions Improve Selectivity to ER for Ben-zothiophene SERMs.
Design, synthesis and biological evaluation of novel imidazopyridines as potential antidiabetic GSK3 inhibitors.
Discovery of a potent thiadiazole class of histamine h3 receptor antagonist for the treatment of diabetes.
Antiprotozoal sesquiterpene pyridine alkaloids from Maytenus ilicifolia.
Discovery of novel benzylidene-1,3-thiazolidine-2,4-diones as potent and selective inhibitors of the PIM-1, PIM-2, and PIM-3 protein kinases.
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
Contribution of indazolinone tautomers to kinase activity.
The First Dual ChE/FAAH Inhibitors: New Perspectives for Alzheimer's Disease?
BACE1 Inhibitor Peptides: Can an Infinitely Small k cat Value Turn the Substrate of an Enzyme into Its Inhibitor?
A comparative study on anti-inflammatory activities of the enantiomers, shikonin and alkannin.
Design, synthesis, and evaluation of novel thienopyrrolizinones as antitubulin agents.
Effects of indole fatty alcohols on the differentiation of neural stem cell derived neurospheres.
Pomiferin, histone deacetylase inhibitor isolated from the fruits of Maclura pomifera.
Three New Eudesmane Sesquiterpenes from Pluchea arguta
In vitro PAI-1 inhibitory activity of oxalamide derivatives.
Natural products, small molecules, and genetics in tuberculosis drug development.
4-(2-pyridyl)-2,2-dimethylnaphthalen-1-ones as new potassium channel activators with increased airways selectivity
Conformationally restricted piperidinyl benzamides as 5-HT3 receptor antagonists.
Novel synthesis of nucleoside 5-polyphosphates
Modulation of human neutrophils' oxidative burst by flavonoids.
Modulation of v3- and 51-integrin-mediated adhesion by dehydro--amino acids containing peptidomimetics.
Atropisomeric 4-phenyl-4H-1,2,4-triazoles as selective glycine transporter 1 inhibitors.
Synthesis, antimicrobial and cytotoxic activities of some novel thiazole clubbed 1,3,4-oxadiazoles.
Psammaplysin F: a unique inhibitor of bacterial chromosomal partitioning.
Hit identification and optimization in virtual screening: practical recommendations based on a critical literature analysis.
One-pot synthesis and cytotoxicity studies of new Mannich base derivatives of polyether antibiotic--lasalocid acid.
Synthesis of novel analogs of 2-pyrazoline obtained from [(7-chloroquinolin-4-yl)amino]chalcones and hydrazine as potential antitumor and antimalarial agents.
Synthesis, antiproliferative and anti-inflammatory activities of some novel 6-aryl-2-(p-(methanesulfonyl)phenyl)-4,5-dihydropyridazi-3(2H)-ones.
Synthesis and antibacterial activity of doxycycline neoglycosides.
Bioactive polyprenylated acylphloroglucinol derivatives from Hypericum cohaerens.
Synthesis and biological evaluation of pyrazolo[4,3-d]pyrimidine analogues.
Synthesis and antiprotozoal activity of original porphyrin precursors and derivatives.
Synthesis of imine-pyrazolopyrimidinones and their mechanistic interventions on anticancer activity.
Structure-activity relationships for ketamine esters as short-acting anaesthetics.
N-aryl-6-methoxy-1,2,3,4-tetrahydroquinolines: a novel class of antitumor agents targeting the colchicine site on tubulin.
Stabilized cyclopropane analogs of the splicing inhibitor FD-895.
Synthesis and anticancer activity evaluation of a series of [1,2,4]triazolo[1,5-a]pyridinylpyridines in vitro and in vivo.
New pyridazine-fluorine derivatives: synthesis, chemistry and biological activity. Part II.
Optimization of diarylazines as anti-HIV agents with dramatically enhanced solubility.
Prediction of glucagon receptor antagonist activities of some substituted imidazoles using combined radial basis function neural network and density functional theory
Facile synthesis of novel quinoline derivatives as anticancer agents
Synthesis and Biological Evaluation of the First Example of NO-Donor Histone Deacetylase Inhibitor.
Overcoming doxorubicin-resistance in the NCI/ADR-RES model cancer cell line by novel anthracene-9,10-dione derivatives.
Synthesis, radiofluorination, and in vivo evaluation of novel fluorinated and iodinated radiotracers for PET imaging and targeted radionuclide therapy of melanoma.
Discovery and characterization of synthetic 4'-hydroxyflavones-New CK2 inhibitors from flavone family.
Triazole-dithiocarbamate based selective lysine specific demethylase 1 (LSD1) inactivators inhibit gastric cancer cell growth, invasion, and migration.
Selection and optimization of hits from a high-throughput phenotypic screen against Trypanosoma cruzi. Exported from HEOS 25-Oct-2013. See also related datasets CHEMBL3137440 and CHEMBL3137386.
UCSF DeRisi Lab MMV Box Apicoplast Screening
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
Structure-activity data for a series of P-glycoprotein inhibitors (Supplementary Data to CHEMBL1142990)
Open TG-GATES in vivo data: Biochemistry
Open TG-GATES in vivo data: Organ Weight
Synthesis, fungicidal activity, and QSAR of pyridazinonethiadiazoles.
Involvement of melanin synthesis and reactive oxygen species in phytotoxic action of l-DOPA in carrot cells
Potential new fungicides: N-acyl-5-methyl-3(2H)-isoxazolone derivatives
7-Hydroxy-coumarin derivatives: synthesis, characterization and preliminary antimicrobial activities
A simple synthesis of trans-3,4,5-trimethoxycinnamamides and evaluation of their biologic activity
Integrated control of cotton root rot disease by mixing fungal biocontrol agents and resistance inducers
Antitumor and antileishmanial evaluation of novel heterocycles derived from quinazoline scaffold: a molecular modeling approach
Pharmacological profile of green tea and its polyphenols: a review
The synthesis, anti-inflammatory, and anti-microbial activity evaluation of new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives
Radiolabeling of EGCG with 131I and biodistribution in rats
QSAR Analysis of BABQ compounds via calculated molecular descriptors
Synthesis and Fungicidal Activity of New 6-Alkyl-2-alkylamino-4H-1, 3, 2-benzodioxaphosphorin 2-Sulfides
Control of crown rot-causing fungal pathogens of banana by inorganic salts and a surfactant
Synthetic sialic-acid-containing polyvalent antiviral inhibitors
Synthesis, preliminary cytotoxicity evaluation of new 3-formylchromone hydrazones and phosphorohydrazone derivatives of coumarin and chromone
Synthesis and evaluation of antioxidant and antimicrobial properties of thymol containing pyridone moieties
Synthesis of inhibitors of imidazole glycerol phosphate dehydratase
2-Substituted-8-methyl-3,6-dihydroimidazo[4,5-c]pyrazolo[3,4-e]pyridazine as an anti-inflammatory agent
Colchicine and its various physicochemical and biological aspects
Insect antifeedant potent 6-substituted -bromo-2-naphthones
Synthesis and biological evaluation of 1-(3-chloro-2-oxo-4-phenylazetidin-1-yl)-3-(2-oxo-2-(10H-phenothiazin-10-yl)ethyl)urea derivatives
Comparison of Phytotoxicities between 4-Fluorinated and Non-fluorinated 2-Chloro-5-(3, 4, 5, 6-tetrahydrophthalimido)benzoates
Metabolism of thymol and trans-anethole in larvae of Spodoptera litura and Trichoplusia ni (Lepidoptera: Noctuidae).
Managing weeds with drip-applied herbicides in tomato
Phytotoxicity Caused by Peroxidizing Herbicides Is Alleviated by 2-Substituted 4, 6-Bis(ethylamino)-1, 3, 5-triazines
Synthesis and antidepressant-like action of N-(2-hydroxyethyl) cinnamamide derivatives in mice
Microwave-assisted synthesis and antimicrobial activity of some imidazo[2,1-b][1,3,4]thiadiazole derivatives
A rapid access to new coumarinyl chalcone and substituted chromeno[4,3-c]pyrazol-4(1H)-ones and their antibacterial and DPPH radical scavenging activities
Survival and developmental impairment induced by the trypsin inhibitor bis-benzamidine in the velvetbean caterpillar (Anticarsia gemmatalis)
Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of lacidipine analogues
Pharmacopore hypothesis generation of BACE-1 inhibitors and pharmacophore-driven identification of potent multi-target neuroprotective agents
Synthesis and anticancer activity of some new s-triazine derivatives
Synthesis and biological evaluation of novel condensed pyrimidinylmethylsulfinylbenzimidazoles as antiulcer agent
Synthesis, analgesic, anti-inflammatory, and in vitro antimicrobial activities of some novel quinazolin-4(3H)-one derivatives
Mini-plot field experiments using seed dressings to control slug damage to oilseed rape
Discovery of 2-(4-cyano-3-trifluoromethylphenyl amino)-4-(4-quinazolinyloxy)-6-piperazinyl(piperidinyl)-s-triazines as potential antibacterial agents
Neurological activities of lapachol and its furano derivatives from Kigelia africana
Synthesis, anti-inflammatory activity, and QSAR study of some Schiff bases derived from 5-mercapto-3-(4-pyridyl)-4H-1,2,4-triazol-4-yl-thiosemicarbazide
Synthesis of promising antimicrobial agents: a novel series of N-(4-(2,6-dichloroquinolin-3-yl)-6-(aryl)pyrimidin-2-yl)-2-morpholinoacetamides
Evaluation of biological activity of new hemiesters of 17-hydroxy-16,17-secoestra-1,3,5(10)-triene-16-nitrile
Insecticide selectivity and behavioral response of the earwig Doru luteipes
Nontraditional approaches to the synthesis of some biologically active substituted p-benzoquinones
Mechanisms and Issues Relating to the Use of D1-like Dopamine Receptor Agonists for Age-related Illnesses: Parkinson?s Disease and Memory and Cognition
4-Sulfenyl-2-carbamoyl-4-isoxazolin-3-ones: biological isostere to 4-chloro-2-carbamoyl-4-isoxazolin-3-ones.
Design, synthesis, and anticonvulsant screening of some substituted piperazine and aniline derivatives of 5-phenyl-oxazolidin-2,4-diones and 5,5-diphenylimidazolidin-2,4 diones
Synthesis of B-ring substituted flavones and evaluation of their antitumor and antioxidant activities
Microwave-mediated synthesis of triazolothiadiazoles as anti-inflammatory, analgesic, and anti-oxidant agents
Effects of propylene oxide doses on Cyperus and Belonolaimus control and nutrient absorption in tomato
Biological Activity of Some 2-Arylamino-4-aryloxyacetyl-2-1, 3, 4-thiadiazolidine Derivatives
Synthesis, antiproliferation, and docking studies of N-phenyl-lipoamide and 8-mercapto-N-phenyloctanamide derivatives: effects of C6 position thiol moiety
Design, synthesis and anticonvulsant evaluation of novel 8-substituted-4(3H)-quinazolines
Docking-based 3D-QSAR modeling of the inhibitors of IMP metallo--lactamase
Movento, an innovative ambimobile insecticide for sucking insect pest control in agriculture: Biological profile and field performance
In vitro antiproliferative effect of -phenylethylamine derivatives and doxorubicin combinations on MCF/ADR cell lines
cDNA structure, genomic organization, and promoter analysis of the mouse intestinal peptide transporter PEPT1.
Screening of multidrug-resistance sensitive drugs by in situ brain perfusion in P-glycoprotein-deficient mice.
Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2.
Carbamazepine is not a substrate for P-glycoprotein.
rOCT2 is a basolateral potential-driven carrier, not an organic cation/proton exchanger.
In vitro cytotoxic activities of 2-alkyl-4,6-diheteroalkyl-1,3,5-triazines: new molecules in anticancer research.
Molecular design of cholesterols as inhibitors of DNA polymerase alpha.
Diaminopyrimidine and diaminopyridine 5-HT7 ligands.
Interpreting steep dose-response curves in early inhibitor discovery.
Design, synthesis, and SAR studies on a series of 2-pyridinylpiperazines as potent antagonists of the melanocortin-4 receptor.
Indole-glucosides as novel sodium glucose co-transporter 2 (SGLT2) inhibitors. Part 2.
Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-kaitocephalin.
Search for new pharmacophores for antimalarial activity. Part II: synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines.
Novel anti-infection agents: small-molecule inhibitors of bacterial transcription factors.
Hypoxia-driven elimination of thiopurines from their nitrobenzyl prodrugs.
Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.
Novel phomactin analogues as PAF receptor ligands.
Enantioselective synthesis of a pyrrolo-benzothiadiazine derivative S 18986, a new AMPA receptor positive modulator
Dual inhibition of neutral endopeptidase and angiotensin-converting enzyme by N-phosphonomethyl and N-carboxyalkyl dipeptides
Antheliatin and Zahavins A and B, Three New Cytotoxic Xenicane Diterpenes from Two Soft Corals
Nitrogen and sulfur analogues of the secoCI alkylating agent: Synthesis and cytotoxicity
[des His1, des Phe6, Glu9]glucagon amide: A newly designed pure glucagon antagonist
The heparin-like antiproliferative activity of sulfated tetrasaccharides is sensitive to structural variation
Molecular design of novel PGI2 agonists without PG skeleton. I
5,5-Diaryl-2-thiohydantoins and 5,5-diaryl-N3-substituted-2-thiohydantoins as potential hypolipidemic agents.
Studies in antifertility agents. 50. Stereoselective binding of d- and l-centchromans to estrogen receptors and their antifertility activity.
Ecteinascidins 770 and 786 from the Thai tunicate Ecteinascidia thurstoni.
The synthesis of SO-3, a conopeptide with high analgesic activity derived from Conus striatus.
Novel Cleistanthane Diterpenoids from Pogostemon auricularis
Isolation and synthesis of an alpha-malamic acid derivative from Justicia ghiesbreghtiana.
DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORS
Synthesis of bicyclic thiazolidine PAF antagonists
Tricyclic cephems as inhibitors of human leukocyte elastase. Furo[3,4-c]cepham sulfones
Physicochemical analysis of the factors governing distribution of solutes between blood and brain
N-sulfonyl derivatives of 6,7-dichloro 3,4-dihydro-3-oxo-quinoxalinecarboxylate as glycine-site NMDA and AMPA antagonists
Synthesis and cognition activating properties of some mono- and bicyclic lactam derivatives.
Tormentic acid derivatives: synthesis and apoptotic activity.
Lipophilic Isosteres of a - Stacking Interaction: New Inhibitors of the Bcl-2-Bak Protein-Protein Interaction.
Fragment-Based Discovery of 7-Azabenzimidazoles as Potent, Highly Selective, and Orally Active CDK4/6 Inhibitors.
Chemical optimization of new ligands of the low-density lipoprotein receptor as potential vectors for central nervous system targeting.
4-quinolones as noncovalent inhibitors of high molecular mass penicillin-binding proteins.
Low Doses of Allyphenyline and Cyclomethyline, Effective against Morphine Dependence, Elicit an Antidepressant-like Effect.
Identification and In-Vitro ADME Assessment of a Series of Novel Anti-Malarial Agents Suitable for Hit-to-Lead Chemistry.
Synthesis and functionalization of cyclic sulfonimidamides: a novel chiral heterocyclic carboxylic Acid bioisostere.
Discovery of novel allosteric mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors possessing bidentate Ser212 interactions.
Identification of 4,5-dihydro-4-hydroxygeldanamycins as shunt products of geldanamycin biosynthesis.
Chiral cyclohexane 1,3-diones as inhibitors of mutant SOD1-dependent protein aggregation for the treatment of ALS.
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.
Synthesis and biological evaluation of crown ether fused quinazoline analogues as potent EGFR inhibitors.
Liver-stage malaria parasites vulnerable to diverse chemical scaffolds.
A novel 3,4-dihydropyrimidin-2(1H)-one: HIV-1 replication inhibitors with improved metabolic stability.
Characterization of TAE684 as a potent LRRK2 kinase inhibitor.
N-Methylated sst2 Selective Somatostatin Cyclic Peptide Analogue as a Potent Candidate for Treating Neurogenic Inflammation.
Synthetic N-alkylated iminosugars as new potential immunosuppressive agents.
The myo-1,2-Diaminocyclitol Scaffold Defines Potent Glucocerebrosidase Activators and Promising Pharmacological Chaperones for Gaucher Disease.
Synthesis and evaluation of novel marine bromopyrrole alkaloid-based hybrids as anticancer agents.
Synthesis and anticancer activity of novel spiro-isoxazoline and spiro-isoxazolidine derivatives of -santonin.
Preparation and antimalarial activity of semisynthetic lycorenine derivatives.
Rhazinilam-Leuconolam-Leuconoxine Alkaloids from Leuconotis griffithii.
Synthesis and biological evaluation of oleanolic acid derivatives as PTP1B inhibitors.
Novel indoline-2,3-dione derivatives as inhibitors of aminopeptidase N (APN).
Discovery of novel 2,6-disubstituted pyridazinone derivatives as acetylcholinesterase inhibitors.
Synthesis of (R)-norbgugaine and its potential as quorum sensing inhibitor against Pseudomonas aeruginosa.
Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties.
Design and synthesis of 1-aryl-5-anilinoindazoles as c-Jun N-terminal kinase inhibitors.
Synthesis and pharmacokinetic profile of highly deuterated brecanavir analogs.
Coumarins hinged directly on benzimidazoles and their ribofuranosides to inhibit hepatitis C virus.
Synthetic oligoureas of metaphenylenediamine mimic host defence peptides in their antimicrobial behaviour.
Synthesis of pyrazole encompassing 2-pyridone derivatives as antibacterial agents.
Synthesis and structure-activity relationship of pyripyropene A derivatives as potent and selective acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors: part 2.
Novel 5-(benzyloxy)pyridin-2(1H)-one derivatives as potent c-Met inhibitors.
Neomaclafungins A-I: oligomycin-class macrolides from a marine-derived actinomycete.
N,N-Dimethyl-[9-(arylsulfonyl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl]amines as novel, potent and selective 5-HT6 receptor antagonists.
Meroterpenoid and diphenyl ether derivatives from Penicillium sp. MA-37, a fungus isolated from marine mangrove rhizospheric soil.
Production of cytotoxic glidobactins/luminmycins by Photorhabdus asymbiotica in liquid media and live crickets.
Enhanced Ca2+ entry, ceramide formation, and apoptotic death of erythrocytes triggered by plumbagin.
Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.
Aryl Piperazinyl Ureas as Inhibitors of Fatty Acid Amide Hydrolase (FAAH) in Rat, Dog, and Primate.
Antiviral chromones from the stem of Cassia siamea.
Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.
A straightforward approach for engineering efficacy and selectivity at GPCRs.
Fluorescent Human EP3 Receptor Antagonists.
Structure-based discovery of substituted 4,5'-bithiazoles as novel DNA gyrase inhibitors.
Griseusins F and G, spiro-naphthoquinones from a tin mine tailings-derived alkalophilic Nocardiopsis species.
Solid-phase total synthesis of cherimolacyclopeptide E and discovery of more potent analogues by alanine screening.
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Design and in vitro activities of N-alkyl-N-[(8-R-2,2-dimethyl-2H-chromen-6-yl)methyl]heteroarylsulfonamides, novel, small-molecule hypoxia inducible factor-1 pathway inhibitors and anticancer agents.
Heterocyclic methylsulfone hydroxamic acid LpxC inhibitors as Gram-negative antibacterial agents.
The lipogenesis pathway as a cancer target.
Chrolactomycins from the actinomycete actinospica.
Rational approaches to improving selectivity in drug design.
Uvaridacols E-H, highly oxygenated antiausterity agents from Uvaria dac.
Life beyond kinases: structure-based discovery of sorafenib as nanomolar antagonist of 5-HT receptors.
Inhibition of human topoisomerases I and II by simocyclinone D8.
Strynuxlines A and B, alkaloids with an unprecedented carbon skeleton from Strychnos nux-vomica.
Phenylalanine derivatives as GPR142 agonists for the treatment of type II diabetes.
Identification of small molecule inhibitors of the HIV-1 nucleocapsid-stem-loop 3 RNA complex.
Design, synthesis, and evaluation of potential prodrugs of DFMO for reductive activation.
Multidrug resistance reversal and apoptosis induction in human colon cancer cells by some flavonoids present in citrus plants.
Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.
Cytostatic activity of novel 4'-aminochalcone-based imides.
5-Substituted 4-anilinoquinazolines as potent, selective and orally active inhibitors of erbB2 receptor tyrosine kinase.
Synthesis and antiinflammatory activity of coumarin derivatives.
The 3-Deoxy Analogue of -GalCer: Disclosing the Role of the 4-Hydroxyl Group for CD1d-Mediated NKT Cell Activation.
Heteroaromatic Moieties in the Sphingosine Backbone of -Galactosylceramides for Noncovalent Interactions with CD1d.
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.
Activity-based fluorescent probes for monitoring sulfatase activity.
Triterpenoid saponins from Xanthoceras sorbifolia Bunge and their inhibitory activity on human cancer cell lines.
Diazaspirocyclic compounds as selective ligands for the 42 nicotinic acetylcholine receptor.
3-Bromo-3-deazaneplanocin and 3-bromo-3-deazaaristeromycin: synthesis and antiviral activity.
Design, synthesis and vasodilative activity of tanshinone IIA derivatives.
Discovery of novel 1,2,4-thiadiazole derivatives as potent, orally active agonists of sphingosine 1-phosphate receptor subtype 1 (S1P(1)).
Synthesis and biological activity of novel bifunctional isoxazolidinyl polycyclic aromatic hydrocarbons.
Synthesis, biological evaluation, and molecular docking studies of 2,5-substituted-1,4-benzoquinone as novel urease inhibitors.
Discovery and structure-activity relationships of urea derivatives as potent and novel CCR3 antagonists.
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation.
Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: synthesis and pharmacological evaluation.
Potential Agents for Treating Cystic Fibrosis: Cyclic Tetrapeptides that Restore Trafficking and Activity of F508-CFTR.
Discovery of GS-9451: an acid inhibitor of the hepatitis C virus NS3/4A protease.
Benzodiazepinone Derivatives as CRTH2 Antagonists.
Novel substituted 9-norbornylpurines and their activities against RNA viruses.
Rigid Analogues of Antimitotic Indolobenzazepinones: New Insights into Tubulin Binding via Molecular Modeling.
Growth inhibition of Mycobacterium smegmatis by prodrugs of deoxyxylulose phosphate reducto-isomerase inhibitors, promising anti-mycobacterial agents.
Assessment of partially deoxygenated deoxynojirimycin derivatives as glucosylceramide synthase inhibitors.
Synthesis and Cardiac Imaging of (18)F-Ligands Selective for 1-Adrenoreceptors.
Towards the preparation of radiolabeled 1-aryl-3-benzyl ureas: Radiosynthesis of [(11)C-carbonyl] AR-A014418 by [(11)C]CO(2) fixation.
Discovery of P2X3 selective antagonists for the treatment of chronic pain.
Screening for GPCR Ligands Using Surface Plasmon Resonance.
Amphilectane diterpenes from Salvia sclarea: biosynthetic considerations.
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
Synthesis and evaluation of 2-amido-3-carboxamide thiophene CB2 receptor agonists for pain management.
Adamantyl N-benzylbenzamide: new series of depigmentation agents with tyrosinase inhibitory activity.
Pyridyl aminothiazoles as potent inhibitors of Chk1 with slow dissociation rates.
Optimization of the First Selective Steroid-11-hydroxylase (CYP11B1) Inhibitors for the Treatment of Cortisol Dependent Diseases.
Synthesis, resolution and anticonvulsant activity of chiral N-1'-ethyl,N-3'-(1-phenylethyl)-(R,S)-2'H,3H,5'H-spiro-(2-benzofuran-1,4'-imidazolidine)-2',3,5'-trione diastereomers.
Structure-Activity Relationship Studies of HIV-1 Integrase Oligonucleotide Inhibitors.
Synthesis of a novel suppressor of beta-cell apoptosis via diversity-oriented synthesis.
Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists.
Synthesis of new sulfonamides as lipoxygenase inhibitors.
NO-SSRIs: Nitric Oxide Chimera Drugs Incorporating a Selective Serotonin Reuptake Inhibitor.
Novel alkynylphosphonate analogue of calcitriol with potent antiproliferative effects in cancer cells and lack of calcemic activity.
Bivalent Ligands for the Serotonin 5-HT3 Receptor.
Agonists for the Chemokine Receptor CXCR4.
Optimization of Potent Inhibitors of P. falciparum Dihydroorotate Dehydrogenase for the Treatment of Malaria.
Optimisation of fenarimol series for the treatment of Chagas disease
Synthesis and antitumor activity of emodin quaternary ammonium salt derivatives.
Total synthesis of the marine cyclic depsipeptide viequeamide a.
Potent and Orally Bioavailable GPR142 Agonists as Novel Insulin Secretagogues for the Treatment of Type 2 Diabetes.
FPRL-1 Receptor Modulators May Provide Treatment for Inflammation.
Chiral Effect of a Phe Residue in Position 3 of the Dmt(1)-L(or D)-Tic(2) Analogues on Opioid Functional Activities.
Rational Design of Novel Pyridinol-Fused Ring Acetaminophen Analogues.
Synthesis and Metabolic Studies of Host Directed Inhibitors for Anti Viral Therapy.
Structure-based design of flavone-based inhibitors of wild-type and T315I mutant of ABL.
Confirmation of quinolone-induced formation of gyrase-DNA conjugates using AFM.
C-Glucopyranosyl-1,2,4-triazoles As New Potent Inhibitors of Glycogen Phosphorylase.
Discovery of novel insulin-like growth factor-1 receptor inhibitors with unique time-dependent binding kinetics.
An optimized pyrimidinol multifunctional radical quencher.
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter.
Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A.
ERK2 Inhibitors May Provide Treatment for Cancer.
Discovery of Pyridones As Oral AMPK Direct Activators.
Inhibitors of the renal outer medullary potassium channel.
ABCB1 Structural Models, Molecular Docking, and Synthesis of New Oxadiazolothiazin-3-one Inhibitors.
Integrated Synthesis and Testing of Substituted Xanthine Based DPP4 Inhibitors: Application to Drug Discovery.
Small-Molecule Allosteric Activation of Human Glucokinase in the Absence of Glucose.
Identification of vitamin d3-based hedgehog pathway inhibitors that incorporate an aromatic a-ring isostere.
Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds.
Development of a chimeric c-Src kinase and HDAC inhibitor.
Epimeric methylsulfinyladenosine derivatives from the marine ascidian Herdmania momus.
Inhibitors of ATR Kinase for Treatment of Cancer.
Adenosine Dioxolane Nucleoside Phosphoramidates as Antiviral Agents for Human Immunodeficiency and Hepatitis B Viruses.
Structure and Property Based Design of Pyrazolo[1,5-a]pyrimidine Inhibitors of CK2 Kinase with Activity in Vivo.
Contribution of Cage-Shaped Structure of Physalins to Their Mode of Action in Inhibition of NF-B Activation.
Optimization of Arylamides as Novel, Potent and Brain-penetrant Antiprion Lead Compounds.
Xanthone glycoside constituents of Swertia kouitchensis with -glucosidase inhibitory activity.
-Secretase Inhibitors for the Treatment of Alzheimer's Disease and Down's Syndrome.
Discovery of Inhibitors of Burkholderia pseudomallei Methionine Aminopeptidase with Antibacterial Activity.
Novel pyrazoline amidoxime and their 1,2,4-oxadiazole analogues: synthesis and pharmacological screening.
Synthesis and the 5-HT6 receptor antagonistic effect of 3-arylsulfonylamino-5,6-dihydro-6-substituted pyrazolo[3,4]pyridinones for neuropathic pain treatment.
Guanidine alkaloids from Plumbago zeylanica.
Deconstruction of a nutlin: dissecting the binding determinants of a potent protein-protein interaction inhibitor.
Structural and biological exploration of phe(3)-phe(4)-modified endomorphin-2 peptidomimetics.
Pyrazolo[3,4-d]pyrimidine Prodrugs: Strategic Optimization of the Aqueous Solubility of Dual Src/Abl Inhibitors.
Design, synthesis, and evaluation of novel VEGFR2 kinase inhibitors: discovery of [1,2,4]triazolo[1,5-a]pyridine derivatives with slow dissociation kinetics.
Unveiling the mode of action of antibacterial labdane diterpenes from Alpinia nigra (Gaertn.) B. L. Burtt seeds.
Advancement of Imidazo[1,2-a]pyridines with Improved Pharmacokinetics and Nanomolar Activity Against Mycobacterium tuberculosis.
Structural modification of pantothenamides counteracts degradation by pantetheinase and improves antiplasmodial activity.
Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.
Tyrosinase inhibitors from the wood of Artocarpus heterophyllus.
Trigohowilols A-G, degraded diterpenoids from the stems of Trigonostemon howii.
Fluostatins I-K from the South China Sea-derived micromonospora rosaria SCSIO N160.
Discovery of MK-7725, A Potent, Selective Bombesin Receptor Subtype-3 Agonist for the Treatment of Obesity.
Acetylcholinesterase inhibitors from the leaves of Macaranga kurzii.
Imidazo-benzothiazoles a potent microRNA modulator involved in cell proliferation.
Pharmacophore-based virtual screening and biological evaluation of small molecule inhibitors for protein arginine methylation.
Imidazo[1,2-a]pyridines That Directly Interact with Hepatitis C NS4B: Initial Preclinical Characterization.
A Divergent SAR Study Allows Optimization of a Potent 5-HT2c Inhibitor to a Promising Antimalarial Scaffold.
Recent results in protein kinase inhibition for tropical diseases.
A new class of selective and potent 7-dehydrocholesterol reductase inhibitors.
Synthesis and preliminary biological profile of new NO-donor tolbutamide analogues.
Synthesis and biological characterization of protease-activated prodrugs of doxazolidine.
Small molecule inhibitors of signal transducer and activator of transcription 3 (Stat3) protein.
Mitigating heterocycle metabolism in drug discovery.
Identification of the Significant Involvement and Mechanistic Role of CYP3A4/5 in Clopidogrel Bioactivation.
Discovery and development of spleen tyrosine kinase (SYK) inhibitors.
5-Arylidenethioxothiazolidinones as inhibitors of tyrosyl-DNA phosphodiesterase I.
Macrocyclic peptoid-Peptide hybrids as inhibitors of class I histone deacetylases.
Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors.
Novel histone deacetylase 8 ligands without a zinc chelating group: exploring an 'upside-down' binding pose.
Syntheses and biological activities of sulfoximine-based acyclic triaryl olefins.
Synthesis physicochemical profile and PAMPA study of new NO-donor edaravone co-drugs.
Binding Model for the Interaction of Anticancer Arylsulfonamides with the p300 Transcription Cofactor.
Synthesis of a Microcystis aeruginosa predicted metabolite with antimalarial activity.
Bisdionin C-a rationally designed, submicromolar inhibitor of family 18 chitinases.
Discovery of novel tricyclic compounds as squalene synthase inhibitors.
Novel synthetic route to the C-nucleoside, 2-deoxy benzamide riboside.
Efficient synthesis and 5-LOX/COX-inhibitory activity of some 3-hydroxybenzo[b]thiophene-2-carboxylic acid derivatives.
AM-8553: a novel MDM2 inhibitor with a promising outlook for potential clinical development.
Preparation of 3-substituted-1-isopropyl-1H-pyrazolo[3,4-d]pyrimidin-4-amines as RET kinase inhibitors.
Synthesis and evaluation of water-soluble resveratrol and piceatannol via BGLation.
Design and synthesis of potent antagonists containing rigid spirocyclic privileged structures for the CGRP receptor.
Potent and Selective Inhibitors of Long Chain l-2-Hydroxy Acid Oxidase Reduced Blood Pressure in DOCA Salt-Treated Rats.
Isolation, structure elucidation, and antibacterial activity of methiosetin, a tetramic acid from a tropical sooty mold (Capnodium sp.).
Inhibition of cholinesterase activity and amyloid aggregation by berberine-phenyl-benzoheterocyclic and tacrine-phenyl-benzoheterocyclic hybrids.
Cytotoxic cardiac glycosides and other compounds from Asclepias syriaca.
Discovery of new quinoline ether inhibitors with high affinity and selectivity for PDGFR tyrosine kinases.
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families.
Synthesis and Evaluation of the Metabolites of AMG 221, a Clinical Candidate for the Treatment of Type 2 Diabetes.
Chemical synthesis and biological evaluation of triazole derivatives as inhibitors of InhA and antituberculosis agents.
The discovery of potent and selective pyridopyrimidin-7-one based inhibitors of B-RafV600E kinase.
Aryltriflates as a Neglected Moiety in Medicinal Chemistry: A Case Study from a Lead Optimization of CXCL8 Inhibitors.
Metabolism of 4-Aminopiperidine Drugs by Cytochrome P450s: Molecular and Quantum Mechanical Insights into Drug Design.
CoA Adducts of 4-Oxo-4-Phenylbut-2-enoates: Inhibitors of MenB from the M. tuberculosis Menaquinone Biosynthesis Pathway.
N-phosphonocarbonylpyrrolidine derivatives of guanine: a new class of bi-substrate inhibitors of human purine nucleoside phosphorylase.
Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.
Fused heterocyclic compounds as ion channel modulators: patent highlight.
'Inverted' analogs of the antibiotic gramicidin S with an improved biological profile.
Rational design of 4-aryl-1,2,3-triazoles for indoleamine 2,3-dioxygenase 1 inhibition.
Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1.
Synthesis and biological evaluation of a new vitamin D2 analogue.
Identification of Hydroxybenzoic Acids as Selective Lactate Receptor (GPR81) Agonists with Antilipolytic Effects.
Novel interleukin-5 inhibitors based on hydroxyethylaminomethyl-4H-chromen-4-one scaffold.
Synthesis and Antitumor Activity of Ellagic Acid Peracetate.
Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.
RXR Partial Agonist CBt-PMN Exerts Therapeutic Effects on Type 2 Diabetes without the Side Effects of RXR Full Agonists.
Potassium channel modulators as possible treatment for pain: patent highlight.
Discovery of Selective Small Molecule ROMK Inhibitors as Potential New Mechanism Diuretics.
Discovery of BIIB042, a Potent, Selective, and Orally Bioavailable -Secretase Modulator.
3-Hydroxy-1-alkyl-2-methylpyridine-4(1H)-thiones: Inhibition of the Pseudomonas aeruginosa Virulence Factor LasB.
Synthesis and antimicrobial activity of amido linked pyrrolyl and pyrazolyl-oxazoles, thiazoles and imidazoles.
DNA Sequence Preference and Adduct Orientation of Pyrrolo[2,1-c][1,4]benzodiazepine Antitumor Agents.
Creation of readily accessible and orally active analogue of cortistatin a.
Development of 'DFG-out' inhibitors of gatekeeper mutant kinases.
Fatty Acid synthase inhibitors as possible treatment for cancer: patent highlight.
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta.
Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973).
Derivatives of heteroarylsulfonamides, their preparation, and their application in human therapy: patent highlight.
Synthesis and evaluation of the anti-proliferative and NF-B activities of a library of simplified tylophorine analogs.
A novel bitriazolyl acyclonucleoside endowed with dual antiproliferative and immunomodulatory activity.
Antimicrobial Activity of Adenine-Based Inhibitors of NAD(+)-Dependent DNA Ligase.
Substituted benzimidazole and imidazopyridine compounds useful as cyp17 modulators: patent highlight.
Discovery of Phenylaminopyridine Derivatives as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors.
Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy.
Synthesis and pharmacological evaluation of N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide as cyclooxygenase inhibitors.
Labeled Ligand Displacement: Extending NMR-Based Screening of Protein Targets.
Synthesis of 1,5-diarylhaloimidazole analogs and their inhibitory activities against PGE2 production from LPS-treated RAW 264.7 cells.
A potent and orally active antagonist (SM-406/AT-406) of multiple inhibitor of apoptosis proteins (IAPs) in clinical development for cancer treatment.
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
Investigation of the protein alkylation sites of the STAT3:STAT3 inhibitor Stattic by mass spectrometry.
Synthesis, Antiplasmodial Activity, and -Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids.
Synthesis of 2-heteroarylalkyl active vitamin d3 with therapeutic effect on enhancing bone mineral density in vivo.
Novel synthetic acridine derivatives as potent DNA-binding and apoptosis-inducing antitumor agents.
Identification of a series of compounds with potent antiviral activity for the treatment of enterovirus infections.
Pharbinilic acid, an allogibberic acid from morning glory (Pharbitis nil).
Synthesis and antimicrobial activity of imidazole and pyridine appended cholestane-based conjugates.
4-Substituted 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as a Novel Class of HIV-1 Integrase Inhibitors.
Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.
Discovery and characterization of carbamothioylacrylamides as EP2 selective antagonists.
Synthesis and anticancer activities of 5,6,7-trimethoxy-N-phenyl(ethyl)-4-aminoquinazoline derivatives.
Tropolones as lead-like natural products: the development of potent and selective histone deacetylase inhibitors.
Sulphonamido-quinoxalines: search for anticancer agent.
Potent DGAT1 Inhibitors in the Benzimidazole Class with a Pyridyl-oxy-cyclohexanecarboxylic Acid Moiety.
Tetrahydroquinoline-derived macrocyclic toolbox: the discovery of antiangiogenesis agents in zebrafish assay.
Structure-Activity Relationships and in Vivo Evaluation of Quinoxaline Derivatives for PET Imaging of -Amyloid Plaques.
Semisynthesis, cytotoxic activity, and oral availability of new lipophilic 9-substituted camptothecin derivatives.
DABCO-promoted one-pot synthesis of heteroaryl-substituted benzenes and their biological evaluation
Thrombin inhibitory activity of some polyphenolic compounds.
Molecular docking- and genetic algorithm-based approaches to produce robust 3D-QSAR models
Design and synthesis of non-TZD peroxisome proliferator-activated receptor (PPAR) modulator
Withanolides isolated from Withania somnifera with -glucosidase inhibition
Synthesis and pharmacological evaluation of novel 1-(piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one derivatives as potential antimicrobial agents
3-Carboxy-pyrazolinalanine as a new scaffold for developing potent and selective NMDA receptor antagonists.
Inhibitors of switch kinase 'spleen tyrosine kinase' in inflammation and immune-mediated disorders: a review.
Design, synthesis and biological evaluation of 4-(1-(4(sulphanilamide)phenyl)-3-(methyl)-1H-pyrazol-5-yl)dine urea and N-acyl derivatives as a soluble epoxide hydrolase inhibitors
Synthesis, in vitro evaluation and molecular modelling of naphthalimide analogue as anticancer agents.
Synthesis of new indazole derivatives as potential antioxidant agents
Descriptors requirement for QSAR analysis of pyrazolo-triazolo-pyrimidine derivative as human A3 receptor antagonists: design of novel furan derivatives and validation by docking
Synthesis and biological evaluation of novel quinazoline derivatives obtained by Suzuki CC coupling
Discovery of new antitubercular agents by combining pyrazoline and benzoxazole pharmacophores: design, synthesis and insights into the binding interactions
A comparative study of antimicrobial properties of cyclo(l-Pro- l-Asp) with its 2-ketopiperazine analog
Synthesis of halogenated derivatives of thymol and their antimicrobial activities
New synthetic approach to coumarino[4,3-b]pyridine systems and potential cytotoxic evaluation
Synthesis, molecular docking studies, and in vitro screening of barbiturates/thiobarbiturates as antibacterial and cholinesterase inhibitors
Highly potent HIV-1 protease inhibitors with novel tricyclic P2 ligands: design, synthesis, and protein-ligand X-ray studies.
Cytotoxicity and DNA-binding property of water-soluble naphthalene diimide derivatives bearing 2-oligoethoxy ethanamine side chain end-labeled with tertiary amino groups
Synergistic effects of berberines with antibiotics on clinical multi-drug resistant isolates of methicillin-resistant Staphylococcus aureus (MRSA)
Optimization of phage heptapeptide library-screening process for developing inhibitors of the isocitrate lyase homologue from Mycobacterium tuberculosis
Synthetic polyamines activating autophagy: effects on cancer cell death.
Mannich bases of 7-piperazinylquinolones and kojic acid derivatives: synthesis, in vitro antibacterial activity and in silico study.
SIRT1 modulation as a novel approach to the treatment of diseases of aging.
Design, synthesis, and pharmacological evaluation of novel hybrid compounds to treat sickle cell disease symptoms. part II: furoxan derivatives.
Synthesis of C-Pseudonucleosides Bearing Thiazolidin-4-one as a Novel Potential Immunostimulating Agent.
Synthesis and biological activity of obatoclax derivatives as novel and potent SHP-1 agonists.
Exploration of novel 3-substituted azetidine derivatives as triple reuptake inhibitors.
Pyridone alkaloids from a marine-derived fungus, Stagonosporopsis cucurbitacearum, and their activities against azole-resistant Candida albicans.
Sacchathridine A, a prostaglandin release inhibitor from Saccharothrix sp.
Cinnamic acid derivatives as inhibitors for chorismatases and isochorismatases.
Magnolia Extract, Magnolol, and Metabolites: Activation of Cannabinoid CB2 Receptors and Blockade of the Related GPR55.
Identification of Tetrahydropyrido[4,3-d]pyrimidine Amides as a New Class of Orally Bioavailable TGR5 Agonists.
Montmorillonite K-10 catalyzed green synthesis of 2,6-unsubstituted dihydropyridines as potential inhibitors of PDE4.
Design, structure-activity relationship and in vivo efficacy of piperazine analogues of fenarimol as inhibitors of Trypanosoma cruzi.
Selective Cyp11B1 Inhibitors for the Treatment of Cortisol Dependent Diseases.
Principles and applications of halogen bonding in medicinal chemistry and chemical biology.
Antioxidant and anti-inflammatory meroterpenoids from the brown alga Cystoseira usneoides.
Cytotoxic polyketide derivatives from the South China Sea sponge Plakortis simplex.
Deuterated clopidogrel analogues as a new generation of antiplatelet agents.
Anthraquinone Derivatives as Potent Inhibitors of c-Met Kinase and the Extracellular Signaling Pathway.
Design and synthesis of 3,5-diaryl-4,5-dihydro-1H-pyrazoles as new tyrosinase inhibitors.
Scopoletin and scopolin isolated from Artemisia iwayomogi suppress differentiation of osteoclastic macrophage RAW 264.7 cells by scavenging reactive oxygen species.
Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator.
Scutellarin from Scutellaria baicalensis suppresses adipogenesis by upregulating PPAR in 3T3-L1 cells.
Multivalent Interactions: Synthesis and Evaluation of Melanotropin Multimers - Tools for Melanoma Targeting.
Structural investigation and biological activity of sesquiterpene lactones from the traditional Chinese herb Inula racemosa.
Polycyclic hybrid isoprenoids from a reed rhizosphere soil derived Streptomyces sp. CHQ-64.
Growth inhibition of human colon carcinoma cells by sesquiterpenoids and tetralones of Zygogynum calothyrsum.
Structure-activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent.
Isocoumarin derivatives and benzofurans from a sponge-derived Penicillium sp. fungus.
Radiolytic transformation of rotenone with potential anti-adipogenic activity.
Antiproliferative withanolides from Datura wrightii.
Inhibition of notch pathway signaling: a one compound mission to treat cancer.
De novo prediction of p-glycoprotein-mediated efflux liability for druglike compounds.
Synthesis and in vitro cytotoxic activity evaluation of novel heterocycle bridged carbothioamide type isosteviol derivatives as antitumor agents.
Solvent Selection for Insoluble Ligands, a Challenge for Biological Assay Development: A TNF-/SPD304 Study.
Alstoniaphyllines A-C, unusual nitrogenous derivatives from the bark of Alstonia macrophylla.
Pyridine alkaloids from Senna multijuga as acetylcholinesterase inhibitors.
The central valine concept provides an entry in a new class of non peptide inhibitors of the p53-MDM2 interaction.
Targeting anthracycline-resistant tumor cells with synthetic aloe-emodin glycosides.
Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam().
Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility.
Hepatitis C RNA-dependent RNA polymerase inhibitors: a review of structure-activity and resistance relationships; different scaffolds and mutations.
Rational Drug Design Leading to the Identification of a Potent 5-HT(2C) Agonist Lacking 5-HT(2B) Activity.
Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.
Systematic Chemical Mutagenesis Identifies a Potent Novel Apratoxin A/E Hybrid with Improved in Vivo Antitumor Activity.
Discovery of Potent Dual PPAR Agonists/CB1 Ligands.
An Invitation to Open Innovation in Malaria Drug Discovery: 47 Quality Starting Points from the TCAMS.
Ianthellamide A, a selective kynurenine-3-hydroxylase inhibitor from the Australian marine sponge Ianthella quadrangulata.
Discovery of Novel 42 Neuronal Nicotinic Receptor Modulators through Structure-Based Virtual Screening.
The Discovery of VX-745: A Novel and Selective p38 Kinase Inhibitor.
Benzoylbenzimidazole-based selective inhibitors targeting Cryptosporidium parvum and Toxoplasma gondii calcium-dependent protein kinase-1.
Structure-activity relationship data for a series of N-(phenylmehtyl)-2-(1H-pyrazol-4-yl)acetamide and N-(phenylmethyl)2-(4-isoxazolyl) acetamide antagonists of the P2X7 receptor (Supplementary Bioactivity Data for publication CHEMBL1157114)
Daphnimacropodines A-D, alkaloids from Daphniphyllum macropodum.
Evaluation of the tubulin-bound paclitaxel conformation: synthesis, biology, and SAR studies of C-4 to C-3' bridged paclitaxel analogues.
Glycosidase profiling with immobilised glycosidase-inhibiting iminoalditols--a proof-of-concept study.
A cell-penetrating peptidic GRP78 ligand for tumor cell-specific prodrug therapy.
A Novel Insect Antifeedant Nonprotein Amino Acid from Calotropis gigantea
Morphinane alkaloids with cell protective effects from Sinomenium acutum.
DNA topoisomerase I inhibitors from Rinorea anguifera.
Synthesis and biological evaluation of 10,11-dihydrodictyostatin, a potent analogue of the marine anticancer agent dictyostatin.
An endoplasmic reticulum (ER) stress-suppressive compound and its analogues from the mushroom Hericium erinaceum.
Selective Dual Inhibitors of the Cancer-Related Deubiquitylating Proteases USP7 and USP47.
Formylated polyamines as peptidomimetics.
Identification of a Natural Product Antagonist against the Botulinum Neurotoxin Light Chain Protease.
Attenuation of collagen-induced arthritis by orally available imidazoline-based NF-B inhibitors.
4-Substituted-2-phenylquinazolines as inhibitors of BCRP.
Imidazotriazinone compounds: patent highlight.
Synthesis and structure-activity relationship of berberine analogues in LDLR up-regulation and AMPK activation.
Synthesis and properties of cationic 2'-O-[N-(4-aminobutyl)carbamoyl] modified oligonucleotides.
Structure-activity relationships for side chain oxysterol agonists of the hedgehog signaling pathway.
Synthesis and characterization of some new quinoline based derivatives endowed with broad spectrum antimicrobial potency.
Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.
Identification of aminopyridazine-derived antineuroinflammatory agents effective in an Alzheimer's mouse model.
Novel use of leflunomide and malononitrilamides: patent highlight.
4-Isoxazolyl-1,4-dihydropyridines exhibit binding at the multidrug-resistance transporter.
Effect of alkyl chain length on sphingosine kinase 2 selectivity.
The antitumor agent doxorubicin binds to Fanconi anemia group F protein.
Discovery of SCH 900229, a Potent Presenilin 1 Selective -Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Synthesis and structure-activity relationships of nitrobenzyl phosphoramide mustards as nitroreductase-activated prodrugs.
Development of programmable small DNA-binding molecules with epigenetic activity for induction of core pluripotency genes.
Synthesis of Lithocholic Acid Derivatives as Proteasome Regulators.
1,4-naphthoquinone cations as antiplasmodial agents: hydroxy-, acyloxy-, and alkoxy-substituted analogues.
Novel coumarin derivatives bearing N-benzyl pyridinium moiety: potent and dual binding site acetylcholinesterase inhibitors.
Carnitine palmitoyltransferase (CPT) modulators: a medicinal chemistry perspective on 35 years of research.
Discovery of Imidazoquinolines with Toll-Like Receptor 7/8 Independent Cytokine Induction.
Ranking high affinity ligands of low solubility by NMR spectroscopy.
Structure-activity relationship data for chemical series of antagonists of the P2X7 receptor (Supplementary Bioactivity Data for publication CHEMBL1157114)
Data associated with the publication PLoS ONE, 8(3), e57888, (2013) PMID: 23505445. Compounds: GSK PKIS; Assays: NIH NCATS
Malaria Box Schistosomiasis Screening Data
Discovery of novel (1S)-(-)-verbenone derivatives with anti-oxidant and anti-ischemic effects.
Synthesis, characterization, and computational studies on phthalic anhydride-based benzylidene-hydrazide derivatives as novel, potential anti-inflammatory agents
In silico accounting of novel pyridazine analogues as h-PTP 1B inhibitors: pharmacophore modelling, atom-based 3D QSAR and docking studies
Design, synthesis, and evaluation of 4-(substituted)phenyl-2-thioxo-3,4-dihydro-1H-chromino[4,3-d]pyrimidin-5-one and 4-(substituted)phenyl-3,4-dihydro-1H-chromino[4,3-d]pyrimidine-2,5-dione analogs as antitubercular agents
Microwave-assisted synthesis and anticonvulsant activity of 5,6-bisaryl-1,2,4-triazine-3-thiol derivatives
Synthesis of novel bioactive pyrazolothiazoles
Structure-based design, synthesis, and anticonvulsant activity of isatin-1-N-phenylacetamide derivatives
Synthesis and anticancer activity evaluation of new 1,2,3-triazole-4-carboxamide derivatives
Nucleophilic substitution reactions of 1,4-naphthoquinone and biologic properties of novel S-, S,S-, N-, and N,S-substituted 1,4-naphthoquinone derivatives
Synthesis and pharmacological activities of some novel 5-chloro-N-(4-(1,5-(disubstituted)-4,5-dihydro-1H-pyrazol-3-yl)phenyl)-2-methoxybenzamide derivatives
An efficient synthesis, characterization, and antimicrobial screening of tetrahydropyrimidine derivatives
Phosphorylated ganciclovir derivatives: design, synthesis and in vitro and in vivo immunomodulatory activity
Reversible redox system-based drug design, synthesis, and evaluation for targeting nitrogen mustard across brain
Synthesis and antiproliferative activity of new cytotoxic tri- and tetraazabenzo[3,2-a]fluorene-5,6-dione derivatives.
Synthesis, characterization, and antimicrobial evaluation of novel trichalcones containing core s-triazine moiety
Optimization of enzyme-based ultrasonic/microwave-assisted extraction and evaluation of antioxidant activity of orcinol glucoside from the rhizomes of Curculigo orchioides Gaertn.
Design, synthesis and biological evaluation of peptide derivatives of L-dopa as anti-parkinsonian agents.
Design, synthesis, and evaluation of novel 1-methyl-3-substituted quinazoline-2,4-dione derivatives as antimicrobial agents
Comparative QSAR and pharmacophore analysis for a series of 2,4-dihydro-3H-1,2,4-triazol-3-ones derivatives as angiotensin II AT1 receptor antagonists
[(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor.
Synthesis and cytotoxicity of (3)-3-acetyloxy-5(6)-androsten-7-one oxime and 3,5(6)-androstadien-7-one oxime
Synthesis and analgesic activity of monoterpenoid-derived 2-aryl-4,4,7-trimethyl-4a,5,8,8a-tetrahydro-4H-benzo[d][1,3]dioxin-8-ols
Potent P-glycoprotein inhibition of emodin derivative: synthesis and biological evaluation
Molecular modeling studies of substituted 3,4-dihydroxychalcone derivatives as 5-lipoxygenase and cyclooxygenase inhibitors
MT-Stabilizer, Dictyostatin, Exhibits Prolonged Brain Retention and Activity: Potential Therapeutic Implications.
Synthesis, antimicrobial, and cytotoxicity studies of novel sulfur-linked quinolinecoumarin bisheterocycles
Novel 2,6-bis(4-methoxyphenyl)-1-methylpiperidin-4-one oxime esters: synthesis and a new insight into their antioxidant and antimicrobial potential
Computational POM evaluation of experimental in vitro Trypanosoma cruzi and Mycobacterium tuberculosis inhibition of heterocyclic-2-carboxylic acid (3-cyano-1,4-di-noxidequinoxalin-2-yl)amide derivatives
Novel Macrocyclic Amidinoureas: Potent Non-Azole Antifungals Active against Wild-Type and Resistant Candida Species.
Synthesis, biological evaluation, and molecular modeling of (E)-2-aryl-5-styryl-1,3,4-oxadiazole derivatives as acetylcholine esterase inhibitors
Aminopyrazole-Phenylalanine Based GPR142 Agonists: Discovery of Tool Compound and in Vivo Efficacy Studies.
Expedient Synthesis of SMAMPs via Click Chemistry.
Synthesis and antitumor properties of novel curcumin analogs
DFT-based prediction of antifungal and insecticidal activities of perfluorophenyl antimony(III) and antimony(V) chlorides
Trichinenlides A-T, mexicanolide-type limonoids from Trichilia sinensis.
Inhibitors of tick-borne flavivirus reproduction from structure-based virtual screening.
Diterpenoids and sesquiterpenoids from the roots of Illicium majus.
Design of novel focal adhesion kinase inhibitors using 3D-QSAR and molecular docking
Synthesis, docking, and in vitro studies of some substituted bischalcones on acid and alkaline phosphatases
Synthesis and structure evaluation of new complex butylarylpiperazin-1-yl derivatives.
Discovery of ML314, a Brain Penetrant Non-Peptidic -Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.
Synthesis and cytotoxic activity of novel hybrid compounds between 2-alkylbenzofuran and imidazole
Eco-friendly synthesis and antimicrobial activities of substituted-5-(1H-indol-3-yl)methylene)-2,2-dimethyl-1,3-dioxane-4,6-dione derivatives
Selective arylsulfonamide inhibitors of ADAM-17: hit optimization and activity in ovarian cancer cell models.
Synthesis and antiseizure evaluation of isoindoline-1,3-dione derivatives in mice
The cytotoxicity of 8-O-4' neolignans from the seeds of Crataegus pinnatifida.
Cyclic 3-alkyl pyridinium alkaloid monomers from a New Zealand Haliclona sp. marine sponge.
Synthesis and antibacterial activity evaluation of 2,6-bis(6-substituted-1,2,4-triazolo[3,4-b][1,3,4]thiadiazol-3-yl)pyridine derivatives
Synthesis and anti-inflammatory activity of three nitro chalcones.
Synthesis, antimicrobial and cytotoxic activity of 2-azetidinone derivatives of pyridyl benzimidazoles
QSAR studies on diclofenac analogues as potent cyclooxygenase inhibitors using CoMFA and CoMSIA
Withanolide-based steroids from the cultured soft coral Sinularia brassica.
Substituted Benzylspiroindolin-2-one Analogues as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1.
Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.
Evaluation of 2-thioxo-2,3,5,6,7,8-hexahydropyrimido[4,5-d]pyrimidin-4(1H)-one analogues as GAA activators.
Synthesis and anti-tumor activities of methyl 2-O-aryl-6-O-aryl'-D-glucopyranosides.
Koninginin G, a new metabolite from trichoderma aureoviride
Natural polyphenols (vegetable tannins) as drugs: possible modes of action.
Compounds from Syzygium aromaticum possessing growth inhibitory activity against oral pathogens.
Synthesis, docking studies, and evaluation of pyrimidines as inhibitors of SARS-CoV 3CL protease.
The Lignans of Polygala polygama (Polygalaceae): Deoxypodophyllotoxin and Three New Lignan Lactones
Bioactive asterosaponins from the starfish Culcita novaeguineae.
Antiviral Activity of Ternatin and Meliternatin, 3-Methoxyflavones from Species of Rutaceae
A Novel Hydrolyzable Tannin and Related Compounds Isolated from the Leaf Surface of Chrysolepis sempervirens
Synthesis and biological activity of 3,4,5-trihydroxy etoposide
7-Silylcamptothecins (silatecans): A new family of camptothecin antitumor agents
2-(Aminomethyl)phenols, a new class of saluretic agents. 4. Effects of oxygen and/or nitrogen substitution.
Antimalarials. 14. 5-(aryloxy)-4-methylprimaquine analogues. A highly effective series of blood and tissue schizonticidal agents.
Ulongapeptin, a cytotoxic cyclic depsipeptide from a Palauan marine cyanobacterium Lyngbya sp.
Core-modified sordaricin derivatives: synthesis and antifungal activity.
De novo design of a picomolar nonbasic 5-HT(1B) receptor antagonist.
Unique overlap in the prerequisites for thrombin inhibition and oral bioavailability resulting in potent oral antithrombotics.
Exploiting the P-1 pocket of BRCT domains toward a structure guided inhibitor design.
Structure-activity studies of some berberine analogs as inhibitors of Toxoplasma gondii.
Discovery of novel 2-piperidinol-3-(arylsulfonyl)quinoxalines as phosphoinositide 3-kinase (PI3K) inhibitors.
Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists.
Inhibitors of Ketohexokinase: Discovery of Pyrimidinopyrimidines with Specific Substitution that Complements the ATP-Binding Site.
A Novel (18)F-Labeled Imidazo[2,1-b]benzothiazole (IBT) for High-Contrast PET Imaging of -Amyloid Plaques.
Identification of Inhibitors of NOD1-Induced Nuclear Factor-B Activation.
Host-directed Inhibitors of Myxoviruses: Synthesis and in vitro Biochemical Evaluation.
Examination of acylated 4-aminopiperidine-4-carboxylic acid residues in the phosphotyrosyl+1 position of Grb2 SH2 domain-binding tripeptides.
Synthesis and antifungal activities of 5-(3,4,5-trimethoxyphenyl)-2-sulfonyl-1,3,4-thiadiazole and 5-(3,4,5-trimethoxyphenyl)-2-sulfonyl-1,3,4-oxadiazole derivatives.
Identification of novel benzimidazole series of potent and selective ORL1 antagonists.
Estradiol dimers as a new class of steroid sulfatase reversible inhibitors.
Retapamulin inhibition of translation and 50S ribosomal subunit formation in Staphylococcus aureus cells.
The role of QSAR in dopamine interactions.
Type 1 phototherapeutic agents, part I: preparation and cancer cell viability studies of novel photolabile sulfenamides.
2-anilino-4-aryl-8H-purine derivatives as inhibitors of PDK1.
Inhibition of platelet adhesion by peptidomimetics mimicking the interactive -hairpin of glycoprotein Ib.
Identification of a Potent and Selective Cannabinoid CB1 Receptor Antagonist from Auxarthron reticulatum.
Serendipity in discovery of proteasome inhibitors.
-Lactones Inhibit N-acylethanolamine Acid Amidase by S-Acylation of the Catalytic N-Terminal Cysteine.
Synthesis and biological evaluation of truncated -galactosylceramide derivatives focusing on cytokine induction profile.
Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
Discovery of inhibitors of soluble epoxide hydrolase: a target with multiple potential therapeutic indications.
A Back-to-Front Fragment-Based Drug Design Search Strategy Targeting the DFG-Out Pocket of Protein Tyrosine Kinases.
Getting the MAX out of Computational Models: The Prediction of Unbound-Brain and Unbound-Plasma Maximum Concentrations.
Structural requirements for the antitubercular quaternized triflupromazine pharmacophore.
Antitrypanosomal and antioxidant properties of 4-hydroxycoumarins derivatives.
Water-soluble progesterone analogues are effective, injectable treatments in animal models of traumatic brain injury.
Polyhydroxylated steroidal glycosides from Paris polyphylla.
Targeting peroxisome proliferator-activated receptors (PPARs): development of modulators.
Near-infrared fluorescent divalent RGD ligand for integrin v3-targeted optical imaging.
Design, synthesis and molecular docking studies of sinomenine derivatives.
Optimization of highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Synthesis and antioxidant activity of thymol and carvacrol based Schiff bases.
Synthesis of novel chromene derivatives of expected antitumor activity.
Asymmetric synthesis and anti-protozoal activity of the 8,4'-oxyneolignans virolin, surinamensin and analogues.
Design and synthesis of alkoxyindolyl-3-acetic acid analogs as peroxisome proliferator-activated receptor-/ agonists.
Novel 2-aminooctahydrocyclopentalene-3a-carboxamides as potent CCR2 antagonists.
Sulfated pentagalloylglucoside is a potent, allosteric, and selective inhibitor of factor XIa.
Docking-based virtual screening of covalently binding ligands: an orthogonal lead discovery approach.
Design, synthesis and bioevalution of novel benzamides derivatives as HDAC inhibitors.
A remarkable series of vinblastine analogues displaying enhanced activity and an unprecedented tubulin binding steric tolerance: C20' urea derivatives.
Organosilicon molecules with medicinal applications.
Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes.
The extremo--carbonic anhydrase (CA) from Sulfurihydrogenibium azorense, the fastest CA known, is highly activated by amino acids and amines.
Discovery of 4-phenyl-2-phenylaminopyridine based TNIK inhibitors.
Discovery of coumarin-monastrol hybrid as potential antibreast tumor-specific agent.
Pyrazole-based arylalkyne cathepsin S inhibitors. Part III: modification of P4 region.
2D QSAR of heteroaryl-substituted propanolamines as antihypertensive agents
Potent cytotoxic flavonoids from Iranian Securigera securidaca
New route for synthesis, spectroscopy, and X-ray studies of 2-[aryl-(6-hydroxy-4,4-dimethyl-2-oxocyclohex-6-enyl)methyl]-3-hydroxy-5,5-dimethylcyclohex-2-enone and 1,8-dioxo-octahydroxanthenes and antitumor evaluation
A new trypsin inhibitory phthalic acid ester from Heliotropium strigosum
Designed Trpzip-3 -Hairpin Inhibits Amyloid Formation in Two Different Amyloid Systems.
Synthesis and cytotoxicity of novel 4-(4-(substituted)-1H-1,2,3-triazol-1-yl)-N-phenethylbenzenesulfonamides
Synthesis, characterization, and cytotoxicity of N-2-hydroxyethyl-substituted azastigmastanes
Exploring multitarget interactions to reduce opiate withdrawal syndrome and psychiatric comorbidity.
Phomapyrrolidones A-C, antitubercular alkaloids from the endophytic fungus Phoma sp. NRRL 46751.
Synthesis of 5-benzyl-4-aryl-octahydro-1H-benzo[b][1,5]diazepin-2-ones as potent antidepressant and antimicrobial agents
Trisubstituted imidazoles as positive modulators of metabotropic glutamate receptor subtype 5.
Synthesis, antibacterial screening, and POM analyses of novel bis-isoxazolyl/pyrazolyl-1,3-diols
Synthesis and anticonvulsant activity evaluation of 7-alkoxy-2,4-dihydro-1H-benzo[b][1,2,4]triazolo[4,3-d][1,4]thiazin-1-ones in various murine experimental seizure models
Computer-assisted design of dual-target anti-HIV-1 compounds
Structure-activity studies of divin: an inhibitor of bacterial cell division.
Design, synthesis, and evaluation of prodrugs of ertapenem.
Pharmacological evaluation of some novel synthesized compounds derived from spiro(cyclohexane-1,2-thiazolidines)
Antimycobacterial labdane diterpenes from Leucas stelligera.
Synthesis, antitubercular and anticancer activity of new BaylisHillman adduct-derived N-cinnamyl-substituted isatin derivatives
A new class of bactericidal agents against S. aureus, MRSA and VRE derived from bisindolylmethane
Theoretical studies, synthesis, and biological activity of 1-[(4-methylphenyl)sulfonyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine-4-carbonitrile (C9) as a non-peptide antagonist of the arginine vasopressin V1a and V2 receptors
Synthesis and antitumor activity evaluation of 2-arylisoquinoline-1,3(2H,4H)-diones in vitro and in vivo
Synthesis and characterization of 2-(4-((1-alkyl or aryl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)naphtho[1,2-d]oxazoles for protein tyrosine phosphatase 1B inhibitory activity
Phthaloyl amino acids as anti-inflammatory and immunomodulatory prototypes
Design, synthesis, and antimicrobial activity of some novel homodrimane sesquiterpenoids with diazine skeleton
Inhibitors of PI3K as Potential Treatment for Cancer.
Synthesis and evaluation of new chalcones, derived pyrazoline and cyclohexenone derivatives as potent antimicrobial, antitubercular and antileishmanial agents
Gardovatine, a novel Strychnos-Strychnos bisindole alkaloid with cytotoxicity from Gardneria oveta.
Influences of hydrocarbon linkers on the receptor binding affinities of gonadotropin-releasing hormone peptides.
Synthesis and pharmacological evaluation of pyrazolopyrimidopyrimidine derivatives: anti-inflammatory agents with gastroprotective effect in rats.
N-Glucosides as human sodium-dependent glucose cotransporter 2 (hSGLT2) inhibitors.
Synthesis and antimicrobial evaluation of 1,3,4-oxadiazole-based chalcone derivatives
New aminoadamantane derivatives with antiproliferative activity
Selective inhibition of heme oxygenase-2 activity by analogs of 1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzimidazole (clemizole): Exploration of the effects of substituents at the N-1 position.
Computational neural network analysis of the affinity of 2-pyridyl-3,5-diaryl pyrroles analogs for the human glucagon receptor using density functional theory
Approaches to protozoan drug discovery: phenotypic screening.
Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group.
Synthesis and in vitro and in vivo evaluation of antimalarial polyamines.
Nitroreductase-activated nitric oxide (NO) prodrugs.
Novel promising linezolid analogues: rational design, synthesis and biological evaluation.
Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
Quinolinyl- and phenantridinyl-acetamides as bradykinin B1 receptor antagonists.
Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer.
Structure-activity analysis and cell-based optimization of human galactokinase inhibitors.
Phosphonium lipocations as antiparasitic agents.
Structure-based ligand design of novel bacterial RNA polymerase inhibitors.
Homology Model and Docking-Based Virtual Screening for Ligands of the 1 Receptor.
The SAR development of dihydroimidazoisoquinoline derivatives as phosphodiesterase 10A inhibitors for the treatment of schizophrenia.
Monoenomycin: A Simplified Trienomycin A Analogue that Manifests Anticancer Activity.
Synthesis and fungicidal activity of tubulin polymerisation promoters. Part 2: pyridazines.
Footprint-based identification of viral entry inhibitors targeting HIVgp41.
Design, synthesis and cytotoxic activities of novel hybrid compounds between 2-phenylbenzofuran and imidazole.
3D Pharmacophore Model-Assisted Discovery of Novel CDC7 Inhibitors.
Preparation, gram-negative antibacterial activity, and hydrolytic stability of novel siderophore-conjugated monocarbam diols.
Discovery and Hit-to-Lead Optimization of Non-ATP Competitive MK2 (MAPKAPK2) Inhibitors.
Discovery of an orally-bioavailable CC Chemokine Receptor 2 antagonist derived from an acyclic diaminoalcohol backbone.
Synthesis and biological evaluation of novel potent angiotensin II receptor antagonists with anti-hypertension effect.
Identification of NAE Inhibitors Exhibiting Potent Activity in Leukemia Cells: Exploring the Structural Determinants of NAE Specificity.
Novel potent dual inhibitors of CK2 and Pim kinases with antiproliferative activity against cancer cells.
Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity.
New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, and -amyloid-reducing properties.
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
Mannitol Bis-phosphate Based Inhibitors of Fructose 1,6-Bisphosphate Aldolases.
Optimization of Pharmacokinetics through Manipulation of Physicochemical Properties in a Series of HCV Inhibitors.
Bromophenols as inhibitors of protein tyrosine phosphatase 1B with antidiabetic properties.
Synthesis of natural flutimide and analogous fully substituted pyrazine-2,6-diones, endonuclease inhibitors of influenza virus.
Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein.
The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein 1 (MRP-1).
Direct interaction between a quinoline derivative, MS-209, and multidrug resistance protein (MRP) in human gastric cancer cells.
Design, solvent free synthesis, and antimicrobial evaluation of 1,4 dihydropyridines.
A highly sensitive fluorescent viscosity sensor.
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.
Synthesis and characterization of quinoline-based thiosemicarbazones and correlation of cellular iron-binding efficacy to anti-tumor efficacy.
Halogenated anthraquinones from the marine-derived fungus Aspergillus sp. SCSIO F063.
Anti-inflammatory Effect of a Cell-Penetrating Peptide Targeting the Nrf2/Keap1 Interaction.
Compounds: GSK PKIS; Assays: Nanosyn kinase panel
Sirtuin 2 inhibitors rescue alpha-synuclein-mediated toxicity in models of Parkinson's disease.
Constrained analogs of CB-1 antagonists: 1,5,6,7-Tetrahydro-4H-pyrrolo[3,2-c]pyridine-4-one derivatives.
Synthesis and biological activity of quinolinone and dihydroquinolinone p38 MAP kinase inhibitors.
Tanikolide, a toxic and antifungal lactone from the marine cyanobacterium Lyngbya majuscula.
Cytotoxic terpenoids from the Formosan soft coral Nephthea brassica.
Synthesis and biological evaluation of polymethoxylated 4-heteroarylcoumarins as tubulin assembly inhibitor.
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
Alkyne-quinuclidine derivatives as potent and selective muscarinic antagonists for the treatment of COPD.
First CoMFA characterization of vesamicol analogs as ligands for the vesicular acetylcholine transporter.
A novel pyrene-guanidiniocarbonyl-pyrrole cation efficiently differentiates between ds-DNA and ds-RNA by two independent, sensitive spectroscopic methods.
In Vitro Action of ent -Manoyl Oxides against Leishmania donovani
Absolute Configuration of 2,6-Dimethylheptyl Sulfate and Its Distribution in Ascidiacea
One pot solvent free synthesis and in vitro antitubercular screening of 3-Aracylphthalides against Mycobacterium tuberculosis.
Systematic exploration of dual-acting modulators from a combined medicinal chemistry and biology perspective.
The discovery of potent and selective 4-aminothienopyridines as B-Raf kinase inhibitors.
Synthesis, crystal structure and antidiabetic activity of substituted (E)-3-(Benzo [d]thiazol-2-ylamino) phenylprop-2-en-1-one.
Sirtuins as emerging anti-parasitic targets.
Inhibition of protein glycation by urea and thiourea derivatives of glycine/proline conjugated benzisoxazole analogue - synthesis and structure-activity studies.
Discovery and evaluation of novel inhibitors of mycobacterium protein tyrosine phosphatase B from the 6-Hydroxy-benzofuran-5-carboxylic acid scaffold.
Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase.
A natural product inspired hybrid approach towards the synthesis of novel pentamidine based scaffolds as potential anti-parasitic agents.
Design, synthesis and biological evaluation of novel aliphatic amido/sulfonamido-quaternary ammonium salts as antitumor agents.
Synthesis of cembranoid analogues and evaluation of their potential as quorum sensing inhibitors.
Pentacyclic hemiacetal sterol with antifouling and cytotoxic activities from the soft coral Nephthea sp.
Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors.
Antiviral activity of (+)-sattabacin against varicella zoster.
Synthesis, characterization, and anticancer studies of S and N alkyl piperazine-substituted positional isomers of 1,2,4-triazole derivatives
Synthesis and antibacterial evaluation of 3,3-diindolylmethane derivatives
Flavone-based analogues inspired by the natural product simocyclinone D8 as DNA gyrase inhibitors.
Synthesis and HDAC inhibitory activity of isosteric thiazoline-oxazole largazole analogs.
2-(2-Hydrazinyl)thiazole derivatives: design, synthesis and in vitro antimycobacterial studies.
Synthesis, cytotoxicity, and DNA-binding property of berberine derivatives
Design, synthesis and biological evaluation of a novel class of potent TGR5 agonists based on a 4-phenyl pyridine scaffold.
Multicomponent synthesis and anticonvulsant activity of monocyclic 2,6-diketopiperazine derivatives.
Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor.
Synthesis and antimicrobial activity of polyhalobenzonitrile quinazolin-4(3H)-one derivatives.
Morphological changes of some pathogenic microbial strains induced by novel thiadiazole derivatives
Potent inhibition of norovirus by dipeptidyl -hydroxyphosphonate transition state mimics.
New combination of pharmacophoric elements of potent 1 ligands: design, synthesis and receptor affinity of aminoethyl substituted tetrahydrobenzothiophenes.
Synthesis and cytotoxic activity of some novel steroidal C-17 pyrazolinyl derivatives.
Discovery of DF-461, a Potent Squalene Synthase Inhibitor.
3D-QSAR using pharmacophore-based alignment and virtual screening for discovery of novel MCF-7 cell line inhibitors.
Pharmacokinetics, metabolism, and in vivo efficacy of the antimalarial natural product bromophycolide A.
Fighting Obesity and Metabolic Disorders with MGAT-2 Inhibitors.
Replacement of Thr32 and Gln34 in the C-terminal neuropeptide Y fragment 25-36 by cis-cyclobutane and cis-cyclopentane -amino acids shifts selectivity toward the Y(4) receptor.
Synthesis, pharmacological and structural characterization, and thermodynamic aspects of GluA2-positive allosteric modulators with a 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxide scaffold.
Design and Synthesis of 4-(4-Benzoylaminophenoxy)phenol Derivatives As Androgen Receptor Antagonists.
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
Perindopril and ramipril phosphonate analogues as a new class of angiotensin converting enzyme inhibitors.
Design, synthesis, and bioevaluation of viral 3C and 3C-like protease inhibitors.
Serendipity in drug-discovery: a new series of 2-(benzyloxy)benzamides as TRPM8 antagonists.
Fused 3-Hydroxy-3-trifluoromethylpyrazoles Inhibit Mutant Huntingtin Toxicity.
Synthesis and Evaluation of Quinazolone Derivatives as a New Class of c-KIT G-Quadruplex Binding Ligands.
Phenyl substituted 3-hydroxypyridin-2(1H)-ones: inhibitors of influenza A endonuclease.
Optimization of activity, selectivity, and liability profiles in 5-oxopyrrolopyridine DPP4 inhibitors leading to clinical candidate (Sa)-2-(3-(aminomethyl)-4-(2,4-dichlorophenyl)-2-methyl-5-oxo-5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)-N,N-dimethylacetamide (BMS-767778).
Design, synthesis, and activity of a series of arylpyrid-3-ylmethanones as type I positive allosteric modulators of 7 nicotinic acetylcholine receptors.
Involvement of MDR1 P-glycoprotein in multifactorial resistance to methotrexate.
Effects of bile salt flux variations on the expression of hepatic bile salt transporters in vivo in mice.
Flavonoid permeability across an in situ model of the blood-brain barrier.
Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver.
Enhanced drug-induced apoptosis associated with P-glycoprotein overexpression is specific to antimicrotubule agents.
Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15+C1007G, by using transient expression systems of HeLa and HEK293 cells.
Cloning and functional characterization of a novel rat organic anion transporter mediating basolateral uptake of methotrexate in the kidney.
P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro.
Hepatobiliary excretion of acetaminophen glutathione conjugate and its derivatives in transport-deficient (TR-) hyperbilirubinemic rats.
Characterization, cDNA cloning, and functional expression of mouse ileal sodium-dependent bile acid transporter.
Inhibitory effect of novel oral hypoglycemic agent nateglinide (AY4166) on peptide transporters PEPT1 and PEPT2.
Alternative strategies towards the identification of chemical lead compounds by rational design
2-Aryl-1-azabicyclo[2.2.2]octanes as novel nonpeptide substance P antagonists
Quinoline-4-carboxylic acids as angiotensin II receptor antagonists
2,3,6-Substituted quinazolinones as angiotensin II receptor antagonists
Design, synthesis, X-ray analysis, and dopamine receptor-modulating activity of mimics of the "C5" hydrogen-bonded conformation in the peptidomimetic 2-oxo-3(R)-[(2(S)-pyrrolidinylcarbonyl)amino]-1- pyrrolidineacetamide.
Bridged 1,2,5,6-tetrahydropyridine esters and oxime ethers related to arecoline are novel and potent muscarinic agonists
Synthesis and pharmacological evaluation of vinyl sulfone based anticancer agents
Lactones from a brown alga endophytic fungus (No. ZZF36) from the South China Sea and their antimicrobial activities.
Structure-based de novo design, synthesis, and biological evaluation of the indole-based PPARgamma ligands (I).
Compounds: GSK PKIS; Assays: UNC Frye lab
Bioactive 3,4-seco-Triterpenoids from the Fruits of Acanthopanax sessiliflorus.
Synthesis of benzamide derivatives and their evaluation as antiprion agents.
Biotin analogues with antibacterial activity are potent inhibitors of biotin protein ligase.
Intestinally Targeted Diacylglycerol Acyltransferase 1 (DGAT1) Inhibitors Robustly Suppress Postprandial Triglycerides.
Synthesis and antibacterial activity of 6-O-(heteroaryl-isoxazolyl)propynyl 2-fluoro ketolides.
Integrated virtual screening for the identification of novel and selective peroxisome proliferator-activated receptor (PPAR) scaffolds.
Novel Cyclopropyl-Indole Derivatives as HIV Non-Nucleoside Reverse Transcriptase Inhibitors.
Structure-Activity Relationship for Thiirane-Based Gelatinase Inhibitors.
Drugs for stroke: action of nitrone (Z)-N-(2-bromo-5-hydroxy-4-methoxybenzylidene)-2-methylpropan-2-amine oxide on rat cortical neurons in culture subjected to oxygen-glucose-deprivation.
Avicholic Acid: A Lead Compound from Birds on the Route to Potent TGR5 Modulators.
Discovery of HDAC Inhibitors That Lack an Active Site Zn(2+)-Binding Functional Group.
Triazole Appending Agent (TAAG): A New Synthon for Preparing Iodine-Based Molecular Imaging and Radiotherapy Agents.
Evolution of a Compact Photoprobe for the Dopamine Transporter Based on ()-threo-Methylphenidate.
Cyclooxygenase-1-selective inhibitors based on the (E)-2'-des-methyl-sulindac sulfide scaffold.
Set-up of a new series of HDAC inhibitors: the 5,11-dihydrodibenzo[b,e]azepin-6-ones as privileged structures.
An Orally Available 3-Ethoxybenzisoxazole Capsid Binder with Clinical Activity against Human Rhinovirus.
The Rhodadyns, a New Class of Small Molecule Inhibitors of Dynamin GTPase Activity.
Design of a Potent CB1 Receptor Antagonist Series: Potential Scaffold for Peripherally-Targeted Agents.
Discovery of MK-5172, a Macrocyclic Hepatitis C Virus NS3/4a Protease Inhibitor.
Identification of Simple Compounds with Microtubule-Binding Activity That Inhibit Cancer Cell Growth with High Potency.
SAR studies around a series of triazolopyridines as potent and selective PI3K inhibitors.
Type 1 Phototherapeutic Agents. 2. Cancer Cell Viability and ESR Studies of Tricyclic Diarylamines.
Sesquiterpenoids from Incarvillea arguta: absolute configuration and biological evaluation.
Fungal bis-Naphthopyrones as Inhibitors of Botulinum Neurotoxin Serotype A.
Dual-Specificity Phosphatase CDC25A/B Inhibitor Identified from a Focused Library with Nonelectrophilic Core Structure.
Targeted kinase selectivity from kinase profiling data.
Synthesis and antimalarial activity of 3,3-spiroanellated 5,6-disubstituted 1,2,4-trioxanes.
Discovery of a novel broad-spectrum antifungal agent derived from albaconazole.
Synthesis of 8-hydroxyquinoline derivatives as novel antitumor agents.
Polyamino geranic derivatives as new chemosensitizers to combat antibiotic resistant gram-negative bacteria.
Identification of Potent and Selective Diphenylpropanamide ROR Inhibitors.
Optimization of peptide hydroxamate inhibitors of insulin-degrading enzyme reveals marked substrate-selectivity.
QSAR investigation of NaV1.7 active compounds using the SVM/Signature approach and the Bioclipse Modeling platform.
Discovery of HSD-621 as a Potential Agent for the Treatment of Type 2 Diabetes.
Synthesis of novel analogs of cabergoline: improving cardiovascular safety by removing 5-HT2B receptor agonism.
Interrogation of the Active Sites of Protein Arginine Deiminases (PAD1, -2, and -4) Using Designer Probes.
A Fluorescent Styrylquinoline with Combined Therapeutic and Diagnostic Activities against Alzheimer's and Prion Diseases.
Discovery of novel Trypanosoma brucei phosphodiesterase B1 inhibitors by virtual screening against the unliganded TbrPDEB1 crystal structure.
Rapid Determination of Ionization Constants (pK a) by UV Spectroscopy Using 96-Well Microtiter Plates.
Aldosterone synthase inhibitors: targeting chronic kidney disease and diabetic nephropathy.
PDE10 Inhibitors as Potential Treatment for Schizophrenia.
Multifunctional radical quenchers for the treatment of mitochondrial dysfunction.
Development and evaluation of novel phosphotyrosine mimetic inhibitors targeting the Src homology 2 domain of signaling lymphocytic activation molecule (SLAM) associated protein.
Novel Inverse Binding Mode of Indirubin Derivatives Yields Improved Selectivity for DYRK Kinases.
Biological active analogues of the opioid peptide biphalin: mixed /(3)-peptides.
Synthesis and antimycobacterial activity of 2,1'-dihydropyridomycins.
Synthesis, Optimization, and Evaluation of Novel Small Molecules as Antagonists of WDR5-MLL Interaction.
Genomics-guided discovery of thailanstatins A, B, and C As pre-mRNA splicing inhibitors and antiproliferative agents from Burkholderia thailandensis MSMB43.
Steroids glycosylated with both D- and L-arabinoses from the South China Sea gorgonian Dichotella gemmacea.
Discovery of dopamine D4 receptor antagonists with planar chirality.
Structure-Based Design and Synthesis of an HIV-1 Entry Inhibitor Exploiting X-Ray and Thermodynamic Characterization.
Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists.
Structure-based design, synthesis and evaluation of novel anthra[1,2-d]imidazole-6,11-dione derivatives as telomerase inhibitors and potential for cancer polypharmacology.
Extracellular signal-regulated kinases (ERK) inhibitors from Aristolochia yunnanensis.
-mangostin and gambogic acid as potential inhibitors of the p53-MDM2 interaction revealed by a yeast approach.
Solphenazines A-F, glycosylated phenazines from Streptomyces sp. strain DL-93.
Xanthoquinodins from the endolichenic fungal strain Chaetomium elatum.
Aza-BODIPY: improved synthesis and interaction with soluble A1-42 oligomers.
Spiro heterocycles as potential inhibitors of SIRT1: Pd/C-mediated synthesis of novel N-indolylmethyl spiroindoline-3,2'-quinazolines.
(M)- and (P)-bicelaphanol A, dimeric trinorditerpenes with promising neuroprotective activity from Celastrus orbiculatus.
Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist.
Identification of HIV-1 inhibitors targeting the nucleocapsid protein.
ATP-binding site of bacterial enzymes as a target for antibacterial drug design.
Structural investigation of anti-Trypanosoma cruzi 2-iminothiazolidin-4-ones allows the identification of agents with efficacy in infected mice.
Bacterial reduction as means for colonic drug delivery: can other chemical groups provide an alternative to the azo bond?
Synthesis and biological evaluation (in vitro and in vivo) of cyclic arginine-glycine-aspartate (RGD) peptidomimetic-paclitaxel conjugates targeting integrin V3.
3-Alkoxy-1,2-Dioxolanes: Synthesis and Evaluation as Potential Antimalarial Agents.
Nonpeptidic lysosomal modulators derived from z-phe-ala-diazomethylketone for treating protein accumulation diseases.
Nitazoxanide Disrupts Membrane Potential and Intrabacterial pH Homeostasis of Mycobacterium tuberculosis.
Discovery of novel inhibitors of amyloid -peptide 1-42 aggregation.
Hepatoprotective iridoid glycosides from the roots of Rehmannia glutinosa.
Structure-based design of novel inhibitors of the MDM2-p53 interaction.
Plakilactones from the marine sponge Plakinastrella mamillaris. Discovery of a new class of marine ligands of peroxisome proliferator-activated receptor .
Virtual screening and optimization yield low-nanomolar inhibitors of the tautomerase activity of Plasmodium falciparum macrophage migration inhibitory factor.
Kinetic profile of amyloid formation in the presence of an aromatic inhibitor by nuclear magnetic resonance.
Discovery of the First Potent Inhibitors of Mutant IDH1 That Lower Tumor 2-HG in Vivo.
Anticancer activity and cellular repression of c-MYC by the G-quadruplex-stabilizing 11-piperazinylquindoline is not dependent on direct targeting of the G-quadruplex in the c-MYC promoter.
Potential use of selective and nonselective Pim kinase inhibitors for cancer therapy.
Synthesis and SAR Studies of Fused Oxadiazines as -Secretase Modulators for Treatment of Alzheimer's Disease.
Factor D Inhibitors for the Treatment of AMD: Patent Highlight.
Jatrophane diterpenes from Euphorbia mellifera and their activity as P-glycoprotein modulators on multidrug-resistant mouse lymphoma and human colon adenocarcinoma cells.
Antifungal spectrum, in vivo efficacy, and structure-activity relationship of ilicicolin h.
Discovery of benzodiazepine sulfonamide-based bombesin receptor subtype 3 agonists and their unusual chirality.
A convenient synthesis of 2-amino-2-oxazolines and their pharmacological evaluation at cloned human adrenergic receptors
Novel HO-DPAT (hydroxy-2-dipropylaminotetralin) isomers: Stereoselective synthesis and receptor binding studies
Acyl CoA:cholesterol acyltransferase (ACAT) inhibitors: ureas bearing heterocyclic groups bioisosteric for an imidazole
Inhibitors of human collagenase: dipeptide mimetics with lactam and azalactam moieties at the position
The anti-rheumatic potential of a series of 2,4-di-substituted-4H-naphtho[1,2-b]pyran-3-carbonitriles
The Abu-pocket paradox of the cyclophilin a / cyclosporin a interaction
Chemical modification of ring c of himbacine: Discovery of a pharmacophoric element for M2-selectivity
An efficient synthesis of the benzhydrylpiperazine delta opioid agonist (+)-BW373U86
Antitumor activity of 9(R)-dihydrotaxane analogs.
4-Diazinyl- and 4-pyridinylimidazoles: potent angiotensin II antagonists. A study of their activity and computational characterization.
Synthesis of conformationally-constrained stereospecific analogs of glutamic acid as antagonists of metabotropic receptors
Structure-activity studies of the natural product substance P antagonist win 64821
Aporphine alkaloids, CD45 protein tyrosine phosphatase inhibitors, from Rollinia ulei
N-(Quinuclidin-3-yl)-2-(1-methyl-1H-indol-3-yl)-2-oxo-acetamide: a high affinity 5-HT3 receptor partial agonist
Synthetic inhibitors of interleukin-6 II: 3,5-diaryl pyridines and meta-terphenyls
Tricyclic cephems as inhibitors of human leukocyte elastase. thieno[3,4-c]cepham sulfones and pyrrolo[3,4-c]cepham sulfones
Synthesis of indane derivatives as mechanism-based inhibitors of dopamine -hydroxylase
Synthesis and characterization of cyclic ATP-ribose: a potent mediator of calcium release
Novel tricyclic aminoacetyl and sulfonamide inhibitors of Ras farnesyl protein transferase
The design and synthesis of novel adenosine agonists
Synthesis and pharmacological evaluation of highly potent dual histamine H2 and gastrin receptor antagonists
Identification and structure-activity relationship studies of osthol, a cytotoxic principle from Cnidium monnieri
Inhibition of protein phosphatase 2A by cyclic peptides modelled on the microcystin ring
Synthesis of highly potent RXR-specific retinoids: The use of a cyclopropyl group as a double bond isostere
Mercaptoacyl matrix metalloproteinase inhibitors: The effect of substitution at the mercaptoacyl moiety
Identification of the first retinoid X, receptor homodimer antagonist.
Synthesis and anticonvulsant evaluation of a series of (R)- and (S)-N-Cbz--aminoglutarimide and succinimide
Tetrazole NK1 receptor antagonists: The identification of an exceptionally potent orally active antiemetic compound
2-[(Alkylsulfonyl)oxy]-6-substituted-1H-isoindole-1,3(2H)-dione mechanism-based inhibitors of human leukocyte elastase
Novel conformationally constrained analogues of diacylglycerol. Protein kinase C binding affinity of simplified compounds based on a 6-membered lactam moiety
Selective cytotoxicity of certain 9-substituted ellipticines for leukemia cells in a variety of leukemia cell cultures
Synthesis and biological evaluation of 5,6-diarylimidazo[2.1-b]thiazole as selective COX-2 inhibitors
Tetracyclic analogues of [+]-S 14297: Synthesis and determination of affinity and selectivity at cloned human dopamine D3 vs D2 receptors
Cyclic homopentapeptides 2. Synthetic modifications of viomycin
Validation of EGSITE2, a mixed integer program for deducing objective site models for experimental binding data.
Alstilobanines A-E, new indole alkaloids from Alstonia angustiloba.
Chemical characterization and pharmacological activity of nazlinin, a novel indole alkaloid from Nitraria schoberi.
Halogenated metabolites from the new Okinawan red alga Laurencia yonaguniensis.
8-Hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors.
Mechanism of action of pyridazine analogues on protein tyrosine phosphatase 1B (PTP1B).
Synthesis and pharmacological characterization of a novel nitric oxide-releasing diclofenac derivative containing a benzofuroxan moiety.
Synthesis and antihyperglycemic evaluation of various protoberberine derivatives.
New 5-hydroxytryptamine(1A) receptor ligands containing a norbornene nucleus: synthesis and in vitro pharmacological evaluation.
Structural characterization and antimicrobial evaluation of atractyloside, atractyligenin, and 15-didehydroatractyligenin methyl ester.
HIV-1 Integrase Inhibitor-Inspired Antibacterials Targeting Isoprenoid Biosynthesis.
Boron-Based 4-Hydroxytamoxifen Bioisosteres for Treatment of de Novo Tamoxifen Resistant Breast Cancer.
Synthesis and biochemical evaluation of thiochromanone thiosemicarbazone analogues as inhibitors of cathepsin L.
Identification of a sirtuin 3 inhibitor that displays selectivity over sirtuin 1 and 2.
-Lapachone analogs with enhanced antiproliferative activity.
Truncated phosphonated C-1'-branched N,O-nucleosides: a new class of antiviral agents.
Discovery of Natural Phenols as G Protein-Coupled Receptor-35 (GPR35) Agonists.
Pharmacophore Refinement Guides the Rational Design of Nanomolar-Range Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease.
Steroidomimetic Tetrahydroisoquinolines for the Design of New Microtubule Disruptors.
Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors.
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models.
(18)F-labeled phenyldiazenyl benzothiazole for in vivo imaging of neurofibrillary tangles in Alzheimer's disease brains.
Synthesis and evaluation of 11-(4-substituted phenyl) estradiol analogs: transition from estrogen receptor agonists to antagonists.
Application of MM-GB/SA and WaterMap to SRC Kinase Inhibitor Potency Prediction.
Cytotoxic alkaloids from Fusarium incarnatum associated with the mangrove tree Aegiceras corniculatum.
S-Farnesyl-Thiopropionic Acid (FTPA) Triazoles as Potent Inhibitors of Isoprenylcysteine Carboxyl Methyltransferase.
Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode.
Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria.
Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia.
Synthesis, anticonvulsant activity, and neuropathic pain-attenuating activity of N-benzyl 2-amino-2-(hetero)aromatic acetamides.
Discovery, design and synthesis of Y-shaped peroxisome proliferator-activated receptor agonists as potent anti-obesity agents in vivo.
Antimicrobial metabolites from the Paracel Islands sponge Agelas mauritiana.
Discovery and optimization of benzenesulfonanilide derivatives as a novel class of 11-HSD1 inhibitors.
5-Arylbenzothiadiazine Type Compounds as Positive Allosteric Modulators of AMPA/Kainate Receptors.
Dual-target virtual screening by pharmacophore elucidation and molecular shape filtering.
Bis-spirolabdane diterpenoids from Leonotis nepetaefolia.
Ring Structure and Aromatic Substituent Effects on the pK a of the Benzoxaborole Pharmacophore.
Multifunctional mercapto-tacrine derivatives for treatment of age-related neurodegenerative diseases.
Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core.
Isoprenylated flavonoid and adipogenesis-promoting constituents of Dodonaea viscosa.
Design, synthesis, anti-HIV evaluation and molecular modeling of piperidine-linked amino-triazine derivatives as potent non-nucleoside reverse transcriptase inhibitors.
Alkylidene branched lupane derivatives: synthesis and antitumor activity.
Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.
Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones as 5-HT2C receptor agonists.
Non-benzimidazole containing inhibitors of respiratory syncytial virus.
A nitrophenyl-based prodrug type for colorectal targeting of prednisolone, budesonide and celecoxib.
Five-membered iminocyclitol -glucosidase inhibitors: synthetic, biological screening and in silico studies.
Bromotyrosine alkaloids from the Australian marine sponge Pseudoceratina verrucosa.
Hybrids consisting of the pharmacophores of salmeterol and roflumilast or phthalazinone: dual 2-adrenoceptor agonists-PDE4 inhibitors for the treatment of COPD.
Cytotoxic, antitopoisomerase II, and anti-HIV-1 activities of triterpenoids isolated from leaves and twigs of Gardenia carinata.
Isolation of ciliatamide D from a marine sponge Stelletta sp. and a reinvestigation of the configuration of ciliatamide A.
Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors.
Inhibition of mTOR Kinase and Cancer Treatment.
Targeting CCR2 Receptor To Treat Inflammation Diseases and Disorders.
Chemo-Immunotherapeutic Anti-Malarials Targeting Isoprenoid Biosynthesis.
N-(Phenoxyalkyl)amides as MT(1) and MT(2) ligands: antioxidant properties and inhibition of Ca(2+)/CaM-dependent kinase II.
Synthesis and cytotoxicity of 3-aryl acrylic amide derivatives of the simplified saframycin-ecteinascidin skeleton prepared from L-dopa.
Dorsamin-A's, glycerolipids carrying a dehydrophenylalanine ester moiety from the seed-eating larvae of the bruchid beetle Bruchidius dorsalis.
Development of N-Hydroxycinnamamide-Based Histone Deacetylase Inhibitors with Indole-Containing Cap Group.
Antioxidant lignans and chromone glycosides from Eurya japonica.
Cyclopropyl-Fused 1,3-Thiazepines as BACE1 and BACE2 Inhibitors.
Synthetic approaches to DNMT inhibitor SGI-1027 and effects on the U937 leukemia cell line.
Isolation and characterization of unusual hydrazides from Streptomyces sp. impact of the cultivation support and extraction procedure.
Positive allosteric modulators of nicotinic acetylcholine receptor.
Syntheses and anti-allergic activity of 2-((bis(trimethylsilyl)methylthio/methylsulfonyl)methyl)-5-aryl-1,3,4-oxadiazoles.
Bioactive indole alkaloids and phenyl ether derivatives from a marine-derived Aspergillus sp. Fungus.
Structure and absolute configuration of fumiquinazoline L, an alkaloid from a gorgonian-derived Scopulariopsis sp. fungus.
Design and synthesis of D1 agonist/D2 antagonist for treatment of schizophrenia.
Synthesis and antitubercular activity of amino alcohol fused spirochromone conjugates.
Design, Synthesis, and Pharmacological Evaluation of Fluorescent and Biotinylated Antagonists of 1 GABAC Receptors.
Spirocyclic compounds, potent CCR1 antagonists.
Applicability of a blood-brain barrier specific artificial membrane permeability assay at the early stage of natural product-based CNS drug discovery.
Orally active fumagillin analogues: transformations of a reactive warhead in the gastric environment.
Flavaglines as potent anticancer and cytoprotective agents.
Inhibition of hypoxia inducible factor-2 transcription: isolation of active modulators from marine sponges.
10'-Fluorovinblastine and 10'-Fluorovincristine: Synthesis of a Key Series of Modified Vinca Alkaloids.
Peptido sulfonyl fluorides as new powerful proteasome inhibitors.
Bile acid-based 1,2,4-trioxanes: synthesis and antimalarial assessment.
Rational design of potent non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Bivalent ligands targeting multiple pathological factors involved in Alzheimer's disease.
Melittin suppresses VEGF-A-induced tumor growth by blocking VEGFR-2 and the COX-2-mediated MAPK signaling pathway.
The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase .
Sulfonyl fluoride inhibitors of fatty acid amide hydrolase.
Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2.
()-Tylopilusins, diphenolic metabolites from the fruiting bodies of Tylopilus eximius.
Redox potentials, laccase oxidation, and antilarval activities of substituted phenols.
GPR119 Modulators for the Treatment of Diabetes, Obesity, and Related Diseases: Patent Highlight.
Nonsteroidal androgen receptor ligands: versatile syntheses and biological data.
Synthesis and anti-hyperglycemic activity of hesperidin derivatives.
Specific interactions between adenosine and streptavidin/avidin.
Synthesis and cytotoxicity evaluation of highly functionalized pyranochromenes and pyranopyrans.
D-amino acid based protein arginine deiminase inhibitors: Synthesis, pharmacokinetics, and in cellulo efficacy.
Discovery of AC710, a Globally Selective Inhibitor of Platelet-Derived Growth Factor Receptor-Family Kinases.
Synthesis and biological evaluation of a bicyclo [7.4.1]enediyne
New directions in antibacterial research.
N-Phthalimidoalkyl derivatives of 2-carbomethoxy-3-(4-iodophenyl)tropane (-CIT): Brain monoamine transporter affinity
A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.
Development of a high-affinity ligand that binds irreversibly to Mel1b melatonin receptors.
Synthesis and evaluation of polycyclic pyrazolo[3,4-d]pyrimidines as PDE1 and PDE5 cGMP phosphodiesterase inhibitors.
7-O-acylpaclitaxel analogues: potential probes to map the paclitaxel binding site
Chemoenzymatic synthesis of iminocyclitol derivatives: a useful library strategy for the development of selective fucosyltransfer enzymes inhibitors.
Phosphodiesterase inhibitory properties of losartan. Design and synthesis of new lead compounds.
Discovery of novel nonsteroidal glucocorticoid receptor modulators.
Synthesis and antimicrobial activity of symmetrical two-tailed dendritic tricarboxylato amphiphiles.
Design and synthesis of novel opioid ligands with an azabicyclo[2.2.2]octane skeleton and their pharmacologies.
Effects of tacrolimus and cyclosporin A on peptide transporter PEPT1 in Caco-2 cells.
Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells.
A transfected cell model for the renal toxin transporter, rOCT2.
A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells.
Absence of the mdr1a P-Glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A.
Identification and characterization of a prostaglandin transporter.
Up-regulation of organic anion transporter 1 protein is induced by chronic furosemide or hydrochlorothiazide infusion in rat kidney.
Modulation of the function of P-glycoprotein by estramustine.
Characterization of the transport of the bicyclic peptide phalloidin by human hepatic transport proteins.
Evaluation of an immortalized retinal endothelial cell line as an in vitro model for drug transport studies across the blood-retinal barrier.
Discovery of a Novel Series of CRTH2 (DP2) Receptor Antagonists Devoid of Carboxylic Acids.
Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.
Toward Overcoming Staphylococcus aureus Aminoglycoside Resistance Mechanisms with a Functionally Designed Neomycin Analogue.
Trigoxyphins H and I: two new daphnane diterpenoids from Trigonostemon xyphophylloides.
Potentiating Metronidazole Scaffold against Resistant Trichomonas: Design, Synthesis, Biology and 3D-QSAR Analysis.
Bioactive quassinoids from the seeds of Brucea javanica.
Synthesis and biological evaluation of cyclic sulfamide derivatives as 11-hydroxysteroid dehydrogenase 1 inhibitors.
Small Molecule Inhibitors of Regulator of G Protein Signalling (RGS) Proteins.
Sphingolipid analogues inhibit development of malaria parasites.
Binding of ibuprofen, ketorolac, and diclofenac to COX-1 and COX-2 studied by saturation transfer difference NMR.
1,2,4-Oxadiazoles: a new class of anti-prostate cancer agents.
Discovery and synthesis of namalide reveals a new anabaenopeptin scaffold and peptidase inhibitor.
Synthesis and evaluation of fluorobenzoylated di- and tripeptides as inhibitors of cyclooxygenase-2 (COX-2).
Synthesis and structure-activity relationship (SAR) study of 4-azabenzoxazole analogues as H3 antagonists.
Structure-activity relationship study of selective benzimidazole-based inhibitors of Cryptosporidium parvum IMPDH.
One pot synthesis and anticancer activity of dimeric phloroglucinols.
Potent norovirus inhibitors based on the acyclic sulfamide scaffold.
-Carboline alkaloids from the leaves of Trigonostemon lii Y.T. Chang.
Design, synthesis, single-crystal and preliminary antitumor activity of novel arenesulfonylimidazolidin-2-ones.
Thieno[2,3-d]pyrimidinedione derivatives as antibacterial agents.
Imidazo[1,2-a]pyrazines as novel PI3K inhibitors.
Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
Benzanilide-Biphenyl Replacement: A Bioisosteric Approach to Quinoline Carboxamide-Type ABCG2 Modulators.
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Oxo-heterocyclic fused naphthalimides as antitumor agents: synthesis and biological evaluation.
Benzimidazole-carboxamides as potent and bioavailable stearoyl-CoA desaturase (SCD1) inhibitors from ligand-based virtual screening and chemical optimization.
Tetracyclic diterpenoids with isomerized isospongian skeleton and labdane diterpenoids from the fruits of Amomum kravanh.
Synthesis of tetrazole analogues of phosphonohydroxamic acids: an attempt to improve the inhibitory activity against the DXR.
Anti-inflammatory lanostanoids and lactone derivatives from Antrodia camphorata.
Nocardiamides A and B, two cyclohexapeptides from the marine-derived actinomycete Nocardiopsis sp. CNX037.
Synthesis, biological evaluation and molecular modeling of aloe-emodin derivatives as new acetylcholinesterase inhibitors.
Arundinols A-C and arundinones A and B from the plant endophytic fungus Microsphaeropsis arundinis.
Examination of the mode of action of the almiramide family of natural products against the kinetoplastid parasite Trypanosoma brucei.
Antiallodynic and analgesic effects of maslinic acid, a pentacyclic triterpenoid from Olea europaea.
Diarylheptanoids and flavonoids from viscum album inhibit LPS-stimulated production of pro-inflammatory cytokines in bone marrow-derived dendritic cells.
The discovery of novel isoflavone pan peroxisome proliferator-activated receptor agonists.
Discovery and Preliminary SAR of Arylpiperazines as Novel, Brainpenetrant Antiprion Compounds.
Vegfrecine, an inhibitor of VEGF receptor tyrosine kinases isolated from the culture broth of Streptomyces sp.
Evaluation of constituents of Piper retrofractum fruits on neurotrophic activity.
Synthesis and antiplasmodial and antimycobacterial evaluation of new nitroimidazole and nitroimidazooxazine derivatives.
Mycoleptodiscins A and B, cytotoxic alkaloids from the endophytic fungus Mycoleptodiscus sp. F0194.
Garcinia xanthones as orally active antitumor agents.
Trisubstituted Sulfonamides: a New Chemotype for Development of Potent and Selective CB2 Receptor Inverse Agonists.
Structure-based design and synthesis of novel pseudosaccharine derivatives as antiproliferative agents and kinase inhibitors.
Rapid microwave-enhanced synthesis of C5-alkynyl pyranonucleosides as novel cytotoxic antitumor agents.
Nudibaccatumone, a trimer comprising a phenylpropanoid and two sesquiterpene moieties from Piper nudibaccatum.
Design and synthesis of bicyclic pyrazinone and pyrimidinone amides as potent TF-FVIIa inhibitors.
Design and Synthesis of Potent Bivalent Peptide Agonists Targeting the EphA2 Receptor.
New diterpene furanoids from the Antarctic lichen Huea sp.
Strategy for Imidazotetrazine Prodrugs with Anticancer Activity Independent of MGMT and MMR.
Structure-Based Design of Potent and Selective CK1 Inhibitors.
Development of Synthetic Aminopeptidase N/CD13 Inhibitors to Overcome Cancer Metastasis and Angiogenesis.
Synopsis of some recent tactical application of bioisosteres in drug design.
Lanostanoids from fungi: a group of potential anticancer compounds.
SAR and Lead Optimization of an HIV-1 Vif-APOBEC3G Axis Inhibitor
Discovery and Structural Modification of 1-Phenyl-3-(1-phenylethyl)urea Derivatives as Inhibitors of Complement.
Inhibitors of the NAD(+)-Dependent Protein Desuccinylase and Demalonylase Sirt5.
A new approach to explore the binding space of polysaccharide-based ligands: selectin antagonists.
Synthesis and Anti-influenza A Virus Activity of 2,2-Dialkylamantadines and Related Compounds.
Isolation and synthesis of two antiproliferative calamenene-type sesquiterpenoids from Sterculia tavia from the Madagascar rain forest.
Minimizing Drug Exposure in the CNS while Maintaining Good Oral Absorption.
Novel bivalent ligands for D2/D3 dopamine receptors: Significant co-operative gain in D2 affinity and potency.
Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
Synthesis and antimycobacterial activity of calpinactam derivatives.
Synthesis and biological evaluation of a selective N- and p/q-type calcium channel agonist.
From 42 Nicotinic Ligands to the Discovery of 1 Receptor Ligands: Pharmacophore Analysis and Rational Design.
Design, synthesis and biological evaluation of N-arylphenyl-2,2-dichloroacetamide analogues as anti-cancer agents.
Peptide-chlorambucil conjugates combat pgp-dependent drug efflux.
Synthesis and structure-activity relationships of a novel series of pyrimidines as potent inhibitors of TBK1/IKK kinases.
Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.
Facile synthesis and anticancer activity of C-10 non-acetal deoxoartemisinin dimers.
Structure-Based Discovery of a Novel Pentamidine-Related Inhibitor of the Calcium-Binding Protein S100B.
Design, synthesis and molecular simulation studies of dihydrostilbene derivatives as potent tyrosinase inhibitors.
Synthesis and Evaluation of 5-Fluoro-2-aryloxazolo[5,4-b]pyridines as -Amyloid PET Ligands and Identification of MK-3328.
Clerodane diterpenoids from Croton crassifolius.
Disubstituted quinazoline derivatives as a new type of highly selective ligands for telomeric G-quadruplex DNA.
Crucial Role of 3-Bromoethyl in Removing the Estrogenic Activity of 17-HSD1 Inhibitor 16-(m-Carbamoylbenzyl)estradiol.
The Discovery of MK-4256, a Potent SSTR3 Antagonist as a Potential Treatment of Type 2 Diabetes.
Design and synthesis of procollagen C-proteinase inhibitors.
Synthesis of retinoid enhancers based on 2-aminobenzothiazoles for anti-cancer therapy.
A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.
An unusually cold active nitroreductase for prodrug activations.
Influence of antipsychotic, antiemetic, and Ca(2+) channel blocker drugs on the cellular accumulation of the anticancer drug daunorubicin: P-glycoprotein modulation.
Reversal of multidrug resistance in human leukemia K562 by tamolarizine, a novel calcium antagonist.
Electrophysiological characteristics of the proton-coupled peptide transporter PEPT2 cloned from rat brain.
Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor.
Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver.
Influence of passive permeability on apparent P-glycoprotein kinetics.
Inhibitory potencies of 1,4-dihydropyridine calcium antagonists to P-glycoprotein-mediated transport: comparison with the effects on CYP3A4.
Time-dependent inhibition of neuronal nitric oxide synthase by N-propargylguanidine
Design and synthesis of hapten to induce phospholipase A2-like catalytic antibody
The synthesis of CD - ring modified 1,25-dihydroxy vitamin D analogues: Six-membered D-ring analogues II
Synthesis and structure-activity relationships of some novel oxetane carbapenems
Inhibition of the her2 tyrosine kinase and characterization of a hydrophobic site near the nucleotide binding domain
Covalent binding of catechols to src family SH2 domains
Inhibition of nematode induced root damage by derivatives of methylenecyclopropane acetic acid
Phthalimidomethyl as a drug pro-moiety. Probing its reactivity.
Synthesis and structure-activity relationships of 2-pyridones: II. 8-(Fluoro-substituted pyrrolidinyl)-2-pyridones as antibacterial agents.
Discovery of potent, achiral matrix metalloproteinase inhibitors.
Investigations of neurotrophic inhibitors of FK506 binding protein via Monte Carlo simulations.
Dimers of 5HT1 ligands preferentially bind to 5HT1B/1D receptor subtypes.
2-Fluoro-4-pyridinylmethyl analogues of linopirdine as orally active acetylcholine release-enhancing agents with good efficacy and duration of action.
Nonpeptidic SH2 inhibitors of the tyrosine kinase ZAP-70.
Substituted furans as inhibitors of the PDE4 enzyme.
Novel cytokine release inhibitors. Part IV: analogs of podocarpic acid.
Synthesis of piperazine derivatives and evaluation of their antihistamine and antibradykinin effects.
Synthesis of a phostone glycomimetic of the endothelin converting enzyme inhibitor phosphoramidon.
Synthesis of phosphonate 3-phthalidyl esters as prodrugs for potential intracellular delivery of phosphonates.
Inhibitors of human histone deacetylase with potent activity against the African trypanosome Trypanosoma brucei.
Proteasome inhibitors for cancer therapy.
Antiviral effect of geraniin on human enterovirus 71 in vitro and in vivo.
Thieno[3,2-b]thiophene-2-carboxylic acid derivatives as GPR35 agonists.
Peptidolipins B-F, antibacterial lipopeptides from an ascidian-derived Nocardia sp.
Kinase inhibitory potencies and in vitro antiproliferative activities of N-10 substituted pyrrolo[2,3-a]carbazole derivatives.
Exploring activity cliffs in medicinal chemistry.
Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor.
Inhibitors of the FEZ-1 metallo-beta-lactamase.
Synthesis and cytotoxic evaluation of C-9 oxidized podophyllotoxin derivatives.
Saponins from the flower buds of Buddleja officinalis.
Sulfemodin 8-O-beta-D-glucoside, a new sulfated anthraquinone glycoside, and antioxidant phenolic compounds from Rheum emodi.
Design and synthesis of novel CCR3 antagonists.
Synthesis and CB1 receptor activities of novel arachidonyl alcohol derivatives.
Carbonic anhydrase activators: the first X-ray crystallographic study of an adduct of isoform I.
Synthesis and anti-angiogenesis activity of coumarin derivatives.
The role of fluorine substitution in the structure-activity relationships (SAR) of classical cannabinoids.
Cytotoxic and antimalarial beta-carboline alkaloids from the roots of Eurycoma longifolia.
An Antibiotic from Trichoderma Koningii Active Against Soilborne Plant Pathogens
X-ray crystal structure of acrovestone, a cytotoxic principle from Acronychia pedunculata.
Synthesis and in vitro antileukemic activity of some new 1,3-(oxytetraethylenoxy)cyclotriphosphazene derivatives.
Effect of Fungal Natural Products in an Agrobacterium tumefaciens Potato Disc Assay
(+)-Laburnamine, a natural selective ligand and partial agonist for the 42 nicotinic receptor subtype.
Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.
Identification of inhibitors against interaction between pro-inflammatory sPLA2-IIA protein and integrin v3.
The structure of anthracycline derivatives determines their subcellular localization and cytotoxic activity.
Identification of RO4597014, a Glucokinase Activator Studied in the Clinic for the Treatment of Type 2 Diabetes.
Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design.
Evidence for the involvement of descending pain-inhibitory mechanisms in the antinociceptive effect of hecogenin acetate.
A series of thiazole derivatives bearing thiazolidin-4-one as non-competitive ADAMTS-5 (aggrecanase-2) inhibitors.
Structure-activity relationship study of tachykinin peptides for the development of novel neurokinin-3 receptor selective agonists.
Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
Design, synthesis, and structure-activity relationship studies of novel 3-alkylindole derivatives as selective and highly potent myeloperoxidase inhibitors.
Structure-activity relationship data for chemical series of achiral agonists of the ghrelin (growth hormone secretagogue) receptor (Supplementary Bioactivity Data for publication CHEMBL1140573)
Synthesis and ionophoric activities of functionalized bis(choloyl) conjugates with a rigid core.
Development of Novel Alkene Oxindole Derivatives As Orally Efficacious AMP-Activated Protein Kinase Activators.
Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
Synthetic tactics of new class of 4-aminothieno[2,3-d]pyrimidine-6-carbonitrile derivatives acting as antimicrobial agents.
Identification of Selective Nanomolar Inhibitors of the Human Neuraminidase, NEU4.
Identification of New Nonsteroidal ROR Ligands; Related Structure-Activity Relationships and Docking Studies.
Development of Unsymmetrical Dyads As Potent Noncarbohydrate-Based Inhibitors against Human -N-Acetyl-d-hexosaminidase.
PAK1: A Therapeutic Target for Cancer Treatment.
Role of Amphiphilicity in the Design of Synthetic Mimics of Antimicrobial Peptides with Gram-negative Activity.
Discovery of a New Class of Potent MMP Inhibitors by Structure-Based Optimization of the Arylsulfonamide Scaffold.
New Peptide-based antimicrobials for tackling drug resistance in bacteria: single-cell fluorescence imaging.
Metabolically Stable tert-Butyl Replacement.
Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development.
Discovery of tetrahydropyrazolopyrimidine carboxamide derivatives as potent and orally active antitubercular agents.
Sesquiterpenes and alkaloids from the roots of Alangium chinense.
Geranylated flavonoids displaying SARS-CoV papain-like protease inhibition from the fruits of Paulownia tomentosa.
ABSOLUTE CONFIGURATION AND BIOLOGICAL PROPERTIES OF ENANTIOMERS OF CFTR INHIBITOR BPO-27.
Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles.
Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease.
Pharmacological activity of retinoic acid receptor alpha-selective antagonists in vitro and in vivo.
Design, synthesis and antiproliferative activity of a novel class of indole-2-carboxylate derivatives.
Design, synthesis and biological evaluation of brain targeting l-ascorbic acid prodrugs of ibuprofen with "lock-in" function.
Potent and orally efficacious bisthiazole-based histone deacetylase inhibitors.
Novel and high affinity fluorescent ligands for the serotonin transporter based on (s)-citalopram.
Tetraoxane-pyrimidine nitrile hybrids as dual stage antimalarials.
Design and synthesis of quinolinopropellane derivatives with selective opioid receptor agonism.
The design and synthesis of novel SGLT2 inhibitors: C-glycosides with benzyltriazolopyridinone and phenylhydantoin as the aglycone moieties.
Cyclohexadepsipeptides of the isaridin class from the marine-derived fungus Beauveria felina EN-135.
Characterization of proapoptotic compounds from the bark of Garcinia oblongifolia.
Synthesis and in vivo SAR study of indolin-2-one-based multi-targeted inhibitors as potential anticancer agents.
Bromopyrrole alkaloids isolated from the Patagonian bryozoan Aspidostoma giganteum.
Aplysinellamides A-C, bromotyrosine-derived metabolites from an Australian Aplysinella sp. marine sponge.
Dimeric flavonoids from Arrabidaea brachypoda and assessment of their anti-Trypanosoma cruzi activity.
Tuning the antimicrobial pharmacophore to enable discovery of short lipopeptides with multiple modes of action.
Delayed and Prolonged Histone Hyperacetylation with a Selective HDAC1/HDAC2 Inhibitor.
Toward the Development of Bivalent Ligand Probes of Cannabinoid CB1 and Orexin OX1 Receptor Heterodimers.
Muchimangins G-J, fully substituted xanthones with a diphenylmethyl substituent, from Securidaca longepedunculata.
Design, synthesis and biological evaluation of hydroxy- or methoxy-substituted 5-benzylidene(thio) barbiturates as novel tyrosinase inhibitors.
Thiosemicarbazide, a fragment with promising indolamine-2,3-dioxygenase (IDO) inhibition properties.
4-Benzofuranyloxynicotinamide derivatives are novel potent and orally available TGR5 agonists.
Discovery of potent anticancer agent HJC0416, an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3).
Iron chelators in photodynamic therapy revisited: synergistic effect by novel highly active thiosemicarbazones.
Tabercarpamines A-J, apoptosis-inducing indole alkaloids from the leaves of Tabernaemontana corymbosa.
Experimental in vitro DMPK and physicochemical data on a set of publicly disclosed compounds
Fragment-based discovery of type I inhibitors of maternal embryonic leucine zipper kinase.
Pyrimidine-based tricyclic molecules as potent and orally efficacious inhibitors of wee1 kinase.
Wnt/-Catenin Signaling Pathway Inhibitors: A Promising Cancer Therapy.
Discovery of a Potent Analgesic NOP and Opioid Receptor Agonist: Cebranopadol.
Design, synthesis and evaluation of novel indole derivatives as AKT inhibitors.
Pyrrolizines: Promising scaffolds for anticancer drugs.
Antimicrobial activity of de novo designed cationic peptides against multi-resistant clinical isolates.
Probing the Binding Site of Bile Acids in TGR5.
Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.
Synthesis of a novel series of artemisinin dimers with potent anticancer activity involving Sonogashira cross-coupling reaction.
Exploring the chemical space of multitarget ligands using aligned self-organizing maps.
Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Synthesis of licochalcone analogues with increased anti-inflammatory activity.
Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation.
Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.
From NMDA receptor antagonists to discovery of selective 2 receptor ligands.
Design and Synthesis of Peptide YY Analogues with C-terminal Backbone Amide-to-Ester Modifications.
Discovery of potent and selective inhibitors of Toxoplasma gondii thymidylate synthase for opportunistic infections.
Urea/oxalamide tethered -lactam-7-chloroquinoline conjugates: synthesis and in vitro antimalarial evaluation.
Design and Discovery of 2-Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases.
Synthesis and anticancer evaluation of 3-substituted quinolin-4-ones and 2,3-dihydroquinolin-4-ones.
Fragment-based discovery of 6-azaindazoles as inhibitors of bacterial DNA ligase.
(E)-Alkenes as replacements of amide bonds: development of novel and potent acyclic CGRP receptor antagonists.
Antitumor potential of conjugable valinomycins bearing hydroxyl sites: in vitro studies.
Influenza RNA-Dependent RNA Polymerase (RdRp) Inhibitors: Potential New Therapy for Influenza Treatment.
Discovery of Pyridyl Bis(oxy)dibenzimidamide Derivatives as Selective Matriptase Inhibitors.
Design, Synthesis, and Antiviral Evaluation of Chimeric Inhibitors of HIV Reverse Transcriptase.
Synthesis and preliminary evaluation of a new fluorine-18 labelled triazine derivative for PET imaging of cannabinoid CB2 receptor.
Synthesis and biological evaluation of novel N-substituted 1H-dibenzo[a,c]carbazole derivatives of dehydroabietic acid as potential antimicrobial agents.
Design, synthesis and evaluation of 7-azaindazolyl-indolyl-maleimides as glycogen synthase kinase-3 (GSK-3) inhibitors.
Synthesis of novel 2-cyano substituted glycyrrhetinic acid derivatives as inhibitors of cancer cells growth and NO production in LPS-activated J-774 cells.
Identification and optimization of an aminoalcohol-carbazole series with antimalarial properties.
New inhibitors of cytomegalovirus DNA polymerase.
Design, synthesis and anti-Alzheimer properties of dimethylaminomethyl-substituted curcumin derivatives.
Synthesis, molecular docking, and cardioprotective activity of 2-methylthio-1,4-dihydropyrimidines
Isolation of terrestribisamide from Peltophorum pterocarpum (DC.) Baker ex. K. Heyne and its antimicrobial, antioxidant, and cytotoxic activities
Exacerbative role of vitamn A on radiation damage in vivo
Synthesis and antitumor activities of unsymmetrically disubstituted acylthioureas fused with hydrophenanthrene structure
Design, synthesis, and evaluation of novel indomethacinantioxidant codrugs as gastrosparing NSAIDs
Study on the quantitative structuretoxicity relationships of aconitine compounds basing on PCA-ANN method
QSAR studies of antituberculosis drug using three-dimensional structure descriptors
Involvement of Esterase in Phytotoxicity of a New Pyrrolinone Compound, Methyl 1-[1-(3,5-Dichlorophenyl)-1-methylethyl]-2,3-dihydro-4-methyl-2-oxo-3-phenyl-1H-pyrrole-3-carboxylate, to Early Watergrass (Echinochloa oryzicola) and Rice (Oryza sativa)
Thiourea and thioether derivatives of sorafenib: synthesis, crystal structure, and antiproliferative activity
Benzoxepin derivatives: design, synthesis, and pharmacological evaluation with sedativehypnotic effect
Synthesis of new piperidyl indanone derivatives as anticonvulsant agents
Synthesis and hypoglycemic activity evaluation of 7-alkoxyl-rhein
Synthesis and evaluation of fused pyrimidine derivatives as anti-inflammatory, antiproliferative and antimicrobial agents
In vivo peritoneal antiangiogenesis and in vitro antiproliferative properties of some bischalcone derivatives
-Methyl as a bioisostere for the oxygen link between the aromatic rings of aryloxyphenoxypropionate herbicides
Novel N-aryl(alkaryl)-2-[(3-R-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazoline-6-yl)thio]acetamides: synthesis, cytotoxicity, anticancer activity, COMPARE analysis and docking
Synthesis and antibacterial evaluation of series of novel tri-substituted-s-triazine derivatives
INHIBITORS OF FILARIAL GAMMA-GLUTAMYL CYCLE ENZYMES AS POSSIBLE MACROFILARICIDAL AGENTS
Synthesis and biological activity studies of new hybrid molecules containing tryptamine moiety
Identification of Novel Non-nucleoside Reverse Transcriptase Inhibitors Using Fragment-based Lead Generation
Design, synthesis, and potential CNS activity of some new bioactive 1-(4-substituted-phenyl)-3-(4-oxo-2-methyl-4H-quinazolin-3-yl)-urea
Antifeedant and toxic effects of naturally occurring and synthetic quinones to the cabbage looper, Trichoplusia ni
Pyrazolo[3,4-d]pyrimidine analogues: synthesis, characterization and their in vitro antiamoebic activity
Synthesis and antidepressant activity of di substituted-5-aryl-1,2,4-triazoles
Bioisosteric synthesis of nitrogen containing derivatives of salicyl alcohol, their in vivo pharmacological studies with molecular modeling
Synthesis and antimicrobial activity of some new 3[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2- styrylquinazoline-4(3H)-ones
QSAR studies on substituted 3- or 4-phenyl-1,8-naphthyridine derivatives as antimicrobial agents
Synthesis and evaluation of some pyrimidine analogs against toxoplasmosis
Synthesis and antitumor evaluation of some novel pyrrolizine derivatives
Synthesis, cytotoxicity, and structureactivity insight of NH- and N-methyl-3,5-bis-(arylidenyl)-4-piperidones
Design, synthesis, and evaluation of fluorescent cell-penetrating peptidic antagonists of Grb2-SH2 for targeting MCF-7 breast cancer cells
Synthesis and Selective Bioactivity of New Pyrazolecarboxamide Derivatives
Antitumor activities of some new 1,3,2-oxaza- and 1,3,2-diazaphosphorinanes against K562, MDA-MB-231, and HepG2 cells
Synthesis and evaluation of some new 4-aminopyridine derivatives as a potent antiamnesic and cognition enhancing drugs
Development of a New Acaricide, Fenpyroximate
Normalizing effects of Costus speciosus rhizome crude extracts and its fractions on diabetic complications in STZ-induced diabetic rats
Effect of side-chain alteration on hormonal activity of nonsteroidal estrogen antagonists
In vitro anti-inflammatory potential and QSAR analysis of oxazolo/thiazolo pyrimidine derivatives
Synthesis of biphenyl derivatives as ACE and -amylase inhibitors
Antidiabetic and antioxidant activity of hydroxycinnamic acids from Calamintha Officinalis Moench.
Sensitivity of Botrytis cinerea to chitosan and acibenzolar-S-methyl.
Synthesis and antimicrobial activities of highly functionalised novel -lactam and thiazolidine-grafted tetrahydrobenzothiophenes
Chemistry of insect antifeedants from Azadirachta indica (part 11): Characterisation and structure activity relationships of some novel rearranged azadirachtins.
Design, synthesis and structure-activity relationship of novel coumarin derivatives.
Ajugatakasins A and B, New Diterpenoids fromAjuga decumbens, and Feeding Stimulative Activity of Related Neoclerodane Analogs toward the Turnip Sawfly
Three-dimensional common-feature hypotheses for hypoglycemic flavonyl-2,4-thiazolidinedione derivatives
Antifungal activity of prenylated flavonoids isolated from Tephrosia apollinea L. against four phytopathogenic fungi
Antitussive effects of azepino[2,1-b]quinazolones
Computational and thermodynamic analyses of the phospholipase A2 inhibition by erucic acid and linoleic acid
The Veratrum alkaloids jervine, veratramine, and their analogues as prostate cancer migration and proliferation inhibitors: biological evaluation and pharmacophore modeling
Inhibition of Cathepsin D protease activity by Punica granatum fruit peel extracts, isolates, and semisynthetic analogs
Synthesis of new 2(1H)-quinoxalinone derivatives for antimicrobial and antiinflammatory evaluation
Antitumour activity of 5-[(2E)-1-(1H-benzimidazol-2-yl)-3-substituted phenylprop-2-en-1-ylidene] pyrimidine-2,4,6(1H,3H,5H)-triones against Daltons ascitic lymphoma in mice
Expedient synthesis of some novel pregnane derivatives and their evaluation as anti-oxidant and anti-dyslipidemic agents
Design, synthesis, and anticonvulsant evaluation of some novel 1, 3 benzothiazol-2-yl hydrazones/acetohydrazones
Novel antifeeding limonoids from Dysoxylum hainanense
Some remarkable reactions of the diterpene eriocephalin: Neo-clerodane derivatives with insect antifeedant activity
QSAR analysis of 2-benzoxazolyl hydrazone derivatives for anticancer activity and its possible target prediction
Synthesis, characterization and antimicrobial activity of 4-amino-1-alkyl pyridinium salts
Design and synthesis of 1-(benzothiazol-5-yl)-1H-1,2,4-triazol-5-ones as protoporphyrinogen oxidase inhibitors.
4-Thiazolidinone and 1-thia-3,4,9-triaza fluorene conjugates: synthesis, characterization and antimicrobial screening
Synthesis and antimicrobial activity of coumarin pyrazole pyrimidine 2,4,6(1H,3H,5H)triones and thioxopyrimidine4,6(1H,5H)diones
New Insecticidal 4-Acetoxy-2-alkenylquinolines
Computational QSAR models with high-dimensional descriptor selection improve antitumor activity design of ARC-111 analogues
Isonicotinic acid hydrazide derivatives: synthesis, antimicrobial activity, and QSAR studies
Synthesis of piperineamino acid ester conjugates and study of their cytotoxic activities against human cancer cell lines
Synthesis and pharmacological evaluation of 4-[2-hydroxy-3-(4-phenyl-piperazin-1-yl)-propoxy]-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione
QSAR analysis of 2-sulfonylphenyl-3-phenyl-indole derivatives as novel anti-inflammatory compounds
Synthesis and Cytotoxic Activity of 6-(Substituted-Phenyl)Amino-5,8-Quinazolinediones
Pyrithiobac reduces control of green foxtail (Setaria viridis) and bristly foxtail (Setaria verticillata) by propaquizafop
Quinolone derivatives as antitubercular drugs
Structure-dependent phytotoxicity of catechins and other flavonoids: flavonoid conversions by cell-free protein extracts of Centaurea maculosa (spotted knapweed) roots.
Design, synthesis, and docking studies of telmisartan analogs for the treatment of metabolic syndrome
Prenylated xanthones: antiproliferative effects and enhancement of the growth inhibitory action of 4-hydroxytamoxifen in estrogen receptor-positive breast cancer cell line
Docking and QSAR studies of new 1,4-dihydropyridines containing 4(5)-chloro-2-methyl-5(4)-imidazolyl substituent
Synthesis and pharmacological screening of some novel chalconyl derivatives of substituted phenyl semicarbazide
Synthesis, in vitro cytotoxicity, and anti-microbial studies of 1,4-bis(4-substituted-5-mercapto-1,2,4-triazol-3-yl)butanes
Ligand-based in silico 3D-QSAR study of PPAR- agonists
Fungitoxic Properties of N-Phenylformamidoximes in Control of Benzimidazole-Resistant Isolates of Fungi
Evaluation of the curative and protectant activity of fungicides and fungicide-adjuvant mixtures on Phomopsis cane and leaf spot of grape: A controlled environment study
In vitro and in vivo antifungal activity of synthetic pure isothiocyanates against Sclerotinia sclerotiorum.
3D-QSAR study of tyrosine and propanoic acid derivatives as PPAR/ dual agonists using CoMSIA
Green approach towards the facile synthesis of dihydropyrano(c)chromene and pyrano[2,3-d]pyrimidine derivatives and their biological evaluation
Comparison of Acaricidal, Insecticidal, and Nerve Activities of Halfenprox (MTI-732) and Related Compounds
Synthesis and biological evaluation of novel AM80 derivatives as antileukemic agents
Synthesis and biological evaluation of novel 4,5-dihydropyrazole derivatives as potent anticancer and antimicrobial agents
Antifeedant effects and chemical composition of essential oils from different populations of Lavandula luisieri L.
In vivo antidiabetic activity and in silico studies on adenosine monophosphate-activated protein kinase (AMPK) of (2E,5E)-2,5-bis(4-hydroxy-3-methoxybenzylidene) cyclopentanone
Synthesis, cytostatic and anti-viral activity evaluation of the novel acyclic nucleoside analogues containing a sterically constrained (Z)-4-amino-2-butenyl moiety
3D QSAR kNN-MFA studies on thiouracil derivatives as hepatitis C virus inhibitors
3-(4-Methylfuran-3-yl)propan-1-ol: a white-spotted Stinkbug ( Eysarcoris ventralis ) repellent produced by an endophyte isolated from green foxtail.
Antihyperglycaemic activity of Sinularia firma and Sinularia erecta in streptozotocin-induced diabetic rats
Evaluation of mefenamic acid mutual prodrugs
Design, synthesis, and QSAR study of novel 2-(2,3-dioxo-2,3-dihydro-1H-indol-1-yl)-N-phenylacetamide derivatives as cytotoxic agents
Synthesis and evaluation of anti-inflammatory and analgesic activity of 3-[(5-substituted-1,3,4-oxadiazol-2-yl-thio)acetyl]-2H-chromen-2-ones
Design and synthesis of new 2,4,5-triarylimidazole derivatives as selective cyclooxygenase (COX-2) inhibitors
Protoporphyrinogen-IX Oxidase Inhibition by N-(2, 4, 5-Trisubstituted phenyl)-3, 4, 5, 6-tetrahydrophthalimides
Synthesis of bioactive spiro-2-[3-(2-phenyl)-3H-indolyl]-1-aryl-3-phenylaziridines and SAR studies on their antimicrobial behavior
A novel approach to the synthesis of 1,2,3-triazoles and their SAR studies
New thiazolidinedione-5-acetic acid amide derivatives: synthesis, characterization and investigation of antimicrobial and cytotoxic properties
Synthesis, characterization and herbicidal activity of new thiazoline derivatives
Chemico-biological investigation of rhizome essential oil of Zingiber morannative to Northeast India
Beta-aminoketones as prodrugs for selective irreversible inhibitors of type-1 methionine aminopeptidases.
Discovery and structure-based optimization of adenain inhibitors.
Structure-based optimization of non-peptidic Cathepsin D inhibitors.
Analysis of subpocket selectivity and identification of potent selective inhibitors for matriptase and matriptase-2.
In vitro antiplasmodial and cytotoxic activities of asymmetrical pyridinium derivatives.
Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents.
Novel antiproliferative chimeric compounds with marked histone deacetylase inhibitory activity.
Repurposing the antihistamine terfenadine for antimicrobial activity against Staphylococcus aureus.
Benzophenone C- and O-glucosides from Cyclopia genistoides (Honeybush) inhibit mammalian -glucosidase.
Novel N-biphenyl-2-ylmethyl 2-methoxyphenylpiperazinylalkanamides as 5-HT7R antagonists for the treatment of depression.
Discovery of Potent and Simplified Piperidinone-Based Inhibitors of the MDM2-p53 Interaction.
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
Halogenated diarylacetylenes repress c-myc expression in cancer cells.
Optimization of Rutaecarpine as ABCA1 Up-Regulator for Treating Atherosclerosis.
Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors.
2-(4-Chlorobenzyl)-6-arylimidazo[2,1-b][1,3,4]thiadiazoles: synthesis, cytotoxic activity and mechanism of action.
Rhytidenones A-F, Spirobisnaphthalenes from Rhytidhysteron sp. AS21B, an Endophytic Fungus.
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
Pyrrolopyridines-quinazolines Inhibitors of PKR-Like ER Kinase.
Design, synthesis and evaluation of novel HDAC inhibitors as potential antitumor agents.
Synthesis and evaluation of 9-deoxy analogues of (-)-thysanone, an inhibitor of HRV 3C protease.
Pim kinase inhibitors for the treatment of cancer and possibly more.
Design and synthesis of 4-heteroaryl 1,2,3,4-tetrahydroisoquinolines as triple reuptake inhibitors.
Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Ligand-based virtual screening identifies a family of selective cannabinoid receptor 2 agonists.
Discovery of a series of aryl-N-(3-(alkylamino)-5-(trifluoromethyl)phenyl)benzamides as TRPA1 antagonists.
Phosphocalyculin C as a pyrophosphate protoxin of calyculin C in the marine sponge Discodermia calyx.
Discovery heralds new approach to the treatment of cystic fibrosis.
Inhibitors of Mutant IDH for the Treatment of Cancer.
Modulation of Activity Profiles for Largazole-Based HDAC Inhibitors through Alteration of Prodrug Properties.
Design, synthesis and evaluation of 2-aminothiazole derivatives as sphingosine kinase inhibitors.
Synthesis, screening and docking of small heterocycles as glycogen phosphorylase inhibitors.
Unambiguous Determination of the Absolute Configuration of Dimeric Stilbene Glucosides from the Rhizomes of Gnetum africanum.
Cytotoxic Spliceostatins from Burkholderia sp. and Their Semisynthetic Analogues.
Structure-based design of novel human Pin1 inhibitors (III): optimizing affinity beyond the phosphate recognition pocket.
Phorbaketals L-N, cytotoxic sesterterpenoids isolated from the marine sponge of the genus Phorbas.
Potent, orally available, selective COX-2 inhibitors based on 2-imidazoline core.
Fragment-based hit discovery and structure-based optimization of aminotriazoloquinazolines as novel Hsp90 inhibitors.
Identification of a New RXR Antagonist Targeting the Coregulator-Binding Site.
Inhibition of O-GlcNAcase (OGA): A Potential Therapeutic Target to Treat Alzheimer's Disease.
Discovery and Development of LX7101, a Dual LIM-Kinase and ROCK Inhibitor for the Treatment of Glaucoma.
Borrelidin B: isolation, biological activity, and implications for nitrile biosynthesis.
P21-Activated Kinase 4 (PAK4) Inhibitors as Potential Cancer Therapy.
Cytotoxic and Antibacterial Quinone Sesquiterpenes from a Myrothecium Fungus.
Ganoboninketals A-C, Antiplasmodial 3,4-seco-27-Norlanostane Triterpenes from Ganoderma boninense Pat.
Synthesis and evaluation of 4-anilinoquinazoline bioisosteres as potential anti-breast cancer agents.
Structure-Based Design of Type II Inhibitors Applied to Maternal Embryonic Leucine Zipper Kinase.
Acyclic tethers mimicking subunits of polysaccharide ligands: selectin antagonists.
Bioreductively Activated Reactive Oxygen Species (ROS) Generators as MRSA Inhibitors.
Design and synthesis of tamoxifen derivatives as a selective estrogen receptor down-regulator.
Preparation and evaluation of deconstruction analogues of 7-deoxykalafungin as AKT kinase inhibitors.
Discovery of Novel Putative Inhibitors of UDP-GlcNAc 2-Epimerase as Potent Antibacterial Agents.
Hydrogen sulfide donors in research and drug development
Synthesis of hetero annulated carbazoles: exploration of in vitro cytotoxicity and molecular docking studies
Structureactivity relationship studies of miniproteins targeting the androgen receptorcoactivator interaction
Synthesis and Antimicrobial Activities of His(2-aryl)-Arg and Trp-His(2-aryl) Classes of Dipeptidomimetics.
Development of CBAP-BPyne, a probe for -secretase and presenilinase.
Design and synthesis of a novel series of N,4-diphenylpyrimidin-2-amine derivatives as potent and selective PI3K inhibitors
Novel inhibitors of breast cancer relevant kinases Brk and HER2
Synthesis and in vitro pharmacological evaluation of indolyl carboxylic amide analogues as D3 dopamine receptor selective ligands.
4-Chlorocolchicine derivatives bearing a thiourea side chain at the C-7 position as potent anticancer agents
Crafting precise multivalent architectures
Development of new N-Arylbenzamides as STAT3 Dimerization Inhibitors.
Synthesis and biological evaluation of 2-acetamidothiophene-3-carboxamide derivatives against Leishmania donovani
Synthesis, Activity and Metabolic Stability of Non-Ribose Containing Inhibitors of Histone Methyltransferase DOT1L.
Phage display libraries of differently sized bicyclic peptides
Synthesis, structureactivity relationships and stereochemical investigations of new tricyclic pyridazinone derivatives as potential STAT3 inhibitors
A new class of fluorinated 5-pyrrolidinylsulfonyl isatin caspase inhibitors for PET imaging of apoptosis
Synthesis, Activity and Structure-Activity Relationship of Noroviral Protease Inhibitors.
Design and synthesis of a novel series of cyclohexyloxy-pyridyl derivatives as inhibitors of diacylglycerol acyl transferase 1
Investigating -secretase protein interactions in live cells using active site-directed clickable dual-photoaffinity probes
Construction of phenoxazine rings containing nitro and sulfonic acid groups leading to phenoxazine-3-sulfonamide derivatives: their evaluation as novel and potential insulin secretagogues
The effect of a thieno[2,3-b]pyridine PLC- inhibitor on the proliferation, morphology, migration and cell cycle of breast cancer cells
Repurposing human Aurora kinase inhibitors as leads for anti-protozoan drug discovery.
-Aminophosphonates as novel anti-leishmanial chemotypes: synthesis, biological evaluation, and CoMFA studies
Discovery of novel RIP derivatives by alanine scanning for the treatment of S. aureus infections
Flavans from Desmos cochinchinensis as potent aromatase inhibitors
Validation of host factors of HIV integration as novel drug targets for anti-HIV therapy
Design, synthesis and biological evaluation of TAR and cTAR binders as HIV-1 nucleocapsid inhibitors
Fragment growing to retain or alter the selectivity of anchored kinase hinge-binding fragments
4-Aminocyclopentane-1,3-diols as platforms for diversity: synthesis of a screening library
Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography
Transformation of a selective factor Xa inhibitor rivaroxaban into a dual factor Xa/thrombin inhibitor by modification of the morpholin-3-one moiety
Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones; potential imaging agents of the metabotropic glutamate 2 receptor
The advantage of biosensor analysis over enzyme inhibition studies for slow dissociating inhibitors characterization of hydroxamate-based matrix metalloproteinase-12 inhibitors
Design, synthesis and biochemical investigation, by in vitro luciferase reporter system, of peptide nucleic acids as new inhibitors of miR-509-3p involved in the regulation of cystic fibrosis disease-gene expression
Synthesis of amphiphilic, chalcogen-based redox modulators with in vitro cytotoxic activity against cancer cells, macrophages and microbes
Novel proteinprotein interaction inhibitor of Nrf2Keap1 discovered by structure-based virtual screening
Structureactivity relationships of tetrahydrocarbazole derivatives as antifungal lead compounds
Design, synthesis and biological evaluation of imidazo[1,5-a]pyridinePBD conjugates as potential DNA-directed alkylating agents
Design, synthesis and docking-based 3D-QSAR study of novel 2-substituted 2-aminopropane-1,3-diols as potent and selective agonists of sphingosine-1-phosphate 1 (S1P1) receptor
Biologically active binaphthol-scaffolded imidazolium salts
Identification of orally bioavailable small-molecule inhibitors of hematopoietic prostaglandin D2 synthase using X-ray fragment based drug discovery
Design, synthesis and biological evaluation of novel ligustrazinylated derivatives as potent cardiovascular agents
Synthesis and biological evaluation of new conformationally restricted S-DABO hybrids as non-nucleoside inhibitors of HIV-1 reverse transcriptase
Design, synthesis and evaluation of N6-substituted 2-aminoadenosine-5-N-methylcarboxamides as A3 adenosine receptor agonists
Cytotoxic, immunomodulatory, antimycotic, and antiviral activities of semisynthetic 14-hydroxyabietane derivatives and triptoquinone C-4 epimers
Polyhydroxylated pyrrolidine and 2-oxapyrrolizidine as glycosidase inhibitors
A new route towards fimbrolide analogues: importance of the exomethylene motif in LuxR dependent quorum sensing inhibition
Effect of the 4-substituted phenylalanine moiety of sansalvamide A peptide on antitumor activity
Mapping histamine H4receptorligand binding modes
Improved synthesis of 4-/6-substituted 2-carboxy-1H-indole-3-propionic acid derivatives and structureactivity relationships as GPR17 agonists
Exploring the effect of N-substitution in nor-lobelane on the interaction with VMAT2: discovery of a potential clinical candidate for treatment of methamphetamine abuse.
Novel FK506 and FK520 analogues via mutasynthesis: mutasynthon scope and product characteristics
Imidazolium salts as antifungal agents: activity against emerging yeast pathogens, without human leukocyte toxicity
Synthesis, functional and binding profile of (R)-apomorphine based homobivalent ligands targeting the dopamine D2 receptor
Novel sphingosine-containing analogues selectively inhibit sphingosine kinase (SK) isozymes, induce SK1 proteasomal degradation and reduce DNA synthesis in human pulmonary arterial smooth muscle cells.
Synthesis and biological evaluation of substituted N-alkylphenyl-3,5-dinitrobenzamide analogs as anti-TB agents
Ketorolac beats ketoprofen: lower photodecarboxylation, photohemolysis and phototoxicity
The development of thieno[2,3-b]pyridine analogues as anticancer agents applying in silico methods
Identification of novel inhibitors of p53MDM2 interaction facilitated by pharmacophore-based virtual screening combining molecular docking strategy
Meridianin G and its analogs as antimalarial agents
Azole derivatives as novel non-iron-chelating inhibitors of prolyl hydroxylase 3 for HIF-1 activation
An integrated approach to the discovery of potent agelastatin A analogues for brain tumors: chemical synthesis and biological, physicochemical and CNS pharmacokinetic analyses
Synthesis and biological evaluation of novel quinoxalinone-based HIV-1 reverse transcriptase inhibitors
Synthesis of new 13-diphenylalkyl analogues of berberine and elucidation of their base pair specificity and energetics of DNA binding
Dual mode of action of phenyl-pyrazole-phenyl (6-5-6 system)-based PPI inhibitors: alpha-helix backbone versus alpha-helix binding epitope
Chemical motifs that redox cycle and their associated toxicity
Exceptionally strong intermolecular association in hydrophobic DNA minor groove binders and their potential therapeutic consequences
The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface.
Novel benzofuranchromone and coumarin derivatives: synthesis and biological activity in K562 human leukemia cells
Development and evaluation of selective, reversible LSD1 inhibitors derived from fragments
Exploring novel strategies for AIDS protozoal pathogens: -helix mimetics targeting a key allosteric protein-protein interaction in C. hominis TS-DHFR.
Synthesis and biological evaluation of tetrahydropyridinepyrazoles (PFPs) as inhibitors of STAT3 phosphorylation
Design, synthesis and activities of 4/5-acyl-2-aminoimidazolyl analogues of oroidin for biofilm inhibition
Introduction of methionine mimics on 3-arylthiophene: influence on protein farnesyltransferase inhibition and on antiparasitic activity
Synthesis and antibacterial evaluation of anziaic acid and analogues as topoisomerase I inhibitors.
Heterocycle-fused lupane triterpenoids inhibit Leishmania donovani amastigotes
2-Hydroxy-substituted cinnamic acids and acetanilides are selective growth inhibitors of Mycobacterium tuberculosis
Dinaphthonaphthyridines a class of novel molecules with potent antioxidant and anticancer activity
Optimisation of biphenyl acetic acid inhibitors of diacylglycerol acetyl transferase 1 the discovery of AZD2353
Novel 1-(1-benzyl-1H-indol-3-yl)-N,N,N-trimethylmethanaminium iodides are competitive antagonists for the human 42 and 7 nicotinic acetylcholine receptors
Novel radioiodinated 1,3,4-oxadiazole derivatives with improved in vivo properties for SPECT imaging of -amyloid plaques
Discovery of novel pyridazinylthioacetamides as potent HIV-1 NNRTIs using a structure-based bioisosterism approach
Preparation of phenylethylbenzamide derivatives as modulators of DNMT3 activity
Investigation of a tetrahydroisoquinoline scaffold as dual-action steroid sulfatase inhibitors generated by parallel solid-phase synthesis
Quinazoline and tetrahydropyridothieno[2,3-d]pyrimidine derivatives as irreversible EGFR tyrosine kinase inhibitors: influence of the position 4 substituent
In vitro anticancer activity and SAR studies of triazolyl aminoacyl(peptidyl) penicillins
Optimization of triazole-based TGR5 agonists towards orally available agents
Discovery of a Potent Anti-tumor Agent through Regioselective Mono-N-acylation of 7H-Pyrrolo[3,2-f]quinazoline-1,3-diamine.
Hedgehog signalling pathway inhibitors as cancer suppressing agents
Design of Potential Bisubstrate Inhibitors against Mycobacterium tuberculosis (Mtb) 1-Deoxy-D-Xylulose 5-Phosphate Reductoisomerase (Dxr)-Evidence of a Novel Binding Mode.
3,4,2-Trimethoxy-trans-stilbene a potent CYP1B1 inhibitor
Synthesis and biological activity of NOSH-naproxen (AVT-219) and NOSH-sulindac (AVT-18A) as potent anti-inflammatory agents with chemotherapeutic potential.
Biological evaluation and molecular modelling of didanosine derivatives
Structure-based drug design of chromone antagonists of the adenosine A2A receptor
VUT-MK142 : a new cardiomyogenic small molecule promoting the differentiation of pre-cardiac mesoderm into cardiomyocytes.
Synthesis of chromenoindole derivatives from Robinia pseudoacacia
Discovery of BET bromodomain inhibitors and their role in target validation
Multitarget-directed resveratrol derivatives: anti-cholinesterases, anti--amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease
Synthesis and biological evaluation of coumarin1,2,3-triazoledithiocarbamate hybrids as potent LSD1 inhibitors
Synthesis of metergoline analogues and their evaluation as antiplasmodial agents
Discovery of novel inhibitors for human farnesyltransferase (hFTase) via structure-based virtual screening
Acyl protein thioesterase inhibitors as probes of dynamic S-palmitoylation.
Design and discovery of 4-anilinoquinazoline ureas as multikinase inhibitors targeting BRAF, VEGFR-2 and EGFR
Synthesis, anticancer evaluation and docking study of vadimezan derivatives with carboxyl substitution
Pseudopeptides with a centrally positioned alkene-based disulphide bridge mimetic stimulate kallikrein-related peptidase 3 activity
Glycosidase inhibition by novel guanidinium and urea iminosugar derivatives
Bioactive prenylated phenyl derivatives derived from marine natural products: novel scaffolds for the design of BACE inhibitors
5-Nor carbocyclic nucleosides: unusual nonnucleoside inhibitors of HIV-1 reverse transcriptase
Achieving improved permeability by hydrogen bond donor modulation in a series of MGAT2 inhibitors
More than just a GPCR ligand: structure-based discovery of thioridazine derivatives as Pim-1 kinase inhibitors
Facile synthesis of a polyether-tethered dimeric berberine as a highly effective DNA-cleaving agent in the presence of Cu(ii) ion
Synthesis and anticancer activity evaluation of resveratrolchalcone conjugates
Synthesis and antiviral evaluation of 4-(1,2,3-triazol-1-yl)thymidines
Novel pyrazolo[1,5-a]pyridines as PI3K inhibitors: variation of the central linker group
Design, synthesis and biological evaluation of novel indano- and thiaindano-pyrazoles with potential interest for Alzheimer's disease
6-Alkyl-, 6-aryl- or 6-hetaryl-7-deazapurine ribonucleosides as inhibitors of human or MTB adenosine kinase and potential antimycobacterial agents
Synthesis and biological evaluation of a post-synthetically modified Trp-based diketopiperazine
The A-CD analogue of 16,17-estriol is a potent and highly selective estrogen receptor agonist
Developing novel C-4 analogues of pyrrole-based antitubulin agents: weak but critical hydrogen bonding in the colchicine site.
Design, synthesis, and biological activity of novel 4-(3,4-dimethoxyphenyl)-2-methylthiazole-5-carboxylic acid derivatives.
Synthesis and leishmanicidal activity of quinolinetriclosan and quinolineeugenol hybrids
Synthesis, molecular docking study, and anticancer activity of triaryl-1,2,4-oxadiazole
Quinolinedione nucleus as a novel scaffold for A1 and A2A adenosine receptor antagonists
Anti-HIV, antimycobacterial and antimicrobial studies of newly synthesized 1,2,4-triazole clubbed benzothiazoles
Synthesis and antimicrobial activity of 5-chloroindoline-2,3-dione derivatives
Expression of OPN in rat kidney with different doses of vitamin K3 injection
Metabolites of the fungistatic agent 2-methoxyclovan-9-ol by Macrophomina phaseolina.
Synthesis of some novel 3,5-disubstituted 1,3,4-oxadiazole derivatives and anticancer activity on EAC animal model
Design, synthesis, and biological activity of certain quinazolinedione derivatives as potent phosphodiestrase4 inhibitors
Anti-inflammatory effects of two new methyl and morpholine derivatives of diphenhydramine on rats
New N-arylamino biquinoline derivatives: microwave-assisted synthesis and their antimicrobial activities
Synthesis and microbial evaluation of novel N(1)-Arilidene-N(2)-t(3)-methyl-r(2),c(6)-diaryl-piperidin-4-one azine derivatives
Synthesis and cytotoxicity of novel 6H-indolo[2,3-b]quinoxaline derivatives
SnO2 nanoparticles mediated nontraditional synthesis of biologically active 9-chloro-6,13-dihydro-7-phenyl-5H-indolo [3,2-c]-acridine derivatives
Synthesis and antibacterial activity of novel 7-haloanilino-8-nitrofluoroquinolone derivatives
3D-QSAR CoMFA and CoMSIA studies on a set of diverse 1a-adrenergic receptor antagonists
Synthesis and theoretic calculations of benzoxazoles and docking studies of their interactions with triosephosphate isomerase
Comprehensive two and three-dimensional QSAR studies of 3-substituted 6-butyl-1,2dihydropyridin-2-ones derivatives as angiotensin II receptor antagonists
Synthesis of imidazole-derived steroidal hybrids as potent aromatase inhibitors
Control of Rice Blast Disease by Submerged Treatment with SSF-126
Synthesis, characterization and antimicrobial evaluation of novel derivatives of isoniazid
Synthesis and evaluation of p-N,N-dialkyl substituted chalcones as anti-cancer agents
Synthesis, characterization and in vitro cytotoxic properties of some new Schiff and Mannich bases in Hep G2 cells
In-silico design, synthesis and evaluation of novel DNA-gyrase B inhibitors
A study on the reactions of alkyl 4,6-bis(4-fluorophenyl)-2-oxocyclohex-3-ene-1-carboxylate and in vitro antioxidant activity of derivatives
Mechanism of the Phytotoxic Action of Herbicidal N-Isobutyl-N-(4-substituted benzyl)-4-halo-2-pentenamides
Synthesis and antimicrobial activities of 2-azetidinyl-4-quinazolinone derivatives of diclofenac analogue
Effect of doses of fungicides and plant resistance activators on the control of Rhizoctonia foliar blight of soybean, and on Rhizoctonia solani AG1-IA in vitro development
Predicting anti-HIV activity of 1,1,3-trioxo[1,2,4]-thiadiazine (TTD) derivatives: 3D QSAR approach
CoMFA AND CoMSIA STUDIES ON A SET OF BENZYL PIPERAZINES, PIPERADINES, PYRAZINOPYRIDOINDOLES, PYRAZINOISOQUINOLINES AND SEMI RIGID ANALOGS OF DIPHENHYDRAMINE
Synthesis and QSAR analysis of chalcone derivatives as nitric oxide inhibitory agent
Effect of tropine derivatives, antimuscarinic agents, on the growth of Bombyx mori larvae.
Synthesis and anti-congestive heart failure activity of novel levosimendan analogues
Synthesis and Biological Activity of 1,2-Dithiolanes and 1,2-Dithianes Bearing a Nitrogen-containing Substituent
Antibacterial and antifungal activities of some trimethoprim salts
Synthesis and antihyperlipidemic efficiency of berberine-based HMG-CoA reductase inhibitor
Synthesis and herbicidal activity of diphenyl ether derivatives containing unsaturated carboxylates.
A new isoflavone from Blepharis ciliaris of an Egyptian origin
Comparison between antioxidant activity of 2,5-disubstituted 1,3,4-oxadiazoles containing heteroaromatic ring and aromatic ring at 2nd position
A Method for Monitoring the Sensitivity of Botrytis cinerea to Mepanipyrim
Screening and evaluation of thiourea derivatives for their HIV capsid and human cyclophilin A inhibitory activity
Synthesis and insecticidal activity of 1,2,4-oxadiazole and 1,2,4-thiadiazole derivatives
Evaluation of fungicides and sterilants for potential application in the management of Fusarium wilt of banana
Synthesis and phytotoxic activity of novel acylthiourea and 2H-1,2,4-thiadiazolo[2,3-]pyrimidine derivatives
Modification and biological evaluation of novel 4-hydroxy-pyrone derivatives as non-peptidic HIV-1 protease inhibitors
QSAR and pharmacophore analysis of thiosemicarbazone derivatives as ribonucleotide reductase inhibitors
Synthesis of 1-(4-((E)-3-arylacryloyl) phenyl)-3,4-dibromo-1H-pyrrole-2,5-diones and screening for anti-Candida and antituberculosis activity
Coumarinyl pyrazole derivatives of INH: promising antimycobacterial agents
Design and synthesis of new N-substituted amino methyl-[1,2,3] triazolyl moieties of fluoroquinolones as antibacterial agents
Molecular bases for resistance to acetyl-coenzyme A carboxylase inhibitor in Japanese foxtail (Alopecurus japonicus).
QSAR for Binding Affinity of Substituted Dibenzoylhydrazines to Intact Sf-9 Cells
Design and synthesis of niflumic acid-based N-acylhydrazone derivatives as novel anti-inflammatory and analgesic agents
Synthesis and Herbicidal Activity of New Oxazolidinedione Derivatives
Synthesis and pharmacological evaluation of N-(6-chlorobenzo[d]thiazol-2-yl)hydrazine carboxamide derivatives of benzothiazole
Apteniols AF, oxyneolignans from the leaves of Aptenia cordifolia
Design and synthesis of thienopyridines as novel templates for acetylcholinesterase inhibitors
Susceptibility of field populations of Spodoptera litura (Fabricius) (Lepidoptera: Noctuidae) in China to chlorantraniliprole and the activities of detoxification enzymes
Synthesis and antiviral activity of benzimidazolyl- and triazolyl-1,3,5-triazines
Iodine (III)-mediated synthesis of some 2-aryl/hetarylbenzoxazoles as antibacterial/antifungal agents
Evaluation of antidepressant-like effect of 2-pyrazoline derivatives
Benzo[d][1,3] oxathiols: synthesis and biological evaluation as potential atypical antipsychotic agents
5-Aryl-1,3,4-oxadiazole-2-thiols as a New Series of trans-Cinnamate 4-Hydroxylase Inhibitors
Preparation and phytotoxicity of novel kaurane diterpene amides with potential use as herbicides.
Design, synthesis, antimicrobial, anticancer evaluation, and QSAR studies of 4-(substituted benzylidene-amino)-1,5-dimethyl-2-phenyl-1,2-dihydropyrazol-3-ones
Partition coefficient determination of a series of isoindolines-2-substituted and its correlation with their antiproliferative activity on HeLa cells
Cross resistance, genetic analysis and stability of resistance to buprofezin in cotton whitefly, Bemisia tabaci (Homoptera: Aleyrodidae)
Computational and experimental evaluation of ornithine derivatives as ornithine decarboxylase inhibitors
Mutations in the mitochondrial cytochrome b of Tetranychus urticae Koch (Acari: Tetranychidae) confer cross-resistance between bifenazate and acequinocyl.
Synthesis and Herbicidal Activity of 1-Arylalkyl-3-pyrrolin-2-one Derivatives
Synthesis and biological evaluation of resveratrolcoumarin hybrid compounds as potential antitumor agents
Quantitative Structure-Activity Relationships of Herbicidal N-Alkyl-N-(4-substituted benzyl)-4-chloro-2-pentenamides against Echinochloa oryzicola
Assessment of antithyroid activity of 2,8-disulfanyl-1,9-dihydro-6H-purin-6-one in vitro and in vivo
Synthesis and antimicrobial evaluation of 4,5-diaryl-2-[4-(t-amino)-2-butynyl]-2,4-dihydro-3H-1,2,4-triazol-3-ones
Synthesis and antimicrobial activity of 7-alkoxyhesperetin derivatives
Neoclerodane diterpenoids from Teucrium polium subsp. polium and their antifeedant activity
Synthesis of new N-arylamino(2-furyl)methylphosphonic acid diesters, and in vitro evaluation of their cytotoxicity against esophageal cancer cells
Synthesis of some 3,4-disubstituted-6,7-dihydro-imidazo[2,1-b][1,3]thiazole and 3,4-disubstituted-7,8-dihydro-6H-imidazo[2,1-b][1,3]thiazine derivatives and evaluation of their cytotoxicities against F2408 and 5RP7 cells
Insecticidal Activities of the Enantiomers of Asymmetric 1-[1-(6-Chloro-3-pyridyl)ethyl]-2-nitroiminoimidazolidine against American Cockroach, Cucurbit Leaf Beetle, Green Rice Leafhopper and Green Peach Aphid Following Injection, Dipping and Spraying
Synthesis of potential antitubercular and antimicrobial s-triazine-based scaffolds via Suzuki cross-coupling reaction
Design, synthesis and evaluation of aminobenzophenone derivatives containing nitrogen mustard moiety as potential central nervous system antitumor agent
Cross-resistance relationships between neonicotinoids and pymetrozine in Bemisia tabaci (Hemiptera: Aleyrodidae).
A facile synthesis of some 3-cyano-1,4,6-trisubstituted-2(1H)-pyridinones and their biological evaluation as anticancer agents
Synthesis of new cyclic imides derivatives with potential hypolipidemic activity
Synthesis and biological evaluation of some new Thiazolo[3,2-a][1,3,5]triazine derivatives
Docking, synthesis, and pharmacological investigation of novel substituted thiazole derivatives as non-carboxylic, anti-inflammatory, and analgesic agents
Synthesis and biological evaluation of gallic acid analogs
Synthesis and Insecticidal Activity of New 2- and 6-Substituted 4-Acetoxyquinolines
Synthesis, structure, anticancer, and antioxidant activity of para-xylyl linked bis-benzimidazolium salts and respective dinuclear Ag(I) N-heterocyclic carbene complexes (Part-II)
Docking and CoMFA study on novel human CCR5 receptor antagonists
Synthesis and biological evaluation of anti-inflammatory activity of 1,3 diphenyl propenone derivatives
Quantitative Structure-Activity Relationships of Larvicidal N-[5-(Substituted phenyl)-1, 3, 4-thiadiazol-2-yl]-benzamides in the Inhibition of N-Acetylglucosamine Incorporation into a Cultured Integument System
2,4,6-Trihydroxybenzaldehyde as a potent antidiabetic agent alleviates postprandial hyperglycemia in normal and diabetic rats
Antifeedant activity of neo-clerodane diterpenoids from Teucrium arduini
Identification of ZINC02765569: a potent inhibitor of PTP1B by vHTS
Challenges in docking 2-hydroxy and 2,4-dihydroxychalcones into the binding site of ALR2
MMV Malaria Box anti-babesial screening.
MMV Malaria Box screening against Plasmodium falciparum Deoxyhypusine hydroxylase
MMV Malaria Box HIV and cytotoxicity screening.
MMV Malaria Box screening against the the NCI60 panel of human tumor cell lines.
Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
Discovery of novel 2-[2-(3-hydroxy-pyridin-2-yl)-thiazol-4-yl]-acetamide derivatives as HIF prolyl 4-hydroxylase inhibitors; SAR, synthesis and modeling evaluation.
Amine-linked diquercitols as new -glucosidase inhibitors.
Isolation and total syntheses of cytotoxic cryptolactones A1, A2, B1, and B2: ,-unsaturated -lactones from a Cryptomyzus sp. aphid.
Structure-activity relationship studies of antiplasmodial aminomethylthiazoles.
Synthesis and evaluation of benzimidazole carbamates bearing indole moieties for antiproliferative and antitubulin activities.
Oxidized derivatives of macroline, sarpagine, and pleiocarpamine alkaloids from Alstonia angustifolia.
Polyyne hybrid compounds from Notopterygium incisum with peroxisome proliferator-activated receptor gamma agonistic effects.
Design and synthesis of azaisoflavone analogs as phytoestrogen mimetics.
Synthesis of novel 10-hydroxycamptothecin derivatives utilizing topotecan hydrochloride as ortho-quinonemethide precursor.
Design, synthesis and biological evaluation of (E)-3-(3,4-dihydroxyphenyl)acrylylpiperazine derivatives as a new class of tubulin polymerization inhibitors.
New N-aryl-N'-(3-(substituted)phenyl)-N'-methylguanidines as leads to potential PET radioligands for imaging the open NMDA receptor.
Potent bisimidazole-based HCV NS5A inhibitors bearing annulated tricyclic motifs.
Discovery of Spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as Potent NOP and Opioid Receptor Agonists.
Tailor-made fluorescent trilobolide to study its biological relevance.
The design and implementation of a generic lipopeptide scanning platform to enable the identification of 'locally acting' agonists for the apelin receptor.
Antimalarial activity of abietane ferruginol analogues possessing a phthalimide group.
Synthesis and Structure-Activity Relationship Study of 5a-Carbasugar Analogues of SL0101.
Design and synthesis of novel azapeptide activators of apoptosis mediated by caspase-9 in cancer cells.
Exploring in vitro and in vivo Hsp90 inhibitors activity against human protozoan parasites.
Development of first lead structures for phosphoinositide 3-kinase-C2 inhibitors.
Neuroprotective Xanthones from the Root Bark of Cudrania tricuspidata.
Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.
Synthesis and antitumor activity of feruloyl and caffeoyl derivatives.
Progress in the discovery and development of heat shock protein 90 (Hsp90) inhibitors.
Structural evidence of N6-isopentenyladenosine as a new ligand of farnesyl pyrophosphate synthase.
Eurifoloids A-R, structurally diverse diterpenoids from Euphorbia neriifolia.
Modulators of GPR40 as Treatment for Diabetes.
Structure-Based Drug Design of Novel, Potent, and Selective Azabenzimidazoles (ABI) as ATR Inhibitors.
Novel FTY720-Based Compounds Stimulate Neurotrophin Expression and Phosphatase Activity in Dopaminergic Cells.
Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.
Discovery of covalent inhibitors of glyceraldehyde-3-phosphate dehydrogenase, a target for the treatment of malaria.
Recent progress in the identification of BRAF inhibitors as anti-cancer agents.
Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new ROR inhibitors using virtual screening, synthesis and biological evaluation.
A,D-seco-limonoids from the stems of Clausena emarginata.
Arabinose 5-phosphate isomerase as a target for antibacterial design: studies with substrate analogues and inhibitors.
Diamidine compounds for selective inhibition of protein arginine methyltransferase 1.
Design, synthesis and molecular modeling of pyrazole-quinoline-pyridine hybrids as a new class of antimicrobial and anticancer agents.
Structure-activity relationships for withanolides as inducers of the cellular heat-shock response.
Synthesis and evaluation of carbon-linked analogs of dual orexin receptor antagonist filorexant.
Design and synthesis of silicon-containing steroid sulfatase inhibitors possessing pro-estrogen antagonistic character.
Design and synthesis of conformationally restricted inhibitors of active thrombin activatable fibrinolysis inhibitor (TAFIa).
Emergence of pyrido quinoxalines as new family of antimalarial agents.
Therapeutic utility of cannabinoid receptor type 2 (CB(2)) selective agonists.
5,10-seco-neo-clerodanes and neo-clerodanes from Salvia microphylla.
Discovery of 4-anilino -carbolines as novel Brk inhibitors.
Synthesis of potent inhibitors of histidinol dehydrogenase
Acid promoted intramolecular formation of 3,5-anhydro-1,4-furano-7-ulose derivatives via the Wittig-cyclization procedure and their antimicrobial properties
Promising antitumor effect of alpha-tocopheryl succinate in human colon and liver cancer cells
Synthesis and antitumor activity of novel 4-aminoquinoline derivatives
Molecular docking and 3D QSAR studies of substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as insulin-like growth factor-1 receptor (IGF1R) inhibitors
Dimeric 2-(2-chlorophenyl)-quinazolin-4-ones as potential antimicrobial agents
Relation between Penetration Rates of Pesticides and Partition Coefficients in Topical Application to Spodoptera litura
Insights into the molecular mechanism of tolerance to carboxylic acid amide (CAA) fungicides in Pythium aphanidermatum.
Synthesis, spectral studies, antimicrobial and insect antifeedant potent keto oxiranes
Protective effect of Centaurea pallescens Del. against CCl4-induced injury on a human hepatoma cell line (Huh7)
Synthesis of new 4-(2,5-dimethylpyrrol-1-yl)/4-pyrrol-1-yl benzoic acid hydrazide analogs and some derived oxadiazole, triazole and pyrrole ring systems: a novel class of potential antibacterial, antifungal and antitubercular agents
Synthesis of a new series of 2-(2-oxo-2H-chromen-3-yl)-5H-chromeno[4,3-b]pyridin-5-ones by two facile methods and evaluation of their antimicrobial activity
6-Imino-2-thioxo-pyrimidinones as a new class of dipeptidyl peptidase IV inhibitors
Synthesis, antimicrobial, analgesic activity, and molecular docking studies of novel 1-(5,7-dichloro-1,3-benzoxazol-2-yl)-3-phenyl-1H-pyrazole-4-carbaldehyde derivatives
Synthesis and immunostimulating activity of C-pseudonucleosides containing N-phenyl thiazolidin-4-one
Repellent, insecticidal and phytotoxic activities of isoalantolactone from Inula racemosa
Synthesis, biological evaluation and QSAR study of a series of substituted quinazolines as antimicrobial agents
Synthesis, antimicrobial, antioxidant, anti-inflammatory, and analgesic activities of some new 3-(2-thienyl)pyrazole-based heterocycles
Characterization of sensitivity of Rhizoctonia solani, causing rice sheath blight, to mepronil and boscalid
Inhibitive Effect of Prodigiosin on the Proliferation of Human Malignant Pancreatic Cancer Cells
Bioactive saponin from tea seed pomace with inhibitory effects against Rhizoctonia solani.
Compounds against inflammation and oxidative insult as potential agents for neurodegenerative disorders
Effects of Enantiomerism on Fungicidal and Insecticidal Activities of (-Methoxybenzyl)isoxazoles
Novel glycol benzyl ether herbicides: Herbicidal activity of 3,3a,5,9b-tetrahydro-2H-furo[3,2-c][2]benzopyran derivatives
Synthesis and evaluation in vitro of 1-[2-(10-dihydroartemisininoxy) ethyl]-3-phenylurea derivatives as potential agents against cancer
Synthesis of new bicyclo[4.1.0]heptane-2,4-dione derivatives and their herbicidal activity
Synthesis and biological evaluation of novel pyrimidine-2(1H)-ones/thiones as potent anti-inflammatory and anticancer agents
Diversity and antifeedant activity of diterpenes from Turkish species of Sideritis.
Substituted urea/thiourea derived from fluoxetine as potent appetite suppressants
Synthesis, pharmacological evaluation and molecular docking studies of indanone derivatives
Synthesis and anticonvulsant activity of 4-(2-phenoxyphenyl)semicarbazones
Synthesis and pharmacological evaluation of some new naphthol derived aryloxy derivatives as cognition enhancers
In vitro biological activities of new heterocyclic chalcone derivatives
The application of comparative molecular field analysis for the design of -anilino substituted-3-phenyl propanoic acids as novel PPAR/ dual ligands
Lethal and Antifeedant Substance from Rhizome of Alpinia galanga SW. (Zingiberaceae)
A useful new insecticide bioassay using first-instar larvae of a net-spinning caddisfly, Cheumatopsyche brevilineata (Trichoptera: Hydropsychidae)
Synthesis and evaluation of 2-amino-5-sulfanyl-1,3,4-thiadiazoles as antidepressant, anxiolytic, and anticonvulsant agents
Synthesis and evaluation of thiopyrano[3,4-c]quinoline-9-carboxamide derivatives as inhibitors of poly(ADP-ribose) polymerase-1 (PARP-1)
Synthesis, antifungal activity and SAR of N-substituted and N,N-disubstituted 2,4-dihydroxythiobenzamides
Efficient synthesis of piperazine-2,6-dione and 4-(1H-indole-2-carbonyl)piperazine-2,6-dione derivatives and their evaluation for anticancer activity
Synthesis of spirothiohydantoin analogues of hydantocidin
Anti-inflammatory and antioxidant activities of some extracts and pure natural products isolated from Rhus tripartitum (Ucria)
Synthesis and Fungicidal Activities of 2-Alkoxyiminoacetamides with a 4, 5-Dihydroisoxazole Ring
Synthesis and antifungal activity of cinnamic acid esters.
Synthesis and anticonvulsant evaluation of 3-substituted-4-(4-hexyloxyphenyl)-4H-1,2,4-triazoles
3D-QSAR CoMFA and CoMSIA studies for design of potent human steroid 5-reductase inhibitors
Synthesis and herbicidal potential of substituted aurones.
Design, synthesis and in vitro PDE4 inhibition activity of certain quinazolinone derivatives for treatment of asthma
Antifeedant Activity Evaluation of Withanolides from Jaborosa integrifolia
Sesquiterpene lactones: antispasmodic principles of the freshwater algae Hydrodictyon reticulatum
Response of sweet maize (Zea mays L.) hybrids to halosulfuron
Synthesis, antibacterial and antifungal activity of some novel 3-[5-(4-substituted phenyl) 1,3,4-thiadiazole-2-yl]-2-styryl quinazoline-4(3H)-ones
Translocation and distribution of 32P labelled potassium phosphonate in black pepper (Piper nigrum L)
Synthesis of benzo[b][1,4]oxazin-3(4H)-ones via smiles rearrangement for antimicrobial activity
Efficient entry to diversely functionalized spirooxindoles from isatin and their biological activity
Inhibitory Activity of Indanofan and Its Enantiomers on Biosynthesis of Very-Long-Chain Fatty Acids
Isolation, characterization, antibacterial, antihelminthic, and in silico studies of polyprenol from Kirganelia reticulata Baill
Synthesis, evaluation of antimicrobial activity, and molecular modeling of novel 2-((4-(2H-benzo[d] [1,2,3] triazol-2-yl)piperidin-1-yl)methyl)-5-substituted phenyl-1,3,4-oxadiazoles
Synthesis of curcumin and ethylcurcumin bioconjugates as potential antitumor agents
Induction of Phytoalexin Formation in Suspension-cultured Rice Cells byN-Acetyl-chitooligosaccharides
3D QSAR STUDIES OF INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN (CETP) BY CoMFA, CoMSIA AND GFA METHODOLOGIES
Design and synthesis of 3-[3-(substituted phenyl)-4-piperidin-1-ylmethyl/-4-morpholin-4-ylmethyl-4,5-dihydro-isoxazol-5-yl]-1H-indoles as potent anti-inflammatory agents
Tolerance of two Bifora radians Bieb populations to ALS inhibitors in winter wheat.
Toxicity of imidacloprid to developmental stages of Rhynchophorus ferrugineus (Curculionidae: Coleoptera): Laboratory and field tests
EBHU18, a novel derivative of fatty acid bile acid conjugates, prevents cholesterol gallstone formation in experimental mice
Preparation and activity study of new organophosphate insecticide candidates
Synthesis of 1-amidoalkyl-2-naphthols and oxazine derivatives with study of their antibacterial and antiviral activities
Nitrogen Analogues of Aldrin as Noncompetitive Antagonists of GABAA Receptor
The simple synthesis and antimicrobial activity of novel fluoroquinolone derivatives from natural amino acid salts
Design and synthesis of new 1,2-diaryl-4,5,6,7-tetrahydro-1H-benzo[d] imidazoles as selective cyclooxygenase (COX-2) inhibitors
4-Fluorophenylhydrazones as potential COX-2 inhibitors: a novel, efficient, one pot solid phase synthesis, docking study and pharmacological evaluation
Azoxystrobin resistance of French Mycosphaerella graminicola strains assessed by four in vitro bioassays and by screening of G143A substitution
Effect of isoxaflutole on the growth, nodulation and nitrogen fixation of chickpea (Cicer arietinum L.)
Synthesis and in vitro antimicrobial activity of some newer quinazolinonesulfonamide linked hybrid heterocyclic entities derived from glycine
Metabolic effects of benzylidene thiazolidinedione derivatives in high-fat fed mice
Study of binding of pyridoacridine alkaloids on topoisomerase II using in silico tools
The effects of luteolin on phenoloxidase and the growth of Spodoptera exigua (Hubner) larvae (Lepidoptera: Noctuidae)
Fungicidal Activities of -Methoxyphenylacetic Acid Derivatives
Fungicidal properties of the essential oil of Hesperozygis marifolia on Aspergillus flavus link.
Quantitative structure activity relationship (QSAR) studies of a series of 2,5-disubstituted-1,3,4-oxadiazole derivatives as biologically potential compounds
Development of a New Herbicide, Indanofan
Synthesis and metal ion binding activity of methyl 12-amino-13-nitro-7-oxo dehydrodeisopropylabietate derivatives
Design, synthesis, and biological evaluation of sulfonic acid ester and benzenesulfonamide derivatives as potential CETP inhibitors
A study on the genotoxic activities of some new benzoxazoles
Antifungal constituents from the seeds of Allium fistulosum L.
Discovery of a series of novel compounds with moderate anti-avian H5N1 influenza virus activity in chick embryo
Insecticidal and repellent action of allyl esters against Acyrthosiphon pisum (Hemiptera: Aphididae) and Tribolium castaneum (Coleoptera: Tenebrionidae)
Synthesis of new compounds derived from metronidazole and amino acids and their esters as antiparasitic agents
Synthesis and evaluation of 1-benzhydryl-sulfonyl-piperazine derivatives as inhibitors of MDA-MB-231 human breast cancer cell proliferation
Synthesis of phenoxyphenyl pyridine and pyrazine carboxamides. Activity against Cydia pomonella (L.) eggs.
Synthesis and antimicrobial screening of novel series of imidazo-[1,2-a]pyridine derivatives
Synthesis and biologic evaluation of new 3-phenoxyazetidin-2-one derivatives as selective cyclooxygenase-2 inhibitors
A quantitative structure-activity relationship study of anti-HIV activity of substituted HEPT using nonlinear models.
Synthesis, cytotoxicity, and molecular properties prediction of novel 1,3-diarylpyrazole derivatives
Synthesis and Fungicidal Activity of New Thiophosphorylated Monoterpenoids and Related Compounds
Synthesis and Acaricidal Activity of N-(1,3,4-Thiadiazol-2-yl)pyrazole-5-carboxamides and N-(1,3,4-Thiadiazol-2-yl)thiazole-5-carboxamides
Synthesis and Herbicidal Activity of Sulfonylureas with Fused Heterocyclic Moiety
PCR-RFLP detection of the E198A mutation conferring resistance to benzimidazoles in field isolates of Monilinia laxa from Greece
Xenortide Biosynthesis by Entomopathogenic Xenorhabdus nematophila.
Inhibitory activities of propolis and its promising component, caffeic acid phenethyl ester, against amyloidogenesis of human transthyretin.
Discovery of 4-aminoquinazoline--urea derivatives as Aurora kinase inhibitors with antiproliferative activity.
Limonoids from the Leaves and Twigs of Walsura yunnanensis.
Rupestonic acids B-G, NO inhibitory sesquiterpenoids from Artemisia rupestris.
Spongiapyridine and related spongians isolated from an Indonesian Spongia sp.
Synthesis and biological evaluations of new analogs of 2-methoxyestradiol: inhibitors of tubulin and angiogenesis.
Nostosins, Trypsin Inhibitors Isolated from the Terrestrial Cyanobacterium Nostoc sp. Strain FSN.
Design and synthesis of lactam-thiophene carboxylic acids as potent hepatitis C virus polymerase inhibitors.
Synthesis and Biological Evaluation of Pyrazolo[1,5-a]pyrimidine Compounds as Potent and Selective Pim-1 Inhibitors.
Lithocarpic Acids A-N, 3,4-seco-Cycloartane Derivatives from the Cupules of Lithocarpus polystachyus.
Differential modes of peptide binding onto replicative sliding clamps from various bacterial origins.
Quinalozinones as Inhibitors of Class I PI3K Kinases.
A comprehensive review on synthetic approach for antimalarial agents.
Indoleamine 2,3-dioxygenase inhibitors: potential treatment for cancer, sepsis, and more.
Synthesis and SAR of thieno[3,2-b]pyridinyl urea derivatives as urotensin-II receptor antagonists.
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
Carbonic Anhydrase Inhibition with Benzenesulfonamides and Tetrafluorobenzenesulfonamides Obtained via Click Chemistry.
Chemical constituents isolated from Disporum viridescens leaves and their inhibitory effect on nitric oxide production in BV2 microglial cells.
Discovery of a Type III Inhibitor of LIM Kinase 2 That Binds in a DFG-Out Conformation.
-Agarofurans and Sesquiterpene Pyridine Alkaloids from Maytenus spinosa.
'Click' assembly of glycoclusters and discovery of a trehalose analogue that retards A40 aggregation and inhibits A40-induced neurotoxicity.
Synthesis and Pharmacological Evaluation of DHE Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists.
Azapropellanes with anti-influenza a virus activity.
Small Molecule that Reverses Dexamethasone Resistance in T-cell Acute Lymphoblastic Leukemia (T-ALL).
Bioactive triterpenoid saponins and phenolic compounds against glioma cells.
Trichormamides A and B with Antiproliferative Activity from the Cultured Freshwater Cyanobacterium Trichormus sp. UIC 10339.
Griseorhodins D-F, neuroactive intermediates and end products of post-PKS tailoring modification in Griseorhodin biosynthesis.
Synthesis and biological evaluation of novel thiadiazole amides as potent Cdc25B and PTP1B inhibitors.
Confronting the challenges of discovery of novel antibacterial agents.
Antiprotozoal activity of 8-acyl and 8-alkyl incomptine A analogs.
Class II but Not Second Class-Prospects for the Development of Class II PI3K Inhibitors.
Multiple fragment docking and linking in primary and secondary pockets of dopamine receptors.
Design, synthesis and SAR exploration of tri-substituted 1,2,4-triazoles as inhibitors of the annexin A2-S100A10 protein interaction.
Alkylidene Oxapenem -Lactamase Inhibitors Revisited: Potent Broad Spectrum Activity but New Stability Challenges.
Inhibition of activated STAT5 in Bcr/Abl expressing leukemia cells with new pimozide derivatives.
Phytochemical analysis and antileukemic activity of polyphenolic constituents of Toona sinensis.
Indazole-type alkaloids from Nigella sativa seeds exhibit antihyperglycemic effects via AMPK activation in vitro.
Identification of N-{[6-chloro-4-(2,6-dimethoxyphenyl)quinazolin-2-yl]carbonyl}-l-leucine (NTRC-808), a novel nonpeptide chemotype selective for the neurotensin receptor type 2.
The SAR development of substituted purine derivatives as selective CB2 agonists for the treatment of chronic pain.
Novel azaindazole sulfonamides inhibitors of serum and glucocorticoid regulated kinase.
Pyrrolo- and pyridomorphinans: non-selective opioid antagonists and delta opioid agonists/mu opioid partial agonists.
Antimicrobial Constituents of the Mature Carpels of Manglietiastrum sinicum.
Unfolded Protein Response in Cancer: IRE1 Inhibition by Selective Kinase Ligands Does Not Impair Tumor Cell Viability.
Design, synthesis and biological evaluation of metronidazole-thiazole derivatives as antibacterial inhibitors.
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Membrane active phenylalanine conjugated lipophilic norspermidine derivatives with selective antibacterial activity.
Anti-Inflammatory Spirostanol and Furostanol Saponins from Solanum macaonense.
Synthesis and biological evaluation of pyridinone analogues as novel potent HIV-1 NNRTIs.
CoMFA and CoMSIA analysis of ACE-inhibitory, antimicrobial and bitter-tasting peptides.
Two Potent OXE-R Antagonists: Assignment of Stereochemistry.
RET Kinase Inhibitors May Treat Cancer and Gastrointestinal Disorders.
Alkylsulfone-containing trisubstituted cyclohexanes as potent and bioavailable chemokine receptor 2 (CCR2) antagonists.
Identification of novel SIRT2-selective inhibitors using a click chemistry approach.
Biological evaluation of new mimetics of annonaceous acetogenins: alteration of right scaffold by click linkage with aromatic functionalities.
Synthesis, antiproliferative and antibacterial activity of new amides of salinomycin.
Two sarcoviolins with antioxidative and -glucosidase inhibitory activity from the edible mushroom Sarcodon leucopus collected in Tibet.
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
Ultrasound promoted one pot synthesis of novel fluorescent triazolyl spirocyclic oxindoles using DBU based task specific ionic liquids and their antimicrobial activity.
Core modification of substituted piperidines as novel inhibitors of HDM2-p53 protein-protein interaction.
Fragment-to-hit-to-lead discovery of a novel pyridylurea scaffold of ATP competitive dual targeting type II topoisomerase inhibiting antibacterial agents.
Thermodynamic and structural characterization of halogen bonding in protein-ligand interactions: a case study of PDE5 and its inhibitors.
One-pot, four-component synthesis of novel cytotoxic agents 1-(5-aryl-1,3,4-oxadiazol-2-yl)-1-(1H-pyrrol-2-yl)methanamines.
TNF- inhibition elicited by mansoins A and B, heterotrimeric flavonoids isolated from Mansoa hirsuta.
Oseltamivir analogues bearing N-substituted guanidines as potent neuraminidase inhibitors.
Impact of stereospecific intramolecular hydrogen bonding on cell permeability and physicochemical properties.
In vivo optimization of 2,3-diaminopyrazine Rho Kinase inhibitors for the treatment of glaucoma.
Synthesis and evaluation of antioxidant activity of 2-styrylchromones
Insect growth regulatory effects by diterpenes from Calceolaria talcana Grau & Ehrhart (Calceolariaceae: Scrophulariaceae) against Spodoptera frugiperda and Drosophila melanogaster
Photosynthetic Electron Transport Inhibitory and Herbicidal Activities of 2-(N-Acylbenzylamino)-4-methyl-6-fluoroalkyl-1, 3, 5-triazine Derivatives
Molecular recognition of long chain fatty acids by peroxisome proliferator-activated receptor
Synthesis, computational studies, and preliminary pharmacological evaluation of new arylpiperazines as potential antipsychotics
Nicotinic acid hydrazones: a novel anticonvulsant pharmacophore
Ligand-based pharmacophore detection, screening of potential pharmacophore and docking studies, to get effective glycogen synthase kinase inhibitors
Synthesis and biological activity of hydrazidehydrazones and their corresponding 3-acetyl-2,5-disubstituted-2,3-dihydro-1,3,4-oxadiazoles
Ethyl 4-[(1-substituted indol-2-yl)methoxy]benzoates and indoline derivatives: Anti-juvenile hormone and juvenile hormone activities
Ultrastructural effects of pyridalyl, an insecticidal agent, on epidermal cells of Spodoptera litura larvae and cultured insect cells Sf9
Synthesis and bioevaluation of novel analogues of justicidin A
Hansch analysis of novel pyrimidine derivatives as highly potent and specific COX-2 inhibitors
Prediction of anti-HIV activity of imidoyl thioureas: QSAR approach
Assessment of the impact of insecticides on Anagrus nilaparvatae (Pang et Wang) (Hymenoptera: Mymanidae), an egg parasitoid of the rice planthopper, Nilaparvata lugens (Hemiptera: Delphacidae)
Activity landscape analysis, CoMFA and CoMSIA studies of pyrazole CB1 antagonists
Solid-Supported Parallel Synthesis of Hydroxybenzylamine Libraries Possessing Antileishmial Activity
In silico studies on 2,3-dihydro-1,5-benzothiazepines as cholinesterase inhibitors
Synthesis of an indolizidinedione oxime inhibitor of acetyl-coenzyme a carboxylase (ACCase)
Synthesis of steroidal thiazolidinones as antibacterial agents based on the in vitro and quantum chemistry calculation
Phytochemical based strategies for nematode control.
Synthesis of novel pyrazole and pyrimidine derivatives bearing sulfonamide moiety as antitumor and radiosensitizing agents
Synthesis and analgesic, anti-inflammatory activities of 3-(3-methoxyphenyl)-2-substituted amino-quinazolin-4(3H)-ones
Synthesis and biological evaluation of novel curcumin analogues as anti-inflammatory, anti-cancer and anti-oxidant agents
Synthesis and antimicrobial screening of novel 2,6-ditertiarybutylpiperidin-4-ones
Novel Mechanisms of Drug Action: Functional Selectivity at D2 Dopamine Receptors
Insecticidal, antifeedant and antifungal activities of two glucosides isolated from the seeds of Simmondsia chinensis
Synthesis, anti-HSV-1, and cytotoxic activities of some new pyrazole- and isoxazole-based heterocycles
Synthesis and anticholinesterase activity of fumaramide derivatives
Inhibitors of biotin biosynthesis as potential herbicides
Multiple Pro-197 substitutions in the acetolactate synthase of rigid ryegrass (Lolium rigidum) and their impact on chlorsulfuron activity and plant growth
QSAR and pharmacophore studies of telomerase inhibitors
Design, synthesis and preliminary antiviral screening of new N-phenylpyrazole and dihydroisoxazole derivatives
Coumarin: a potential nucleus for anti-inflammatory molecules
Synthesis, antioxidant evaluation, and quantitative structureactivity relationship studies of chalcones
Influence of 1, 3, 5-Triazine Compounds on Ammonia Oxidizing Activity of Cell-Free Extracts from Nitrosomonas europaea
Insecticidal Activity of Pyridalyl: Acute and Sub-Acute Symptoms in Spodoptera litura Larvae
Inhibitory effect of curcumin analogs on tissue factor procoagulant activity and their preliminary structureactivity relationships
Synthesis of benzothiazole derivatives and their biological evaluation as anticancer agents
Synthesis of novel optically pure -amino acid functionalised-7-trifluoromethyl substituted quinolone derivatives and their antibacterial activity
Synthesis and biological evaluation of , -unsaturated ketone as potential antifungal agents
Benzimidazole derivatives: synthesis, leishmanicidal effectiveness, and molecular docking studies
Design, Synthesis and Growth Inhibition Activity of Bis-Epoxyethyl Derivatives of Stallimycin Modified on the Amidino Moiety
Preparation of 5-chloro-6-fluoroimidacloprid analogs and comparison of their insecticidal activity in a laboratory test with a 6-chloro-5-fluoro analog
Antifungal activity of simple compounds with maleic anhydride or dimethylmaleimide structure against Botrytis cinerea
Epimerization of epigallocatechin gallate to gallocatechin gallate and its anti-diabetic activity
3-(6-Chloronicotinyl)-2-nitromethylene-thiazolidine as a New Class of Insecticide Acting against Lepidoptera Species
Differential activity against aphid settling of flavones obtained from Clytostoma callistegioides (Bignoniaceae)
In Vitro and In Vivo Characterization of Alpha-1A Selective Agonists and Their Utility for Stress Incontience
Synthesis and Fungicidal Activity of New Six-membered Cyclic Phosphates
Enantioselective Herbicidal Activity of Chiral -Methylbenzylphenylureas against Cyperaceae and Echinochloa Paddy Weeds.
Pharmacophore modeling and structure-based virtual screening for a novel switch region target of bacterial RNA polymerase
Synthesis and bioactivity of novel 3-(1-hydroxyethylidene)-5-substituted-pyrrolidine-2,4-dione derivatives
Cyclophosphamide analogues: synthesis, spectroscopic study, and antitumor activity of diazaphosphorinanes
Antidepressant activity of carbamates and urea derivatives
Antifungal and insecticidal activities of daphnodorins A, B and C.
Synthesis and biological evaluation of novel hydroquinone dimethyl ethers as potential anticancer and antimicrobial agents
Multifunctionalised benzoxazinones in the systems Oryza sativa-Echinochloa crus-galli and Triticum aestivum-Avena fatua as natural-product-based herbicide leads.
Acute toxicity and sublethal effects of methoxyfenozide and thiodicarb on survival, development and reproduction of Helicoverpa armigera (Lepidoptera: Noctuidae)
3D-QSAR studies of thiosemicarbazone and thiocarbamoylpyrazoline antiamebics
Conyza canadensis (L.) Cronquist response to pre-plant application of residual herbicides in cotton (Gossypium hirsutum L.)
Synthesis and pharmacological investigation of novel 3-(benzyl)-2-substituted amino-3H-quinazolin-4-ones as analgesic and anti-inflammatory agents
Synthesis and Insecticidal Activity of 4-1, 2, 4-Thiadiazolin-3-ones
Synthesis and Antifungal Activities of Furoxan Derivatives Designed as Novel Fungicide.
Microwave assisted synthesis of novel pyrimidine derivatives and investigation of their analgesic and ulcerogenic activity
Synthesis, X-ray structure and antiproliferative activity of 3-benzylthio-4-propargylselenoquinoline
Synthesis of substituted benzo[d]thiazol-2-ylcarbamates as potential anticonvulsants
Synthesis and anticancer activity of para-xylyl linked bis-benzimidazolium salts and respective Ag(I) N-heterocyclic carbene complexes
The cytotoxic effects of diketopiperaizes against Leishmania donovani promastigotes and amastigotes
Toxicity of monoterpenes against larvae and adults of Colorado potato beetle, Leptinotarsa decemlineata Say (Coleoptera: Chrysomelidae)
Studies on radioprotective and antiviral activities of some bischalcone derivatives
Antioxidant activities and transition metal ion chelating studies of some hydroxyl Schiff base derivatives
Synthesis and antioxidant studies of novel N-substituted benzyl/phenyl-2-(3,4-dimethyl-5,5-dioxidopyrazolo[4,3-c][1,2]benzothiazin-2(4H)-yl)acetamides
Synthesis, anticancer, anti-HIV-1, and antimicrobial activity of some tricyclic triazino and triazolo[4,3-e]purine derivatives
Synthesis and Herbicidal Activity of Sulfonylurea Compounds with Imidazo [1, 2-a] pyridine Moiety
Nematicidal activity of anion transport blockers against Meloidogyne incognita, Caenorhabditis elegans and Heterorhabditis bacteriophora.
Transition metals in organic synthesis - Part 83#: Synthesis and pharmacological potential of carbazoles
Insecticidal activity of imidacloprid derivatives with an alkoxy group at the C5 position of the pyridine ring
SQ109 analogues as potential antimicrobial candidates
Synthesis of Antifungal 2-Anilino-4-phenylthiazoles and Their Inhibitory Activities on Sterol Biosynthesis
Analytical and biological characterization of quinazoline semicarbazone derivatives
Wound healing phytoconstituents from seed kernel of Entada pursaetha DC. and their molecular docking studies with glycogen synthase kinase 3-
Synthesis, molecular modeling study, preliminary antibacterial, and antitumor evaluation of N-substituted naphthalimides and their structural analogues
Synthesis of some new 3,5-diamino-4-(4-fluorophenylazo)-1-aryl/heteroarylpyrazoles as antimicrobial agents
Novel 4H-1,2,4-triazol-3-yl cycloalkanols as potent antitubercular agents
Synthesis of new series of pyrimido[4,5-b][1,4] benzothiazines as 15-lipoxygenase inhibitors and study of their inhibitory mechanism
Synthesis and Antimuscarinic Activity of Derivatives of 2-Substituted-1,3-Dioxolanes
cAMP-dependent phosphodiesterase inhibition and SAR studies on novel 6,8-disubstituted 2-phenyl-3-(substituted benzothiazole-2-yl)-4[3H]-quinazolinone
Effects of 1,3-dichloropropene as a methyl bromide alternative for management of nematode, soil-borne disease, and weed in ginger (Zingiber officinale) crops in China
Synthesis, characterization and biological evaluation of some pyridine and quinoline fused chromenone derivatives
Synthesis and Cytotoxic Evaluation of 1,2,3-Trisubstituted 2-(2-Oxoalkyl)-2,3-dihydrobenzimidazoles
Spectroscopic characterization of novel d-amino acid-Schiff bases and their Cr(III) and Ni(II) complexes as antimicrobial agents
Synthesis and antitumor evaluation of some 1,3,4-oxadiazole-2(3H)-thione and 1,2,4-triazole-5(1H)-thione derivatives
Synthesis and Acaricidal Activity of Bicyclic Pyrazole-3-carboxamide Derivatives
Lipid lowering and antioxidant activity of flavones in triton treated hyperlipidemic rats
Antiproliferative activity and synthesis of 8-prenylnaringenin derivatives by demethylation of 7-O- and 4'-O-substituted isoxanthohumols.
Structure and Acaricidal Activity of Pyrazolecarboxamides and Thiazole-5-carboxamides
Insecticidal Activity of -Methylene--butyrolactone against Several Insect Pests.
Design and syntheses of novel phthalazin-1(2H)-one derivatives as acetohydroxyacid synthase inhibitors.
Selective Herbicidal Activities of Ethyl 5-(4, 6-Dimethoxypyrimidin-2-ylcarbamoylsulfamoyl)-1-methylpyrazole-4-carboxylate and Its Related Compounds
Pyrrole- and dihydropyrrole-fused neonicotinoids: design, synthesis, and insecticidal evaluation.
Conformational analysis of podophyllotoxin and its congeners. Structure--activity relationship in microtubule assembly.
Phosphonate analogue of 2'-deoxy-5-fluorouridylic acid.
Cyclopropylamines as suicide substrates for cytochromes P-450.
Antianaphylactic agents. 1. 2-(Acylamino)oxazoles.
Ames test of 1-(X-phenyl)-3,3-dialkyltriazenes. A quantitative structure-activity study.
Alkylating nucleosides 1. Synthesis and cytostatic activity of N-glycosyl(halomethyl)-1,2,3-triazoles. A new type of alkylating agent.
A preliminary structure-activity study of the mixed-function oxidase inhibitor 7,8-benzoflavone.
Synthesis and antitumor activity of 4'-O-methyldaunorubicin, 4'-O-methyladriamycin, and their 4'-epi analogues.
Quantitative structure-activity relationships in 1-aryl-2-(alkylamino)ethanol antimalarials.
Synthesis and antitumor activity of water-soluble (2-chloroethyl)nitrosoureas.
N-Acetimidoyl- and N-formimidoylthienamycin derivatives: antipseudomonal beta-lactam antibiotics.
Aminotetralins as narcotic antagonists. Synthesis and opiate-related activity of 1-phenyl-2-aminotetralin derivatives.
Synthesis and pharmacological activity of 2,3,4,5,-tetrahydro-1,5-methano-1H-3-benzazepines.
An attempt to apply lethal synthesis to the design of chemotherapeutic agents. Fluorinated 5 beta-(hydroxyethyl)-4-methylthiazoles.
trans-5-(3,3,3-Trifluoro-1-propenyl-)-2'-deoxyuridylate: a mechanism-based inhibitor of thymidylate synthetase.
Synthesis and estrogenic properties of 17-epi-ethynylestradiol and its ether derivatives epimestranol and epiquinestrol.
Enzyme affinity of the 5,6-dihydro derivatives of the substrate and product of thymidylate synthetase catalysis.
A new chemical series active against African trypanosomes: benzyltriphenylphosphonium salts.
Propiolaldehyde, a pargyline metabolite that irreversibly inhibits aldehyde dehydrogenase. Isolation from a hepatic microsomal system.
A structural modification study of procarbazine.
Synthesis and cytotoxic evaluation of novel ester-triazole-linked triterpenoid-AZT conjugates.
Biased and unbiased strategies to identify biologically active small molecules.
The Oxeatamides: nitrogenous spongian diterpenes from the New Zealand marine sponge Darwinella oxeata.
Azepinone-Containing Tetrapeptide Analogues of Melanotropin Lead to Selective hMC4R Agonists and hMC5R Antagonist.
Pure Diastereomers of a Tranylcypromine-Based LSD1 Inhibitor: Enzyme Selectivity and In-Cell Studies.
Melanocortin antagonist tetrapeptides with minimal agonist activity at the mouse melanocortin-3 receptor.
Design, synthesis and biological evaluation of pyridazino[3,4,5-de]quinazolin-3(2H)-one as a new class of PARP-1 inhibitors.
Diphenylpyrazoles as replication protein a inhibitors.
Bis(aminomethyl)phosphinic Acid, a Highly Promising Scaffold for the Development of Bacterial Urease Inhibitors.
Search for factors affecting antibacterial activity and toxicity of 1,2,4-triazole-ciprofloxacin hybrids.
Potent Irreversible Inhibitors of LasR Quorum Sensing in Pseudomonas aeruginosa.
Combinatorial Libraries As a Tool for the Discovery of Novel, Broad-Spectrum Antibacterial Agents Targeting the ESKAPE Pathogens.
Absolute configuration of labdane diterpenoids from Physalis nicandroides.
Discovery of autophagy inhibitors with antiproliferative activity in lung and pancreatic cancer cells.
Withanolides with antibacterial activity from Nicandra john-tyleriana.
Allosteric modulators: an emerging concept in drug discovery.
1,19-seco-Avermectin analogues from a aveCDE mutant Streptomyces avermectinius strain.
Regioselective chemical and rapid enzymatic synthesis of a novel redox Antiproliferative molecular hybrid.
Improved Synthesis of Biotinol-5'-AMP: Implications for Antibacterial Discovery.
Synthesis and QSAR study of novel anti-inflammatory active mesalazine-metronidazole conjugates.
Design, synthesis, and biological evaluation of ring-constrained novobiocin analogues as hsp90 C-terminal inhibitors.
Structure-activity relationships of the prototypical TRPM8 agonist icilin.
Novel Pyridyloxadiazole Agonists of Sphingosin-1-phosphate.
Treating pain with somatostatin receptor subtype 4 agonists.
Design, synthesis and antibacterial activity of cinnamaldehyde derivatives as inhibitors of the bacterial cell division protein FtsZ.
Sandensone A, a novel sesquiterpenoid from the Formosan soft coral Sinularia sandensis.
Conformational Restriction Leading to a Selective CB2 Cannabinoid Receptor Agonist Orally Active Against Colitis.
SAR Studies of Diphenyl Cationic Trypanocides: Superior Activity of Phosphonium over Ammonium Salts.
Structure-activity relationship and properties optimization of a series of quinazoline-2,4-diones as inhibitors of the canonical Wnt pathway.
Identification of 8-aminoadenosine derivatives as a new class of human concentrative nucleoside transporter 2 inhibitors.
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.
Synthesis of a New Peptide-Coumarin Conjugate: A Potential Agent against Cryptococcosis.
Synthesis and Evaluation of Heterocyclic Catechol Mimics as Inhibitors of Catechol-O-methyltransferase (COMT).
Synthesis and Structure-Activity Relationship Study of 1-Phenyl-1-(quinazolin-4-yl)ethanols as Anticancer Agents.
Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist.
Pyrido[4,3-e][1,2,4]triazolo[4,3-a]pyrazines as Selective, Brain Penetrant Phosphodiesterase 2 (PDE2) Inhibitors.
Sesquiterpenoid tropolone glycosides from Liriosma ovata.
Azide-alkyne cycloaddition-mediated cyclization of phosphonopeptides and their evaluation as PTP1B binders and enrichment tools.
4,6-Diarylaminothiazines as BACE1 Inhibitors and Their Use for the Reduction of Beta-Amyloid Production.
Cytotoxic ent-kaurane diterpenoids from Isodon wikstroemioides.
Pyrazoles as non-classical bioisosteres in prolylcarboxypeptidase (PrCP) inhibitors.
3-Aryl-as-triazines as potential antiinflammatory agents.
Analgesic and tranquilizing activity of 5,8-disubstituted 2-aminomethyl-3,4-dihydronaphthalenes.
A comparison of the antiserotonin, antihistamine, and anticholinergic activity of cyproheptadine with analogues having furan nuclei fused to the 10,11-vinylene bridge.
Plant antitumor agents. 17. Structural requirements for antineoplastic activity in quassinoids.
Synthesis and screening of 8-(4'-thiazolyl)purines.
Synthesis and biological activity of 8-arylergolines.
Methotrexate analogues. 11. Unambiguous chemical synthesis and in vitro biological evaluation of alpha- and gamma-monoesters as potential prodrugs.
Synthesis of two metabolites of (+)-propoxyphene.
Methotrexate analogues. 12. Synthesis and biological properties of some aza homologues.
Novel anxiolytic agents derived from alpha-amino-alpha-phenyl-o-tolyl-4H-triazoles and -imidazoles.
Synthesis and antinociceptive activity of 7-methoxycodeine.
Guanylhydrazones with potential antileukemic activity. 2. Synthesis and structure-activity relationships of analogues of 4,4'-diacetyl-N,N'-diphenylurea bis(guanylhydrazone).
Central nervous system activity of a novel class of annelated 1,4-benzodiazepines, aminomethylene-2,4-dihydro-1H-imidazo[1,2-a][1,4]benzodiazepin-1-ones.
Trichloroacetamidines, a new class of positive inotropic agents.
Synthesis and antiallergic activity of some mono- and disubstituted xanthone-2-carboxylic acids.
Carbocyclic arabinosyladenine, an adenosine deaminase resistant antiviral agent.
Nucleoside 5'-monophosphate analogues. Synthesis of 5'-sulfamino-5'-deoxynucleosides.
Synthesis of mono- and bifunctional alpha-methylene lactone systems as potential tumor inhibitors.
Design, synthesis, characterization, and in vitro antimicrobial action of novel trisubstituted s-triazines
Synthesis and pharmacological evaluation of some novel 2-pyrazolines bearing benzenesulfonamide as anti-inflammatory and blood glucose lowering agents
Abdominal color of the Asian citrus psyllid, Diaphorina citri, is associated with susceptibility to various insecticides.
Structureactivity relationship study of thiosemicarbazones on an African trypanosome: Trypanosoma brucei brucei
Synthesis and pharmacological evaluation of some novel 4-isopropyl thiazole-based sulfonyl derivatives as potent antimicrobial and antitubercular agents
Anti-angiogenic/proliferative behavior of a 4-aryl-4H-chromene on blood vessels endothelial cells: A possible evidence on dual anti-tumor activity
Chemical characterization of the aphid antifeedant extracts from Dittrichia viscosa and Ferula communis
Pyraclostrobin sensitivity of baseline and fungicide exposed isolates of Pyrenophora tritici-repentis
Structural insights for 3H-1, -2, -4 triazolinones as angiotensin II receptor antagonists using QSAR techniques
Preparation of Dinotefuran Related Compounds and Agonistic Action on SAD2 Hybrid Nicotinic Acetylcholine Receptors Expressed in Xenopus laevis Oocytes
Synthesis and herbicidal activity of sulfonanilides having a pyrimidinyl-containing group at the 2-position
Synthesis and anti-bacterial activities of some novel pyrazolobenzothiazine-based chalcones and their pyrimidine derivatives
Antihepatotoxic, nephroprotective, and antioxidant activities of phenolic compounds from Satureja macrostema leaves against carbon tetrachloride-induced hepatic damage in mice
3D quantitative structureactivity relationship for quinoline, benzimidazole and benzofuran-based analogs as phosphodiesterases IV (PDE-IV) inhibitors
A facile synthesis of new 3,3-disubstituted phthalides of pharmacological interest
Synthesis and calcium channel antagonist activity of novel 1,4-dihydropyridine derivatives possessing 4-pyrone moieties
Structure-activity relationship of carboxin-related carboxamides as fungicide
Synthesis, characterization and in vitro hydrolysis studies of ester and amide prodrugs of dexibuprofen
Fungicidal Activities of 2-(Substituted Phenoxymethyl)phenyl-2-methoxyiminoacaetamide Derivatives
Design, synthesis, anti-inflammatory, analgesic screening, and molecular docking of some novel 2-pyridyl (3H)-quinazolin-4-one derivatives
Evaluation of the anti-inflammatory activity of some pyrrolo[2,3-d]pyrimidine derivatives
Effect on Insecticidal Activity of Substituents at the 1,4-Benzodioxanyl Moiety of Haedoxan
Development of robust QSAR model using rapid overlay of crystal structures (ROCS) based alignment: a test case of Tubulin inhibitors
Qsar for Acetylcholinesterase and Butyrylcholinesterase Inhibition by Cardiovascular Drugs and Benzodiazepines
Carbamate derivatives of felbamate as potential anticonvulsant agents
Evaluating anti-Toxoplasma gondii activity of new serie of phenylsemicarbazone and phenylthiosemicarbazones in vitro
Preparation and antimicrobial activity evaluation of some new bi- and triheterocyclic azoles
Synthesis of damnacanthal, a naturally occurring 9,10-anthraquinone and its analogues, and its biological evaluation against five cancer cell lines
Facile synthesis of furoquinoline and effects on radical-induced oxidation of DNA
Photodynamic activities of protoporphyrin IX and its dopamine conjugate against cancer and bacterial cell viability
Insights into the structural requirement of 6-nitroquinolone-3-carboxylic acids as antimycobacterial agent: chemometric approaches
Evaluation of fungicides to control circular leaf spot of persimmon caused by Mycosphaerella nawae
Alpha2-Adrenergic Receptors in Intestinal Epithelial Cells: Mechanisms of Signaling, Role, and Regulation
Identification of liver X receptor and farnesoid X receptor dual agonists from Tithonia diversifolia
CoMFA, ADVANCE CoMFA AND CoMSIA STUDIES ON THE OXADIAZOLE SUBSTITUTED -ISOPROPOXY PHENYLPROPIONIC ACIDS FOR PPAR AGONISTIC ACTIVITY
Hydrolysis and Phytotoxic Activity ofN-Aryl-3,4,5,6-tetrahydroisophthalimides
Synthesis and antitubercular activity of novel pyrazolequinazolinone hybrid analogs
Weed control efficacy and winter wheat safety of a novel herbicide HW02
Synthesis, characterization & anticonvulsant activity of amide derivatives of 4-amino-1,2-naphthoquinone
In vitro antimicrobial and antitubercular studies of novel 6-substituted (pyrrolidin-1-yl)-2(1H)-pyridinones
Insulinotropic activity of chromonyl-2,4-thiazolidinediones
2D and 3D QSAR study on amino nicotinic acid and isonicotinic acid derivatives as potential inhibitors of dihydroorotate dehydrogenase (DHODH)
Resistance buster compounds for MBI-D insensitive rice blast fungus—Inquiry on effective compounds among derivatives of MBI-D fungicides—
Synthesis and herbicidal activities of novel 3-N-substituted amino-6-methyl-4-(3-trifluoromethylphenyl)pyridazine derivatives.
Synthesis and Fungicidal Activities of 4,5-Dihydro-7H-pyrano[3,4-c]isoxazole Derivatives.
Controlling Efficacy of Strobilurin Derivatives against Wheat Powdery Mildew and Eyespot
Flubendiamide, a Novel Insecticide Highly Active against Lepidopterous Insect Pests
Synthesis, characterization, and biological evaluation of some N-aryl hydrazones and their 2,3-disubstituted-4-thiazolidinone derivatives
Synthesis of novel cyclobutylphosphonic acids as inhibitors of imidazole glycerol phosphate dehydratase
Zn(Proline)2-catalyzed Knoevenagel condensation under solvent-free/aqueous conditions and biological evaluation of products
Efficacy of neem limonoids on Cnaphalocrocis medinalis (Guenee) (Lepidoptera: Pyralidae) the rice leaffolder.
Synthesis and antimicrobial study of fluoroquinolone-based 4-thiazolidinones
Phytotoxic Compounds Cochlioquinones Are Inhibitors of Mitochondrial NADH-Ubiquinone Reductase
Synthesis and biological evaluation of some pyrazole derivatives as anti-inflammatoryantibacterial agents
Synthesis of novel 2-phenyl-3-[2-(substituted amino) ethylamino] quinazolin-4(3H)-ones as a new class of H1-antihistaminic agents
Synthesis and antitumor activity of (4-hydroxyphenyl)[5-substituted alkyl/aryl)-2-thioxo-1,3,4-thiadiazol-3-yl]methanone and [(3,4-disubstituted)-1,3-thiazol-2ylidene]-4-hydroxybenzohydrazide
2D-QSAR of purine-scaffold novel class of Hsp90 binders that inhibit the proliferation of cancer cells
Protection of protein carbonyl formation by quercetin in erythrocytes subjected to oxidative stress
Synthesis and biological evaluation of N 1,N 2-bis-[4-(t-amino)-2-butynyl]phthalamides as oxotremorine and acetylcholine antagonists
In vitro antiproliferative activity of 11-aminoalkylamino-substituted 5H-indolo[2,3-b]quinolines; improving activity of neocryptolepines by installation of ester substituent
-Glucosidase inhibitory and antioxidant properties and antidiabetic activity of Hypericum ascyron L.
NAD+-dependent DNA ligase (Rv3014c) from M. tuberculosis: Strategies for inhibitor design
Pharmacophore-based 3D-QSAR study of fungal chitin synthase inhibitors
Novel potential nonsedating H1 antagonists related to the gauche rotamer of PROS-NH-histamine
Analgesic study of novel pyrimidine derivatives linked with coumarin moiety
QSAR analysis on PfPK7 inhibitors using HQSAR, CoMFA, and CoMSIA
Molecular drug design, synthesis and pharmacophore site identification of spiroheterocyclic compounds: Trypanosoma crusi inhibiting studies
QSAR modeling of the inhibition of reverse transcriptase enzyme with benzimidazolone analogs
Evaluation of some weed control treatments for long season weed control in maize (Zea mays L.) under zero and minimum tillage at Samaru, in Nigeria
Tautomeric origin of dual effects of N1-nicotinoyl-3-(4-hydroxy-3-methyl phenyl)-5-[(sub)phenyl]-2-pyrazolines on bacterial and viral strains: POM analyses as new efficient bioinformatics platform to predict and optimize bioactivity of drugs
Synthesis of simplified herboxidiene aromatic hybrids.
Computational studies on structurally diverse dipeptidyl peptidase IV inhibitors: an approach for new antidiabetic drug development
Statistically validated QSAR study of some antagonists of the human CCR5 receptor using least square support vector machine based on the genetic algorithm and factor analysis
Design and synthesis of 2-chloroquinoline derivatives as non-azoles antimycotic agents
Synthesis of some new 3,4-dihydro-2H-1,3-benzoxazines under microwave irradiation in solvent-free conditions and their biological activity
Inhibitory Activity of N-Substituted-2-piperidones with a 1, 4-Benzodioxan Ring on Germination of Barnyardgrass
Simple and efficient synthetic routes to bioactive s-triazinyl dithiocarbamate derivatives
Synthesis and biological evaluation of a novel anti-malarial lead
Pyrethroid resistance in the tomato red spider mite, Tetranychus evansi, is associated with mutation of the para-type sodium channel.
Comparative quantitative structureactivity relationship study of some 1-aminocyclopentyl-3-carboxyamides as CCR2 inhibitors using stepwise MLR, FA-MLR, and GA-PLS
Design, synthesis, and particular biological behaviors of chain-opening nitromethylene neonicotinoids with cis configuration.
Bioanalytical method development and validation for simultaneous estimation of (R)- and (S)-isomers of S002-333: a potent novel anti-thrombotic agent using LCMS/MS
Investigating the mode of action of sulfoxaflor: a fourth-generation neonicotinoid.
Synthesis and Microbiological Evaluation of Novel [N-Acetyl-2,6-Diarylpiperidin-4-YL]-5-Spiro-4-Acetyl-2-(Acetylamino)-2-1,3,4-Thiadiazolines
Microwave-assisted synthesis and antimicrobial screening of new imidazole derivatives bearing 4-thiazolidinone nucleus
Synthesis, biological evaluation, and molecular modeling studies of novel heterocyclic compounds as anti-proliferative agents
Effects of inositol 1,2,6-triphosphate on human liver cancer SMMC-7721 cells
Sterile oat (Avena sterilis L.) cross-resistance profile to ACCase-inhibiting herbicides in Greece
Steroidal saponins from the leaves of Yucca de-smetiana and their in vitro antitumor activity: structure activity relationships through a molecular modeling approach
Pharmacological Effects of Imidacloprid and Its Related Compounds on the Nicotinic Acetyicholine Receptor with Its Ion Channel from the Torpedo Electric Organ
Synthesis and antihypertensive activity evaluation in spontaneously hypertensive rats of nitrendipine analogues
In vitro antimycobacterial activity of novel N-(4-(substituted phenyl amino)-6-(pyridin-2-ylamino)-1,3,5-triazin-2-yl)isonicotinohydrazide
Potential applications of violacein: a microbial pigment
Synthesis, antimicrobial and DNA cleavage studies of some 4-aryloxymethylcoumarins obtained by reaction of 4-bromomethylcoumarins with bidentate nucleophiles
3D-QSAR studies on betulinic acid and betulin derivatives as anti-HIV-1 agents using CoMFA and CoMSIA
Synthesis, structure characterization, and biological evaluation of some new 1,2,3-benzotriazole derivatives
QSAR of 2,4-diphenyl-1,3-oxazolines for ovicidal activity against the two-spotted spider mite Tetranychus urticae
Synthesis and evaluation of antibacterial and antitubercular activities of some novel imidazo[2,1-b][1,3,4]thiadiazole derivatives
Baseline sensitivity of Pestalotiopsis microspora, which causes black spot disease on Chinese hickory (Carya cathayensis), to pyraclostrobin
Synthesis and Insecticidal Activity of 2-Alkoxy-4H-l,3,2-benzoxazaphosphorin-2-thiones
Synthesis and studies on antidepressant activity of 2,4,6-trihydroxychalcone derivatives
Rational exploration of new pyridinium-based HSP90 inhibitors tailored to thiamine structure
Stereocontrolled synthesis of spirosuccinimide derivative of (+)-hydantocidin
Synthesis, anticancer and MRP1 inhibitory activities of 4-alkyl/aryl-3,5-bis(carboethoxy/carbomethoxy)-1,4-dihydro-2,6-dimethylpyridines
Synthesis of Some 2-Aryloxymethyl-1, 3, 4-thiadiazolo[2, 3-b]-quinazolin-4-ones and 2-Aryloxymethyl-5-substituted-1, 3, 4-thiadiazolo[3, 2-a]-s-triazin-7-thiones as Potential Biocides
Synthesis and cytotoxic activity of diaryl urea derivatives with a 4-methylpiperazinylcarbonyl moiety
MMV Box Cryptosporidium parvum screening set
Indimicins A-E, Bisindole Alkaloids from the Deep-Sea-Derived Streptomyces sp. SCSIO 03032.
Diterpenoids with Immunosuppressive Activities from Cinnamomum cassia.
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
Studies toward the Development of Antiproliferative Neoclerodanes from Salvinorin A.
Synthesis of genistein coupled with sugar derivatives and their inhibitory effect on nitric oxide production in macrophages.
Inhibition of the Bacterial Adhesin FimH May Potentially Treat Inflammatory Bowel Diseases (IBD).
Identification of potent and selective hydantoin inhibitors of aggrecanase-1 and aggrecanase-2 that are efficacious in both chemical and surgical models of osteoarthritis.
In vitro antitumor activity evaluation of some 1,2,4-triazine derivatives bearing piperazine amide moiety against breast cancer cells.
Discovery of 1H-indole-2-carboxamides as novel inhibitors of the androgen receptor binding function 3 (BF3).
Synthesis and analgesic activity of alkylated, reduced and constrained oligoheterocyclic peptidomimetic analogs of Leu-enkephalin.
Flexible, polymer-supported synthesis of sphingosine derivatives provides ceramides with enhanced biological activity.
Optimization of 1,2,4-Triazolopyridines as Inhibitors of Human 11-Hydroxysteroid Dehydrogenase Type 1 (11-HSD-1).
Total Synthesis and Biological Studies of TMC-205 and Analogues as Anticancer Agents and Activators of SV40 Promoter.
Eleganketal A, a highly oxygenated dibenzospiroketal from the marine-derived fungus Spicaria elegans KLA03.
Microwave-assisted synthesis and biological evaluation of 3,4-diaryl maleic anhydride/N-substituted maleimide derivatives as combretastatin A-4 analogues.
Probing linker design in citric acid-ciprofloxacin conjugates.
-Nitro substituted carboxylic acids and their cytotoxicity.
Synthesis of novel tylophorine derivatives and evaluation of their anti-inflammatory activity.
Sulfonamides with Potent Inhibitory Action and Selectivity against the -Carbonic Anhydrase from Vibrio cholerae.
Synthesis and Pharmacology of a Novel Opioid Receptor (KOR) Agonist with a 1,3,5-Trioxazatriquinane Skeleton.
Naphthyridinone (NTD) integrase inhibitors 4. Investigating N1 acetamide substituent effects with C3 amide groups.
C-terminal residue optimization and fragment merging: discovery of a potent Peptide-hybrid inhibitor of dengue protease.
Semisynthesis of triptolide analogues: effect of B-ring substituents on cytotoxic activities.
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
ASK1 pharmacophore model derived from diverse classes of inhibitors.
Antiprotozoal Activity Profiling of Approved Drugs: A Starting Point toward Drug Repositioning
Synthesis and biological evaluation of picolinamides as potent inhibitors of 11-hydroxysteroid dehydrogenase type 1 (11-HSD1).
Novel inhibitors of platelet aggregation.
The discovery of novel 3-(pyrazin-2-yl)-1H-indazoles as potent pan-Pim kinase inhibitors.
Hydroxamic acids block replication of hepatitis C virus.
Non-transpeptidase binding arylthioether -lactams active against Mycobacterium tuberculosis and Moraxella catarrhalis.
Interconversion of Functional Activity by Minor Structural Alterations in Nonpeptide AT2 Receptor Ligands.
Structural Insights for the Optimization of Dihydropyrimidin-2(1H)-one Based mPGES-1 Inhibitors.
Development of novel Asf1-H3/H4 inhibitors.
Evaluation and synthesis of polar aryl- and heteroaryl spiroazetidine-piperidine acetamides as ghrelin inverse agonists.
Discovery of dual leucine zipper kinase (DLK, MAP3K12) inhibitors with activity in neurodegeneration models.
Synthesis of oolongtheanins and their inhibitory activity on micellar cholesterol solubility in vitro.
An Orally Available BACE1 Inhibitor That Affords Robust CNS A Reduction without Cardiovascular Liabilities.
Amphirionin-2, a novel linear polyketide with potent cytotoxic activity from a marine dinoflagellate Amphidinium species.
Pyridine and pyridinone-based factor XIa inhibitors.
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
The role of enhancer of zeste homologue 2 inhibitors in controlling epigenetics and their potential for cancer treatment.
6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.
Inhibitors of c-Jun N-terminal kinases: an update.
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
Synthesis and antitubercular evaluation of 4-carbonyl piperazine substituted 1,3-benzothiazin-4-one derivatives.
Synthesis and antiproliferative activity of novel polynuclear heterocyclic compounds derived from 2,3-diaminophenazine.
Synthesis and biological evaluation of 4-nitroindole derivatives as 5-HT2A receptor antagonists.
Methotrexate analogues. 8. Synthesis and biological evaluation of bisamide derivatives as potential prodrugs.
Angiotensin II analogues. 12. Role of the aromatic ring of position 8 phenylalanine in pressor activity.
Structure-activity relationships in antitumor aniline mustards.
Synthesis and antiviral and enzymatic studies of certain 3-deazaguanines and their imidazolecarboxamide precursors.
Synthesis of episilon-rhodomycinone glycosides.
Synthesis and antiinflammatory activity of trisubstituted pyrimidines and triazines.
Modifications of primaquine as antimalarials. 1. 5-Phenoxy derivatives of primaquine.
Modifications of primiaquine as antimalarials. 2. 5-Phenylthio and 5-anilino derivatives of primaquine.
New inhibitors of platelet aggregation. 5'-Phosphate, 5'-phosphorothioate, and 5'-O-sulfamoyl derivatives of 2-substituted adenosine analogues.
Antiparasitic agents. 3. Synthesis and anthelmintic activities of novel 2-pyridinyl-5-isothiocyanatobenzimidazoles.
Nitrones. 7. alpha-Quinoxalinyl-N-substituted nitrone 1,4-dioxides.
Structure-activity relationship of aniline mustards acting against B-16 melanoma in mice.
Synthesis of 2-substituted primaquine analogues as potential antimalarials.
5-Chloro-2-phenyl-1-benzo[b]thiophene-3-alkanimines, potential antipsychotic agents.
Synthesis and gastric antisecretory properties of an 8-aza-and a 10-oxa-8,12-secoprostaglandin.
9-hydroxy-1,2,3,4,5,6-hexahydro-1,5-methano-3-benzazocine derivatives as analgesics.
Ultraviolet photoelectron spectroscopy of cyclic amidines. 1. Electronic structure of some alpha-adrenergic benzylimidazolines.
Novel arabinofuranosyl derivatives of cytosine resistant to enzymatic deamination and possessing potent antitumor activity.
Syntheses and biological activities of basically substituted isoalloxazines.
(1-(3-(Phenothiazin-10-yl)propyl)-4-piperidinyl)phenylmethanones, a novel class of long-acting neuroleptic agents.
Synthesis of some conformationally restricted analogues of fentanyl.
Experimental antiulcer drugs. 2. 2-Substituted 2,4,5,6-tetrahydro-1,3,4,6,6-pentamethylcyclopenta[c]pyrrole-4-carboxamides.
Synthesis and antitumor properties of 7-deoxy-7-[(cis- and trans-3-aminocyclohexane)thio]carminomycinone.
Hetacillin (R)- and (S)-sulfoxides. Synthesis and structure-activity relationships.
8-Carboxy-6-sulfamyldibenz[b,f][1,4]oxazepines and -thiazepines as potential high-ceiling diuretics.
Antifeedant activity of sesquiterpenes from celastraceae
Synthesis, biological activity and docking study of some new isatin Schiff base derivatives
Antifungal activity of a novel quercetin derivative bearing a trifluoromethyl group on Candida albicans
Lethal and sublethal effects of buprofezin and imidacloprid on Bemisia tabaci (Hemiptera: Aleyrodidae)
Baseline sensitivity of Monilinia laxa from Greece to fenhexamid and analysis of fenhexamid-resistant mutants
Design, synthesis, and in vitro evaluation of cytotoxic activity of new substituted 1,4-benzoquinones and hydroquinones
Synthesis and Fungicidal Activities of (-Methoxybenzyl) isoxazoles
Design and synthesis of some thiazolotriazolyl esters as anti-inflammatory and analgesic agents
Design and synthesis of some azole derivatives as potential antimicrobial agents
Organophosphorus derivatives containing piperazine dithiosemicarbazones as chemotherapeutants against fungal pathogens of sugarcane.
Studies on the synthesis of some new substituted benzylamino and phenyl-acrylamido-methyl flavone derivatives
Bioactive metabolites from an endophytic fungus of Aspergillus species isolated from seeds of Gloriosa superba Linn.
Novel furoxan NO-donor pemetrexed derivatives: design, synthesis, and preliminary biological evaluation
Antinociceptive activities of some triazole and pyrazoline moieties-bearing compounds
In vitro antimicrobial and molecular docking of dichloro substituted benzoxazole derivatives
Synthesis and local anaesthetic activities of 2-aminothiazole/thiadiazole analogues of lidocaine
1-Phenoxyalkyl-4-[(N,N-disubstitutedamino)alkyl]piperazine derivatives as non-imidazole histamine H3-antagonists
Synthesis and antibacterial, antifungal activities of some 2r,4c-diaryl-3-azabicyclo[3.3.1]nonan-9-one-4-aminobenzoyl hydrazones
Biocontrol of rice blast by the phenaminomethylacetic acid producer of Bacillus methylotrophicus strain BC79
Synthesis and Herbicidal Activity of New 1-Alkyl-3-aryloxypyrazole-4-carboxamide Derivatives
Efficient isolation of catechins from green tea and characterization of interaction property of catechins with proteins by HPLCUV/DAD combined with ultrafiltration
Synthesis and Biological Activities of Fluorinated Plant Growth Regulators, 4, 4, 4-Trifluoro-3-(3-indolyl)butyric Acids and 4, 4, 4-Trifluoro-3-(2-indolyl)butyric Acid Bearing a Methyl Group on the Indole Nucleus
Anti-tubercular agents from Ammannia baccifera (Linn.)
Design, multicomponent synthesis, and bioactivities of novel neonicotinoid analogues with 1,4-dihydropyridine scaffold.
Overexpression of the sterol 14-demethylase gene (MgCYP51) in Mycosphaerella graminicola isolates confers a novel azole fungicide sensitivity phenotype.
Peroxidizing Phytotoxicities of 1, 2-Dialkyl-1, 2, 4-triazolidines and 3, 4-Dialkyl-1, 3, 4-thiadiazolidines
Resistance monitoring to deltamethrin and chlorpyriphos-ethyl in 13 populations of Typhlodromus pyri Scheuten (Acari: Phytoseiidae) from vineyards in the southwest of France
Synthesis and bioactivity of some new 1-tolyl-3-aryl-4-methylimidazole-2-thiones
A search of novel antimicrobial based on benzimidazole and 2-pyridone heterocycles
Synthesis, single crystal X-ray studies and antimicrobial activities of novel Indole barbiturates
Synthesis and in vitro study of antibacterial, antifungal activities of some novel bisquinolines
Fungicidal Activities of 2-Methoxy-2-[2-(benzylideneaminooxymethyl)phenyl]-N-methylacetamide Derivatives
Synthesis and Structure-Activity Relationships of Dinotefuran Derivatives: Modification in the Nitroguanidine Part
Heterodimerization of G-Protein-Coupled Receptors Reveals an Unexpected Level of Pharmacological Diversity
Synthesis and antimycobacterial activities of some new N-acylhydrazone and thiosemicarbazide derivatives of 6-methyl-4,5-dihydropyridazin-3(2H)-one
Synthesis of some 1,3,4-thiadiazole derivatives as inhibitors of Entamoeba histolytica
Synthesis and Herbicidal Activity of New Pyrazole-4-carboxamide Derivatives
Synthesis of new series of pyrazolo[4,3-d]pyrimidin-7-ones and pyrido[2,3-d]pyrimidin-4-ones for their bacterial and cyclin-dependent kinases (CDKs) inhibitory activities
Synthesis and anticonvulsant activity of novel imidazol5(4H)one and 5-oxo-4,5-dihydroimidazol-1-yl)propanamide derivatives
Syntheses of tetrahydronaphthalenes. Part II
Synthesis and antimicrobial activity of bischalcone derivatives
QSAR study of some CCR5 antagonists as anti-HIV agents using radial basis function neural network and general regression neural network on the basis of principal components
17-Oximino-5-androsten-3-yl esters: synthesis, antiproliferative activity, acute toxicity, and effect on serum androgen level
Effect of chronic treatment with new benzylidene-thiazolidine-2,4-dione (LPSF/GQ-06) with potential hypoglycemic on rat Leydig cell steroidogenesis
Novel 1,3-diarylpyrazole acrylamides: synthesis, antiplatelet activity screening, and in silico evaluation studies
Regioselective synthesis and cannabinoid receptor binding affinity of N-alkylated 4,5-diaryl-1,2,3-triazoles
Khayasin and 2S-methylbutanoylproceranolide: Promising candidate insecticides for the control of the coconut leaf beetle, Brontispa longissima
Herbicidally Active N-(1-Arylethenyl)-2-chloroacetamides Bearing an Alkyloxyalkyl Moiety.
Fungitoxic and Phytotoxic Activities of Cinnamic Acid Esters and Amides
Hydrogenated and Dichiorinated N-Phthaloyl-L-threonines and Their Dehydrated Phthalimides with Root Growth-promoting Activity for Rice Seedings
Cytotoxicity and QSAR study of (thio)ureas derived from phenylalkylamines and pyridylalkylamines
Photodimerization of heteroaryl chalcones: comparative antimicrobial activities of chalcones and their photoproducts
Synthesis and evaluation of DPPH and anti-inflammatory activities of 2,6-bisbenzylidenecyclohexanone and pyrazoline derivatives
Schiff bases as potential fungicides and nitrification inhibitors.
Apoptotic effects of some carbazole derivatives on lung carcinoma and glioma cell lines
Quantum chemical QSAR study of flavones and their radical-scavenging activity
Fate of cyromazine applied in nutrient solution to a gerbera (Gerbera jamesonii) crop grown in a closed hydroponic system
Synthesis and Biological Evaluation of Allosteric A1-Adenosine Receptor Modulators Structurally Related to (2-Amino-4,5,6,7-Tetrahydro-Benzo[B]Thiophen-3-YL)-(4-Chloro-Phenyl)-Methanone, a Potent Compound Useful to Reduce Neuropathic Pain
Synthesis, cytotoxic, and DNA binding studies of novel fluorinated condensed pyrano pyrazoles
STUDIES ON NOVEL NON-IMIDAZOLE HUMAN H4 RECEPTOR ANTAGONISTS USING GFA AND FREE-WILSON ANALYSIS
Hypoglycemic and insulin mimetic impact of catechin isolated from Cassia fistula: a substantiate in silico approach through docking analysis
Synthesis in vitro/in vivo evaluation and in silico physicochemical study of prodrug approach for brain targeting of alkylating agent
In vitro cytotoxicity, antimicrobial, and metal-chelating activity of triterpene saponins from tea seed grown in Kangra valley, India
Design, synthesis, and biological evaluation of benzofuran derivatives as ET receptor antagonists
Insecticide resistance of the oriental fruit fly, Bactrocera dorsalis (Hendel) (Diptera: Tephritidae), in mainland China.
Synthesis of Esters, Amides, N-Alkylamides and N, N-Dialkylamides of 2, 3-Dimethyl-5-(2, 5-disubstituted phenylaminocarbonyl)-6-pyrazinecarboxylic Acid and Their Phytotoxicity
Molecular design, synthesis and biological activities of amidines as new ketol-acid reductoisomerase inhibitors
Synthesis and bioevaluation of Schiff and Mannich bases of isatin derivatives with 4-amino-5-benzyl-2,4-dihydro-3H-1,2,4-triazole-3-thione
A new fatty alcohol from Terminalia arjuna leaves with antileishmanial activity
Synthesis and Octopaminergic-Agonist Activity of 2-(Arylimino)oxazolidines and 2-(Substituted Benzylamino)-2-oxazolines
Baseline susceptibility of Bemisia tabaci (Genn.) biotype B in southern Florida to cyantraniliprole
Diastereoselective synthesis of the model insect antifeedants related to azadiradione and epoxyazadiradione based on intramolecular insertion of -aryl--diazoketones
Evidence of stereoselective and segmental-dependant transport of chiral antidiabetic drug nateglinide along the rat small intestine: possible role of efflux transporters
Synthesis of lactosylated piperazinyl porphyrins and their hepatocyte-selective targeting
Anti-inflammatory and analgesic activities of a new cucurbitacin isolated from Citrullus colocynthis seeds
Molecular docking study on anticancer activity of plant-derived natural products
Otebo bean (Phaseolus vulgaris) sensitivity to pre-emergence herbicides
Isoxazole derivatives as a potential insecticide for managing Callosobruchus chinensis
New thiazolidine-2,4-diones as antimicrobial and cytotoxic agent
Antitumor and Anti-Pneumocystis Carinii Activities of Novel Bisbenzamidines
3D QSAR STUDIES OF INHIBITORS OF EPIDERMAL GROWTH FACTOR RECEPTOR [EGFR] USING CoMFA AND GFA METHODOLOGIES
QSAR analysis of caffeoyl naphthalene sulfonamide derivatives as HIV-1 integrase inhibitors
Synergistic application of target structure-based alignment and 3D-QSAR study of protein tyrosine phosphatase 1B (PTP1B) inhibitors
Designing hypothesis of diaryl pyrimidine analogs as anti-HIV agent: QSAR approach
Identification of novel inhibitors of HIV-1 integrase using pharmacophore-based virtual screening combined with molecular docking strategies
Synthesis and biological activities of some N-hydroxymethylene and N-methoxymethylene thiazines
Herbicidal, plant growth inhibitory, and cytotoxic activities of bismuthines containing aromatic heterocycles.
Study of mangiferin-receptor affinity by cell membrane chromatography using rat pancreas
Control of Muhlenbergia frondosa (wirestem muhly) with post-emergence sulfonylurea herbicides in maize (Zea mays)
Cheminformatic designing of de novo inhibitors to 3-methyl adenine DNA glycosylase I (LiTagA) from Leptospira interrogans serovar lai strain 56601
The effect of pyridazine compounds on the cardiovascular system
Substituted aminoalcohol ester analogs of indomethacin with reduced toxic effects
Novel glitazones: glucose uptake and cytotoxic activities, and structureactivity relationships
Molecular simulations of bergenin as a new urease inhibitor
Synthesis and antimicrobial activity of pyrimidine chalcones
Synthesis and Precocious Metamorphosis-Inducing Activity of 3-(1-Alkenyl) pyridines
Discovery of triazine mimetics as potent antileishmanial agents.
Caesalminaxins A-L, cassane diterpenoids from the seeds of Caesalpinia minax.
SAR-based optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as highly potent EP1 receptor antagonists.
Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues.
Neuroprotective benzyl benzoate glycosides from Disporum viridescens roots in HT22 hippocampal neuronal cells.
Hygrocins C-G, cytotoxic naphthoquinone ansamycins from gdmAI-disrupted Streptomyces sp. LZ35.
Fluorine Scanning by Nonselective Fluorination: Enhancing Raf/MEK Inhibition while Keeping Physicochemical Properties.
Adamantyl derivative as a potent inhibitor of Plasmodium FK506 binding protein 35.
Kadcotriones A-C: tricyclic triterpenoids from Kadsura coccinea.
Bisindole alkaloids with neural anti-inflammatory activity from Gelsemium elegans.
Characterization and anti-inflammatory effects of iodinated acetylenic acids isolated from the marine sponges Suberites mammilaris and Suberites japonicus.
PDE2 inhibition: potential for the treatment of cognitive disorders.
Antiangiogenic tocotrienol derivatives from Garcinia amplexicaulis.
6-(4-Pyridyl)pyrimidin-4(3H)-ones as CNS penetrant glycogen synthase kinase-3 inhibitors.
Discovery of tetrahydroisoquinoline-based CXCR4 antagonists.
Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.
Analogs of the Allosteric Heat Shock Protein 70 (Hsp70) Inhibitor, MKT-077, as Anti-Cancer Agents.
Secoemestrin D, a cytotoxic epitetrathiodioxopiperizine, and emericellenes A-E, five sesterterpenoids from Emericella sp. AST0036, a fungal endophyte of Astragalus lentiginosus1.
N-[4-(1H-Pyrazolo[3,4-B]pyrazin-6yl)-phenyl]-sulonamides and Their Use As Pharmaceuticals.
Chlorophenylpiperazine analogues as high affinity dopamine transporter ligands.
Strepsesquitriol, a rearranged zizaane-type sesquiterpenoid from the deep-sea-derived actinomycete Streptomyces sp. SCSIO 10355.
Synthesis and evaluation of the antimalarial, anticancer, and caspase 3 activities of tetraoxane dimers.
Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues.
Structures of human acetylcholinesterase bound to dihydrotanshinone I and territrem B show peripheral site flexibility.
Potent oxazolidinone antibacterials with heteroaromatic C-ring substructure.
Homosecoiridoid alkaloids with amino acid units from the flower buds of Lonicera japonica.
Molecular basis for the long duration of action and kinetic selectivity of tiotropium for the muscarinic M3 receptor.
New 5-Aryl-1H-imidazoles display in vitro antitumor activity against apoptosis-resistant cancer models, including melanomas, through mitochondrial targeting.
Cytotoxic and antibacterial marfuraquinocins from the deep South China Sea-derived Streptomyces niveus SCSIO 3406.
Phenylspirodrimanes with anti-HIV activity from the sponge-derived fungus Stachybotrys chartarum MXH-X73.
New synthetic enediynes and their conjugates may provide effective treatment for cancer.
Dibenzoyl and isoflavonoid glycosides from Sophora flavescens: inhibition of the cytotoxic effect of D-galactosamine on human hepatocyte HL-7702.
Pyrido[2,3-d]pyrimidines: discovery and preliminary SAR of a novel series of DYRK1B and DYRK1A inhibitors.
Chromenylchalcones with inhibitory effects on monoamine oxidase B.
Discovery of Octahydroindenes as PAR1 Antagonists.
Protease inhibitors from Microcystis aeruginosa bloom material collected from the Dalton Reservoir, Israel.
The discovery of novel N-(2-pyrimidinylamino) benzamide derivatives as potent hedgehog signaling pathway inhibitors.
Desmethyl Macrolides: Synthesis and Evaluation of 4,8,10-Tridesmethyl Cethromycin.
Isoquinoline derivatives as potent CRTH2 antagonists: design, synthesis and SAR.
Novel glycosylated endomorphin-2 analog produces potent centrally-mediated antinociception in mice after peripheral administration.
Synthesis of Novel 3,5-Disubstituted-2-oxindole Derivatives As Antitumor Agents against Human Nonsmall Cell Lung Cancer.
Medicinal uses, phytochemistry and pharmacology of family Sterculiaceae: a review.
Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.
Chalcones and their therapeutic targets for the management of diabetes: structural and pharmacological perspectives.
Xanthone analogues as potent modulators of intestinal P-glycoprotein.
Exploring the 7-oxo-thiazolo[5,4-d]pyrimidine core for the design of new human adenosine A3 receptor antagonists. Synthesis, molecular modeling studies and pharmacological evaluation.
N-benzoyl-1,5-benzothiazepine and its S-oxide as vasopressin receptor ligands: insight into the active stereochemistry around the seven-membered ring.
Targeting DNA methylation with small molecules: what's next?
Activity of 2-aryl-2-(3-indolyl)acetohydroxamates against drug-resistant cancer cells.
New platelet aggregation inhibitors based on pyridazinone moiety.
Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer.
Discovery of the 2-phenyl-4,5,6,7-Tetrahydro-1H-indole as a novel anti-hepatitis C virus targeting scaffold.
Macrocyclic compounds as anti-cancer agents: design and synthesis of multi-acting inhibitors against HDAC, FLT3 and JAK2.
Novel naftopidil-related derivatives and their biological effects as alpha1-adrenoceptors antagonists and antiproliferative agents.
Synthesis, molecular modeling, and biological evaluation of novel RAD51 inhibitors.
Design, synthesis and biological evaluation of quinazoline derivatives as anti-trypanosomatid and anti-plasmodial agents.
Efficient synthesis and biological activity of Psammaplin A and its analogues as antitumor agents.
Design, synthesis and structure-activity relationship of oxazolidinone derivatives containing novel S4 ligand as FXa inhibitors.
Recent advances of chroman-4-one derivatives: synthetic approaches and bioactivities.
Synthesis of some substituted furan-2(5H)-ones and derived quinoxalinones as potential anti-microbial and anti-cancer agents
Binding of sodium houttuyfonate analogues to bovine serum albumin revealed by fluoresence quenching study
Quantitative structureactivity relationships of imidacloprid and its analogs with substituents at the C5 position on the pyridine ring in the neuroblocking activity
Synthesis and fungicidal activity of hydrazones containing 4-methylbenzo[d]thiazole moiety
Synthesis and Acaricidal Activities of New 2-Polyfluorophenylbenzazole Derivatives
Khayanolides, rearranged phragmalin limonoid antifeedants from Khaya senegalensis
Synthesis of novel Hantzsch dihydropyridines and Biginelli dihydropyrimidines of biological interest: a 3D-QSAR study on their cytotoxicity
Design, synthesis and biological evaluation of some novel 3-cinnamoyl-4-hydroxy-2H-chromen-2-ones as antimalarial agents
Insecticidal and Neuroblocking Activities of Thiacloprid and Its Acyclic Analogues and Their Related Cyanoguanidine Derivatives
Synthesis and pharmacological evaluation of m-terphenyl amines as cyclooxygenase inhibitors
Synthesis and in vitro antimicrobial activity of benzo[b][1,4]thiazin-3(4H)-ones via smiles rearrangement
Synthesis, crystal structure and -glucuronidase inhibition activity of some new hydrazinecarboxamides and their 1,2,4-triazole derivatives
N-[2(3-Carboxyl-9-benzyl-carboline-1-yl)ethyl-1-yl]-amino acids: correlation of spectral property with in vivo anti-tumor activity
1-(7-Chloroquinolin-4-yl)-2-[(1H-pyrrol-2-yl)methylene]hydrazine: a potent compound against cancer
Feeding cessation effects of chlorantraniliprole, a new anthranilic diamide insecticide, in comparison with several insecticides in distinct chemical classes and mode-of-action groups.
Quantitative structure activity relationship (QSAR) of N 6-substituted adenosine receptor agonists as potential antihypertensive agents
Residual and sublethal effects of fenpyroximate and pyridaben on the instantaneous rate of increase of Tetranychus urticae
Okaramine C, a New Insecticidal Indole Alkaloid from Penicillium simplicissimum.
Synthesis and comparative bioefficacy of N-(1-phenethyl-4-piperidinyl)propionanilide (fentanyl) and its 1-substituted analogs in Swiss albino mice
Synthesis and preliminary evaluation of 2-substituted-1,3-benzoxazole and 3-[(3-substituted)propyl]-1,3-benzoxazol-2(3H)-one derivatives as potent anticancer agents
Synthesis of 2-[4,5-dimethyl-1-(phenylamino)-1H-imidazol-2-ylthio]-N-(thiazole-2-yl)acetamide derivatives and their anticancer activities
Synthesis and Insecticidal Activity of 3, 5-Dimethylbenzoyl Moiety Modified Analogues of N-tert-Butyl-N-(4-ethylbenzoyl)-3, 5-dimethylbenzohydrazide
Synthesis and evaluation of antibacterial and antifungal activities of new (Z)-3-bromo-4-(1,3-diaryl-1H-pyrazol-4-yl)but-3-en-2-ones and 4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)-1,3-diaryl-1H-pyrazoles
Effect of propiconazole and difenoconazole on the control of anthracnose of chilli fruits caused by Colletotrichum capsici
Biological evaluation of imidazole derivatives as inhibitors of hydroperoxide lyase, a key enzyme in plant volatile biosynthesis
Synthesis and biologic activities of some novel heterocyclic chalcone derivatives
Antifeedant, insect growth regulatory and insecticidal effects of Calceolaria talcana (Calceolariaceae) on Drosophila melanogaster and Spodoptera frugiperda
Design and synthesis of some novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2-phenylquinazoline-4(3H)-ones as possible anticonvulsant agent
Antimycobacterial activity of fractions and isolated compounds from Vetiveria zizanioides
Syntheses and antiproliferative activity of some sulfated hydroximinosterols
Synthesis and Pesticidal Activities of N-Phosphinoyl Heterocycles
Management of tomato leaf mould caused by Cladosporium fulvum with trifloxystrobin
Tests for Evaluating the Side Effects of Chlorothalonil (TPN) and Spinosad on the Parasitic Wasp (Aphidius colemani)
Zn(OTf)2-catalyzed three component, one-pot cyclocondensation reaction of some new octahydroquinazolinone derivatives and access their bio-potential
Interaction studies of E. coli uracil phosphoribosyltransferase with 5-fluorouracil for potent anti cancer activity
Synthesis of novel 2-alkyl-4-substituted-amino-pyrazolo[3,4-d]pyrimidines as new leads for anti-bacterial and anti-cancer activity
Sensitivity of four isolates of Clonostachys rosea to pesticides used in the strawberry crop in Brazil
QSAR studies of 7-methyljuglone derivatives as antitubercular agents
Influence of soil fumigation on 2,4-D and dicamba carryover in fresh market tomato
Identification of an antiepileptic lead compound with a more selective activity and its analogues for GABA-AT using in silico approach
Synthesis and analgesic activity of new 1,3,4-oxadiazoles and 1,2,4-triazoles
Docking, synthesis, and pharmacological evaluation of isoindoline derivatives as anticonvulsant agents
Synthesis of 2-amino-6-oxocyclohexenylsulfonamides and their activity against Botrytis cinerea.
Synthesis and potential antibacterial activity of new rhodanine-3-acetic acid derivatives
Synthesis and antimicrobial activities of novel bisacridine-1,8-dione derivatives
Synthesis of coumarin-based 1,3,4-oxadiazol-2ylthio-N-phenyl/benzothiazolyl acetamides as antimicrobial and antituberculosis agents
Adzuki bean (Vigna angularis) responses to post-emergence herbicides
Synthesis, biological evaluation and molecular modeling studies of Schiff bases derived from 4-methylsalicylic acid as potential immunosuppressive agents
Insecticidal activities of crude extracts and phospholipids from Chenopodium ficifolium against melon and cotton aphid, Aphis gossypii
Synthesis of (substituted benzamidostyryl) lH-benzimidazoles and their screening for anti-inflammatory activity
Molecular modeling, structure activity relationship and immunomodulatory properties of some lupeol derivatives
Aromatic sulfonyl hydrazides and sulfonyl hydrazones: antimicrobial activity and physical properties
Synthesis and in vitro antimicrobial and anti-tubercular evaluation of some quinoline-based azitidinone and thiazolidinone analogues
N9- and N7-(Chloromethyl Phenymethyl)Chloropurine Derivatives from , '-Dichloroxylenes: Synthesis and Anticancer Activity
Design and synthesis of positional isomers of 1-alkyl-2-trifluoromethyl-5 or 6-substituted benzimidazoles and their antimicrobial activity
Synthesis and Antifungal Activities of Some Novel Pyrimidine Derivatives
Effect of Antibiotics on Formation of Aerial Mycelium and Production of Phytotoxins in Streptomyces spp.
Synthesis and biological evaluation of some stilbene derivatives
Synthesis, characterization, and antimicrobial studies of novel 1,3,4-thiadiazolium-5-thiolates
Piperamides and their derivatives as potential anti-trypanosomal agents
QSAR modeling of bifunctional quinolonyl diketo acid derivatives as integrase inhibitors
Antifeedant activities of tutin and 7-hydroxycoumarin acylation derivatives against Mythimna separata
Synthesis and cytotoxic activity of novel benzopyrano[3,2-c]chromene-6,8-dione derivatives
QSAR modeling of anthocyanins, anthocyanidins and catechins as inhibitors of lipid peroxidation using three-dimensional descriptors
Synthesis and biological evaluation of some new quinazolin-4(3H)-ones derivatives as anticonvulsants
Microwave-assisted synthesis of some novel and potent antibacterial and antifungal compounds with biological screening
Degradation of the Herbicides Thiobencarb, Butachlor and Molinate by a Newly Isolated Aspergillus niger
Synthesis and Rice-Blast Control Activity of Sulfonylamidines
Synthesis and antihyperlipidemic activity of novel condensed 2-fluoromethylpyrimidines
Induction of disease resistance by acibenzolar-S-methyl and o-hydroxyethylorutin against Botrytis cinerea in tomato plants
Synthesis and insect antifeedant activity of C-2 and C-5 substituted perhydrofurofurans and 3a-hydroxy-perhydrofurofurans (Part I)
Synthesis, antimalarial-, and antibacterial activity evaluation of some new 4-aminoquinoline derivatives
Natural products-based insecticidal agents 13. Semisynthesis and insecticidal activity of novel phenazine derivatives of 4-acyloxypodophyllotoxin modified in the E-ring against Mythimna separata Walker in vivo
Synthesis and preliminary evaluation activity studies of novel 4-(aryl/heteroaryl-2-ylmethyl)-6-phenyl-2-[3-(4-substituted-piperazine-1-yl)propyl]pyridazin-3(2H)-one derivatives as anticancer agents
Synthesis and herbicidal activity of N-oxide derivatives.
Molecular modeling and protection against pentylenetetrazole-induced seizure of new 1,4-dihydropyridines containing 5(4)-imidazolyl substituent
Synthesis, characterization and biological activity of Schiff bases derived from metronidazole
Synthesis and insecticidal activities of novel N-sulfenyl-N'-tert-butyl-N,N'-diacylhydrazines. 3. N-(alkyldithio), n-(aminothio), and N,N-dithio derivatives.
Safening efficacy of halogenated acetals, ketals and amides and relationship between the structure and effect on glutathione and glutathione S-transferases in maize
Synthesis, characterization, antioxidant, and anticancer studies of 6-[3-(4-chlorophenyl)-1H-pyrazol-4-yl]-3-[(2-naphthyloxy)methyl][1,2,4]triazolo[3,4-b][1,3,4]thiadiazole in HepG2 cell lines
Synthesis of some new glutamine linked 2,3-disubstituted quinazolinone derivatives as potent antimicrobial and antioxidant agents
Synthesis, characterization, and antimicrobial activity of some new 2-diazo-benzimidazole derivatives and their Ni(II), Cu(II), and Ag(I) complexes
Herbicidal potential of pseudoguaninolide sesquiterpenes on wild oat, Avena fatua L.
Synthesis, characterization, and pharmacological evaluation of new GABA analogs as potent anticonvulsant agents
Studies on fused heterocyclic 3,6-disubstituted-1,2,4-triazolo-1,3,4-thiadiazoles: synthesis and biological evaluation
Synthesis, spectral studies and biological evaluation of a novel series of 2-substituted-5,6-diarylsubstituted imidazo(2,1-b)-1,3,4-thiadiazole derivatives as possible anti-tubercular agents
Synthesis and QSAR modeling 1-[3-methyl-2-(aryldiazenyl)-2H-aziren-2-yl]ethanones as potential antibacterial agents
Effect of phenolic compounds on growth and ligninolytic enzyme production in Botryosphaeria isolates
Synthesis of pyrazole-based 1,5-diaryl compounds as potent anti-inflammatory agents
Homology modeling of human CCR2 receptor
Structure-based molecular design, synthesis, and in vivo anti-inflammatory activity of pyridazinone derivatives as nonclassic COX-2 inhibitors
Synthesis and Acaricidal Activities of New Benzophenone O-Methyloximes
Syntheses, spectral, crystallographic, antimicrobial, and antioxidant studies of few Mannich bases
Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of nicotinic acid benzylidene hydrazide derivatives
Pyrazolecarboxylic acid derivative induces systemic acquired resistance in tobacco.
Search of antimycobacterial activities in hybrid molecules with benzopyran skeleton
In vivo evaluation of substituted 3-phenyl,7-methoxy-benzopyrans as modified estrogens
Design of potent human steroid 5-reductase inhibitors: 3D-QSAR CoMFA, CoMSIA and docking studies
Synthesis of Alkylene-Tethered Bis-Imidacloprid Derivatives as Highly Insecticidal and Nerve-Exciting Agents with Potent Affinity to [3H] Imidacloprid-Binding Sites on Nicotinic Acetylcholine Receptor
Photooxygenation of Nimonol, a Tetranortriterpenoid from Azadirachta indica. A. Juss.
Molecular properties of fatty acids related to PPAR binding and metabolic diseases
QSAR study of 1,3dioxo-4-methyl-2,3-dihydro-1h-pyrrolo[3,4-c]quinolines as caspase-3 inhibitors
QSAR modeling of synthesized 3-(1,3-benzothiazol-2-yl) 2-phenyl quinazolin-4(3H)-ones as potent antibacterial agents
Synthesis and preliminary antibacterial evaluation of hydroxamic acid and N-formyl hydroxylamine derivatives bearing oxazole ring
Cytotoxic and genotoxic potentials of newly synthesized antiviral aminopyrazoloquinoline derivatives
Modifications to five-substituted 3,3-diethyl-4,5-dihydro-2(3H)-furanones en route to novel muscarinic receptor ligands
Design, synthesis, and cytotoxic activities of new 2,4,5-triarylimidazoles
Broad-spectrum antimicrobial activity in vitro of the synthetic peptide D4E1.
Synthesis and antifungal activity of 1-substitutedphenyl-3-(5-halobenzimidazol-2-yl) acylurea
Synthesis and biological evaluation of new [1,3,4]thiadiazepino[7,6-b]quinolin-2-amines as potent anti-microbial agents
Molecular insights to explore abietane diterpenes as new LOX inhibitors
11-Chloro-3-methyl-3H-imidazo[4,5-a]acridine (CMIA) as a potent and selective antimicrobial agent against clinical isolates of highly antibiotic-resistant Acinetobacter baumannii
Kinetic studies of novel inhibitors of endomorphin degrading enzymes.
Mode of Action of Cyanohydrins in Insects
Quinolactacide, a new quinolone insecticide from Penicillium citrinum Thom F 1539.
Effects of imidacloprid on transmission of tomato spotted wilt tospovirus to pepper, tomato and tobacco by Frankliniella fusca Hinds (Thysanoptera: Thripidae)
Lonazolac analogues: molecular modeling, synthesis, and in vivo anti-inflammatory activity
Initial activity and persistence of insecticides for the control of bollworms (Lepidoptera: Noctuidae) in cotton crops
Isolation and anxiolytic activity of 3,4-bis(3,4-dimethoxyphenyl)furan-2,5-dione from the ethanolic extract of heart wood of Cedrus deodara
Synthesis and in vitro antimicrobial evaluation of penta-substituted pyridine derivatives bearing the quinoline nucleus
Comparison of the declining triazole sensitivity of Gibberella zeae and increased sensitivity achieved by advances in triazole fungicide development
Sensitivity of Cucumber Powdery Mildew Fungus (Sphaerotheca fuliginea) to Several Fungicides
Introduction to Receptors in Aging Diseases: GABA Receptors
Synthesis and antimicrobial activity of novel bis-azaphenothiazines
Synthesis, characterization and antimicrobial activity of novel ethyl 1-(N-substituted)-5-phenyl-1H-pyrazole-4-carboxylate derivatives
Effects of Pyridalyl on ATP Concentrations in Cultured Sf9 Cells
Isocoumarin Derivative as a Novel GABA Receptor Ligand from Neosartorya quadricincta
New brassinosteroid analogs having nitrogenated functionalities at C3 to provide more information about the brassinosteroidreceptor interaction
Synthesis and Herbicidal Activity of N-Alkyl-N-(substituted benzyl)-4-halo-2-alkenamides
Synthesis, anti-inflammatory, and structure antioxidant activity relationship of novel 4-quinazoline
Design, synthesis, and biological evaluation of novel pyridine acid esters of podophyllotoxin and esters of 4-demethylepipodophyllotoxin
Biological evaluation of novel 1,4-dithiine derivatives as potential antimicrobial agents
Seed and leaf treatments with natural compounds to induce resistance against Peronospora parasitica in Brassica oleracea
Synthesis and biological evaluation of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives as antidepressant, anxiolytics and anticonvulsant agents
Synthesis and Insecticidal Activity of O-Aryl N-Alkoxycarbonyl-N-alkylmethylphosphonamidothionates
Antihepatotoxic activity of a sterol glucoside from aerial parts of Clerodendrum phlomidis
New antiepileptic agents: structureactivity relationships
QSAR analysis of centrally fused 1,5-diaryl pyrazoles for cyclooxygenase inhibition using MOE-Qua-SAR descriptors
1-(6-Chloronicotinyl)-2-nitroimino-imidazolidines and Related Compounds as Potential New Insecticides
Synthesis, spectral, and antimicrobial evaluation of some new 8-membered phosphorus heterocyclic compounds
Synthesis, characterization, and pharmacological evaluation of benzothiopyran derivatives as a novel class of calcium channel blockers
Synthesis and evaluation of 7-substituted-3,4-dihydrobenzo[f][1,4]oxazepin-5(2H)-ones as anticonvulsant and hypnotic agents
Antibacterial and antifungal screening of newly synthesized benzimidazole-clubbed chalcone derivatives
Synthesis of new phenylcarbamoylbenzoic acid derivatives and evaluation of their in vitro antioxidant activity
Design, synthesis and pharmacological screening of hybrid molecules as antihypertensives
Synthesis and anti-juvenile hormone activity of ethyl 4-[(6-substituted 2,2-dimethyl-2H-chromen-7-yl)methoxy]benzoates
Resistance of Helicoverpa assulta (Guenee) (Lepidoptera: Noctuidae) to fenvalerate, phoxim and methomyl in China
Fungicidial Activity of Benthiavalicarb-isopropyl against Phytophthora infestans and Its Controlling Activity against Late Blight Diseases
Synthesis of pyrimidine and condensed pyrimidine derivatives and their evaluation for anti-inflammatory activity
Exploring QSAR of antiamoebic agents of isolated natural products by MLR, ANN, and RTO
Synthesis of piperazinyl benzothiazole/benzoxazole derivatives coupled with 1,3,4-oxadiazole-2-thiol: novel hybrid heterocycles as anticancer agents
Molecular modeling studies of some substituted chalcone derivatives as cysteine protease inhibitors
Effect of s-metolachlor application timing on cabbage tolerance
Antioxidant potential and antimicrobial screening of some novel imidazole derivatives: greenway efficient one pot synthesis
Design and synthesis of 2-quinolones as antioxidants and antimicrobials: a rational approach
Biologically active secondary metabolites of endophytic Pezicula species
Synthesis and blood glucose lowering activity of some novel benzenesulfonylurea derivatives substituted with 6-aryl-4,5-dihyropyridazin-3(2H)-ones
Antifeedant activity of plant extracts and of new natural diglyceride compounds isolated from Ajuga pseudoiva leaves against Spodoptera littoralis larvae
Evaluation of a new lead for acetylcholinesterase inhibition
Synthesis and in vivo anticancer and antiangiogenic effects of novel thioxothiazolidin-4-one derivatives against transplantable mouse tumor
Synthesis of 2-R1-2-(4-(2-fluoroethoxy)benzamido)acetate as potential PET imaging agents
7-Piperazinylquinolones with methylene-bridged nitrofuran scaffold as new antibacterial agents
Synthesis and antimalarial evaluation of novel pyridine quinoline hybrids
Synthesis and anti-inflammatory evaluation of some new 3,6-disubstituted-1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazoles bearing pyrazole moiety
Novel 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones and cyclohexanols as analgesic and anti-inflammatory agents
Plant tissue distribution and chemical inactivation of six carnation viruses
Total synthesis of cis-solamin and its inhibitory action with bovine heart mitochondrial complex I
Syntheses and in vitro biological screening of 1-aryl-10H-[1,2,4]triazolo[3,4:3,4][1,2,4]triazino[5,6-b]indoles
Novel tetranortriterpenoid derivatives from Munronia henryi
Evaluation of fungicides for the management of Botryosphaeria dieback diseases of grapevines.
Development of a Novel Insecticide, Dinotefuran
The synthesis and investigation of the antimicrobial activity of some new phenylselanyl-1-(toluene-4-sulfonyl)-1H-tetrazole derivatives
Synthesis and antimicrobial activity of new pyridine derivatives-I
1,6-Bis[1-(2-chloro-5-thiazolylmethyl)-2-nitroiminoimidazolidin-3-yl]hexane and 1,3,5-tris[1-(6-chloronicotinyl)-2-nitroiminoimidazolidin-3-ylmethyl]benzeneSynthesis and insecticidal and neuroblocking activities in American cockroaches, Periplaneta americana
Synthesis, antiplatelet aggregation activity, and molecular modeling study of novel substituted-piperazine analogues
Synthesis and pharmacological evaluation of newer thiazolo [3,2-a] pyrimidines for anti-inflammatory and antinociceptive activity
Molecular Mechanism for Selective Toxicity of Nicotinoids and Neonicotinoids
Synthesis and antimicrobial activities of N-chloroacetyl-2,6-diarylpiperidin-4-ones
Design, synthesis, and structureactivity relationship study of 5-amido-1-(2,4-dinitrophenyl)-1H-4-pyrazolecarbonitrils as DD-carboxypeptidase/penicillin-binding protein inhibitors with Gram-positive antibacterial activity
Novel PCU cage diol peptides as potential targets against wild-type CSA HIV-1 protease: synthesis, biological screening and molecular modelling studies
Synthesis of some sulfonamides, disubstituted sulfonylureas or thioureas and some structurally related variants. A class of promising antitumor agents
Six new triterpenoid saponins from the leaves of Ilex oblonga and their inhibitory activities against TMV replication.
MODULATION OF FILARIAL GLUTATHIONE-S-TRANSFERASE(S) ACTIVITY: A POSSIBILITY TOWARDS THE SYNTHESIS OF NEW CLASSES OF ANTIFILARIAL AGENTS
Insecticidal activity influence of beta-cypermethrin on the pathogenicity of Beauveria bassiana against Aleurodicus disperses
Laboratory assays of select candidate insecticides for control of Dendroctonus ponderosae.
Synthesis of some novel amino and thiotetrazole purine derivatives and investigation of their antimicrobial activity and DNA interactions
In vitro and in silico exploration of IL-2 inhibition by small drug-like molecules
Six insecticidal isoryanodane diterpenoids from the bark and twigs of Itoa orientalis
The synthesis and screening of the antimicrobial activity of some novel 3-(furan-2-yl)-1-(aryl)-3-(phenylthio) propan-1-one derivatives
Antimicrobial and insect antifeedant activities of some Trogers bases
Synthesis and investigation of anti-inflammatory activity of novel nitric oxide donating hybrid drugs
Synthesis of novel 4-thiazolidione derivatives as antibacterial agents against drug-resistant Staphylococcus epidermidis
A facile synthesis of novel optically active R,R-2-(4-(2-(4-(5-chloro-3-halo-pyridin-2-yloxy)-phenoxy)-propionyloxy)-phenoxy)-propionic acid esters using cyanuric chloride as potential herbicide
Synthesis of N-Alkyl-2, 3-dimethyl-5-[N-(5-halo-2-methylphenyl)carbamoyl]-6-pyrazinecarboxamides and Their Herbicidal Activity
Quercetin inhibits inflammatory bone resorption in a mouse periodontitis model.
Validation of Reactivity Descriptors to Assess the Aromatic Stacking within the Tyrosine Gate of FimH.
Aza-cycloisodityrosine analogue of RA-VII, an antitumor bicyclic hexapeptide.
Endothelial lipase inhibitors for the treatment of atherosclerosis and cardiovascular disorders.
Benzoxazine Derivatives As CRAC Modulators.
Structure-activity relationships of retro-dihydrochalcones isolated from Tacca sp.
Aminopyridyl/Pyrazinyl Spiro[indoline-3,4'-piperidine]-2-ones As Highly Selective and Efficacious c-Met/ALK Inhibitors.
The most effective influence of 17-(3-ethoxypropyl) substituent on the binding affinity and the agonistic activity in KNT-127 derivatives, opioid receptor agonists.
Protein-Ligand Interactions: Thermodynamic Effects Associated with Increasing the Length of an Alkyl Chain.
Melosuavines A-H, cytotoxic bisindole alkaloid derivatives from Melodinus suaveolens.
Function-regulating pharmacophores in a sulfonamide class of glucocorticoid receptor agonists.
Improved Cav2.2 Channel Inhibitors through a gem-Dimethylsulfone Bioisostere Replacement of a Labile Sulfonamide.
Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example.
Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates.
Sphingosine-1-phosphate (S1P) Receptor Modulators Provide Potential for Diverse Treatments.
Hinokitiol inhibits cell growth through induction of S-phase arrest and apoptosis in human colon cancer cells and suppresses tumor growth in a mouse xenograft experiment.
Cytotoxic ent-kaurane diterpenoids from Salvia cavaleriei.
Ethoxysanguinarine Induces Inhibitory Effects and Downregulates CIP2A in Lung Cancer Cells.
Synthesis and structure-activity relationship studies of N-terminal analogues of the antimicrobial peptide tridecaptin A(1).
Qualification of LSP1-2111 as a Brain Penetrant Group III Metabotropic Glutamate Receptor Orthosteric Agonist.
Design, synthesis and evaluation of second generation MurF inhibitors based on a cyanothiophene scaffold.
Hydroxy fatty acids for the delivery of dideoxynucleosides as anti-HIV agents.
Small Macrocycles As Highly Active Integrin 21 Antagonists.
Selective EP4 Antagonist May Be Useful in Treating Arthritis and Arthritic Pain.
Biological evaluation of diazene derivatives as anti-tubercular compounds.
Constrained TRPV1 agonists synthesized via silver-mediated intramolecular azo-methine ylide cycloaddition of -iminoamides.
Synthesis and antimicrobial activities of novel 1,2,4-triazolo [3,4-a] phthalazine derivatives.
Discovery of 1-methyl-1H-imidazole derivatives as potent Jak2 inhibitors.
Selective COX-1 inhibition as a target of theranostic novel diarylisoxazoles.
Neutral -Lactams Inactivate High Molecular Mass Penicillin-Binding Proteins of Class B1, Including PBP2a of MRSA.
Novel lung adenocarcinoma and nuclear factor-kappa B (NF-B) inhibitors: synthesis and evaluation of lantadene congeners.
Synthesis and biological activity of polyalthenol and pentacyclindole analogues.
Novel, sulfonamide linked inhibitors of the hepatitis C virus NS3 protease.
MMV box selection for compounds with potential use in combination with artemisinin using S. cerevisiae
Antileishmanial activity of quinazoline derivatives: synthesis, docking screens, molecular dynamic simulations and electrochemical studies.
Recent advances in the development of acetyl-CoA carboxylase (ACC) inhibitors for the treatment of metabolic disease.
Proteasome inhibitors with pyrazole scaffolds from structure-based virtual screening.
Synthesis and antitumor activity of ring A modified 11-keto--boswellic acid derivatives.
Design, synthesis and evaluation of a novel class of glucosamine mimetic peptides containing 1,3-dioxane.
Substituted pyrrolidin-2-ones: Centrally acting orexin receptor antagonists promoting sleep. Part 2.
Synthesis, biological evaluation and 3D QSAR study of 2,4-disubstituted quinolines as anti-tuberculosis agents.
Probes for narcotic receptor mediated phenomena 49. N-substituted rac-cis-4a-arylalkyl-1,2,3,4,4a,9a-hexahydrobenzofuro[2,3-c]pyridin-6-ols.
1,3,4-Thiadiazoles: a potent multi targeted pharmacological scaffold.
Highly selective salicylketoxime-based estrogen receptor agonists display antiproliferative activities in a glioma model.
Design and synthesis of a new class of cryptophycins based tubulin inhibitors.
Exploring new selective 3-benzylquinoxaline-based MAO-A inhibitors: design, synthesis, biological evaluation and docking studies.
Recent advances in the chemistry and biology of pyridopyrimidines.
Development of potent inhibitors of pyocyanin production in Pseudomonas aeruginosa.
Synthesis, characterization, solvatochromic properties, and antimicrobial evaluation of 5-acetyl-2-thioxo-dihydro-pyrimidine-4,6-dione-based chalcones
Synthesis of biotinylated 18-glycyrrhetinic acid and its effect on tumor cells activity
Synthesis of analogues of antihyperglycemic lead karanjin
Synthesis and cytotoxicity of novel N-sulfonyl-1,2,3,4-tetrahydroisoquinoline thiosemicarbazone derivatives
Syntheses and evaluation of 2,5-disubstituted 4-thiazolidinone analogues as antimicrobial agents
Synthesis of novel biologically active methylene derivatives of sydnones
Pharmacophagous feeding stimulant activity of neo-clerodane diterpenoids for the turnip sawfly, Athalia rosae ruficornis
Synthesis and Phytotoxic Activities of N-Substituted Phenyl Isothiazolone Derivatives
Synthesis and evaluation of biological and nonlinear optical properties of some novel 2,4-disubstituted [1,3]-thiazoles carrying 2-(aryloxymethyl)-phenyl moiety
Molecular modeling and pharmacophore approach for structural requirements of some 2-substituted-1-naphthols derivatives as potent 5-lipoxygenase inhibitors
The antimycobacterial MICs, SARs, and QSARs of some ethnobotanically selected phytocompounds
Phyllostictines AD, oxazatricycloalkenones produced by Phyllosticta cirsii, a potential mycoherbicide for Cirsium arvense biocontrol
Synthesis, characterization, in vitro hydrolysis and pharmacodynamic profiles of potential novel mutual prodrugs of N-(2,3-xylyl anthranilic acid)
Structure-based design, synthesis, and molecular modeling studies of 1-(benzo[d]thiazol-2-yl)-3-(substituted aryl)urea derivatives as novel anti-Parkinsonian agents
Isobutyl amides--potent compounds for controlling Diatraea saccharalis.
Polyamines May Modulate Both G Protein-Coupled Receptors and G Proteins
Physcion, a natural anthraquinone derivative, enhances the gene expression of leaf-specific thionin of barley against Blumeria graminis.
Distribution of trunk-injected 14C-imidacloprid in ash trees and effects on emerald ash borer (Coleoptera: Buprestidae) adults
Design, synthesis and in vitro antimicrobial activity of novel phenylbenzamido-aminothiazole-based azasterol mimics
Weed control in sunn hemp and its ability to suppress weed growth
Synthesis and Insecticidal Activity of Lignan Analogs. (1).
Lethal Activity of a Trehalase Inhibitor, Validoxylamine A, against Mamestra brassicae and Spodoptera litura
Design, Synthesis and Evaluation of Trisubstituted Thiazoles Targeting Plasmodium Falciparum Cysteine Proteases
Inhibitory Activities of Rhodanine Derivatives on Plant Growth
Comparative 3D QSAR study on (1)-, (2)-, and (3)-adrenoceptor agonists.
Synthesis, antitubercular and antifungal activities of heteroaryl-substituted oxiranes derived from BaylisHillman adducts
GdCl3 promoted synthesis of novel pyrimidine fused indazole derivatives and their anticancer activity
Chemistry, toxicity and antifeedant activity of the resin of Flourensia thurifera
A brief synthesis of natural antifeedant, 1-(2,4,6-trimethoxyphenyl) but-2(E)-en-1-one
Studies on toxicity of antitubercular drugs namely isoniazid, rifampicin, and pyrazinamide in an in vitro model of HepG2 cell line
Synthesis, characterization, and in vitro anti-Mycobacterium tuberculosis activity of terpene Schiff bases
QSAR modeling of some substituted benzimidazole as Angotensin II AT1 receptor antagonist
3D-QSAR studies on the biological activity of juvenile hormone mimetic compounds for Culex pipiens Larvae
Microwave-assisted synthesis, pharmacological evaluation, and QSAR studies of 1,3-diaryl-2-propen-1-ones
Weed control and sweet maize (Zea mays L.) yield as affected by pyroxasulfone dose
Lethal and sublethal effects of buprofezin and imidacloprid on the whitefly parasitoid Encarsia inaron (Hymenoptera: Aphelinidae)
The action of herbicides on fatty acid biosynthesis and elongation in barley and cucumber.
Simple and Rapid Screening Method for Photosystem II Inhibitory Herbicides Using Photoautotrophically Cultured Plant Cells with Chlorophyll Fluorescence Monitoring
Molecular Basis of Resistance to s-Triazine Herbicides in Poa annua L. and Its Photosynthetic Properties under Different Light Conditions
Synthesis and nematocidal activity of ascaridole derivatives against Meloidogyne incognita and Aphelenchoides besseyi
Carboxylesterase of the Rice Stem Borer, Chilo suppressalis WALKER (Lepidoptera: Pyralidae), Responsible for Fenitrothion Resistance as a Sequestering Protein
Comparing weed and crop seedling response to pre-emergence pendimethalin application in Corchorus olitorius and Abelmoschus esculentus
Evaluation of antiasthmatic activity of 7,8,9,10-tetrahydroazepino[2,1-b]quinazolin-12(6H)-one in combination with ambroxol in Guinea pigs
Synthesis and Structure-Activity Relationships of Vasicine Analogues as Bronchodilatory Agents
In vitro antioxidant properties and in vivo lowering blood lipid of Forsythia suspense leaves
Antihepatotoxic activity of ferolactone, a new furanocoumarin from Feronia limonia
Antifungal activity of some tetranortriterpenoids
Synthesis and biological evaluation of novel benzoquinones as potential antimicrobial agents
Design, synthesis, and biologic evaluation of some novel N-arylpyrazole derivatives as cytotoxic agents
JS399-19, a new fungicide against wheat scab
Nitrogen concentration and application timing affect imazamox efficacy in winter wheat
Synthesis, characterization and anticancer activity of 3-aza-analogues of DP-7
Synthesis and antiprotozoal activity of 1,2,3,4-tetrahydro-2-thioxopyrimidine analogs of combretastatin A-4
Synthesis, in vitro antimicrobial and antioxidant activities of chalcone and flavone derivatives holding allylic substitutions
Morphogenetic and Toxic Activity of Seven Novel 2, 2-Dimethylchromene Derivatives on Larvae of Oncopeltus fasciatus and Pieris brassicae
A comparative study of the efficiency of several sources of induced resistance to powdery mildew (Blumeria graminis f. sp. tritici) in wheat under field conditions
Target-site mutation associated with glufosinate resistance in Italian ryegrass (Lolium perenne L. ssp. multiflorum).
Synthesis and herbicidal activity of alkyl 1-(3-trifluoromethylphenoxyacetoxy)-1-substituted methylphosphonates
QSAR analysis of Mur B inhibitors with antibacterial properties discussing role of physico-chemical parameters
Bloodbrain barrier permeability and transport studies of JLK1486: a new antiglioblastoma drug
Seasonal changes in chemical composition of epicuticular waxes from the leaves of Baccharis linearis
Inhibitory effects on nuclear factor B of the Vietnamese freshwater cyanobacteria
Mode of Action of Herbicidal N-Benzyl-4-chloro-N-isobutyl-2-pentenamides
Antifeedant and mosquitocidal compounds from Delphinium x cultorum cv. Magic fountains flowers.
Evaluation of Benzenesulfonanilide Derivatives for the Control of Crucifers Clubroot
Microwave-induced CAN promoted atom-economic synthesis of 1H-benzo[b]xanthene and 4H-benzo[g]chromene derivatives of N-allyl quinolone and their antimicrobial activity
Carpropamid, a New Fungicide for Rice Blast Control
Design, synthesis, and evaluation of anti-inflammatory and ulcerogenicity of novel pyridazinone derivatives
Synthesis and Acaricidal Activity of 1-Arylmethyl-2-arylimidazolidines
Synthesis and in vitro microbial activities of amides of pyridoquinolone
Design, synthesis and biological evaluation of some novel substituted 2-mercapto-3-phenethylquinazolines as antitumor agents
Synthesis and in vitro anti-Helicobacter pylori activity of 2-[(chlorobenzyl)thio]-5-(5-nitro-2-furyl)-1,3,4-thiadiazoles
New carbodithioate derivatives: synthesis, characterization, and in vitro antibacterial, antifungal, antitubercular, and antimalarial activity
Synthesis, characterization, antibacterial, antifungal, and immunomodulating activities of gatifloxacin derivatives
Docking study, in vitro anticancer screening and radiosensitizing evaluation of some new fluorine-containing quinoline and pyrimidoquinoline derivatives bearing a sulfonamide moiety
Synthesis and Insecticidal Activity of N-(Tolyloxybenzyl)-pyrazolecarboxamide Derivatives
Anticonvulsant activity of 3,5-dimethylpyrazole derivatives in animal models
Synthesis, antimicrobial and cytotoxic activities of novel 4-trifluoromethyl-(1,2,3)-thiadiazolo-5-carboxylic acid hydrazide Schiffs bases
Synthesis and pharmacological investigation of novel 2-substituted-3-carboxamido-4H-pyrimidobenzothiazole derivatives as a new class of H1-antihistaminic agent
Synthesis and biological activities of Schiff bases of gabapentin with different aldehydes and ketones: a structureactivity relationship study
Composition and antifungal activity on soil-borne pathogens of the essential oil of Salvia sclarea from Greece.
Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies
Synthesis and antimicrobial evaluation of some novel 1,2,4-triazole and 1,3,4-thiadiazole derivatives.
Synthesis and biological activity studies of furan derivatives
Synthesis and structureactivity relationships of serotonin derivatives effect on -glucosidase inhibition
Evaluation of systemic acquired resistance inducers for control of Phytophthora capsici on squash
Antiangiogenic and growth inhibitory effects of synthetic novel 1, 5-diphenyl-1,4 pentadiene-3-one-3-yl-ethanone pyridine curcumin analogues on Ehrlich ascites tumor in vivo
Synthesis and biological activities of novel pyrazole oxime derivatives containing a 2-chloro-5-thiazolyl moiety.
Immunomodulatory active steroidal saponins from Asparagus racemosus
Synthesis of N-hydroxycinnamoyl amino acid ester analogues and their free radical scavenging and antioxidative activities
Anti-HIV-1 and cytotoxicity studies of piperidyl-thienyl chalcones and their 2-pyrazoline derivatives
Synthesis and biological evaluation of diamide derivatives of (S)-BINOL and biphenyl as potential anti-inflammatory/anti-arthritic agents
In vitro reactivation of organophosphorus (OP)-inhibited electric eel acetylcholinesterase by novel monoquaternary pyridinium oximes
Molecular docking of glycogen synthase kinase3- inhibitor oleanolic acid and its wound-healing activity in rats
Benzimidazole: a medicinally important heterocyclic moiety
Design, synthesis, and biological evaluation of new 4-thiazolidinone derivatives substituted with benzimidazole ring as potential chemotherapeutic agents
Antimicrobial activity of Schiff bases of coumarin-incorporated 1,3,4-oxadiazole derivatives: an in vitro evaluation
Synthesis and Herbicidal Activity of New 2-(1-Carbamoyl-1, 2, 4-triazol-3-ylsulfonyl) alkanoates
Quantitative Structure-Activity Relationships of Fluazinam and Related Fungicidal N-Phenylpyridinamines
Optimization of biological (Phasmarhabditis hermaphrodita) and chemical (iron phosphate and metaldehyde) slug control
Synthesis and in vitro anticancer activities of novel aryl-naphthalene lignans
Herbicidal Activity and Characteristics of Pyraflufen-ethyl for Controlling Broad-leaved Weeds in Cereals
A facile and single pot strategy for the synthesis of novel naphthyridine derivatives under microwave irradiation conditions using ZnCl2 as catalyst, evaluation of AChE inhibitory activity, and molecular modeling studies
Synthesis and in vitro antiproliferative activity of novel 12(H)-quino[3,4-b][1,4]benzothiazine derivatives.
Synthesis and biological evaluation of novel series of thieno[2,3-d]pyrimidine derivatives as anticancer and antimicrobial agents
Composition of essential oil of Chinese Chenopodium ambrosioides and insecticidal activity against maize weevil, Sitophilus zeamais.
In vivo antifilarial activity of some cyclic and acylic alcohols
Synthesis of analogues of monic acids A and C: Potential herbicides and inhibitors of isoleucyl tRNA synthetase
Synthesis and analgesic activity of new pyridine-based heterocyclic derivatives
Synthesis, antimicrobial evaluation, ot-QSAR and mt-QSAR studies of 2-amino benzoic acid derivatives
Lupeol-3-O-decanoate, a new triterpene ester from Cadaba farinosa Forssk. growing in Saudi Arabia
Chemical control of Prosopis farcta (Banks and Sol.) Macbride in the Jordan Valley
Structureactivity relationship investigation of methoxy substitution on anticancer pyrimido[4,5-c]quinolin-1(2H)-ones
Photosynthetic Electron Transport Inhibitory and Herbicidal Activities of 2-(Fluorinated methyl-4-benzylamino-6-methyl)-1, 3, 5-triazines
QSAR STUDIES ON ADENOSINE KINASE INHIBITORS
Chemical composition and antifungal activity of essential oil of Chrysactinia mexicana gray.
Antibacterial activity of alkyl gallates and related compounds against Ralstonia solanacearum
Microwave-assisted synthesis and evaluation of anti-inflammatory activity of new series of N-substituted 2-butyl-5-chloro-3H-imidazole-4-carbaldehyde derivatives
Investigation of myorelaxant activity of 9-aryl-3,4,6,7-tetrahydroacridine-1,8-(2H,5H,9H,10H)-diones in isolated rabbit gastric fundus
Antimicrobial and antiprotozoal activities of secondary metabolites from the fungus Eurotium repens.
Management of Macrophomina wilt in melons using grafting or fungicide soil application: Pathological, horticultural and economical aspects
Synthesis of antihyperglycemic, -glucosidase inhibitory, and DPPH free radical scavenging furanochalcones
Synthesis and biological evaluation of chalcones and acetyl pyrazoline derivatives comprising furan nucleus as an antitubercular agents
Potential cytotoxic and apoptosis inducing agents: synthesis and evaluation of methoxy-substituted chalcones against human lung and cervical cancers
Effect of Buprofezin on Oviposition of Brown Planthopper, Nilaparvata lugens, at Sub-lethal Dose
Synthesis and bioevaluation of novel arylnaphthalene lignans as anticancer agents
Homology modeling and docking study of recent SHV type -lactamses with traditional and novel inhibitors: an in silico approach to combat problem of multiple drug resistance in various infections
Synthesis, antimicrobial evaluation, and QSAR analysis of 2-isopropyl-5-methylcyclohexanol derivatives
Precocious Metamorphosis-Inducing Activity of 1-Substituted Imidazoles
Optical Resolution and Biological Activities of S-23121, a New Cereal Herbicide.
Action of benzimidazolo-piperazinyl derivatives on dopamine receptors
Microwave-irradiated synthesis and antimicrobial activity of 2-phenyl-7-substitutedalkyl/arylaminoquinoline-4-carboxylic acid derivatives
Antiviral and Antifungal Activities of Some Naphthoquinones Isolated from the Roots of Lithospermum erythrorhizon
Synthesis and Herbicidal Activity of Sulfonylureas; SL-950 and Its Related Compounds
Potent antimalarial activity of newly synthesized substituted chalcone analogs in vitro
Sensitivity difference to insecticides of a riverine caddisfly, Cheumatopsyche brevilineata (Trichoptera: Hydropsychidae), depending on the larval stages and strains
Antimicrobial screening of novel synthesized benzimidazole nucleus containing 4-oxo-thiazolidine derivatives
Synthesis and Herbicidal Activity of Pyrimidinyl Salicylic and Thiosalicylic Acids
Synthesis and antitumor screening of new series of pyrimido-[4,5-b]quinolines and [1,2,4]triazolo[2,3:3,4]pyrimido[6,5-b]quinolines
Synthesis of 3-{4-[4-dimethylamino-6-(4-methyl-2-oxo-2H-chromen-7-yloxy)-[1,3,5]triazin-2-ylamino]-phenyl}-2-phenyl-5-(4-pyridin-2-yl-piperazin-1-ylmethyl)-thiazolidin-4-one and their biological evaluation
Synthesis and characterization of flurbiprofen hydrazide derivatives as potential anti-HCV, anticancer and antimicrobial agents
2D-QSAR of non-benzodiazepines to benzodiazepines receptor (BZR)
Synthesis and Fungitoxic Activity of N-Cinnamoyl--Amino Acid Esters
3D-pharmacophore model based virtual screening to identify dual-binding site and selective acetylcholinesterase inhibitors
New dihydropyridine derivatives: anti-inflammatory, analgesic and docking studies
Synthesis, characterization, bioactivity, and POM analyses of isothiochromeno[3,4-e][1,2]oxazines
Synthesis, biological evaluation and molecular docking studies of 1,3-benzoxazine derivatives as potential anticancer agents
Effects of acibenzolar-S-methyl on the suppression of Fusarium wilt of cyclamen
Microwave-assisted synthesis of pyrido[1,2-a]benzimidazole derivatives of -aryloxyquinoline and their antimicrobial and antituberculosis activities
C(18) acetylenic fatty acids of Ximenia americana with potential pesticidal activity.
Synthesis and pharmacological evaluation of antioxidant chalcone derivatives of 2(3H)-benzoxazolones
Serotonin transporter activity of imidazolidine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives in aspect of their acid-base properties.
Effectiveness of 1,3-dichloropropene as an alternative to methyl bromide in rotations of tomato (Solanum lycopersicum) and cucumber (Cucumis sativus) in China
Synthesis and anticancer effects of pongamol derivatives on mitogen signaling and cell cycle kinases
Synthesis and evaluation of -opioid receptor agonistic activity and antinociceptive effect of novel morphine analogues, 7-phenyl-6,14-endo-etheno-tetrahydrothebaine with substituted o-, m- and p-amino group
ROLE OF INTERMEDIARY BIOMARKERS IN DETERMINING THE ANTICANCER EFFICACY OF MARINE COMPOUNDS
Antimicrobial evaluation of 4-methylsulfanyl benzylidene/3-hydroxy benzylidene hydrazides and QSAR studies
Conventional and microwave-assisted synthesis of imidazole and guanidine derivatives and their biological evaluation
Salicylic acid induced defence responses in Curcuma longa (L.) against Pythium aphanidermatum infection
Synthesis of 3,5-disubstituted isoxazolines as protein tyrosine phosphatase 1B inhibitors
Heteroaromatic analogues of 1,5-diarylpyrazole class as anti-inflammatory agents
,-Dibromoacetophenones mediated synthesis of some new 7H-7-alkoxy-3-alkyl/phenyl-6-aryl-s-triazolo[3,4-b][1,3,4]thiadiazines and their antimicrobial evaluation
Molecular properties prediction, synthesis, and diuretic activity of phenoxy acetic acid bearing pyrazolines
Synthesis and herbicidal activity of novel 5-chloro-3-fluoro-2-phenoxypyridines with a 1,3,4-oxadiazole ring
Skimmianine, a furoquinoline alkaloid from Zanthoxylum nitidum as a potential acetylcholinesterase inhibitor
Synthesis, antioxidant, and antitumor evaluation of certain new N-substituted-2-amino-1,3,4-thiadiazoles
Synthesis, 5-HT1A and 5-HT2A receptor affinity and QSAR study of 1-benzhydryl-piperazine derivatives with xanthine moiety at N4
Synthesis and evaluation of a series of aminocyanopyridines as antimicrobial agents
Design, synthesis, and anti-allergic activities of novel (R)(-)-1-[(4-chlorophenyl)phenyl methyl]piperazine derivatives
Microwave-assisted synthesis of novel 4H-chromene derivatives bearing 2-aryloxyquinoline and their antimicrobial activity assessment
Synthesis of novel isoxazolines via 1,3-dipolar cycloaddition and evaluation of anti-stress activity
Synthesis and biological activity of new cycloalkylthiophene-Schiff bases and their Cr(III) and Zn(II) complexes
Synthesis, anti-inflammatory and antimicrobial evaluation of novel N1-(quinolin-4yl)ethane-1,2-diamine phenyl urea derivatives
Enantioselective Antifungal Activity of Pefurazoate against Pathogens of Rice Seed Diseases
Synthesis and antimicrobial activity studies of some novel substituted phenylhydrazono-1H-tetrazol-5-yl-acetonitriles
Synthesis and SAR investigation of natural phenylpropene-derived methoxylated cinnamaldehydes and their novel Schiff bases as potent antimicrobial and antioxidant agents
New molecular scaffolds for the design of Alzheimers acetylcholinesterase inhibitors identified using ligand- and receptor-based virtual screening
Insecticide resistance traits differ among and within host races in Aphis gossypii.
Stereoselective synthesis of 2-amino-1-hydroxy-3-phenylpropylphosphonic acid
Synthesis, characterization, and biological evaluation of certain 1,3-thiazolone derivatives bearing pyrazoline moiety as potential anti-breast cancer agents
Identification of important structural features of thiazolo[4,5-d]pyrimidines required for potent antifungal activity
Antiviral effects of three novel derivatives of adefovir on the replication of hepatitis B virus
Photosynthetic Electron Transport Inhibitory Activity of 2-Aralkylamino-4-methyl-6-trifluoromethyl-1, 3, 5-triazine Derivatives
Synthesis of new oxadiazole derivatives as anti-inflammatory, analgesic, and antimicrobial agents
Synthesis and Evaluation of Homologous Analogs of Anticonvulsant 5-Substituted 3,3-Diethyl-4,5-Dighdro-2(3H)-Furanones
Influence of Absolute Configuration of Indanofan on Herbicidal Activity
Are traditional neem extract preparations as efficient as a commercial formulation of azadirachtin A
Fungicidal activity of 12-propoxyimino-1, 15-pentadecanlactam on selected crops
Synthesis of new olefin chalcone derivatives as antitumor, antioxidant and antimicrobial agents
Fungicidal Activity of 2-Aminochromone-3-carboxamides
Synthesis of novel building blocks of 1H-pyrrolo[3,4-b]quinolin-3(2H)-one and evaluation of their antitumor activity
Structure and Fungicidal Activities of 2-Methoxyimino-N-methyl-2-[2-(substituted pyridyloxymethyl)phenyl]acetamide Derivatives
Synthesis and Fungicidal Activities of 2-(-Methoxyiminobenzyl)-1-methylimidazole Derivatives
Synthesis, structure, and biological assay of cinnamic amides as potential EGFR kinase inhibitors
Bisubstrate Inhibitors of Biotin Protein Ligase in Mycobacterium tuberculosis Resistant to Cyclonucleoside Formation.
Synthesis of C11-Desmethoxy Soraphen A1: A natural product analog that inhibits acetyl-CoA carboxylase.
New melatonin (MT1/MT2) ligands: design and synthesis of (8,9-dihydro-7H-furo[3,2-f]chromen-1-yl) derivatives.
Truncated norzoanthamine exhibiting similar collagen protection activity, toward a promising anti-osteoporotic drug.
Synthesis of novel ring-A fused hybrids of oleanolic acid with capabilities to arrest cell cycle and induce apoptosis in breast cancer cells.
Total synthesis of thiaplakortone a: derivatives as metabolically stable leads for the treatment of malaria.
Synthesis, nitric oxide release, and -glucosidase inhibition of nitric oxide donating apigenin and chrysin derivatives.
3-(5-)-Amino-o-diarylisoxazoles: regioselective synthesis and antitubulin activity.
Functionally Optimized Neuritogenic Farinosone C Analogs: SAR-Study and Investigations on Their Mode of Action.
IV. Discovery of CXCR3 antagonists substituted with heterocycles as amide surrogates: improved PK, hERG and metabolic profiles.
1,2-Dihydro-2-oxopyridine-3-carboxamides: the C-5 substituent is responsible for functionality switch at CB2 cannabinoid receptor.
Design and Synthesis of Phenylpyrrolidine Phenylglycinamides As Highly Potent and Selective TF-FVIIa Inhibitors.
Synthesis and evaluation of 4-(2-pyrimidinylamino) benzamides inhibitors of hedgehog signaling pathway.
Novel spirooxindole-pyrrolidine compounds: synthesis, anticancer and molecular docking studies.
Synthesis of neoglycosphingolipid from methoxyamino-functionalized ceramide.
Gabapentin hybrid peptides and bioconjugates.
Synthesis and biological evaluation of novel C6-amino substituted 4-azasteroidal purine nucleoside analogues.
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
N1,N1-Dimethyl-N3-(3-(trifluoromethyl)phenethyl)propane-1,3-diamine, a new lead for the treatment of human African trypanosomiasis.
Synthesis and haemolytic activity of novel salts made of nicotine alkaloids and bile acids.
Identification of novel 7-amino-5-methyl-1,6-naphthyridin-2(1H)-one derivatives as potent PI3K/mTOR dual inhibitors.
Modular construction of quaternary hemiaminal-based inhibitor candidates and their in cellulo assessment with HIV-1 protease.
Synthesis of neolignans as microtubule stabilisers.
Structure-based design and synthesis of bicyclic fused-pyridines as MEK inhibitors.
Triazolo[4,5-d]pyrimidine Derivatives as Inhibitors of GCN2.
Plasmepsin inhibitory activity and structure-guided optimization of a potent hydroxyethylamine-based antimalarial hit.
Synthesis and molecular docking studies of potent -glucosidase inhibitors based on biscoumarin skeleton.
Scaffold hopping approach to a new series of smoothened antagonists.
DNDi T. cruzi fenarimol series dataset from which preclinical candidate EPL-BS0967 was identified (see also related datasets: CHEMBL3137386 and CHEMBL2448688)
Nitrogen-containing dihydro--agarofuran derivatives from Tripterygium wilfordii.
Thieno[2,3-b]pyridines--a new class of multidrug resistance (MDR) modulators.
Antiparasitic compounds may potentially treat malaria and other parasitic diseases.
New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase.
A concise diastereoselective approach to enantioenriched substituted piperidines and their in vitro cytotoxicity evaluation.
Difluoro-dioxolo-benzoimidazol-benzamides as potent inhibitors of CK1 and with nanomolar inhibitory activity on cancer cell proliferation.
Identification of Indole Alkaloid Structural Units Important for Stimulus-Selective TRPM8 Inhibition: SAR Study of Naturally Occurring Iboga Derivatives.
Teucrium polium phenylethanol and iridoid glycoside characterization and flavonoid inhibition of biofilm-forming Staphylococcus aureus.
Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei.
Design, synthesis and enzymatic evaluation of 3-O-substituted aryl -D-galactopyranosides as inhibitors of Trypanosoma cruzi trans-sialidase.
Targeting the homologous recombination pathway by small molecule modulators.
The use of spirocyclic scaffolds in drug discovery.
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by bicalutamide.
MoGAT-2 Inhibitors May Provide Effective Treatment for Hypertriglyceridemia.
Synthesis and evaluation of ether-linked demethylepipodophyllotoxin dimers.
Brocazines A-F, Cytotoxic Bisthiodiketopiperazine Derivatives from Penicillium brocae MA-231, an Endophytic Fungus Derived from the Marine Mangrove Plant Avicennia marina.
Carbonic anhydrase inhibitors: design, synthesis, and biological evaluation of novel sulfonyl semicarbazide derivatives.
6-Acetonyldihydrochelerythrine Is a Potent Inducer of Apoptosis in HCT116 and SW620 Colon Cancer Cells.
Effect of pre-sowing and pre-emergence glyphosate applications on weedsin stale seedbed cotton
Cross-resistance patterns and fitness in fufenozide-resistant diamondback moth, Plutella xylostella (Lepidoptera: Plutellidae).
Effect of clomazone on various market classes of dry beans
Importance of some classes of molecular descriptors on classification of antitumor acridinones using factor analysis
Aryl N, N-Dimethylcarbamates, Synergists for Organophosphorus Insecticides against Organophos-phorusresistant Rice Stem Borers
Synthesis and characterization of some heterocyclic schiff bases: potential anticonvulsant agents
Synthesis and antimicrobial activity of some bisoctahydroxanthene-1,8-dione derivatives
Synthesis and crystal structure of chalcones as well as on cytotoxicity and antibacterial properties
The interference between metformin treatment and TSH level in euthyroid type 2 diabetic patients
Design, synthesis, and preliminary in vitro and in vivo pharmacological evaluation of 4-{4-[2-(4-(2-substitutedquinoxalin-3-yl)piperazin-1-yl)ethyl]phenyl}thiazoles as atypical antipsychotic agents
Synthesis, NMR spectral studies and antimicrobial evaluation of some 2-(benzothiazol-2-yl)-1-(alkyl-2r,6c-diarylpiperidin-4-ylidine)hydrazine derivatives
Synthesis and biological evaluation of novel series of chalcone derivatives as inhibitors of cyclooxygenase and LPS-induced TNF- with potent antioxidant properties
Mosquito larvicidal studies of some chalcone analogues and their derived products: structureactivity relationship analysis
Synthesis, spectral, theoretical, and antimicrobial screening of some heterocyclic oximes
Chemoselective synthesis, antiproliferative activities, and SAR study of 1H-pyrazol-5-yl-N,N-dimethylformamidines and pyrazolyl-2-azadienes
Fungicidal activity of indole derivatives against some plant pathogenic fungi
Peroxidizing Phytotoxicities of 1, 2-Alkylene-1, 2, 4-triazolidines and 3, 4-Alkylene-1, 3, 4-thiadiazolidines
Synthesis and structureactivity relationships of aliphatic isothiocyanate analogs as antibiotic agents
QSAR studies on a number of pyrrolidin-2-one antiarrhythmic arylpiperazinyls.
Insecticidal and Antiacetyicholinesterase Activities of Isobutylthioaryl Methanesulfonates
A facile route for the synthesis 1,4-disubstituted tetrazolone derivatives and evaluation of their antimicrobial activity
Pharmacophore-based predictive model generation for potent antimalarials targeting haem detoxification pathway
Alkoxyphenyl methanesulfonamides: synthesis, anti-inflammatory effect, and docking studies
Effect of chloro and fluoro groups on the antimicrobial activity of 2,5-disubstituted 4-thiazolidinones: a comparative study
Synthesis of pregnenolonedanazolethylendiamine conjugate: relationship between descriptors log P, , R m, and V m and its antibacterial activity in S. aureus and V. cholerae
Synthesis and insecticidal activity of N-oxydihydropyrroles: 4-hydroxy-3-mesityl-5,5-dimethyl derivatives with various substituents at the 1-position.
Effect of Optically Active Ethyl 2-Phthalimidooxypropionate on the Growth of Cress, Lepidium sativum.
Synthesis and Herbicidal Activity of Novel 3-Alkoxycarbonyl-3-aryl-2,3-dihydro-2-oxo-1H-pyrrole Derivatives
Mild and highly efficient copper (II) sulfate catalyzed one pot synthesis of 2-aryl benzimidazole using atmospheric air as an oxidant and its antibacterial study
Synthesis and blood glucose lowering activity of some novel benzenesulfonylthiourea derivatives substituted with 6-aryl-4,5-dihyropyridazin-3(2H)-ones
Sensitivity of Fusarium verticillioides isolates from rice to a novel cyanoacrylate fungicide
Design, synthesis, and evaluation of an activity-based probe for cellular imaging of monoamine oxidases
Nematicidal efficacy of isothiocyanates against root-knot nematode Meloidogyne javanica in cucumber
Synthesis, in vitro cytotoxicity, and antibacterial studies of new asymmetric bis-1,2,4-triazoles
Synthesis and Insecticidal Activity of N-(4-Aryloxybenzyl)-pyrazolecarboxamide Derivatives
Multicomponent one-pot synthesis of 2-naphthol derivatives and evaluation of their anticancer activity
Ability of vitamins to induce downy mildew disease resistance and growth promotion in pearl millet
Novel 2(3H)-Benzothiazolones as Highly Potent and Selective Sigma-1 Receptor Ligands
Progress in understanding molecular mechanisms and evolution of resistance to succinate dehydrogenase inhibiting (SDHI) fungicides in phytopathogenic fungi
Synthesis, characterization, and SAR studies of new (1H-indol-3-yl)alkyl-3-(1H-indol-3-yl)propanamide derivatives as possible antimicrobial and antitubercular agents
N 1-{4-[(10S)-Dihydroartemisinin-10-oxyl]}phenylmethylene-N 2-(2-methylquinoline-4-yl)hydrazine derivatives as antiplasmodial falcipain-2 inhibitors
Synthesis of 9-O-glycosyl-berberine derivatives and bioavailability evaluation
Synthesis of piperazino and morpholino derivatives of aryloxypropane with potential analgesic and possible antimigraine activities
Controlling powdery mildew on cucurbit rootstock seedlings in the greenhouse with fungicides and biofungicides
Novel 4(3H)-quinazolinone analogs: synthesis and anticonvulsant activity
Synthesis of 2,4-dihalogenofluorobenzenes and their antimicrobial and antifungal activity studies
Insecticidal activity of sesquiterpenes skeleton synthesized by the conventional Robinson annulations reaction on Drosophila melanogaster
Mannich base derivatives of 1,3,4-oxadiazole: synthesis and screening against Entamoeba histolytica
In vitro cytotoxicity evaluation of diversely substituted N-aryl-2-oxindoles
Synthesis and in vitro microbiological evaluation of novel 2,4-diaryl-3-azabicyclo[3.3.1]nonan-9,5-spiro-1,2,4-triazolidine-3-thiones
Antifeedant properties of natural products from Parthenium argentatum, P. argentatumP. tomentosum (Asteraceae) and Castela emoryi (Simaroubeaceae) against Reticulitermes flavipes
Activities of essential oils from Asarum heterotropoides var. mandshuricum against five phytopathogens
Synthesis and Structure-Activity Relationships of Dinotefuran Derivatives: Modification in the Tetrahydro-3-furylmethyl Part
Unexpected plant-systemic insecticidal properties of alkylene-tethered bis-imidacloprid derivatives
Synthesis and evaluation of meta substituted 1-(aryloxypropyl)-4-(chloroaryl) piperazines as potential atypical antipsychotics
Synthesis of 1,3,5-trisubstituted pyrazoline nucleus containing compounds and screening for antimicrobial activity
Glyphosate resistance in perennial ryegrass (Lolium perenne L.) from Argentina
Isolation of an insecticidal compound oxalicine B from Penicillium sp. TAMA 71 and confirmation of its chemical structure by X-ray crystallographic analysis
Synthesis and Herbicidal Activity of N-(1-Arylethenyl)-2-chloroacetamides.
Design, synthesis and biological evaluation of 3-benzylideneflavanone derivatives as cytotoxic agents
Synthesis and insect antifeedant activity of 2-substituted 2,3-dihydrofuran-3-ols and butenolides (Part II)
Effect of nitrogen insertion on the antitussive properties of menthol and camphor
Insecticide Resistance and Insensitive Acetylcholinesterase in Small Brown Planthopper, Laodelphax striatellus
Synthesis and biological evaluation of some N 4-aryl-substituted 5-fluoroisatin-3-thiosemicarbazones
Synthesis, evaluation of 6,8-dibromo-2-aryl-2,3-dihydroquinolin-4(1H)-ones in MCF-7 (breast cancer) cell lines and their docking studies
Evaluation of fungicide applications to sweet orange at different flowering stages for control of postbloom fruit drop caused by Colletotrichum acutatum
Rapid synthesis, characterization, anticancer and antimicrobial activity studies of substituted thiadiazoles and their dinucleating ligand metal complexes
Synthesis and in vitro anticancer activity of novel thiazacridine derivatives
Synthesis of novel imidazo[2,1-b][1,3,4]thiadiazoles appended to sydnone as anticancer agents
Design, synthesis, and antimalarial evaluation of thiazole-derived amino acids
Synthesis, biological evaluation, and molecular modeling studies of new 1,3,4-oxadiazole- and 1,3,4-thiadiazole-substituted 4-oxo-4H-pyrido[1,2-a]pyrimidines as anti-HIV-1 agents
N-palmitoylethanolamide derivatives: synthesis and studies on anticonvulsant and antidepressant activities
Syntheses and biological activities of dihydro-5,6-dehydrokawain derivatives.
Synthesis, anti-inflammatory, and cytotoxicity evaluation of 9,10-dihydroanthracene-9,10-,-succinimide and bis-succinimide derivatives
Substituted 9-aryl-1,8-acridinedione derivatives and their effects on potassium channels
Screening and evaluation of rat kidney aldose reductase inhibitory activity of some pyridazine derivatives
Synthesis and fungicidal activity of enantiomerically pure (R)- and (S)-silicon-containing azole fungicides.
Efficacy of acibenzolar-S-methyl and two strobilurins, azoxystrobin and trifloxystrobin, for the control of corky root of tomato and verticillium wilt of eggplant
Microbiologically active Mannich bases derived from 1,2,4-triazoles. The effect of C-5 substituent on antibacterial activity.
Free radical scavenging and hepatoprotective effects of salidroside analogs on CCl4-induced cytotoxicity in LO2 cells
Production and optimization of oxytetracycline by a new isolate Streptomyces rimosus using response surface methodology
Synthesis of 2-(5, 7-Difluoro-3-indolyl)-propionic Acid (5, 7-F2-IPA) and 2-(5, 7-Difluoro-3-indolyl)isobutyric Acid (5, 7-F2-IIBA) and Their Respective Auxin and Antiauxin Activities
Novel antitubercular diallyl/dibenzylthiosemicarbazones endowed with high activity toward multi-drug-resistant tuberculosis
Synthesis of 1-(4-aminosulfonylphenyl)-3,5-diarylpyrazoline derivatives as potent antiinflammatory and antimicrobial agents
7-chloro-3-(substituted benzylidene/phenyl ethylidene amino)-2-phenylquinazolin-4(3H)-ones: synthesis, antimicrobial and antitubercular evaluation
QSAR analysis of B-ring-modified diaryl ether derivatives as a InhA inhibitors
Structurecytotoxicity relationship of a novel series of miconazole-like compounds
Synthesis and Insecticidal Activity of 5-Dimethylamino-1, 3dithianes
Design, synthesis, and docking studies of novel ofloxacin analogues as antimicrobial agents
Structural confirmation of 15-norlubiminol and 15-norepilubiminol, isolated from Solanum aethiopicum, by chemical conversion from lubimin and epilubimin, and their antifungal activity.
Synthesis and evaluation of novel carbamate-substituted flavanone derivatives as potent acetylcholinesterase inhibitors and anti-amnestic agents
Diatomaceous earths enhance the insecticidal effect of bitterbarkomycin against stored-grain insects
Cytotoxic Effect of Coscinium Fenestratrum (Gaertn.) Colebr. and its Active Principle Berberine on L929 Cells
Improgan-like Analgesics: A Family of Compounds Derived From Histamine Anatgonists
Trichodermone, a spiro-cytochalasan with a tetracyclic nucleus (7/5/6/5) skeleton from the plant endophytic fungus Trichoderma gamsii.
Inhibition of CK2: An Attractive Therapeutic Target for Cancer Treatment.
3D-QSAR study of adamantyl N-benzylbenzamides as melanogenesis inhibitors.
Diphenylpropane Derivatives as Agonist of PPAR Nuclear Receptors.
Discovery of Clinical Candidate GSK1842799 As a Selective S1P1 Receptor Agonist (Prodrug) for Multiple Sclerosis.
Synthesis, radiosynthesis and first in vitro evaluation of novel PET-tracers for the dopamine transporter: [(11)C]IPCIT and [(18)F]FE@IPCIT.
Unsymmetrical 1,5-diaryl-3-oxo-1,4-pentadienyls and their evaluation as antiparasitic agents.
Thiodiketopiperazines from the marine-derived fungus Phoma sp. OUCMDZ-1847.
New natural products as new leads for antibacterial drug discovery.
Discovery of a benzimidazole series of ADAMTS-5 (aggrecanase-2) inhibitors by scaffold hopping.
Synthesis and activity of substituted heteroaromatics as positive allosteric modulators for 425 nicotinic acetylcholine receptors.
Salicylanilide diethyl phosphates: synthesis, antimicrobial activity and cytotoxicity.
Stapled Vasoactive Intestinal Peptide (VIP) Derivatives Improve VPAC2 Agonism and Glucose-Dependent Insulin Secretion.
Synthesis, anticancer activity and DNA-binding properties of novel 4-pyrazolyl-1,8-naphthalimide derivatives.
Truncated Orexin Peptides: Structure-Activity Relationship Studies.
Structure Guided Optimization, in Vitro Activity, and in Vivo Activity of Pan-PIM Kinase Inhibitors.
Design, synthesis and molecular modeling of novel N-acylhydrazone derivatives as pyruvate dehydrogenase complex E1 inhibitors.
Development of DANDYs, new 3,5-diaryl-7-azaindoles demonstrating potent DYRK1A kinase inhibitory activity.
Resveratrol oligomers inhibit biofilm formation of Escherichia coli O157:H7 and Pseudomonas aeruginosa.
Direct synthesis of C3-mono-functionalized oxindoles from N-unprotected 2-oxindole and their antileishmanial activity.
Design and synthesis of potential dual NK(1)/NK(3) receptor antagonists.
A fragment-based method to discover irreversible covalent inhibitors of cysteine proteases.
Novel pyrrolobenzoxaboroles: design, synthesis, and biological evaluation against Trypanosoma brucei.
Selective 5-HT Receptor Modulators May Deliver Focused Targeting with Fewer Adverse Effects.
Novel delta opioid receptor agonists with oxazatricyclodecane structure.
4-Alkyloxyimino derivatives of uridine-5'-triphosphate: distal modification of potent agonists as a strategy for molecular probes of P2Y2, P2Y4, and P2Y6 receptors.
Analogues of the Natural Product Sinefungin as Inhibitors of EHMT1 and EHMT2.
Novel 2,4-Diarylaminopyrimidine Analogues (DAAPalogues) Showing Potent c-Met/ALK Multikinase Inhibitory Activities.
Design and Evaluation of -Hydroxy Fatty Acids Containing -GalCer Analogues for CD1d-Mediated NKT Cell Activation.
Localization and interaction of hydroxyflavones with lipid bilayer model membranes: a study using DSC and multinuclear NMR.
Three new cembranoid-type diterpenes from Red Sea soft coral Sarcophyton glaucum: isolation and antiproliferative activity against HepG2 cells.
Development of [(3)H]2-Carboxy-4,6-dichloro-1H-indole-3-propionic Acid ([(3)H]PSB-12150): A Useful Tool for Studying GPR17.
Lignan dicarboxylates and terpenoids from the flower buds of Cananga odorata and their inhibitory effects on melanogenesis.
Thiaflavan scavenges radicals and inhibits DNA oxidation: a story from the ferrocene modification.
Antiprotozoal activity and DNA binding of N-substituted N-phenylbenzamide and 1,3-diphenylurea bisguanidines.
Improving the Pharmacokinetics of GPR40/FFA1 Full Agonists.
Liver S9 Fraction-Derived Metabolites of Curcumin Analogue UBS109.
Enhancing a CH- Interaction to Increase the Affinity for 5-HT1A Receptors.
R-Configuration of 4-Aminopyridyl-Based Inhibitors of CYP51 Confers Superior Efficacy Against Trypanosoma cruzi.
Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of /-hydrolase domain containing 6 (ABHD6).
Interkingdom pharmacology of Angiotensin-I converting enzyme inhibitor phosphonates produced by actinomycetes.
Recent developments of metal N-heterocyclic carbenes as anticancer agents.
Phenyl carboxamide analogues as spleen tyrosine kinase (syk) inhibitors.
Preliminary investigations into triazole derived androgen receptor antagonists.
Synthesis of symmetrically substituted 3,3-dibenzyl-4-hydroxy-3,4-dihydro-1H-quinolin-2-ones, as novel quinoline derivatives with antibacterial activity.
Dihydrothiophene-condensed chromones from a marine-derived fungus Penicillium oxalicum and their structure-bioactivity relationship.
Discovery of AZD3199, An Inhaled Ultralong Acting 2 Receptor Agonist with Rapid Onset of Action.
Inhibitors of Factor XIa and Plasma Kallikrein May Treat Thromboembolic Disorders and Many Diabetes Complications.
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Identification of a neuroprotective and selective butyrylcholinesterase inhibitor derived from the natural alkaloid evodiamine.
Discovery of Short Peptides Exhibiting High Potency against Cryptococcus neoformans.
3-Amido-3-aryl-piperidines: A Novel Class of Potent, Selective, and Orally Active GlyT1 Inhibitors.
From virtual to clinical: The discovery of PGN-1531, a novel antagonist of the prostanoid EP4 receptor.
Structure-Activity Relationship of Semicarbazone EGA Furnishes Photoaffinity Inhibitors of Anthrax Toxin Cellular Entry.
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
P3 SAR exploration of biphenyl carbamate based Legumain inhibitors.
Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome.
Oridonin ring A-based diverse constructions of enone functionality: identification of novel dienone analogues effective for highly aggressive breast cancer by inducing apoptosis.
Design, synthesis, and biological evaluation of novel investigational nonapeptide KISS1R agonists with testosterone-suppressive activity.
Identification of elaiophylin derivatives from the marine-derived actinomycete Streptomyces sp. 7-145 using PCR-based screening.
Synthesis and antimicrobial activity of some novel hydrazide, benzochromenone, dihydropyridine, pyrrole, thiazole and thiophene derivatives.
Synthesis and evaluation of novel 4-nitropyrrole-based 1,3,4-oxadiazole derivatives as antimicrobial and anti-tubercular agents.
Extending the record of bis--pyrone polypropionates from marine pulmonate mollusks.
Synthesis and antiproliferative activity of -branched ,-unsaturated ketones.
4-Methyl-5-(3-hydroxyphenyl)morphan opioid agonist and partial agonist derived from a 4-methyl-5-(3-hydroxyphenyl)morphan pure antagonist.
Preparation and in vitro photodynamic activities of folate-conjugated distyryl boron dipyrromethene based photosensitizers.
Hypoxia-targeting carbonic anhydrase IX inhibitors by a new series of nitroimidazole-sulfonamides/sulfamides/sulfamates.
Gallic acid is the major component of grape seed extract that inhibits amyloid fibril formation.
Synthesis, biological evaluation and docking studies of 4-aryloxymethyl coumarins derived from substructures and degradation products of vancomycin.
Self-assembly to function: design, synthesis, and broad spectrum antimicrobial properties of short hybrid E-vinylogous lipopeptides.
Combining in silico and biophysical methods for the development of Pseudomonas aeruginosa quorum sensing inhibitors: an alternative approach for structure-based drug design.
New 7-methylguanine derivatives targeting the influenza polymerase PB2 cap-binding domain.
Discovery of tryptanthrin derivatives as potent inhibitors of indoleamine 2,3-dioxygenase with therapeutic activity in Lewis lung cancer (LLC) tumor-bearing mice.
Design, synthesis, and biological evaluation of indole-2-carboxamides: a promising class of antituberculosis agents.
Chiral 1,3,4-oxadiazol-2-ones as highly selective FAAH inhibitors.
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
Pahangensin A and B, two new antibacterial diterpenes from the rhizomes of Alpinia pahangensis Ridley.
Metabolically stable dibenzo[b,e]oxepin-11(6H)-ones as highly selective p38 MAP kinase inhibitors: optimizing anti-cytokine activity in human whole blood.
Structural and thermodynamic dissection of linear motif recognition by the E. coli sliding clamp.
Nonhydrolyzable ATP analogues as selective inhibitors of human NPP1: a combined computational/experimental study.
Design, synthesis and discovery of picomolar selective 42 nicotinic acetylcholine receptor ligands.
Scaffold hopping approach towards various AFQ-056 analogs as potent metabotropic glutamate receptor 5 negative allosteric modulators.
Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor and inhibition of de novo purine nucleotide biosynthesis.
Conformational modifications of gB from herpes simplex virus type 1 analyzed by synthetic peptides.
Total synthesis of schizocommunin and revision of its structure.
Synthesis and pharmacological evaluation of aminothiazolomorphinans at the mu and kappa opioid receptors.
Design, synthesis, and biological evaluation of 2-oxo-3,4-dihydropyrimido[4,5-d]pyrimidinyl derivatives as new irreversible epidermal growth factor receptor inhibitors with improved pharmacokinetic properties.
Experimental confirmation of new drug-target interactions predicted by Drug Profile Matching.
6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach.
Hepatoprotective prenylaromadendrane-type diterpenes from the gum resin of Boswellia carterii.
Design, optimization, and biological evaluation of novel keto-benzimidazoles as potent and selective inhibitors of phosphodiesterase 10A (PDE10A).
Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus.
Pyrazole scaffold: a remarkable tool in the development of anticancer agents.
Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of 7 nicotinic acetylcholine receptors.
Isolation and Identification of (-)-Jasmonic Acid from Wild Rice, Oryza officinalis, as an Antifungal Substance.
Synthesis and evaluation of analgesic, anti-inflammatory, and anticancer activities of new pyrazole-3(5)-carboxylic acid derivatives
3,4-Dihydropyrimidin-2(1H)-one derivatives: Organocatalysed microwave assisted synthesis and evaluation of their antioxidant activity
Design, synthesis and in vitro antibacterial and antifungal activities of some novel spiro[azetidine-2,3-indole]-2,4(1H)-dione
Synthesis and anticonvulsant activity of 8-alkoxy-5,6-dihydro-4H-benzo[f][1,2,4]triazolo[4,3-a]azepine derivatives
Aryloxyacetic esters structurally related to -Asarone as potential antifungal agents
Toxicity, inheritance of fenpyroximate resistance, and detoxification-enzyme levels in a laboratory-selected fenpyroximate-resistant strain of Tetranychus urticae Koch (Acari: Tetranychidae)
Synthesis and Biological Activity of the Functional Derivatives of 3- and 4-(Dimethyl-aminomethyl)-1,2-dithiolanes
Radical scavenging capacities of some thiazolylthiazolidine-2,4-dione derivatives
Synthesis and Herbicidal Activities of 2-(5-Isoxazolyloxy)-acetamide Derivatives
Quinoline-based azetidinone and thiazolidinone analogues as antimicrobial and antituberculosis agents
Synthesis and biological activity of novel anti-juvenile hormone agents
Synthesis and physiological evaluation of new N-nitroso-2,6-dicarbethoxy-3,5-diaryltetrahydro-1,4-thiazine-1,1-dioxides
Comparative QSTR study of saturated alcohols based on topological, constitutional, geometrical, and getaway descriptors
Antioxidant and antimicrobial studies of novel N-(substituted-2-chloroquinolin-3-yl)methylidene-4-hydroxy-2H-1,2-benzothiazine-3-carbohydrazides 1,1-dioxides
Synthesis, antibacterial, and antifungal activities of biolabile (E)-1-(4-morpholinophenyl)-3-aryl-prop-2-en-1-ones
The discovery of potential cyclin A/CDK2 inhibitors: a combination of 3D QSAR pharmacophore modeling, virtual screening, and molecular docking studies
Design, synthesis, and antiviral activity evaluation of phenanthrene-based antofine derivatives.
Exploring structural requirement and binding interactions of -amyloid cleavage enzyme inhibitors using molecular modeling techniques
A combined 3D QSAR and pharmacophore-based virtual screening for the identification of potent p38 MAP kinase inhibitors: an in silico approach
Synthesis, AntiBacteriol, and Antifungal Activities of Some New Benzimidazoles
Synthesis and antimicrobial activities of some isoxazolyl thiazolyl pyrazoles
Insect antifeedants from tropical plants II: structure of zumsin.
Study on synthesis of thalidomide analogues and their bioactivities; inhibition on iNOS pathway and cytotoxic effects
Triptolide suppresses lipopolysaccharide-induced activity of toll-like receptor 4 in mouse macrophage cell line RAW 264.7
Synthesis of new potential anticancer agents based on 4-thiazolidinone and oleanane scaffolds
Synthesis and insect antifeedant activity of stilbene derivatives against Brontispa longissima Larvae
Insecticidal and Neuroblocking Activities of Acetamiprid and Related Compounds
Structure-based predictive model for some benzimidazole inhibitors of hepatitis C virus NS5B polymerase
Computational studies of new 1,4-dihydropyridines containing 4-(5)-chloro-2-ethyl-5-(4)-imidazolyl substituent: QSAR and docking
Synthesis and antiproliferative activity of 1-[(sub)]-6-fluoro-3-[(sub)]-1, 3,4-oxadiazol-2-yl-7-piperazino-1, 4-dihydro-4-quinolinone derivatives
Synthesis of novel aryl(4-substituted pyridin-3-yl)methyl carbamates and their herbicidal activity
Synthesis, chemical characterization of novel 1,3-dimethyl acridones as cytotoxic agents, and their DNA-binding studies
Further derivatives of 4-benzoyl-1,5-diphenyl-1H-pyrazole-3-carboxylic acid and their antibacterial activities
Synthesis and antifungal action of new tricyclazole analogues.
Synthesis and antiviral activity of new 3-methyl-1,5-diphenyl-1H-pyrazole derivatives
A ligand-based approach for enhancing the pharmacokinetic profile of highly charged antibacterial agents
The novel amidocarbamate derivatives of ketoprofen: synthesis and biological activity
Effect of the lipophilic parameter (log P) on the anti-parasitic activity of imidazo[1,2-a]pyridine derivatives
Synthesis and insecticidal activity of novel 1-alkyl-3-sulfonyloxypyrazole-4-carboxamide derivatives
Structures and Biological Activities of Phytotoxins Produced by the Plant Pathogenic Fungus Bipolaris cynodontis cynA
2-D QSAR studies of steroidal natural products oleanic acid and their semisynthetic derivatives as potent protein tyrosine phosphatase 1B inhibitors
Comparative QSAR and pharmacophore modeling of substituted 2-[2-(dimethylamino) ethyl]-1, 2-dihydro-3H-dibenz[de,h]isoquinoline-1,3-diones derivatives as anti-tumor activity
Efficacy of ketoenols on insecticide resistant field populations of two-spotted spider mite Tetranychus urticae and sweet potato whitefly Bemisia tabaci from Greece
Synthesis of some urea and thiourea derivatives of naphtha[1,2-d]thiazol-2-amine as anti-Parkinsonian agents that cause neuroprotection against haloperidol-induced oxidative stress in mice
Potent in vitro and in vivo antitubercular activity of certain newly synthesized indophenazine 1,3,5-trisubstituted pyrazoline derivatives bearing benzofuran
Synthesis and cytostatic evaluation of some 2-(5-substituted-2-oxoindolin-3-ylidene)-N-substituted hydrazine carbothioamide
3D-QSAR of amino-substituted pyrido[3,2B]pyrazinones as PDE-5 inhibitors
Synthesis and analgesic effects of 2-(2-carboxyphenylsulfanyl)-N-(4-substitutedphenyl)acetamide derivatives
-Amino butyric acid analogs as novel potent GABA-AT inhibitors: molecular docking, synthesis, and biological evaluation
Effect of methomyl and oxamyl soil applications on early control of nematodes and insects.
Antifeedant activity of quinones from Ventilago madaraspatana
Identification of in vitro inhibitors of Mycobacterium tuberculosis Lysine -aminotransferase by pharmacophore mapping and three-dimensional flexible searches
2D- QSAR studies on new stilbene derivatives of resveratrol as a new selective aryl hydrocarbon receptor
Anti-tyrosinase, antioxidant and antimicrobial activities of hydroxycinnamoylamides
Synthesis of -amino carbonyl derivatives of coumarin and benzofuran and evaluation of their biological activity
Synthesis and anticonvulsant activity of novel quinazolin-4(3H)-one derived pyrazole analogs
Synthesis of ester and amide derivatives of 1-phenyl-3-(thiophen-3-yl)-1H-pyrazole-4-carboxylic acid and study of their anticancer activity
Influence on Insecticidal Activity of the 3-(3,4-Methylenedioxyphenyl) Group in the 1,4-Benzodioxanyl Moiety of Haedoxan
Intravenous pharmacokinetics and oral bioavailability of biochanin A in female rats
Synthesis, antimalarial and antibacterial activities of 3-amino acid- and aryl amine-substituted 2-methyl-3H-quinalzolin-4-ones
Baseline susceptibility to chlorantraniliprole of Brazilian populations of Plutella xylostella
Inhibition of pancreatic lipase by berberine and dihydroberberine: an investigation by docking simulation and experimental validation
Novel quinazolinone derivatives: synthesis and antimicrobial activity
Synthesis, antitubercular activity, and QSAR analysis of substituted nitroaryl analogs: chalcone, pyrazole, isoxazole, and pyrimidines
Structureactivity relationship study of growth inhibitory 2-styrylchromones against carcinoma cells
Two-dimensional quantitative structureactivity relationship study on polyphenols as inhibitors of -glucosidase
Physicochemical interaction of antitumor acridinone derivatives with DNA in view of QSAR studies.
Synthesis and cytotoxic activity of genistein derivatives
Synthesis, spectral studies, antimicrobial and insect antifeedant activities of some substituted styryl 4-fluorophenyl ketones
Synthesis and antimicrobial activities of some new 5-((3-(aryl)-1-phenyl-1H-pyrazol-4-yl)methylene)-3-phenylthiazolidine-2,4-diones
Synthesis and Fungicidal Activity of 2-Imino-3-(4-arylthiazol-2-yl)-thiazolidin-4-ones and Their 5-Arylidene Derivatives
Synthesis, spectral correlation and insect antifeedant activities of some 2-benzimidazole chalcones
A cytotoxic agent from Strychnos nux-vomica and biological evaluation of its modified analogues
Synthesis and biological evaluation of some Schiff bases of 4-amino-5-(4-methylsulfonyl)benzyl-2,4-dihydro-3H-[1,2,4]-triazole-3-thione
Pharmacophore modeling and 3D-QSAR (CoMSIA) studies for structural requirements of some triazine derivatives as G-quadruplex binders for telomerase inhibition
Synthesis and anticonvulsant evaluation of 2-(substituted benzylidene/ethylidene)-N-(substituted phenyl)hydrazinecarboxamide analogues
Petra, Osiris and Molinspiration (POM) together as a successful support in drug design: antibacterial activity and biopharmaceutical characterization of some azo Schiff bases
Action mechanism of isoxazoline-type herbicides
Comparative molecular similarity indices analysis of some 1-substituted imidazole analogs as Candida albicans P450-demethylase inhibitors
Hypoglycemic effect of astaxanthin from shrimp waste in alloxan-induced diabetic mice
Antibacterial, antifungal and antioxidant activity of some new water-soluble -diketones
Antimicrobial and antiurease activities of newly synthesized morpholine derivatives containing an azole nucleus.
Synthesis and antibacterial activity of 4-benzoyl-1-(4-carboxy-phenyl)-5-phenyl-1H-pyrazole-3-carboxylic acid and derivatives
Synthesis and hypoglycemic activity evaluation of rhein amide derivatives
A facile green synthesis and in vitro antimicrobial activity 4H-pyrimido[2,1-b][1,3]benzothiazole derivatives using aluminum trichloride under solvent free conditions
Advanced QSRR models of toxicological screening of basic drugs in whole blood by UPLC-TOFMS
Inhibitory effect of bionic fungicide 2-allylphenol on Botrytis cinerea (Pers. ex Fr.) in vitro.
Synthesis and antibacterial evaluation of 6-azapyrimidines with -methylene--(4-substituted phenyl)--butyrolactone pharmacophores
Synthesis and herbicidal activities of novel 3-(substituted benzyloxy or phenoxy)-6-methyl-4-(3-trifluoromethylphenyl)pyridazine derivatives.
In vitro antimicrobial assessment of coumarin-based s-triazinyl piperazines
Synthesis and antimycobacterial activity of novel 4-[5-(substituted phenyl)-1-phenyl-4,5-dihydro-1H-3-pyrazolyl]-2-methylphenol derivatives
Synthesis and biological evaluation of 2-(5-substituted-1-((diethylamino)methyl)-2-oxoindolin-3-ylidene)-N-substituted-hydrazinecarbothioamides
Synthesis and biological activities of new Mannich bases of chlorokojic acid derivatives
Synthesis, characterization, and evaluation of some novel 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents
Synthesis of an Antifungal Naphthoquinone Isolated fromRhinacanthus nasutus(Acanthaceae)
Synthesis, in vitro antimicrobial, antiproliferative, and QSAR studies of N-(substituted phenyl)-2/4-(1H-indol-3-ylazo)-benzamides
Molecular docking and in silico studies on analogues of 2-methylheptyl isonicotinate with DHDPS enzyme of Mycobacterium tuberculosis
Isolation and Insecticidal Activity of Three Acetogenins from Seeds of Pond Apple, Annona glabra L.
Synthesis and anti-inflammatory activity of some pyrazole derivatives
Computational approaches to enhance activity of taxanes as antimitotic agent
Structure of the 1 receptor and its ligand binding site.
Trinorditerpenes from the roots of Flueggea virosa.
Anti-hepatitis C virus dinorditerpenes from the roots of Flueggea virosa.
Himbacine-derived thrombin receptor antagonists: c7-aminomethyl and c9a-hydroxy analogues of vorapaxar.
Potent and selective inhibitors of CDPK1 from T. gondii and C. parvum based on a 5-aminopyrazole-4-carboxamide scaffold.
Is NMR Fragment Screening Fine-Tuned to Assess Druggability of Protein-Protein Interactions?
Differential Induction of Cytoplasmic Vacuolization and Methuosis by Novel 2-Indolyl-Substituted Pyridinylpropenones.
Computation-guided discovery of influenza endonuclease inhibitors.
Discovery of a Novel Class of Imidazo[1,2-a]Pyridines with Potent PDGFR Activity and Oral Bioavailability.
Inhibitors of Tropomyosin-Receptor Kinases (Trk's): Potential Pain Therapy and More.
An Accessible Chiral Linker to Enhance Potency and Selectivity of Neuronal Nitric Oxide Synthase Inhibitors.
Discovery and development of potent and selective inhibitors of histone methyltransferase g9a.
Cytotoxic dammarane-type triterpenoids from the stem bark of Dysoxylum binecteriferum.
Potent Targeting of the STAT3 Protein in Brain Cancer Stem Cells: A Promising Route for Treating Glioblastoma.
Design, synthesis, and osteogenic activity of daidzein analogs on human mesenchymal stem cells.
Inhibitors of factor d may provide a treatment for age-related macular degeneration.
Design of an amide N-glycoside derivative of -glucogallin: a stable, potent, and specific inhibitor of aldose reductase.
Targeting low-druggability bromodomains: fragment based screening and inhibitor design against the BAZ2B bromodomain.
Novel endoperoxide-based transmission-blocking antimalarials with liver- and blood-schizontocidal activities.
Development of novel Vitamin D Receptor-Coactivator Inhibitors.
Design, synthesis and structure-activity relationships of some novel, highly potent anti-invasive (E)- and (Z)-stilbenes.
Discovery of Tertiary Amine and Indole Derivatives as Potent RORt Inverse Agonists.
Diversity-oriented synthesis yields a new drug lead for treatment of chagas disease.
Identification of ML251, a Potent Inhibitor of T. brucei and T. cruzi Phosphofructokinase.
Replacement of the Disulfide Bridge in a KLK3-Stimulating Peptide Using Orthogonally Protected Building Blocks.
Synthesis and in Vitro Evaluation of a Peptidomimetic Inhibitor Targeting the Src Homology 2 (SH2) Domain of STAT6.
Polygonumosides A-D, stilbene derivatives from processed roots of Polygonum multiflorum.
Original Design of Fluorescent Ligands by Fusing BODIPY and Melatonin Neurohormone.
Combatting resistant bacteria with the help of Beta-lactamase inhibitors.
Novel Indole-N-glucoside, TA-1887 As a Sodium Glucose Cotransporter 2 Inhibitor for Treatment of Type 2 Diabetes.
Design, synthesis and anticonvulsant evaluation of N-(benzo[d]thiazol-2-ylcarbamoyl)-2-methyl-4-oxoquinazoline-3(4H)-carbothioamide derivatives: a hybrid pharmacophore approach.
Design, synthesis, and evaluation of hydroxamic acid derivatives as promising agents for the management of Chagas disease.
Identification of a new scaffold for hsp90 C-terminal inhibition.
Evaluation and Structural Basis for the Inhibition of Tankyrases by PARP Inhibitors.
HIV Integrase Inhibitors for Treatment of HIV Infections and AIDS.
The chemical and biological potential of C ring modified triterpenoids.
Preparation and activities of macromolecule conjugates of the CCR5 antagonist Maraviroc.
Synthesis and evaluation of novel cyclic Peptide inhibitors of lysine-specific demethylase 1.
Isomannide-based peptidomimetics as inhibitors for human tissue kallikreins 5 and 7.
FGFR1 Kinase Inhibitors: Close Regioisomers Adopt Divergent Binding Modes and Display Distinct Biophysical Signatures.
Evaluation of aminohydantoins as a novel class of antimalarial agents.
Tankyrase inhibitors: potential treatment of hyperproliferative diseases.
Thioester Bonds of Thiocoraline Can Be Replaced with NMe-Amide Bridges without Affecting Its DNA-Binding Properties.
(S)-N-Methyldihydroquinazolinones are the Active Enantiomers of Retro-2 Derived Compounds against Toxins.
Crystal Structures of PI3K Complexed with PI103 and Its Derivatives: New Directions for Inhibitors Design.
Discovery of Potent and Orally Active p53-MDM2 Inhibitors RO5353 and RO2468 for Potential Clinical Development.
Discovery of Small Molecule RIP1 Kinase Inhibitors for the Treatment of Pathologies Associated with Necroptosis.
Isochromans and -pyrones from Penicillium corylophilum.
Methanocarba ring as a ribose modification in ligands of G protein-coupled purine and pyrimidine receptors: synthetic approaches
Small molecules aimed at type III secretion systems to inhibit bacterial virulence.
Adamantane substituted aminocyclitols as pharmacological chaperones for Gaucher disease
Sulforaphane and erucin, natural isothiocyanates from broccoli, inhibit bacterial quorum sensing
2-[(1,3-Dihydro-2H-isoindol-2-yl)methyl]melatonin a novel MT2-selective melatonin receptor antagonist
New potent, short-linker BODIPY-630/650TM labelled fluorescent adenosine receptor agonists
Small organic molecules targeting PCAF bromodomain as potent inhibitors of HIV-1 replication
Identification of novel farnesoid X receptor modulators using a combined ligand- and structure-based virtual screening
Discovery and Biological Evaluation of Novel Dual EGFR/c-Met Inhibitors.
Dual inhibition of the -glucosidase and butyrylcholinesterase studied by molecular field topology analysis.
Synthesis and identification of chiral aminomethylpiperidine carboxamides as inhibitor of collagen induced platelet activation.
Tranylcypromine substituted cis-hydroxycyclobutylnaphthamides as potent and selective dopamine D3 receptor antagonists.
Digitoxin analogues with improved anticytomegalovirus activity.
Synthesis and preliminary biological evaluation of 1,2,3-triazole-Jaspine B hybrids as potential cytotoxic agents.
Thienoquinolines as novel disruptors of the PKC/RACK2 protein-protein interaction.
Quinoline Derivatives as 5-HT6 Receptor PET Ligands.
C-ring cannabinoid lactones: a novel cannabinergic chemotype.
Dissecting the structure of thiopeptides: assessment of thiazoline and tail moieties of baringolin and antibacterial activity optimization.
Discovery and Optimization of Tetramethylpiperidinyl Benzamides as Inhibitors of EZH2.
Synthesis of stable aromatic and heteroaromatic sulfonyl-amidoximes and evaluation of their antioxidant and lipid peroxidation activity.
Optimizing the Physicochemical Properties of Raf/MEK Inhibitors by Nitrogen Scanning.
Cepharanthine inhibited HIV-1 cell-cell transmission and cell-free infection via modification of cell membrane fluidity.
Lead optimization studies of cinnamic amide EP2 antagonists.
Design, synthesis and evaluation of novel diaryl urea derivatives as potential antitumor agents.
Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B.
Thiazolocarboxamide Analogues as NAMPT Inhibitors.
Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
Symmetric adamantyl-diureas as soluble epoxide hydrolase inhibitors.
In Vitro Membrane Permeation Studies and in Vivo Antinociception of Glycosylated Dmt(1)-DALDA Analogues.
Novel cycloalkenepyrazoles as inhibitors of bub1 kinase.
Antimicrobial peptides from skin secretions of Hypsiboas pulchellus (Anura: Hylidae).
Synthesis and evaluation of a (18)F-labeled diarylpyrazole glycoconjugate for the imaging of NTS1-positive tumors.
A general method for making peptide therapeutics resistant to serine protease degradation: application to dipeptidyl peptidase IV substrates.
Design of novel potent inhibitors of human uridine phosphorylase-1: synthesis, inhibition studies, thermodynamics, and in vitro influence on 5-fluorouracil cytotoxicity.
Advances in the studies of roles of Rho/Rho-kinase in diseases and the development of its inhibitors.
Triazine Analogues as NS5B Inhibitors for the Treatment of HCV.
The versatile nature of the 6-aminoquinolone scaffold: identification of submicromolar hepatitis C virus NS5B inhibitors.
Synthesis of 2-amino-3-cyano-4H-chromen-4-ylphosphonates and their anticancer properties.
Synthesis and tumor inhibitory activity of novel coumarin analogs targeting angiogenesis and apoptosis.
Potential -glucosidase inhibitors from thermal transformation of (+)-catechin.
Inhibitors of NS5A for Treatment of HCV Infection.
Glucal-conjugated sterols as novel vascular leakage blocker: structure-activity relationship focusing on the C17-side chain.
Metabolomics Reveal d-Alanine:d-Alanine Ligase As the Target of d-Cycloserine in Mycobacterium tuberculosis.
Substituted imidazothiazoles as inhibitors of viral polymerase.
Suzuki coupling based synthesis and in vitro cytotoxic evaluation of 7-heteroaryl-substituted camptothecin analogs.
Scrutinizing the scaffolds of marine biosynthetics from different source organisms: Gram-negative cultured bacterial products enter center stage.
Synthesis and Anti-HCV Activity of 4-Hydroxyamino -Pyranone Carboxamide Analogues.
2',4'-Difluoro-2'-methyl Substituted Nucleoside Derivatives as Inhibitors of HCV RNA Replication.
Design, synthesis and biological evaluation of hetero-aromatic moieties substituted pyrrole-2-carbonitrile derivatives as dipeptidyl peptidase IV inhibitors.
Activity of caffeic acid derivatives against Candida albicans biofilm.
Discovery of SCH 900188: A Potent Hepatitis C Virus NS5B Polymerase Inhibitor Prodrug As a Development Candidate.
Study of marine natural products including resorcyclic acid lactones from Humicola fuscoatra that reactivate latent HIV-1 expression in an in vitro model of central memory CD4+ T cells.
Pyrano-isoflavans from Glycyrrhiza uralensis with antibacterial activity against Streptococcus mutans and Porphyromonas gingivalis.
Chemical composition of the bark of Tetrapterys mucronata and identification of acetylcholinesterase inhibitory constituents.
Total synthesis of burkholdacs A and B and 5,6,20-tri-epi-burkholdac A: HDAC inhibition and antiproliferative activity.
A perspective on natural products research and ethnopharmacology in Mexico: the eagle and the serpent on the prickly pear cactus.
Novel Peptidomimetic Hepatitis C Virus NS3/4A Protease Inhibitors Spanning the P2-P1' Region.
Synthesis, structure-activity relationships and brain uptake of a novel series of benzopyran inhibitors of insulin-regulated aminopeptidase.
Discovery and characterization of potent thiazoles versus methicillin- and vancomycin-resistant Staphylococcus aureus.
A 2D image-based method for modeling some c-Src tyrosine kinase inhibitors
Synthesis, molecular modeling and anti-inflammatory screening of new 1,2,3-benzotriazinone derivatives
Synthesis, characterization and pharmacological evaluation of (E)-N-(substituted-benzylidene)isonicotinohydrazide derivatives as potent anticonvulsant agents
QSAR and flexible docking studies of some aldose reductase inhibitors obtained from natural origin
Synthesis and evaluation of the hypoglycemic and hypolipidemic activity of novel 5-benzylidene-2,4-thiazolidinedione analogs in a type-2 diabetes model
Peroxidizing Phytotoxic Activity of Pyrazoles
Synthesis, docking studies and antioxidant activity of some chalcone and aurone derivatives
Role of Alkyl Groups at the Three Position of Bicyclophosphorothionates in Interaction with Insect GABA-Gated Chloride Channel
Several Antifeedants from Neem Oil,Azadirachta indicaA. Juss., againstReticulitermes speratusKolbe (Isoptera: Rhinotermitidae)
Synthesis, characterization and their anticonvulsant, anti-inflammatory studies of some novel chromeno oxadiazoles
Synthesis and evaluation of a series of novel imidazolidinone analogues of 6-aminoflavone as anticancer and anti-inflammatory agents
Antifeedant activity of dihydro--agarofuran sesquiterpenes from Celastraceae against Spodoptera littoralis
Synthesis and structureactivity relationship studies on novel 8-amino-3-[2-(4-fluorophenoxy)ethyl]-1,3-diazaspiro[4.5]decane-2,4-dione derivatives as anticonvulsant agents
Long-term pre-exposure of the pest mite Tyrophagus putrescentiae to sub-lethal residues of bifenthrin on rapeseed did not affect its susceptibility to bifenthrin
Synthesis and antiviral activity of new 4-(phenylamino)/4-[(methylpyridin-2-yl)amino]-1-phenyl-1H-pyrazolo[3,4-b]pyridine-4-carboxylic acids derivatives
Screening of flavonoids for antitubercular activity and their structureactivity relationships
Synthesis and Insecticidal Activity of 1, 3-Dithianes
Synthesis and evaluation of in vitro antitubercular activity and antimicrobial activity of some novel 4H-chromeno[2,3-d]pyrimidine via 2-amino-4-phenyl-4H-chromene-3-carbonitriles
Computational evaluation and experimental in vitro antibacterial, antifungal and antiviral activity of bis-Schiff bases of isatin and its derivatives
Evaluation of fungicides and biocontrol agents against grey blight disease of tea in the field
Synthesis of benzothiazole derivatives having acetamido and carbothioamido pharmacophore as anticonvulsant agents
Combination of flavopiridol and embelin effectively inhibit cell growth in hepatocellular carcinoma depending on regulatory relationship between CDK6 and XIAP
3D-QSAR study of multi-target-directed AchE inhibitors based on autodocking
Synthesis and evaluation of antiinflammatory activity of substituted chalcone derivatives
Thiamethoxam acts as a target-site synergist of spinosad in resistant strains of Frankliniella occidentalis.
In vitro evaluation of the antibacterial and antifungal activity of some new pyrazolyl-quinazolin-4(3H)-one derivatives
Design and synthesis of some pyrazole derivatives of expected anti-inflammatory and analgesic activities
Synthesis, antibacterial, and antitubercular studies of some novel isatin derivatives
Synthesis and Insecticidal Activity of Alkylated N-Benzoyl-N-Phenylureas and Their Toxicity to Aquatic Invertebrate
Synthesis and Neuromuscular Blocking Activity of 16-Piperidino Epiandrosterone Derivatives
Occurrence of the antifeedant 14,15-dihydroajugapitin in the aerial parts of Ajuga iva from Algeria.
The effect of ascorbic acid supplementation on brain oxidative events in experimental diabetes
Mode of Action and QSAR Studies of Nitrification Inhibitors
Synthesis of novel 4,6-diaryl-2-aminopyrimidines as potential antiplasmodial agents
Synthesis and biological evaluation of some stilbene-based analogues
Bioefficacy of violacein against Asian armyworm Spodoptera litura Fab. (Lepidoptera: Noctuidae)
3D-QSAR studies of natural flavonoid compounds as reverse transcriptase inhibitors
Assessments of crop losses in rice ecosystems due to stem borer damage (Lepidoptera: Pyralidae)
Chemical weed control in seedbed sown onion (Allium cepa L.)
Synthesis and antibacterial, antimycobacterial and docking studies of novel N-piperazinyl fluoroquinolones
Ginsenoside Re downregulates ICAM-1 expression, inhibits polymorphonuclear infiltration, and ameliorates ischemia-reperfusion injury
Atomic and molecular parameters-based comparative QSAR study on tetrahydroimidazodiazepinone derivatives
Medicinal chemistry of polycyclic cage compounds in drug discovery research
Synthesis and Herbicidal Activity of 1H-2, 3-Benzoxazine Derivatives
Neocryptolepine analogues containing N-substituted side-chains at C-11: synthesis and antischistosomicidal activity
Relationships between Insecticidal Activity of 6-Alkylthio-2-pyridyl Methanesulfonates and Acetylcholinesterase Inhibition of their Sulfone Derivatives against Nephotettix cincticeps
Design and synthesis of new 2-aryl, 3-benzyl-(1,3-oxazolidine or 1,3-thiazolidine)-4-ones as selective cyclooxygenase (COX-2) inhibitors
Insecticidal Activity and Selective Toxicity of Chloronicotinyl Compounds Having Thiomethyl Groups
Synthesis of some (E)-6-[2-(furan-2-yl)ethenyl]-1,2,4-triazin-5-ones and their biological evaluation as antitumor agents
Design, synthesis of some 2,6,9-trisubstituted purinyl thioureido derivatives and evaluation of antimicrobial activity
Synthesis of some bisindolyl analogs for in vitro cytotoxic and DNA cleavage studies
Synthesis and biological evaluation of some N4-substituted 5-nitroisatin-3-thiosemicarbazones
Synthesis and structureantibacterial activity relationship studies of 4-substituted phenyl-4,5-dihydrobenzo[f][1,4]oxazepin-3(2H)-thiones
Synthesis and Fungicidal Activities of [2-(2, 5-Dimethylphenoxymethyl)--methoxyiminobenzyl]-isoxazole Derivatives
A facile synthesis of novel herbicidal 1-phenyl-piperazine-2,6-diones.
Synthesis and Inhibitory Effect on Photosynthetic Electron Transport of 1,3,5-Triazinylcarboxylic Acid Derivatives
Synthesis of a novel barbiturate from 1-chloro-2,4-dinitrobenzene as an anticonvulsant agent
Inhibition of trans-Cinnamate 4-Hydroxylase by 4-Amino-5-aryl-2,3-dihydro-3H-1,2,4-triazole-3-thiones
Acute and chronic anti-inflammatory evaluation of imidazo[1,2-a]pyridine carboxylic acid derivatives and docking analysis
Synthesis of some imidazolyl-substituted 2-benzylidene indanone derivatives as potent aromatase inhibitors for breast cancer therapy
Synthesis and insecticidal activity of 3,4-dihydropyrimidine-2(1H)-thiones against the pulse beetle, Callosobruchus chinensis
Synthesis and screening of 2-(2-(4-substituted piperazine-1-yl)-5-phenylthiazol-4-yl)-3-aryl quinazolinone derivatives as anticancer agents
Synthesis and Fungicidal Activities of Some 1-Aryloxyaceto-3-(5-aryl-1, 3, 4-oxadiazol-2-yl) thioureas and Corresponding Oxadiazolo [3, 2-a]-s-triazines
Molecular modeling studies, synthesis and biological evaluation of derivatives of N-phenylbenzamide as Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors
Design, characterization, computational studies, and pharmacological evaluation of substituted-N-[(1E) substituted-phenylmethylidene]benzohydrazide analogs
A 2D image-based approach for modelling some glycogen synthase kinase 3 inhibitors
Synthesis of novel benzimidazole derivatives: as potent analgesic agent
Synthesis and anti-tubercular evaluation of some novel pyrazolo[3,4-d]pyrimidine derivatives
Development of 4-aminoquinoline-1,3,5-triazine conjugates as potent antibacterial agent through facile synthetic route
QSAR study of a series of acyl coenzyme A (CoA): cholesterol acyltransferase inhibitors using genetic function approximation
Molluscicidal and insecticidal potential of monoterpenes on the white garden snail, Theba pisana (Muller) and the cotton leafworm, Spodoptera littoralis (Boisduval)
Synthesis and pharmacological evaluation of novel 4-isopropylthiazole-4-phenyl-1,2,4-triazole derivatives as potential antimicrobial and antitubercular agents
Synthesis and insecticidal activity of new pyrethroids.
Synthesis of new pyridazinone derivatives as platelet aggregation inhibitors
Synthesis of aspirin eugenol ester and its biological activity
Conventional and microwave techniques for synthesis and antimicrobial studies of novel 1-[2-(2-chloro(3-quinolyl))-5-(4-nitrophenyl)-(1,3,4-oxadiazolin-3-yl)]-3-(aryl)prop-2-en-1-ones
Synthesis, DNA binding, hemolytic, and anti-cancer assays of curcumin I-based ligands and their ruthenium(III) complexes
Structure-Activity Studies of Insecticidal 2-Methoxy-1, 3, 2-oxazaphospholidine 2-Sulfides against Musca domestica and Tribolium castaneum
Synthesis and antimicrobial evaluation of novel benzo[b]thiophenes comprising -lactam nucleus
Design, synthesis, and docking studies of novel telmisartanglitazone hybrid analogs for the treatment of metabolic syndrome
Synthesis and Insect Growth Regulatory Activity of 1,5-Disubstituted Imidazoles with Non-terpene Chains.
Synthesis of novel 3-chloro-1-(5H-dibenz[b,f]azepine-5yl)propan-1-one derivatives with antioxidant activity
Design and synthesis of novel piperazine unit condensed 2,6-diarylpiperidin-4-one derivatives as antituberculosis and antimicrobial agents
Synthesis and antitumor activities of certain novel 2-amino-9-(4-halostyryl)-4H-pyrano[3,2-h]quinoline derivatives
Investigation on the substitution effects of the flavonoids as potent anticancer agents: a structureactivity relationships study
Synthesis of glucose-fipronil conjugate and its phloem mobility.
5-ZATRYPTAMINE ANALOGS AS h5-HT6 SEROTONIN RECEPTOR LIGANDS
Stereoselective syntheses of all stereoisomers of lariciresinol and their plant growth inhibitory activities.
Synthesis and in vitro antiproliferative activity of diphenyl(sulphonylpiperidin-4-yl)methanol derivatives
Molecular modeling of the Toxoplasma gondii adenosine kinase inhibitors
Novel quinolyl-thienyl chalcones and their 2-pyrazoline derivatives with diverse substitution pattern as antileishmanial agents against Leishmania major
Pyrenocines J-M: four new pyrenocines from the endophytic fungus, Phomopsis sp.
Benzimidazole, Benzoxazole and Benzothiazole Derivatives as 5HT2B Receptor Ligands. Synthesis and Preliminary Pharmacological Evaluation
Synthesis, molecular docking studies, and in vitro screening of sulfanilamide-thiourea hybrids as antimicrobial and urease inhibitors
Synthesis, anti-microbial evaluation, and QSAR studies of 4-amino-3-hydroxy-naphthalene-1-sulfonic acid derivatives
Study on the quantitative structuretoxicity relationships of benzoic acid derivatives in rats via oral LD50
Synthesis and Insecticidal Activity of Novel 1-Benzoyl-3-phenylurea Derivatives with Polyfluoroethylsulfenyl, -sulfonyl, and-sulfinyl Substituents
Novel 2-thiopyrimidine derivatives as CDK2 inhibitors: molecular modeling, synthesis, and anti-tumor activity evaluation
Chemical space as a source for new drugs
Trifluoromethyl derivatives of canonical nucleosides: synthesis and bioactivity studies
(Pd/C-mediated)couplingiodocyclizationcoupling strategy in discovery of novel PDE4 inhibitors: a new synthesis of pyrazolopyrimidines
[4-(6,7-Disubstituted quinazolin-4-ylamino)phenyl] carbamic acid esters: a novel series of dual EGFR/VEGFR-2 tyrosine kinase inhibitors
PRIMACINS, N-cinnamoyl-primaquine conjugates, with improved liver-stage antimalarial activity
Design, synthesis and biological activity evaluation of regioisomeric spiro-(indoline-isoxazolidines) in the inhibition of TNF--induced ICAM-1 expression on human endothelial cells
Blockage of collagen binding to integrin 21: structureactivity relationship of proteinprotein interaction inhibitors
Design, synthesis and initial biological evaluation of a novel pladienolide analog scaffold.
Truncated militarinone fragments identified by total chemical synthesis induce neurite outgrowth
Design of membrane targeting tobramycin-based cationic amphiphiles with reduced hemolytic activity
Binding of 9-O-(-amino) alkyl ether analogues of the plant alkaloid berberine to poly(A): insights into self-structure induction
Total synthesis and anti-cholinesterase activity of marine-derived bis-indole alkaloid fascaplysin
Structure-based design, synthesis, and profiling of a -tryptase inhibitor with a spiro-piperidineamide scaffold, benzylamine P1 group, and a substituted indole P4 group
Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A.
Identification of 3-aminothieno[2,3-b]pyridine-2-carboxamides and 4-aminobenzothieno[3,2-d]pyrimidines as LIMK1 inhibitors
Synthesis and evaluation of novel 5-sulfonyl-indolin-2-ones as potent cytotoxic agents
Structural studies of Enterococcus faecalis methionine aminopeptidase and design of microbe specific 2,2-bipyridine based inhibitors
Experimental validation of in silico target predictions on synergistic protein targets
Synthesis, in silico screening and bioevaluation of dispiro-cycloalkanones as antitubercular and mycobacterial NAD+-dependent DNA ligase inhibitors
Oxazole phosphonic acids as fructose 1,6-bisphosphatase inhibitors with potent glucose-lowering activity
Identification of pyrazolo-pyrimidinones as GHS-R1a antagonists and inverse agonists for the treatment of obesity
Matrix-based multiparameter optimisation of glucokinase activators: the discovery of AZD1092
Unfolded and macrocyclic ammonium derivatives of diterpenoids steviol and isosteviol having choline moieties. Synthesis and inhibitory activities toward acetylcholine- and butyrylcholinesterases
Synthesis of new chromeno-annulated cis-fused pyrano[3,4-c]pyran derivatives via domino Knoevenagelhetero-DielsAlder reactions and their biological evaluation towards antiproliferative activity
The p53-MDM2/MDMX axis - A chemotype perspective.
Diphenylbutylpiperidine-based cell autophagy inducers: Design, synthesis and SAR studies
Deciphering intracellular targets of organochalcogen based redox catalysts
3-Aryl-N-aminoylsulfonylphenyl-1H-pyrazole-5-carboxamides: a new class of selective Rac inhibitors
Aromatic chloride to nitrile transformation: medicinal and synthetic chemistry
Synthesis and bioevaluation of aryl hydroxamates distinguishing between NAD+ and ATP-dependent DNA ligases
The Discovery of Novel 10,11-Dihydro-5H-dibenz[b,f]azepine SIRT2 Inhibitors.
Antifolates as effective antimicrobial agents: new generations of trimethoprim analogs
Optimising pharmacokinetics of glucokinase activators with matched triplicate design sets the discovery of AZD3651 and AZD9485
Selenosemicarbazones as potent cruzipain inhibitors and their antiparasitic properties against Trypanosoma cruzi
Biosynthetic gene cluster and antimicrobial activity of the elfamycin antibiotic factumycin
Natural product inhibitors of glucose-6-phosphate translocase
Discovery of the highly potent PI3K/mTOR dual inhibitor PF-04691502 through structure based drug design
Structure based virtual screening for discovery of novel human neutrophil elastase inhibitors
Structure-based optimization of the piperazino-containing 1,3-disubstituted ureas affording sub-nanomolar inhibitors of soluble epoxide hydrolase.
Design, synthesis, and structureactivity relationships of 1,3,4-oxadiazol-2(3H)-ones as novel FAAH inhibitors
Aminomethyl substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists
Structureactivity relationship studies using peptide arrays: the example of HIV-1 Revintegrase interaction
Peptides: minimal drug surrogates to interrogate and interfere with protein function
Synthesis, SAR and selectivity of 2-acyl- and 2-cyano-1-hetarylalkyl-guanidines at the four histamine receptor subtypes: a bioisosteric approach
Carbazolepyrrolo[2,1-c][1,4]benzodiazepine conjugates: design, synthesis, and biological evaluation
Discovery of a novel benzopyranyl compound as a potent in vitro and in vivo osteogenic agent
3-Diarylethyne quinazolinones: a new class of senescence inducers
Interactions of polysulfanes with components of red blood cells
Synthesis of tetrazoleisoxazoline hybrids as a new class of tubulin polymerization inhibitors
FP Tethering: a screening technique to rapidly identify compounds that disrupt protein-protein interactions.
Design, synthesis and biological evaluation of -lactam hydroxamate based TACE inhibitors
Antimicrobial activity and mode of action of novel, N-terminal tagged tetra-peptidomimetics
Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist.
Synthesis and biological activity of hydroxybenzylidenyl pyrrolidine-2,5-dione derivatives as new potent inhibitors of tyrosinase
A structure-activity relationship study on multi-heterocyclic molecules: two linked thiazoles are required for cytotoxic activity.
Latent antibiotics and the potential of the arylomycins for broad-spectrum antibacterial activity
Redesigning the designer drug ecstasy: non-psychoactive MDMA analogues exhibiting Burkitt's lymphoma cytotoxicity
Binding free energy calculations and biological testing of novel thiobarbiturates as inhibitors of the human NAD+dependent histone deacetylase Sirt2
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
Identification of novel urea derivatives as PTP1B inhibitors: synthesis, biological evaluation and structureactivity relationships
Discovery of a structurally novel, drug-like and potent inhibitor of peptidylarginine deiminase
The structure based design of dual HDAC/BET inhibitors as novel epigenetic probes
INPHARMA-based identification of ligand binding site in fragment-based drug design
Binding region and interaction properties of sulfoquinovosylacylglycerol (SQAG) with human vascular endothelial growth factor 165 revealed by biosensor-based assays
Synthesis and biological evaluation of substituted - and -2,3-dihydrofuran naphthoquinones as potent anticandidal agents
Necrosulfonamide inhibits necroptosis by selectively targeting the mixed lineage kinase domain-like protein
Overcoming retinoic acid receptor- based testicular toxicity in the optimisation of glucokinase activators
Cytotoxic sugar analogues of an optimized novobiocin scaffold
2-Amino-5-arylbenzoxazole derivatives as potent inhibitors of fatty acid amide hydrolase (FAAH)
Synthesis and biological evaluation of novel 1-aryl, 5-(phenoxy-substituted)aryl-1,4-pentadien-3-one derivatives
Developing novel non-hydroxamate histone deacetylase inhibitors: the chelidamic warhead
N1-Benzyl substituted cambinol analogues as isozyme selective inhibitors of the sirtuin family of protein deacetylases
Understanding and overcoming aminoglycoside resistance caused by N-6'-acetyltransferase.
Novel indolizine compounds as potent inhibitors of phosphodiesterase IV (PDE4): structureactivity relationship
Enantiomeric pairs reveal that key medicinal chemistry parameters vary more than simple physical property based models can explain
Preliminary in vitro evaluation of N-(benzofuroxan-5-yl)methylene benzohydrazide derivatives as potential anti-Trypanosoma cruzi agents
Minisci reactions: Versatile CH-functionalizations for medicinal chemists
An approach to enzyme inhibition employing reversible boronate ester formation
Design, synthesis and biological evaluation of imidazopyridine/pyrimidine-chalcone derivatives as potential anticancer agents
Homologous piperazine-alcanols: chiral pool synthesis and pharmacological evaluation
Approaches to discover non-ATP site kinase inhibitors
Selective inhibition of EGFR and VEGFR2 tyrosine kinases controlled by a boronic acid substituent on 4-anilinoquinazolines
Interaction of long telomeric DNAs with macrocyclic hexaoxazole as a G-quadruplex ligand
Design, synthesis and antiproliferative activity of indole analogues of indanocine
Structure and antimicrobial properties of multivalent short peptides
Membrane disrupting antimicrobial peptide dendrimers with multiple amino termini
Identification of a novel nanomolar inhibitor of hIcmt via a carboxylate replacement approach
Synthesis and biological evaluation of tetrazole containing compounds as possible anticancer agents
Synthesis of dual AChE/5-HT4 receptor multi-target directed ligands
Antivascular and anticancer activity of dihalogenated A-ring analogues of combretastatin A-4
Potent growth inhibitory activity of ()-platencin towards multi-drug-resistant and extensively drug-resistant Mycobacterium tuberculosis
Synthesis and biological evaluation of a new class of anti-brucella compounds targeting histidinol dehydrogenase: -O-arylketones and -S-arylketones derived from histidine
Amidines bearing benzofuroxan or benzimidazole 1,3-dioxide core scaffolds as Trypanosoma cruzi-inhibitors: structural basis for their interactions with cruzipain
3,3-Dimethyl-1H-pyrrolo[3,2-g]quinolin-2(3H)-one derivatives as novel Raf kinase inhibitors
Synthesis and antifungal activity of the novel triazole compounds
Discovery of an HIV integrase inhibitor with an excellent resistance profile
Rhodanine carboxylic acids as novel inhibitors of histone acetyltransferases
Structure-activity evaluation of new uracil-based non-nucleoside inhibitors of HIV reverse transcriptase
Indole/triazole conjugates are selective inhibitors and inducers of bacterial biofilms.
Small molecule modulation of stem cells in regenerative medicine: recent applications and future direction
Identification and optimisation of 3,3-dimethyl-azetidin-2-ones as potent and selective inhibitors of 11-hydroxysteroid dehydrogenase type 1 (11-HSD1)
Synthesis and biological evaluation of 2,3-bis(het)aryl-4-azaindole derivatives as protein kinase inhibitors
Library synthesis and cytotoxicity of a family of 2-phenylacrylonitriles and discovery of an estrogen dependent breast cancer lead compound
Alkynylation of N-(3-iodopyridin-2-yl)sulfonamide under Pd/CCu catalysis: a direct one pot synthesis of 7-azaindoles and their pharmacological evaluation as potential inhibitors of sirtuins
Biological evaluation of imidazolium- and ammonium-based salts as HIV-1 integrase inhibitors
A self-immolative dendritic glucuronide prodrug of doxorubicin
Histamine H3 receptor ligands with a 3-cyclobutoxy motif: a novel and versatile constraint of the classical 3-propoxy linker
Analogues of the HIV-Tat peptide containing N-modified arginines as potent inhibitors of protein arginine N-methyltransferases
New substituted aryl esters and aryl amides of 3,4-dihydro-2H-1,2,4-benzothiadiazine 1,1-dioxides as positive allosteric modulators of AMPA receptors
Design and syntheses of some iminosugar derivatives as potential immunosuppressants
The anti-tumor antibiotic PD 113,271 binds to microtubule-associated protein 1B (MAP1B)
Effect of the isosteric replacement of the phenyl motif with furyl (or thienyl) of 4-phenyl-N-arylsulfonylimidazolones as broad and potent anticancer agents
Bioguided discovery and pharmacophore modeling of the mycotoxic indole diterpene alkaloids penitrems as breast cancer proliferation, migration, and invasion inhibitors.
The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists.
Bicyclic imidazole-4-one derivatives: a new class of antagonists for the orphan G protein-coupled receptors GPR18 and GPR55
Carbocyclic 5'-nor "reverse" fleximers. Design, synthesis, and preliminary biological activity.
Synthesis of coumarinchalcone hybrids and evaluation of their antioxidant and trypanocidal properties
Potential Drug Abuse Therapeutics Derived from the Hallucinogenic Natural Product Salvinorin A.
New analyses of MIC90 data to aid antibacterial drug discovery
Inhibition of Ras-Effector Interaction by Cyclic Peptides.
Glyco-Phospho-Glycero Ether Lipids (GPGEL): synthesis and evaluation as small conductance Ca2+-activated K+ channel (SK3) inhibitors
Synthesis and biological activity of furanylindazoles as inhibitors of hypoxia inducible factor (HIF)-1 transcriptional activity
Structureactivity relationships of gramicidin S analogs containing (-3-pyridyl)-,-dehydroalanine residues on membrane permeability
The importance of solvation in the design of ligands targeting membrane proteins
Antimycobacterial activity of spirooxindolo-pyrrolidine, pyrrolizine and pyrrolothiazole hybrids obtained by a three-component regio- and stereoselective 1,3-dipolar cycloaddition
Design, synthesis and biological evaluation of new molecules inhibiting epidermal growth factor receptor threonine790 methionine790 mutant
New 3-amidinophenylalanine-derived inhibitors of matriptase
Optimisation of aqueous solubility in a series of G protein coupled receptor 119 (GPR119) agonists
Chiral diaminocyclohexane coupling polyphenols: A new class of anticancer agents
Synthesis and biological activity evaluation of N-protected isatin derivatives as inhibitors of ICAM-1 expression on human endothelial cells
Evaluation of two cyclic di-peptides as inhibitors of CCL2 induced chemotaxis
Synthesis and study of 2-acetyl amino-3-[4-(2-amino-5-sulfo-phenylazo)-phenyl]-propionic acid: a new class of inhibitor for hen egg white lysozyme amyloidogenesis
The synthesis and receptor binding affinities of DDD-016, a novel, potential, atypical antipsychotic
3-Substituted coumarins as dual inhibitors of AChE and MAO for the treatment of Alzheimer's disease
Biological activity and DNA binding studies of 2-substituted benzimidazo[1,2-a]quinolines bearing different amino side chains
Discovery of potent, non-carbonyl inhibitors of fatty acid amide hydrolase (FAAH)
Synthesis and synergistic antimycobacterial screening of chlorpromazine and its metabolites
A concise synthesis of the potent inflammatory mediator 5-oxo-ETE
Novel benzothiazole derivatives with a broad antifungal spectrum: design, synthesis and structureactivity relationships
Isoquinolines. 6. Potential central nervous system antitumor agents. Nitrogen mustards of 3-amino-4-(p-aminophenyl)isoquinoline.
Dibenztroponeacetic and -propionic acids. Potent new antiinflammatory agents.
Potentiation of the estrogenic activity of stilbestrol by spiro (cyclohexane-1,2'-indan)-1',4-dione.
Stereospecific interaction of the quaternized opiate, N-methyllevorphanol, with opiate receptors.
A series of hexahydro[1,4]oxazino[3,4-a]isoquinolines as potential neuroleptics.
Quantitative structure-activity relationships among steroids. Investigations of the use of steric parameters.
Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 3. omega-(6,11-Dihydro-11-oxodibenz[b,e]oxepin-2-yl)alkanoic acids.
Synthesis and biological actions of 2-substituted quinolizidines.
Antimycotic imidazoles. 3. Synthesis and antimycotic properties of 1-[2-(aryloxyalkyl)-2-phenylethyl]-1H-imidazoles.
Synthesis and biological evaluation of substituted 2,2'-oxybis(propionic acid) derivatives and related compounds.
(Acylaryloxy)acetic acid diuretics. 1. (2-Alkyl- and 2,2-dialkyl-1-oxo-5-indanyloxy)acetic acids.
On the structure of medicinal chemistry.
Synthesis and anticancer activity of 5-diethylaminomethyl derivatives and nitrogen mustards of uracil and 2-thiouracils.
3-Cyanocephems, and carbon-3 heterocyclic-substituted cephems via 1,3-dipolar cycloadditions.
Cholinergic compounds. 9. Cyclohexane analogues of deoxamuscarine and derivatives.
Prostaglandin prodrugs. 5.1 Prostaglandin E2 ethylene ketal.
2,3-Disubstituted 1,8-naphthyridines as potential diuretic agents. 2. 5,7-Dimethyl derivatives.
Potential antitumor agents. 13. 4-Methyl-5-amino-1-formylisoquinoline thiosemicarbazone.
Synthesis of nitrosourea derivatives of sucrose as central nervous system anticancer agents.
A new class of diuretics with the 1,4-dioxino(2,3-g)quinolone structure.
Direct measurement of octanol-water partition coefficients by high-pressure liquid chromatography.
Antimalarials. 9. Methylthio- and methylsulfonyl-substituted 9-phenanthrenemethanols.
A new type of anticonvulsant: 1-aryl-3-oxotetrahydroisoquinolines.
Structure-activity-relationship studies around the 2-amino group and pyridine core of antimalarial 3,5-diarylaminopyridines lead to a novel series of pyrazine analogues with oral in vivo activity.
Synthesis and evaluation of 2-(1H-indol-3-yl)-4-phenylquinolines as inhibitors of cholesterol esterase.
Halting HCV Replication with NS5A Inhibitors and NS5B Polymerase Inhibitors: Effective New Treatments of HCV Infection.
Potent Hepatitis C Virus NS5A Inhibitors Containing a Benzidine Core.
A dynamic G-quadruplex region regulates the HIV-1 long terminal repeat promoter.
Constituents of an extract of Cryptocarya rubra housed in a repository with cytotoxic and glucose transport inhibitory effects.
Inhibitory effect of a callophycin A derivative on iNOS expression via inhibition of Akt in lipopolysaccharide-stimulated RAW 264.7 cells.
Computer-guided approach to access the anti-influenza activity of licorice constituents.
5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC): a novel non-nitrogenous ligand for 5-HT2B receptor.
Combination of amino acid/dipeptide with nitric oxide donating oleanolic acid derivatives as PepT1 targeting antitumor prodrugs.
Cytotoxic clerodane diterpenes from Zuelania guidonia.
One-step semisynthesis of oleacein and the determination as a 5-lipoxygenase inhibitor.
On the histone lysine methyltransferase activity of fungal metabolite chaetocin.
Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents.
Substituted Benzofurans as Inhibitors of HCV NS5B Protein.
Isolation, structure elucidation, and biological activity of altersolanol P using Staphylococcus aureus fitness test based genome-wide screening.
Synthesis of novel 5-(3-alkylquinolin-2-yl)-3-aryl isoxazole derivatives and their cytotoxic activity.
Identification of a methoxynaphthalene scaffold as a core replacement in quinolizidinone amide M(1) positive allosteric modulators.
Unusual fernane and gammacerane glycosides from the aerial parts of Spergula fallax.
MMV Malaria Box screening against Toxoplasma gondii and Entamoeba histolytica.
Indolinone-based acetylcholinesterase inhibitors: synthesis, biological activity and molecular modeling.
Flow synthesis and biological activity of aryl sulfonamides as selective carbonic anhydrase IX and XII inhibitors.
Trends in research of antitrypanosomal agents among synthetic heterocycles.
Pyrazolsulfonamide agonists of oxytocin receptor.
Discovery of novel, highly potent, and selective quinazoline-2-carboxamide-based matrix metalloproteinase (MMP)-13 inhibitors without a zinc binding group using a structure-based design approach.
Design, synthesis and in vitro antikinetoplastid evaluation of N-acylated putrescine, spermidine and spermine derivatives.
Novel cyclic biphalin analogue with improved antinociceptive properties.
Synthesis and antimicrobial activity of 5-((3-aryl-1-phenyl-1H-pyrazol-4-yl)methylene)thiazolidine-2,4-diones
Synthesis and Fungicidal Activity of 2-Alkoxyimino-2-cyanoacetamide Derivatives
Aromatic-ring-functionalised benzoxazinones in the system Oryza sativa-Echinochloa crus-galli as biorational herbicide models.
Synthesis, anticancer, and molecular docking studies of pyranone derivatives
Anti-leukemic activity of sulfonoquinovosyldiacylglyceride (SQDG): a constituent of Azadirachta indica leaves
Synthesis and Fungicidal Activities of Heterocyclic Compounds Having -Methoxyimino-2-phenoxymethylbenzyl Group
Synthesis and insecticidal activity of new phosphoramidates
Synthesis, characterization, and pharmacological evaluation of 1-[2-(6-nitro-4-oxo-2-phenyl-4H-quinazolin-3-yl)-ethyl]-3-phenyl ureas
Xyloccensins QV, six new 8,9,30-phragmalin ortho ester antifeedants from the Chinese mangrove Xylocarpus granatum
Synthesis and antibacterial activity of some new hydrazones
Synthesis and biological activity of novel 1H-1,4-diazepines containing benzene sulfonyl piperazine moiety
Anticonvulsant and sedative-hypnotic activity of some novel 3-[5-(4-substituted) phenyl-1,3,4-oxadiazole-2yl]-2-styrylquinazoline-4(3H)-ones
Chiral Synthesis of Pefurazoate Enantiomers and Their Antifungal Activity to Gibberella fujikuroi
Design, synthesis, and biological evaluation of new 3-hydroxy-2-oxo-3-trifluoromethylindole as potential HIV-1 reverse transcriptase inhibitors
Synthesis and biological activity of heterocycles from chalcone
Evidence of a potential adaptation of Magnaporthe oryzae for increased phosphorothiolate-fungicide resistance on rice
Synthesis and antimicrobial activity of morpholinyl/piperazinylbenzothiazines
Pharmacophore of neonicotinoid insecticides
Novel salicylamide derivatives incorporating neonicotinoid pharmacophore: design, synthesis, characterization, and biological evaluation
Synthesis and evaluation of new potent inhibitors of CK1 and CDK5, two kinases involved in Alzheimers disease
Synthesis, anticonvulsant and toxicity screening of thiazolylthiadiazole derivatives
Synthesis of aryloxyalkylamines as h5-HT1B agonists with potential analgesic activity
Chromano-analogs of Insecticidal Neolignans of the 1,4-Benzodioxane Type
Synthesis of photolabile lac-acetogenin for photoaffinity labeling of mitochondrial complex I
Pharmacophore modeling of some novel indole -diketo acid and coumarin-based derivatives as HIV integrase inhibitors
Structure-activity Relationship for the Insect Antifeedant Activity of Benzofuran Derivatives.
An efficient, solvent-free microwave-assisted synthesis and antimicrobial screening of 1,6-dihydropyrimidine analogues
Synthesis, anticancer and antibacterial activities of piperine analogs
Ultrasound-promoted synthesis, biological evaluation and molecular docking of novel 7-(2-chloroquinolin-4-yloxy)-4-methyl-2H-chromen-2-one derivatives
Synthesis, characterization, and urease inhibition of 5-substituted-8-methyl-2H-pyrido[1,2-a]pyrimidine-2,4(3H)-diones
Design and synthesis of novel pyrethriods containing eugenol moiety
Synthesis and cardiovascular activity of difluro-substituted hexahydroquinoline
Synthesis of new benzotriazepin-5(2H)-one derivatives of expected antipsychotic activity
Reduced Lantadenes A and B: semi-synthetic synthesis, selective cytotoxicity, apoptosis induction and inhibition of NO, TNF- production in HL-60 cells
Molecular modeling studies on structural requirement of diarylpropionitrile for selectivity to estrogen receptor subtypes
Effect of ring A and ring B substitution on the cytotoxic potential of pyrazole tethered chalcones
Synthesis and analgesic activity of new heterocyclic compounds derived from monoterpenoids
Synthesis of novel analogues on the -carbon of houttuyfonate and SAR analysis of antibacterial activity with MOPAC
Synthesis and Antimicrobial Evaluation of Some t(3)-Alkyl and t(3),t(5)-Dimethyl-r(2),c(6)-DI-2-Furfurylpiperidin-4-one and its Derivatives
Synthesis, antitumor activity, and structureactivity relationship of some 4H-pyrano[3,2-h]quinoline and 7H-pyrimido[4,5:6,5]pyrano[3,2-h]quinoline derivatives
Synthesis, antitumor and antioxidant evaluation of some new thiazole and thiophene derivatives incorporated coumarin moiety
Sensitivity to iprodione, difenoconazole and fludioxonil of Rhizoctonia cerealis isolates collected from wheat in China
Synthesis and herbicidal activity of 2-acylimino-3-phenyl-1,3-thiazolines—A new family of bleaching herbicides—
Synthesis, anti-inflammatory and anticancer activity evaluation of some mono- and bis-Schiffs bases
5-phenyl-1-benzofuran-2-yl derivatives: synthesis, antimicrobial, and antioxidant activity
Comparative Studies of Elicitors That Induce Phytoalexin in Oats
Synthesis, cytotoxic evaluation, and in silico studies of substituted N-alkylbromo-benzothiazoles
Synthesis, biological evaluation, and pharmacokinetic profiling of benzophenone derivatives as tumor necrosis factor-alpha and interleukin-6 inhibitors
Antimicrobial and anticancer effects of some 2-(substitutedsulfanyl)-N-(5-methyl-isoxazol-3-yl)acetamide derivatives
A clubbed quinazolinone and 4-thiazolidinone as potential antimicrobial agents
Synthesis of some new 2,6-disubstituted-3(2H)-pyridazinone derivatives and investigation of their analgesic, anti-inflammatory and antimicrobial activities
Asymmetric aza-Michael additions of 4-nitrophthalimide to nitroalkenes and preliminary study of the products for herbicidal activities
Microwave-assisted synthesis and evaluation of naphthalimides derivatives as free radical scavengers
Synthesis, antimicrobial, and antioxidant activities of some new indole analogues containing pyrimidine and fused pyrimidine systems
A Comparative Study: Evaluation of Antioxidant Activity of Melatonin and Some Indole Derivatives
Synthesis and anti-inflammatory evaluation of some pyrazolo[3,4-b]pyridines
Synthesis of benzoxazoles, benzothiazoles and benzimidazoles and evaluation of their antifungal, insecticidal and herbicidal activities.
Synthesis and antifungal activity of novel bisdithiocarbamate derivatives of carbohydrates against Fusarium oxysporum f. sp. lini.
Triterpene saponins of Quillaja saponaria show strong aphicidal and deterrent activity against the pea aphid Acyrthosiphon pisum.
Quantitative relationship between insecticidal activity and Ca2+ pump stimulation by flubendiamide and its related compounds
Synthesis of d-amino acid peptides and their effect on beta-amyloid aggregation and toxicity in transgenic Caenorhabditis elegans
Computer simulation of the in vitro and in vivo anti-inflammatory activities of dihydropyrimidines acid derivatives through the inhibition of cyclooxygenase-2
In vivo evaluation of substituted 2,3-diaryl acrylophenone amide derivatives as anti-implantation agents
Thiazoles: having diverse biological activities
A 4-(o-methoxyphenyl)-2-aminothiazole: an anti-quorum sensing compound
Synthesis, molecular modeling, and biological evaluation of 1,2,4-triazole derivatives containing pyridine as potential anti-tumor agents
Synthesis of a New Series of 4-Aryl-1,4-Dihydropyridines with Calcium Channel Blocking and Vasodilatory Activity
Synthesis and biological evaluation of a novel class as antileishmanial agent
Synthesis of kojic acid-derived copper-chelating apoptosis inducing agents
Synthesis, stereochemistry, and antimicrobial evaluation of t(3)-isopropyl-r(2), c(6)-di-2-furanylpiperidin- 4-one and its derivatives
Natural toxins for use in pest management.
Novel GABA-AT inhibitors: QSAR and docking based virtual screening of phenyl substituted -phenyl ethylidene hydrazine analogues
Iodine catalyzed one-pot synthesis of chloro-substituted linear and angular indoloquinolines and in vitro antiproliferative activity study of different indoloquinolines
Synthesis of 3-methylflavones and their antioxidant and antibacterial activities
Synthesis, structure, and estrogenic activity of 2- and 3-substituted 2,3-dihydro-4H-1-benzopyran-4-ones
Pyridazin-3(2H)-ones: the versatile pharmacophore of medicinal significance
Preparation and testing of homocubyl amines as therapeutic NMDA receptor antagonists
Design and synthesis of 6-alkyoxyl[1,2,4]triazolo[1,5-a]quinazoline derivatives with anticonvulsant activity
Structure-Activity Relationships of the Azole Fungicide Metconazole and Its Related Azolylmethylcycloalkanols
Biososteric Replacement in the Design and Synthesis of Ligands for Nicotinic Acetylcholine Receptors
New thiazolidinyl analogs containing pyridine ring: synthesis, biological evaluation and QSAR studies
Synthesis, characterization and biological activity of some new carbostyril bearing 1H-pyrazole moiety
Pharmacophore modeling and 3D QSAR analysis of isothiazolidinedione derivatives as PTP1B inhibitors
An aphid repellent glycoside from Solanum laxum.
Synthesis and evaluation of 4-amino-5-phenyl-4H-[1,2,4]-triazole-3-thiol derivatives as antimicrobial agents
Synthesis and Fungicidal Activity of 3-1, 2, 4-Thiadiazolines
Effects of a prenyl-baicalein derivative on ER (+) MCF-7 and ER () MDA-MB-231 breast tumor cell lines
Antiproliferative activity of pentadeca-(8E, 13Z) dien-11-yn-2-one and (E)-1,8-pentadecadiene from Echinacea pallida (Nutt.) Nutt. roots
Synthesis of a ligandquencher conjugate for the ligand binding study of the aryl hydrocarbon receptor using a FRET assay
Synthesis, characterization, anticancer activity, and QSAR-studies of some new tetrahydropyrimidines
Evaluating commercially available rodenticide baits for invasive Gambian giant pouched rats (Cricetomys gambianus)
Design, synthesis and molecular modelling of novel 4-thiazolidinones of potential activity against Gram positive bacteria
Flavonoids as lead compounds modulating the enzyme targets in Alzheimers disease
Synthesis and Fungicidal Activity of New 1, 3, 2-Oxazaphospholidine 2-Sulfides
Sensitivity of Podosphaera aphanis isolates to DMI fungicides: distribution and reduced cross-sensitivity.
Synthesis and insect antifeedant activity of plumbagin derivatives
Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinsons agents
Synthesis and biological evaluation of 5,7-diaryl-4,4-dimethyl-4,5,6,7-tetrahydropyridino[3,4-d]-1,2,3-thiadiazoles
Synthesis and fungicidal evaluation of some new anilinopyrimidine derivatives
Synthesis and antiinflammatory activity of certain benzothieno[3,2-d][1,2,4]triazolo[4,3-b] pyridazine derivatives
Synthesis and reactive oxygen species scavenging activity of halogenated alkaloids from boldine
Binding properties and biological characterization of new sugar-derived Ras ligands
Fast and effective identification of the bioactive compounds and their targets from medicinal plants via computational chemical biology approach
Potent and selective inhibitors of human peptidylglycine -amidating monooxygenase
Synthesis and anti-Helicobacter pylori activity of analogues of spirolaxine methyl ether
Triazole-substituted N-hydroxyindol-2-carboxylates as inhibitors of isoform 5 of human lactate dehydrogenase (hLDH5)
Further SAR studies on 3,5-diamino-7-trifluoromethylquinolines as highly potent tyrosine kinase c-Met inhibitors: efforts to correct hERG inhibition
Monocyte and macrophage selective anti-inflammatory kinase inhibitors
Synthesis and binding affinities for sst receptors of cyclic peptoid SRIF-mimetics
3-Hydroxylation of the polycyclic tetramate macrolactam in the biosynthesis of antifungal HSAF from Lysobacter enzymogenes C3
N-Substituted salicylamides as selective malaria parasite dihydroorotate dehydrogenase inhibitors
Second generation analogues of RKA182: synthetic tetraoxanes with outstanding in vitro and in vivo antimalarial activities
The design and synthesis of 5- and 6-isoxazolylbenzimidazoles as selective inhibitors of the BET bromodomains.
Conformational effects on potency of thioimidazoles and dihydrothiazolines
Unprecedented inhibition of resistant penicillin binding proteins by bis-2-oxoazetidinyl macrocycles
Differential activation of soluble guanylate cyclase by a series of aryl disulfanyl dinitrate esters
trans-Stilbenoids: potent and selective inhibitors for human cytochrome P450 1B1
N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators
A class of novel AA-Trp-Trp-OBzl: synthesis, in vitro anti-proliferation, in vivo anti-tumor action, and intercalation mechanism
Structureactivity relationships of novel iodinated quinoline-2-carboxamides for targeting the translocator protein
Preparation and evaluation of BBB-permeable trehalose derivatives as potential therapeutic agents for Huntington's disease
Diacrylamides as selective G-quadruplex ligands in in vitro and in vivo assays
Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence
Design, synthesis and molecular modelling of novel methyl[4-oxo-2-(aroylimino)-3-(substituted phenyl)thiazolidin-5-ylidene]acetates as potent and selective aldose reductase inhibitors
Structure-activity relationship of conformationally constrained peptidomimetics for antiproliferative activity in HER2-overexpressing breast cancer cell lines.
Recent applications of multicomponent reactions in medicinal chemistry
Synthesis of a novel thiophene derivative that induces cancer cell apoptosis through modulation of AKT and MAPK pathways
Prodrug ionic liquids: functionalizing neutral active pharmaceutical ingredients to take advantage of the ionic liquid form
Structureactivity relationships of benzimidazole derivatives as antiparasitic agents: Dual activity-difference (DAD) maps
Synthesis and selective inhibition of human monoamine oxidases of a large scaffold of (4,5-substituted-thiazol-2-yl)hydrazones
Design of symmetrical and nonsymmetrical N,N-dimethylaminopyridine derivatives as highly potent choline kinase alpha inhibitors.
The MEP pathway and the development of inhibitors as potential anti-infective agents
Pharmacokinetics of bendamustine in the central nervous system: chemoinformatic screening followed by validation in a murine model
A rational design to create hybrid -sheet breaker peptides to inhibit aggregation and toxicity of amyloid-
Pyridylthiazole-based ureas as inhibitors of Rho associated protein kinases (ROCK1 and 2).
The discovery of N-1 substituted 2-aminobenzimidazoles as zinc-dependent S. aureus biofilm inhibitors.
Discovery and activity profiling of thailandepsins A through F, potent histone deacetylase inhibitors, from Burkholderia thailandensis E264.
Spiro[[1]benzothiophen-4,4-piperidines] carba analogs of potent 1 ligands
Discovery of a new class of dithiocarbamates and rhodanine scaffolds as potent antifungal agents: synthesis, biology and molecular docking
Synthesis and biological evaluation of imidazolylmethylacridones as cytochrome P-450 enzymes inhibitors
Rational design of small modified peptides as ACE inhibitors
A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
Structureactivity relationships of methyl-lysine reader antagonists
RCAI-133, an N-methylated analogue of KRN7000, activates mouse natural killer T cells to produce Th2-biased cytokines
Improvement of the trypanocidal activity of 3-arylthiophene farnesyltransferase inhibitors by modulation of their 3-aryl group
OH radical production stimulated by (RW)4D, a synthetic antimicrobial agent and indolicidin
Synthesis, modeling, and crystallographic study of 3,4-disubstituted-1,2,5-oxadiazoles and evaluation of their ability to decrease STAT3 activity
Selective antitumour activity and ER molecular docking studies of newly synthesizedd-homo fused steroidal tetrazoles
The discovery and profile of PF-0868087, a CNS-sparing histamine H3 receptor antagonist for the treatment of allergic rhinitis
Optimized glucuronidation of dual pharmacology -2 agonists/M3 antagonists for the treatment of COPD
20-O-IngenolEZ, a catalytic topoisomerase II inhibitor, specifically inhibits cell proliferation and induces double-strand DNA breaks in BLM-/- cells
Synthesis and NMDA receptor affinity of dexoxadrol analogues with modifications in position 4 of the piperidine ring
4-Alkyloxyimino-cytosine nucleotides: tethering approaches to molecular probes for the P2Y6 receptor.
Synthesis, microbial transformation, and pharmacological evaluation of 4,5-dihydronaphtho[2,1-b]furan-2-ones and related analogues
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2). Identification and synthesis of N-propyl-5-substituted isoquinolones
Discovery and structural modification of novel inhibitors of PTP1B inspired by the ACT fragment of scleritodermin A
Alkaloids from Rutaceae: activities of canthin-6-one alkaloids and synthetic analogues on glioblastoma stems cells
Discovery and characterization of novel potent PARP-1 inhibitors endowed with neuroprotective properties: From TIQ-A to HYDAMTIQ
SAR investigations on a novel class of gamma-secretase modulators based on a unique scaffold
Synthesis, cytotoxicity and hDHFR inhibition studies of 2H-pyrido[1,2-a]pyrimidin-2-ones
Novel thalidomide analogues with potent NFB and TNF expression inhibition
HIV-1 protease inhibitors with a tertiary alcohol containing transition-state mimic and various P2 and P1 substituents
Novel 3,5-bis(arylidiene)-4-piperidone based monocarbonyl analogs of curcumin: anticancer activity evaluation and mode of action study
Modular assembly of cytotoxic acetogenin mimetics by click linkage with nitrogen functionalities
Chimerically designed HDAC- and tyrosine kinase inhibitors. A series of erlotinib hybrids as dual-selective inhibitors of EGFR, HER2 and histone deacetylases
The use of phosphate bioisosteres in medicinal chemistry and chemical biology
Design and synthesis of trans-2-substituted-cyclopropane-1-carboxylic acids as the first non-natural small molecule inhibitors of O-acetylserine sulfhydrylase
Relative impact of 3- and 5-hydroxyl groups of cytosporone B on cancer cell viability.
Diaryl ether derivatives as anticancer agents a review
Design of 7-amino-6-chloro-3H-imidazo[4,5-b]pyridine scaffold from 5-chloro-2,4-diaminopyrimidine pharmacophore: identification of potent inhibitors of anaplastic lymphoma kinase
Tacrine-mefenamic acid hybrids for inhibition of acetylcholinesterase
Probing androgen receptor co-factor selectivity profiles: a chemical tool to determine cross-talk between androgen receptor and -catenin in vivo
Syntheses of a new class of phenyl butyraldehyde-derived amines with in vitro trypanocide activities
Identification of 4,6-diaryl-1,4-dihydropyridines as a new class of neuroprotective agents
Designing glucokinase activators with reduced hypoglycemia risk: discovery of N,N-dimethyl-5-(2-methyl-6-((5-methylpyrazin-2-yl)-carbamoyl)benzofuran-4-yloxy)pyrimidine-2-carboxamide as a clinical candidate for the treatment of type 2 diabetes mellitus
Benzisothiazolones arrest the cell cycle at the G2/M phase and induce apoptosis in HeLa cells
Discovery of novel morpholinoquinoxalines as PI3K inhibitors by pharmacophore-based screening
Intramolecular hydrogen bonding to improve membrane permeability and absorption in beyond rule of five chemical space
Potent sirtuin inhibition bestowed by l-2-amino-7-carboxamidoheptanoic acid (l-ACAH), a N-acetyl-lysine analog
Water soluble flavonol prodrugs that protect against ischaemia-reperfusion injury in rat hindlimb and sheep heart
Simplified platensimycin analogues as antibacterial agents
Synthesis and trypanocidal action of new adamantane substituted imidazolines
Pharmacological properties of indolone-N-oxides controlled by a bioreductive transformation in red blood cells?
Design, synthesis and biological evaluation of novel benzothiazole and triazole analogs as falcipain inhibitors
Temocene: the porphycene analogue of temoporfin (Foscan)
Synthetic modulators of the retinoic acid receptor-related orphan receptors
Property based optimisation of glucokinase activators discovery of the phase IIb clinical candidate AZD1656
Structure-function study of gemini derivatives with two different side chains at C-20, Gemini-0072 and Gemini-0097.
Mechanistic insight into inhibition of two-component system signaling.
Discovery of hydroxamate bioisosteres as KAT II inhibitors with improved oral bioavailability and pharmacokinetics
Repairing faulty genes by aminoglycosides: Identification of new pharmacophore with enhanced suppression of disease-causing nonsense mutations
Online parallel fragment screening and rapid hit exploration for nicotinic acetylcholine receptors.
Inhibitors of bacterial tubulin target bacterial membranes in vivo.
Prospective use of molecular field points in ligand-based virtual screening: efficient identification of new reversible Cdc25 inhibitors
Glycosylated porphyrin derivatives and their photodynamic activity in cancer cells
Synthesis of new N-substituted aminoquercitols from naturally available (+)-proto-quercitol and their -glucosidase inhibitory activity
Discovery of novel selective Sigma-1 ligands as cognitive enhancers
A furoxan-amodiaquine hybrid as a potential therapeutic for three parasitic diseases().
Synthesis and SAR of 2,4-diaminopyrimidines as potent c-jun N-terminal kinase inhibitors
Design and synthesis of -amino alcohol based -lactamisatin chimeras and preliminary analysis of in vitro activity against the protozoal pathogen Trichomonas vaginalis
Beta-adrenergic receptor signaling by the isomers of isoproterenol and like drugs in retinal endothelial cells and Muller cells
The development of quinoloneesters as novel antimalarial agents targeting the Plasmodium falciparum bc1protein complex
Identification of a potent salicylic acid-based inhibitor of tyrosine phosphatase PTP1B
Rapid assembly of potent type II dehydroquinase inhibitors viaClick chemistry
Scaffold-hopping from aminoglycosides to small synthetic inhibitors of bacterial protein biosynthesis using a pseudoreceptor model
Synthesis and antifungal activity of 1,5-disubstituted-1,2,3-triazole containing fluconazole analogues
Design, synthesis and antiproliferative activity of urocanic-chalcone hybrid derivatives
Selective inhibition of E. coli 1-deoxy-D-xylulose-5-phosphate synthase by acetylphosphonates().
Discovery of GS-8374, a potent human immunodeficiency virus type 1 protease inhibitor with a superior resistance profile
Evaluation of FR901464 analogues in vitro and in vivo
Synthesis and biological evaluation of 4-chlorocolchicine derivatives as potent anticancer agents with broad effective dosage ranges
Amino-derivatives of the sesquiterpene lactone class of natural products as prodrugs
Synthesis, thiol-mediated reactive oxygen species generation profiles and anti-proliferative activities of 2,3-epoxy-1,4-naphthoquinones
Extended side chain analogues of 8-aminoquinolines: Synthesis and evaluation of antiprotozoal, antimicrobial, -hematin inhibition, and cytotoxic activities
3-Formylchromone based topoisomerase II inhibitors: discovery of potent leads
Activation of a silent phenazine biosynthetic gene cluster reveals a novel natural product and a new resistance mechanism against phenazines
Structures and biofilm inhibition activities of brominated furanones for Escherichia coli and Pseudomonas aeruginosa
l-Penicillamine is a mechanism-based inhibitor of serine palmitoyltransferase by forming a pyridoxal-5-phosphate-thiazolidine adduct
Optimization of a series of dipeptides with a P3 -neopentyl asparagine residue as non-covalent inhibitors of the chymotrypsin-like activity of human 20S proteasome
Synthesis of cyanine dyes and investigation of their in vitro antiprotozoal activities
Inhibition of bromodomain-mediated proteinprotein interactions as a novel therapeutic strategy
Diaryl ureaLDV peptidomimetics as 41integrin antagonists: synthesis, adhesion inhibition and toxicity evaluation on CCRF-CEM cell line
Homodimers of the Antiviral Abacavir as Modulators of P-glycoprotein Transport in Cell Culture: Probing Tether Length.
Synthesis, biological evaluation and X-ray crystallographic studies of imidazo[1,2-a]pyridine-based Mycobacterium tuberculosis glutamine synthetase inhibitors
Oxathiazole-2-one derivative of bortezomib: Synthesis, stability and proteasome inhibition activity
Synthesis and biological activity profile of novel 2-cinnamylidene-1,3-diones related to coruscanone A: promising new antileishmanial agents
Synthesis and antiproliferative activity of some 3-(pyrid-2-yl)-pyrazolines
Phosphofructokinase: structural and functional aspects and design of selective inhibitors
Discovery of highly potent antifungal triazoles by structure-based lead fusion
Matched triplicate design sets in the optimisation of glucokinase activators maximising medicinal chemistry information content
Synthesis and cytotoxicity evaluation of regioisomeric substituted N-phenyl-3-(chrom-4-one-3-yl)-isoxazolidines: induction of apoptosis through a mitochondrial-dependent pathway
Quantitative affinity-based chemical proteomics of TrkA inhibitors
A new route to indoles via in situ desilylationSonogashira strategy: identification of novel small molecules as potential anti-tuberculosis agents
Identification of multifunctional small molecule-based reversible monoamine oxidase inhibitors
Structure-based design, synthesis, and profiling of potent and selective neuronal nitric oxide synthase (nNOS) inhibitors with an amidinothiophene hydroxypiperidine scaffold
Synthesis and antiplasmodial evaluation of aziridine(iso)quinoline hybrids and their ring-opening products
Superiority of a novel EGFR targeted covalent inhibitor over its reversible counterpart in overcoming drug resistance
Discovery and optimization of efficacious neutral 4-amino-6-biphenyl-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-5-one diacylglycerol acyl transferase-1 (DGAT1) inhibitors
Airborne antituberculosis activity of Eucalyptus citriodora essential oil.
HPLC-based activity profiling for GABAA receptor modulators in Adenocarpus cincinnatus.
Bioactive limonoids from the leaves of Azaridachta indica (Neem).
Flavonoids, flavonoid metabolites, and phenolic acids inhibit oxidative stress in the neuronal cell line HT-22 monitored by ECIS and MTT assay: a comparative study.
Novel 8-(p-substituted-phenyl/benzyl)xanthines with selectivity for the A2A adenosine receptor possess bronchospasmolytic activity.
Identification of chromomoric acid C-I as an Nrf2 activator in Chromolaena odorata.
Identification of diverse natural products as falcipain-2 inhibitors through structure-based virtual screening.
Chemical genetics-based discovery of indole derivatives as HCV NS5B polymerase inhibitors.
Biologically active eremophilane-type sesquiterpenes from Camarops sp., an endophytic fungus isolated from Alibertia macrophylla.
Simplified pretubulysin derivatives and their biological effects on cancer cells.
Discovery of ledipasvir (GS-5885): a potent, once-daily oral NS5A inhibitor for the treatment of hepatitis C virus infection.
Synthesis, structure-activity relationship of iodinated-4-aryloxymethyl-coumarins as potential anti-cancer and anti-mycobacterial agents.
Benzofuran derivatives as a novel class of inhibitors of mTOR signaling.
NF-B inhibitors from Eurycoma longifolia.
Bioactive compounds from Vitex leptobotrys.
Indoloditerpenes from a marine-derived fungal strain of Dichotomomyces cejpii with antagonistic activity at GPR18 and cannabinoid receptors.
High-affinity recognition of HIV-1 frameshift-stimulating RNA alters frameshifting in vitro and interferes with HIV-1 infectivity.
Direct interaction of garcinol and related polyisoprenylated benzophenones of Garcinia cambogia fruits with the transcription factor STAT-1 as a likely mechanism of their inhibitory effect on cytokine signaling pathways.
Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors.
Synthesis and evaluation of new coumarin derivatives as potential atypical antipsychotics.
Toward synthesis of third-generation spin-labeled podophyllotoxin derivatives using isocyanide multicomponent reactions.
Lead optimization of HMBA to develop potent HEXIM1 inducers.
Evaluation of intestinal permeability of vicenin-2 and lychnopholic acid from Lychnophora salicifolia (Brazilian arnicao) using Caco-2 cells.
Antiviral compounds for the treatment of HCV.
A review of non-nucleoside anti-hepatitis B virus agents.
Balgacyclamides, antiplasmodial heterocyclic peptides from Microcystis aeruguinosa EAWAG 251.
Use of 2'-spirocyclic ethers in HCV nucleoside design.
Design, synthesis and molecular modeling of aloe-emodin derivatives as potent xanthine oxidase inhibitors.
Synthesis and in vitro urease inhibitory activity of N,N'-disubstituted thioureas.
Novel Quinoline-Based P2-P4 Macrocyclic Derivatives As Pan-Genotypic HCV NS3/4a Protease Inhibitors.
4,4'-Diaminodiphenyl ether derivatives: synthesis, spectral, optical, thermal characterization and in-vitro cytotoxicity against Hep 3B and IMR 32 human cell lines.
Structures and solution conformational dynamics of stylissamides G and H from the Bahamian sponge Stylissa caribica.
3-Amino-N-adamantyl-3-methylbutanamide derivatives as 11-hydroxysteroid dehydrogenase 1 inhibitor.
Discovery of 2-pyridone derivatives as potent HIV-1 NNRTIs using molecular hybridization based on crystallographic overlays.
Sesquiterpenes from Neurolaena lobata and their antiproliferative and anti-inflammatory activities.
Octulosonic acid derivatives from Roman chamomile (Chamaemelum nobile) with activities against inflammation and metabolic disorder.
Antibacterial halogenoacetyl derivatives of amino acids and simple peptides.
3-Aminotetrahydrocarbazoles as a new series of central nervous system agents.
Antiviral activity of some beta-diketones. 4. Benzyl diketones. In vitro activity against both RNA and DNA viruses.
Design, synthesis, and structureactivity relationships of indole-3-carboxamides as novel water soluble cannabinoid CB1 receptor agonists
A highly selective agonist for the metabotropic glutamate receptor mGluR2
De novo design, synthesis and pharmacological evaluation of new azaindole derivatives as dual inhibitors of Abl and Src kinases
Development of second generation epigenetic agents
New insight into the mode of action of vancomycin dimers in bacterial cell wall synthesis
Mannich- and LedererManasse-based analogues of the natural product S-(+)-curcuphenol as cancer proliferation and migration inhibitors
Bridged tetrahydroisoquinolines as selective NADPH oxidase 2 (Nox2) inhibitors.
Synthesis, anti-proliferative and proapoptotic activity of novel oleanolic acid azaheterocyclic derivatives
Triazolopyrimidinones as -secretase modulators: structureactivity relationship, modulator profile, and in vivo profiling
Expanding the horizon of chemotherapeutic targets: From MDM2 to MDMX (MDM4)
Design and synthesis of novel N,N-glycoside derivatives of 3,3-diindolylmethanes as potential antiproliferative agents
Discovery of nitrophenols as GPR35 agonists
Natural products targeting telomere maintenance
Development of substituted 7-phenyl-4-aminobenzothieno[3,2-d] pyrimidines as potent LIMK1 inhibitors
Development of second generation amidinohydrazones, thio- and semicarbazones as Trypanosoma cruzi-inhibitors bearing benzofuroxan and benzimidazole 1,3-dioxide core scaffolds
Synthesis and biological activity of new pyridone diaryl ether non-nucleoside inhibitors of HIV-1 reverse transcriptase
Boronic acids in medicinal chemistry: anticancer, antibacterial and antiviral applications
Affinity selection and sequence-activity relationships of HIV-1 membrane fusion inhibitors directed at the drug-resistant variants
MMV box screening in the Dd2 P. falciparum strain
Reversible and irreversible small molecule inhibitors of monoamine oxidase B (MAO-B) investigated by biophysical techniques.
Cannabidiol (CBD) and its analogs: a review of their effects on inflammation.
Discovery of 7-azaindole derivatives as potent Orai inhibitors showing efficacy in a preclinical model of asthma.
Fingerprint-based consensus virtual screening towards structurally new 5-HT(6)R ligands.
Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice.
Synthesis of novel pleuromutilin derivatives. Part 1: preliminary studies of antituberculosis activity.
Design, synthesis and preliminary bioactivity studies of 2-thioxo-4-thiazolidinone derivatives as Bcl-2 inhibitors.
Novel neurotrophic phenylbutenoids from Indonesian ginger Bangle, Zingiber purpureum.
Synthesis of mycothiol conjugate analogues and evaluation of their antimycobacterial activity.
Synthesis and biological evaluation of benzimidazole acridine derivatives as potential DNA-binding and apoptosis-inducing agents.
Canthinone alkaloids are novel protein tyrosine phosphatase 1B inhibitors.
Discovery of novel S1P2 antagonists. Part 1: discovery of 1,3-bis(aryloxy)benzene derivatives.
Targeting epigenetic modifiers: Inhibitors of histone methyltransferases
Easy Preparation of Methyl 7-epi-Jasmonate and Four Stereoisomers of Methyl Cucurbate, and Assessment of the Stereogenic Effect of Jasmonate on Phytohormonal Activities.
Synthesis and anticonvulsant activity of some new series of pyrrole derivatives
Fungicidal activities of cyflufenamid against various plant-pathogenic fungi
A novel series of homoallylic amines as potential antimicrobials
Synthesis of novel triazole derivatives as potent inhibitor of allene oxide synthase (CYP74A), a key enzyme in jasmonic acid biosynthesis
(Naphthalen-1-yloxy)-acetic acid benzylidene/(1-phenyl-ethylidene)-hydrazide derivatives: synthesis, antimicrobial evaluation, and QSAR studies
Modeling VEGFR kinase inhibition of aminopyrazolopyridine urea derivatives using topological and physicochemical descriptors: a quantitative structure activity analysis study
Structure-Activity Relationships of 2-Chloropyridine-3-carboxamide Fungicides
Enantioselective Relieving Activity of -Methylbenzylphenylureas toward Bensulfuron-methyl Injury to Rice (Oryza sativa).
Synthesis and antimicrobial activity of pyrazolinones and pyrazoles having benzothiazole moiety
Receptor and ligand-based 3D-QSAR study on a series of nonsteroidal anti-inflammatory drugs
Synthesis and biological evaluation of ester derivatives of indomethacin as selective COX-2 inhibitors
Synthesis and in vitro antitumor activity of 1-(3-dimethylamino)propyl indolin-2-one derivatives
Efficacy and effects on yield of different fungicides for control of wet bubble disease of mushroom caused by the mycoparasite Mycogone perniciosa
Occurrence of zearalenone-4-beta-D-glucopyranoside in wheat.
Synthesis and evaluation of 2,4,6-trisubstituted pyrimidine derivatives as novel antileishmanial agents
Synthesis, characterization and antimicrobial activities of some novel bis-chalcones
Synthesis and biological evaluation of new curcumin derivatives as antioxidant and antitumor agents
Structure, Conformation and Absolute Configuration of New Antifeedant Dolabellanes from Trichilia trifolia
Design, synthesis and antidepressant activity evaluation 2-hydroxy-4,6-diisoprenyloxychalcone derivatives
Synthesis and Acaricidal Activity of N-(3-Pyridylmethyl)pyrazolecarboxamide Derivatives
Regulation of glycogen metabolism by anti-dyslipidemic action of gemfibrozil and cholestyramine in a dyslipidemic-diabetic hamster model
5-Nitro-heteroarylidene analogs of 2-thiazolylimino-4-thiazolidinones as a novel series of antibacterial agents
Synthesis, characterization, and antimicrobial screening of some Mannich base sydnone derivatives
Synthesis and antimalarial activity evaluation of some isoquine analogues
Synthesis, Antiviral and Antibacterial Activities of Isatin Mannich Bases
Synthesis, anticonvulsant and neurotoxic activity of some new 2,5-disubstituted-1,3,4-oxadiazoles
Hypolipidemic, hepato-protective and renal damage recovering effects of catechin isolated from the methanolic extract of Cassia fistula stem bark on Streptozotocin-induced diabetic Wistar rats: a biochemical and morphological analysis
Exploration of antimicrobial potential of pyrazolo[3,4-b]pyridine scaffold bearing benzenesulfonamide and trifluoromethyl moieties
Stability of DNA upon interaction with dimethyltin dichloride
Synthesis and Fungicidal Activity of -Cyanoacetamide Derivatives: Discovery of a New Rice Blast Fungicide, Diclocymet (S-2900)
Induction of Resistance against Rice Bacterial Leaf Blight by 3-Chloro-1-methyl-1H-pyrazole-5-carboxylic Acid
Synthesis, characterization, and biological evaluation of novel thiazole and pyrazole derivatives of quinoline-4-carboxylic acid as potential antimicrobial agents
Synthesis and antiviral activities of antofine analogues with different C-6 substituent groups.
Synthesis of potential anticancer derivatives of pyrido[1,2-a]benzimidazoles
Microwave-assisted CAN-catalyzed solvent-free synthesis of N-allyl quinolone-based pyrano[4,3-b]chromene and benzopyrano[3,2-c]chromene derivatives and their antimicrobial activity
Fungicidal activity of pipernonaline, a piperidine alkaloid derived from long pepper, Piper longum L., against phytopathogenic fungi
Mode for Herbicidal Action of 2-Amino-3-chloro-1,4-naphthoquinone (ACN)
Synthesis of Stereoisomers of Ipconazole and Their Fungicidal and Plant Growth Inhibitory Activities
Structural features of GABAA receptor antagonists: pharmacophore modeling and 3D-QSAR studies
In vitro antimicrobial and antimycobacterial activity of some chalcones and their derivatives
Isolation and structural elucidation of eight new related analogues of the mycotoxin (-)-botryodiplodin from Penicillium coalescens.
2-Bromo-1-ethoxy-(2,4-dichloro)styrene and 2,2-dibromo-1-ethoxy-(2,4-dichloro)styrenethe two impurities of bromfenvinphos; their identification, synthesis and full characterization
Studies on characteristics of ATPase activity of cardiac myosin in the presence of daunorubicin
Novel malyngamide structural analogs: synthesis and biological evaluation
Design, synthesis and evaluation of novel indomethacinflavonoid mutual prodrugs as safer NSAIDs
Biological Activity of Carpropamid (KTU 3616)
Design, synthesis and biological evaluation of novel arylidine-malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B
Synthesis and biological studies of a novel series of 4-(4-(1H-imidazol-1-yl)phenyl)-6-arylpyrimidin-2-amines
Antifungal, mosquito deterrent, and larvicidal activity of N-(benzylidene)-3-cyclohexylpropionic acid hydrazide derivatives
Biological evaluation of synthetic analogues of curcumin: chloro-substituted-2-hydroxychalcones as potential inhibitors of tubulin polymerization and cell proliferation
RP-HPLC method for the quantitative determination of fexofenadine hydrochloride in coated tablets and human serum
Development of Selective Ligands for Benzodiazepine Receptor Subtypes by Manipulating the Substituents at Positions 3- and 7- of Optically Active BzR Ligands
Novel 2H-[1,2,4]thiadiazolo[2,3-a]pyrimidine derivatives bearing chiral S()-2-(4-chlorophenyl)-3-methylbutyric acid moiety: Design, synthesis and herbicidal activity
Major alkaloidal constituent from Impatiens niamniamensis seeds as antihyperglycemic agent
I2 catalyzed FriedelCrafts alkylation reaction of substituted anilines with ninhydrin: formation of novel products and their antimicrobial evaluation
Design, synthesis and preliminary evaluation of some novel [1,4]diazepino [5,6-b]pyrrolizine and 6-(2-oxopyrrolidino)-1H-pyrrolizine derivatives as anticonvulsant agents
Effect of 2-allylphenol against Botrytis cinerea Pers., and its residue in tomato fruit
Ligand-based drug design for human endothelin converting enzyme-1 inhibitors
Synthesis and evaluation of some novel methylene-bridged aryl semicarbazones as potential anticonvulsant agents
Affinity of 3-benzylidene- and 3-cinnamylidenemyosmine analogues for Periplaneta americana nicotinic acetylcholine receptors
Sensitivity of Sclerotinia sclerotiorum from oilseed crops to boscalid in Jiangsu Province of China
Prediction of antiproliferative activity of some flavone derivatives: QSAR study
Synthesis and anti-cancer activity of some novel C-17 analogs of ursolic and oleanolic acids
Goat brain enkephalin degrading enzyme: interaction with analgesic and antihypertensive drugs
Insecticide-induced resurgence of the whitebacked planthopper Sogatella furcifera (Horvath) (Hemiptera: Delphacidae) on rice varieties with different levels of resistance
Chalcones as promising pesticidal agents against diamondback moth (Plutella xylostella): microwave-assisted synthesis and structureactivity relationship
Molecular modeling and synthesis of ZINC02765569 derivatives as protein tyrosine phosphatase 1B inhibitors: lead optimization study
Synthesis of combretastatin analogs: evaluation of in vitro anticancer activity and molecular docking studies
Potent, Selective Adenosine A1 Agonists as Potential Analgesics
Bioactivity guided isolation of antiinflammatory, analgesic, and antipyretic constituents from the leaves of Pedilanthus tithymaloides (L.)
3D-QSAR STUDIES ON SUBSTITUTED DIHYDROPYRIDINES FOR THEIR 1A-ADRENERGIC RECEPTOR BINDING AFFINITY
N-Thiophenylethyl-2,2-dichloro-1-cyclopropanecarboxamides: modification of the amide part of carpropamid and examination of fungicidal activity
Antituberculosis activity of hydrazones derived from 4-fluorobenzoic acid hydrazide
Synthesis and antifungal activity of novel 2,5-disubstituted-1,3,4-oxadiazoles containing benzimidazole moiety
Inhibitory effect and structureactivity relationship of some Biginelli-type pyrimidines against HSV-1
Lipophilic 2-(4-chlorophenyl)-4-thiazolyl-1,4-dihydropyridines: synthesis, calcium channel antagonist activity, and protection against pentylenetetrazole-induced seizure
Antifeedant and larvicidal activities of Rhein isolated from the flowers of Cassia fistula L.
Chem-bioinformatics and in vitro approaches for candidate optimization: a case study of NSC745689 as a promising antitumor agent
Antituberculosis and antibacterial evaluations of some novel phenyl pyrazolone-substituted 1h-benzo[g]pyrazolo[3,4-b]quinoline-3-ylamine derivatives
Anti-inflammatory activity of 2,5-dihydroxycyclohepta-2,4,6-trienone in rats
Microwave-assisted synthesis of some new tetrazolo[1,5-a]quinoline-based benzimidazoles catalyzed by p-TsOH and investigation of their antimicrobial activity
Mode of Action of Herbicides Affecting Carotenogenesis
Spore Germination Self-Inhibitors from Plant Pathogenic Fungi
Synthesis and preliminary evaluation of difluorinated 1,3-propanediones as potential agents in the treatment of breast cancer
Pharmacological Characteristics of Insect Nicotinic Acetyicholine Receptor with Its Ion Channel and the Comparison of the Effect of Nicotinoids and Neonicotinoids
Oxadiazolo pyrrolidine carboxamides as enoyl-ACP reductase inhibitors: design, synthesis and antitubercular activity screening
Effects of Two Isoflavonoids, Osajin and Pomiferin, from Maclura pomifera for Growth and Feeding Disruption in Ostrinia nubilalis
Synthesis of some novel triazoloquinazolines and triazinoquinazolines and their evaluation for anti-inflammatory activity
Design, synthesis, and biological evaluation of novel 2,4-thiazolidinedione derivatives as histone deacetylase inhibitors targeting liver cancer cell line
An efficient one-pot cyclization of quinoline thiosemicarbazones to quinolines derivatized with 1,3,4-thiadiazole as anticancer and anti-tubercular agents
Field study of the relative susceptibility of eleven potato (Solanum tuberosum L.) varieties and the efficacy of two fungicides against Rhizoctonia solani attack
Tolerance of tomato, pepper and potato to pre-emergence applications of saflufenacil
Synthesis of novel 3-[5-ethyl-2-(2-phenoxy-ethyl)-pyridin]-5-substituted isoxazoline libraries via 1,3-dipolar cycloaddition and evaluation of antimicrobial activities
Selective Herbicidal Activity of 3, 5-Dichloropyridyloxy-phenoxypropionamidoxyacetic Acid Derivatives between Wheat and Wild Oat
Synthesis and evaluation of anti-inflammatory, analgesic, ulcerogenicity and nitric oxide-releasing studies of novel ibuprofen analogs as nonulcerogenic derivatives
Responses of dry beans (Phaseolus vulgaris L.) to sulfentrazone
Development of a new acaricide, cyflumetofen
Synthesis and cytotoxicity evaluation of novel pyrido[3,4-d]pyrimidine derivatives as potential anticancer agents.
Synthesis and biological evaluation of 7-arylindoline-1-benzenesulfonamides as a novel class of potent anticancer agents
Diaryl- and triaryl-pyrrole derivatives: inhibitors of the MDM2-p53 and MDMX-p53 protein-protein interactionsElectronic supplementary information (ESI) available: Experimental details for compound synthesis, analytical data for all compounds and intermediates. Details for the biological evaluation. Further details for the modeling. Table of combustion analysis data. See DOI: 10.1039/c3md00161jClick here for additional data file.
Synthesis and evaluation of thiadiazole derivatives as inhibitors of 11-hydroxysteroid dehydrogenase type 1
Novel candesartan derivatives as indoleamine 2,3-dioxygenase inhibitors
The discovery of a novel prototype small molecule TLR7 agonist for the treatment of hepatitis C virus infection
Syntheses and biological evaluation of new cephalosporin-oxazolidinone conjugates.
Discovery of potent, proteolytically stable, and cell permeable human sirtuin peptidomimetic inhibitors containing N-thioacetyl-lysine
Synthesis and SAR studies of benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Focus to detune hERG inhibition
Squaric acid: a valuable scaffold for developing antimalarials?
Oxadiazole isomers: all bioisosteres are not created equal
N-substituted sultam carboxylic acids as novel glycogen synthase activators
Combination of biotransformation by P450 BM3 mutants with on-line post-column bioaffinity and mass spectrometric profiling as a novel strategy to diversify and characterize p38 kinase inhibitors
Synthesis and evaluation of stable substrate analogs as potential modulators of cyclodiphosphate synthase IspF.
Identification of CYP1A2 ligands by structure-based and ligand-based virtual screening
A matched molecular pair analysis of in vitro human microsomal metabolic stability measurements for heterocyclic replacements of di-substituted benzene containing compounds identification of those isosteres more likely to have beneficial effects
2-Anilinonicotinyl linked 1,3,4-oxadiazole derivatives: Synthesis, antitumour activity and inhibition of tubulin polymerization
SAR mining and its application to the design of TRPA1 antagonists
Antimalarial peroxides: advances in drug discovery and design
Erythromycin B: conformational analysis and antibacterial activity
Improved biodistribution, pharmacokinetics and photodynamic efficacy using a new photostable sulfonamide bacteriochlorin
Synthesis and biological evaluation of primaquinechloroquine twin drug: a novel heme-interacting molecule prevents free heme and hydroxyl radical-mediated protein degradation
Synthesis and anti HSV-1 evaluation of novel indole-3,4-diones
Potential atypical antipsychotics: synthesis, binding affinity and SAR of new heterocyclic bioisosteric butyrophenone analogues as multitarget ligands
Synthesis and antiproliferative activity of novel erythromycin derivatives
Synthesis, radical scavenging activity and structureactivity relationship of uric acid analogs
A pseudorotaxane umbrella thread with chloride transmembrane transport properties
Identification of an inhibitor of the ubiquitinproteasome system that induces accumulation of polyubiquitinated proteins in the absence of blocking of proteasome function
An Amino-Benzosuberene Analogue That Inhibits Tubulin Assembly and Demonstrates Remarkable Cytotoxicity.
Synthesis of hybrid 4-anilinoquinoline triazines as potent antimalarial agents, their in silico modeling and bioevaluation as Plasmodium falciparumtransketolase and -hematin inhibitors
Optimizing PK properties of cyclic peptides: the effect of side chain substitutions on permeability and clearance().
Synthesis and evaluation of a series of benzothiophene acrylonitrile analogs as anticancer agents.
Peptidomimetic nitriles as selective inhibitors for the malarial cysteine protease falcipain-2
Asymmetric synthesis of potent chroman-based Rho kinase (ROCK-II) inhibitors
Berberine azoles as antimicrobial agents: synthesis, biological evaluation and their interactions with human serum albumin
Searching for innovative quinolone-like scaffolds: synthesis and biological evaluation of 2,1-benzothiazine 2,2-dioxide derivatives
Sangamides, a new class of cyclophilin-inhibiting host-targeted antivirals for treatment of HCV infection
Determination of structural requirements of influenza neuraminidase type A inhibitors and binding interaction analysis with the active site of A/H1N1 by 3D-QSAR CoMFA and CoMSIA modeling
Pharmacokinetics of Agelastatin A in the central nervous system
Inhibition of Pseudomonas aeruginosa biofilms with a glycopeptide dendrimer containing D-amino acids
Synthesis of precursors and macrocycle analogs of aerucyclamides as anti-trypanosomal agents
Sulfonyl-hydrazones of cyclic imides derivatives as potent inhibitors of the Mycobacterium tuberculosis protein tyrosine phosphatase B (PtpB)
Polyamine-based small molecule epigenetic modulators.
Novel aspects in structureactivity relationships of profiled 1-aza-9-oxafluorenes as inhibitors of Alzheimer's disease-relevant kinases cdk1, cdk5 and gsk3
Discovery of a highly selective FLT3 kinase inhibitor from phenotypic cell viability profiling
Preparation of blood-brain barrier-permeable paclitaxel-carrier conjugate and its chemotherapeutic activity in the mouse glioblastoma model
Ester prodrugs of ciprofloxacin as DNA-gyrase inhibitors: synthesis, antiparasitic evaluation and docking studies
Novel selective inhibitors of neutral endopeptidase: discovery by screening and hit-to-lead optimisation
Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B
Mapping of a lipoglycopeptide antibiotic binding site on Staphylococcus aureus penicillin-binding protein 2 using a vancomycin photoaffinity analogue
Reduction of acyl glucuronidation in a series of acidic 11-hydroxysteroid dehydrogenase type 1 (11-HSD1) inhibitors: the discovery of AZD6925
Non-iminosugar glucocerebrosidase small molecule chaperones.
Identification of false positives in HTS hits to lead: The application of Bayesian models in HTS triage to rapidly deliver a series of selective TRPV4 antagonists
Edaravone containing isoindoline nitroxides for the potential treatment of cardiovascular ischaemia
Discovery and pharmacological characterization of a selective delta opiate receptor antagonist (CP-646,777)
Chemical synthesis and biological study of 4-carboxymethyl-epiafzelechin acid, an osteoprotective compound from the rhizomes of Drynaria fortunei
Design and synthesis of novel pyranone-based insulin sensitizers exhibiting in vivo hepatoprotective activity
Small-molecule inhibitors of dimeric transcription factors: Antagonism of proteinprotein and proteinDNA interactions
Potent inhibition of Ca2+-dependent activation of calpain-1 by novel mercaptoacrylates
Small molecules targeting phosphoinositide 3-kinases
Discovery of selective 2,4-diaminopyrimidine-based photoaffinity probes for glyoxalase I
Nitro-based inhibitors against thermolysin
Design, synthesis and biological evaluation of biphenyl urea derivatives as novel VEGFR-2 inhibitors
Biological and computational evaluation of an oxadiazole derivative (MD77) as a new lead for direct STAT3 inhibitors
Attempted inhibition of histidine decarboxylase with beta-alkyl analogues of histidine.
Synthesis and central nervous system activity of 2-arylidene-4-aminoalkyl-2H-1,4-benzoxazin-3(4H)-ones and related compounds.
5-Cyano-2'-deoxyuridine 5'-phosphate: a potent competitive inhibitor of thymidylate synthetase.
Relationships between opiate receptor binding and analgetic properties of prodine-type compounds.
Beta-Adrenergic blocking agents. 15. 1-Substituted ureidophenoxy-3-amino-2-propanols.
Methotrexate analogues. 10. Direct coupling of methotrexate and diethyl L-glutamate in the presence of peptide bond-forming reagents.
Effects of deuteration on locomotor activity of amphetamine.
Preparation and biological actions of some symmetrically N,N-disubstituted dopamines.
Synthesis of carboxyarylindoles and benzofurans as nonsteroidal antiinflammatory agents.
Synthetic sulfur-containing amino acids. Inhibition of transport systems in S37 ascites tumor cells.
Synthesis and biological activity of potential antimetabolites.
(2-Carboxy-1,4-dihydro-4-oxoquinolyl)oxamic acids and (2-carboxy-1,4-dihydro-4-oxobenzo[h]quinolyl)oxamic acids as antiallergy agents.
Synthesis and antibacterial activity of 2'-substituted chelocardin analogues.
Antiallergic activity of some 9H-xanthen-9-one-2-carboxylic acids.
11,12-secoprostaglandins. 4. 7-(N-alkylmethanesulfonamido) heptanoic acids.
Narcotic antagonists. Synthesis and evaluation of some subsituted 1,2,3,4,5,6-hexahydro-1,4:2,6-dimethano-3-benzazocines.
Analgesics and narcotic antagonists in the benzomorphan and 8-oxamorphinan series. 5.
Synthesis of heteroaromatic potential beta-adrenergic antagonists by the glycidol route.
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
2-Azabicyclo (2.2.2)octane analogues of the prodine analgetics.
Synthesis and antihypertensive activity of 1-amino-3,4-dihydroisoquinolines.
Synthesis of prostaglandin synthetase substrate analogues. 2. (8Z,11Z,14Z)-15-Methyl-8,11,14-eicosatrienoic acid.
Quinazolines and 1,4-benzodiazepines. 81. s-Triazolo[4,3-a][1,4]benzodiazepines by oxidative cyclization of hydrazones.
Synthesis and antiinflammatory activity of some 2-substituted 4- and 7-benzoxazoleacetic and alpha-methylacetic acids.
Potential antitumor agents. 24. Dicationic analogues of the 4'-(9-acridinylamino)alkanesulfonanilides.
Synthetic metabolites of neurohypophyseal hormones. (Des-9-glycinamide)oxytocin and (des-9-glycinamide, des-8-leucine)oxytocin.
Biologically active derivatives of angiotensin for labeling cellular receptors.
Central nervous system active 5-oxo-1,4,5,6,7,8-hexahydrocinnolines.
Inhibitors of folate biosynthesis. 1. Inhibition of dihydroneopterin aldolase by pteridine derivatives.
Analgesic agents. 3. New bridged aminotetralins.
Synthesis, antifertility activity, and protein binding affinity of 7(8 leads to 11 alpha)abeo steroids.
A novel prostaglandin endoperoxide mimic, prostaglandin F2alpha acetal.
Clonidine and related analogues. Quantitative correlations.
Basic derivatives of 6,7-dihydroindolo(1,7-ab)(1) benzazepine and 6H-indolo(7,1-cd)(1,5) benzoxazepine as potential antidepressant agents.
(+)- and (-)-3-Methoxycyproheptadine. A comparative evaluation of the antiserotonin, antihistaminic, anticholinergic, and orexigenic properties with cyproheptadine.
Discovery of a 4-aryloxy-1H-pyrrolo[3,2-c]pyridine and a 1-aryloxyisoquinoline series of TRPA1 antagonists.
Plumbagin downregulates Wnt signaling independent of p53 in human colorectal cancer cells.
Synthesis and antitumor activities of novel -aminophosphonate derivatives containing an alizarin moiety.
1-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
Synthesis and identification of cytotoxic diphyllin glycosides as vacuolar H(+)-ATPase inhibitors.
Synthesis and evaluation of (E)-2-(acrylamido)cyclohex-1-enecarboxylic acid derivatives as HCA1, HCA2, and HCA3 receptor agonists.
Ingol-type diterpenes from Euphorbia antiquorum with mouse 11-hydroxysteroid dehydrogenase type 1 inhibition activity.
Antifungal amphidinol 18 and its 7-sulfate derivative from the marine dinoflagellate Amphidinium carterae.
Mahorones, highly brominated cyclopentenones from the red alga Asparagopsis taxiformis.
Discovery of biarylaminoquinazolines as novel tubulin polymerization inhibitors.
Discovery and development of Janus kinase (JAK) inhibitors for inflammatory diseases.
Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists.
Theophylline-7-acetic acid derivatives with amino acids as anti-tuberculosis agents.
Polyhydroxy cyclohexanols from a Dendrodochium sp. fungus associated with the sea cucumber Holothuria nobilis Selenka.
Rhapontigenin suppresses cell migration and invasion by inhibiting the PI3K-dependent Rac1 signaling pathway in MDA-MB-231 human breast cancer cells.
Carpatamides A-C, cytotoxic arylamine derivatives from a marine-derived Streptomyces sp.
Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.
Isolation and structure elucidation of cystargamide, a lipopeptide from Kitasatospora cystarginea.
Design and synthesis of N-methylpyrimidone derivatives as HIV-1 integrase inhibitors.
Scaffold hopping: exploration of acetanilide-containing uracil analogues as potential NNRTIs.
Reemergence of chloroquine (CQ) analogs as multi-targeting antimalarial agents: a review.
Design, synthesis and docking study of novel tetracyclic oxindole derivatives as -glucosidase inhibitors.
Design, synthesis of new -carboline derivatives and their selective anti-HIV-2 activity.
Herbicides for control of isoproturon-resistant Littleseed Canarygrass (Phalaris minor) in wheat
Development of a Novel Fungicide, Cyazofamid
A rational design, synthesis, characterization, and antihypertensive activities of some new substituted benzimidazoles
Synthesis, antimycobacterial, antiviral, antimicrobial activities, and QSAR studies of isonicotinic acid-1-(substituted phenyl)-ethylidene/cycloheptylidene hydrazides
Synthesis and evaluation of novel prodrugs of naproxen
Synthesis and cytotoxicity of 1-phenylethanolamine carboxamide derivatives: effects on the cell cycle
Synthesis and Acaricidal Activity of N-(1,3,4-Thiadiazol-2-yl)carboxamides
Prediction of antimalarial activity of some cyclic peroxy ketals using physico-chemical and topological indices
Synthesis of 2-(aryl)-5-(arylidene)-4-thiazolidinone derivatives with potential analgesic and anti-inflammatory activity
Synthesis, DNA affinity, and antimicrobial activity of 4-substituted phenyl-2,2-bichalcophenes and aza-analogues
A quantitative structure-activity relationship study of herbicidal analogues of alpha-hydroxy-substituted 3-benzylidenepyrrolidene-2,4-diones.
Predictions and correlations of structure activity relationship of some aminoantipyrine derivatives on the basis of theoretical and experimental ground
Synthesis, antimicrobial and antioxidant activities of some new indole derivatives containing pyridopyrimidine and pyrazolopyridine moieties
Control of chickpea blight disease caused by Didymella rabiei by mixing resistance inducer and contact fungicide
Synthesis and antimicrobial screening of 4-thiazolidinone and 2-azetidinone derivatives of piperazine
Synthesis, characterization and antimicrobial screening of hybrid molecules containing benzimidazole-pyrazole and pyridine nucleus
Synthesis of some novel 1,2,4-triazole and 1,3,4-oxadiazole derivatives of biological interest
Solvent-free, green and efficient synthesis of pyrano[4, 3-b]pyrans by grinding and their biological evaluation as antitumor and antioxidant agents
Design, synthesis and biological activities of new strobilurin derivatives containing substituted pyrazoles.
Synthesis and Acaricidal Activity of N-(1,3,4-Thiadiazol-2-yl)cyclopropanecarboxamides
In vivo screening of diarylimidazoles as anticonvulsant agents
Synthesis and antimicrobial screening of N-(1-methyl-1H-pyrazole-4-carbonyl)-thiourea derivatives
Effect of temperature on the toxicity of several insecticides to Apolygus lucorum (Heteroptera: Miridae)
Synthesis and primary evaluation of quinoxalinone derivatives as potent modulators of multidrug resistance
Insecticide interactions with -aminobutyric acid and nicotinic receptors: predictive aspects of structural models
Synthesis and in vitro antibacterial activity of schiff bases of N-substituted isatins as effective scaffolds
Heterocycles 23: Synthesis, characterization and anticancer activity of new hydrazinoselenazole derivatives
Novel 2-pyrazoline derivatives as potential anticonvulsant agents
Mitochondrial impacts of insecticidal formate esters in insecticide-resistant and insecticide-susceptible Drosophila melanogaster.
Safening Effects of 1, 8-Naphthalic Anhydride in Corn Plants Treated with Bensulfuron-methyl and Imazaquin
Synthesis of tetracyclic aza-/oxa-naphthalen-8-ones and their antimicrobial activity
Azadirachtin avoidance by larvae and adult females of the tomato leafminer Tuta absoluta
Synthesis and anti-HIV activity evaluation of novel N-arylidene-2-[1-(naphthalen-1-yl)-1H-tetrazol-5-ylthio]acetohydrazides
Synthesis and study of the antidepressant activity of novel 4,5-dihydro-7-alkoxy(phenoxy)-tetrazolo[1,5-a]quinoline derivatives
New aspect of gallic esters: marked effect on termite feeding
Preliminary evaluation of rat kidney aldose reductase inhibitory activity of 2-phenylindole derivatives: affiliation to antioxidant activity
Increasing antitumor activity in vivo by enhancing acridine dimer solubility with salt preparations
1-(6-Halonicotinyl)-2-nitromethylene-imidazolidines as Potential New Insecticides
Combinatorial approach: identification of potential antifungals from triazole minilibraries
Synthesis and antimicrobial activity of some new 4-triazolylmethoxy-2H-chromen-2-one derivatives
Oxidation of di- and polyamines: in vitro effect of amino aldehydes on the vitality of Leishmania promastigotes
Synthesis and Bleaching Activity of 3-Propargylthio-4-(substituted phenyl)-4H-1, 2, 4-triazoles
Aromatic amino analogues of artemisinin: synthesis and in vivo antimalarial activity
Imidazole as an anti-epileptic: an overview
Synthesis and Fungicidal Activities of 3-(-Alkoxyiminobenzyl)isoxazole Derivatives
Synthesis and evaluation of substituted 5-(3-chloro-2-oxo-4-phenylazetidin-1-ylamino)pyrimidine-2,4,6(1H,3H,5H)-triones against pentylenetetrazole-induced convulsant in mice
Synthesis and characterization of new types of 2-(6-methoxy-2-naphthyl)propionamide derivatives as potential antibacterial and antifungal agents
Antihyperglycemic, -glucosidase inhibitory and DPPH free radical scavenging activity of 5-bromosalicylaldehyde and schiff bases
Utilization of nicotinonitrile-2-thiol in the synthesis of new thiepino[2,3-b]pyridine derivative as an in vitro novel antitumor potent
SYNTHESIS, ANOREXIGENIC ACTIVITY AND QSAR OF SUBSTITUTED ARYLOXYPROPANOLAMINES
Synthesis and Fungicidal Activities of Phenoxyphenyl Alkoxyiminoacetamide Derivatives
Synthesis of new quinoline-2-pyrazoline-based thiazolinone derivatives as potential antimicrobial agents
Synthesis and antimicrobial activity of novel derivatives of Biginelli pyrimidines
Synthesis and Microbiological Evaluation of Some N-Methyl Piperidone Oxime Ethers
Synthesis and anticancer evaluation of novel 3,5-diaryl-thiazolo[4,5-d]pyrimidin-2-one derivatives.
Virtual screening and biochemical evaluation of the inhibitors of dual-specificity phosphatase 26
Design and synthesis of novel N-substituted-3-chloro-2-azetidinone derivatives as potential anticonvulsant agents
Docking simulations, synthesis, and anti-inflammatory activity evaluation of 2-(N-alkyl)amino-3-nitroimidazo[1,2-a]pyridines
Pyridoquinolones containing azetidinones: synthesis and their biological evaluation
Solvent- and catalyst-free synthesis of bis-adducts of 3-formylchromone as potential antimicrobial agents
Effects of sublethal glyphosate rates on fresh market tomato
Antifeedant activity of vicolides from Pentanema indicum
Synthesis and herbicidal evaluation of novel 3-[(alpha-hydroxy-substituted)benzylidene]pyrrolidine-2,4-diones.
Effect of seven new orchard pesticides on Galendromus occidentalis in laboratory studies.
Antitermite activity of 7-alkoxycoumarins and related analogs against Coptotermes formosanus Shiraki
Trypsin inhibitory potential and microbial transformation of rutin isolated from Citrus sinensis
Synthesis and Structure-activity Relationships of Herbicidal Thiophene Sulfonylurea Compounds
A comprehensive structureactivity analysis 2,3,5-trisubstituted 4,5-dihydro-4-oxo-3H-imidazo [4,5-c] pyridine derivatives as angiotensin II receptor antagonists: using 2D- and 3D-QSAR approach
Quantitative structureactivity relationships for estimating the aryl hydrocarbon receptor binding affinities of resveratrol derivatives and the antioxidant activities of hydroxystilbenes
Antifeedant properties and chemotaxonomic implications of sesquiterpene lactones and syringin from Rhaponticum pulchrum
Interaction of 2-(4-Methylphenoxy)triethylamine and Related Compounds with Its Herbicide Target in the Carotenoid Biosynthetic Pathway
Effect of allylisothiocyanate on Sitophilus oryzae, Tribolium confusum and Plodia interpunctella: Toxicity and effect on insect mitochondria
Quantitative structureactivity relationships studies for prediction of antimicrobial activity of synthesized disulfonamide derivatives
Synthesis and Herbicidal Activity of Hydantocidin Analogues: Modification of the Carbonyl Groups in Spirohydantoin
Predictive QSAR modeling on tetrahydropyrimidine-2-one derivatives as HIV-1 protease enzyme inhibitors
Anticandidiasis agents from a Tanzanian plant, Combretum zeyheri
Synthesis and antimicrobial activity of newer indole semicarbazones
Quantitative structure activity relationship analysis of angiotensin II AT1 receptor antagonists
Synthesis and in vitro antimicrobial evaluation of novel 2-amino-6-(phenylthio)-4-(2-(phenylthio)quinolin-3-yl)pyridine-3,5-dicarbonitriles
Synthesis, characterization, in vitro anticancer activity, and docking of Schiff bases of 4-amino-1,2-naphthoquinone
Quantitative structure-activity relationship of terpenoid aphid antifeedants.
Evaluation of three diatomaceous earth and one natural pyrethrum formulations against pupae of Tribolium confusum DuVal (Coleoptera: Tenebrionidae) on wheat and flour
Comparative molecular similarity indices analysis for predicting anti-HIV activity of phenyl ethyl thiourea (PET) derivatives
Synthesis of biologically active drimanes and homodrimanes from ()-sclareol
Synthesis, crystal structure, and anticancer properties of cyclic monocarbonyl analogs of curcumin
Synthesis anti-inflammatory and anticancer activity evaluation of some pyrazole and oxadiazole derivatives
Synthesis, anti-microbial evaluation, and molecular modeling of new pyrazolo[3,4-d]pyrimidine derivatives
Proapoptotic effects of novel pentabromobenzylisothioureas in human leukemia cell lines.
Green approach towards synthesis of substituted pyrazole-1,4-dihydro,9-oxa,1,2,6,8-tetrazacyclopentano[b]naphthalene-5-one derivatives as antimycobacterial agents
Nymania-3: a bioactive triterpenoid from Dysoxylum malabaricum
Biorational glycol diesters as dietary toxins versus bioefficacy of sucrose octanoate against lepidopteran larvae
Mechanisms of Low Susceptibility to Imidacloprid in a Laboratory Strain of the Small Brown Planthopper, Laodelphax striatellus FALLEN
Use of structure-based virtual screening in the investigation of novel human sialidase inhibitors
Synthesis and biological evaluation of naphthalene, furan and pyrrole based chalcones as cytotoxic and antimicrobial agents
In vitro antiplaque properties of a series of alkyl bis(biguanides).
Adamantylthiourea derivatives as antiviral agents.
Potential antiinflammatory compounds. 2. Acidic antiinflammatory 1,2-benzisoxazoles.
Haloacetamido analogues of 2-amino-2-deoxy-D-glucose and 2-amino-2-deoxy-D-galactose. Syntheses and effects on the Friend murine erythroleukemia.
Aroyl- and arylisoquinolineacetic acids as antiinflammatory agents.
Usnic acid derivatives as potential antineoplastic agents.
Synthesis and biochemical evaluation of nucleosides of naphthoquinone heterocycles.
Antiinflammatory activity of 17-esters of 6alpha,9alpha-difluoro-21-deoxyprednisolone.
Antitumor anthracycline antibiotics. Structure-activity and structure-cardiotoxicity relationships of rubidazone analogues.
6-aminopyrazolo[4,3-c]pyridin-4(5H)-one, a novel analogue of guanine.
N7-Substituted 7-aminoactinomycin D analogues. Synthesis and biological properties.
Synthesis and antileukemic activity of 5-substituted 2,3-dihydro-6,7-bis(hydroxymethyl)-1H-pyrrolizine diesters.
Prostaglandins and congeners. 15. Synthesis and bronchodilator activity of dl-11-deoxy-15- or 16-alkylprostaglandins.
A new warfarin metabolite: structure and function.
Nonsteroidal antiinflammatory agents. 2. Derivatives/analogues of dibenz[b,e]oxepin-3-acetic acid.
British National Formulary (72nd edition)
MMV Malaria Box gametocyte functional viability assay screening.
MMV Malaria Box thermal shift screening.
MMV Mararia Box screening against P. falciparum asexual stage parasites under hypoxia and bicarbonate modified culture conditions.
MMV Malaria Box screening in pLDH viability assay against Plasmodium falciparum gametocytes.
MMV Box screening against Plasmodium falciparum protein kinases and aminoacyl tRNA synthetases.
MMV Box Onchocerca lienalis screening set
Open Source Malaria Deposition 2. http://malaria.ourexperiment.org
Prostaglandin isosteres. 1. (8-Aza-, 8,10-diaza-, and 8-aza-11-thia)-9-oxoprostanoic acids and their derivatives.
Synthesis and structure-activity relationship studies of cytotoxic epoxide derivatives of 7-oxabicyclo[2.2.1]heptane.
A potential amphetamine antagonist, adamantanamine derivative of fluphenazine.
Synthesis and biological activity of new 2-substituted analogs of fluphenazine.
Potential hypolipidemic agents derived from 3-hydroxy-17,17-dimethylgona-1,3,5(10),8,11,13-hexaene.
2-(2-Aminoethylamino)-1,2-diphenylethanol derivatives, a new class of topical antiinflammatory agents.
Drugs derived from cannabinoids. 5. delta6a,10a-Tetrahydrocannabinol and heterocyclic analogs containing aromatic side chains.
Quinazolines and 1,4-benzodiazepines. 82.1 5-Pyrimidyl-and 5-pyrazinylbenzodiazepines.
Antimalarials. 8. Synthesis of amino ethers as candidate antimalarials.
Antidepressant and anticonvulsant activity of 1-(5-phenyl-4-oxazolin-2-yl)-4-substituted piperazines.
Potential histidine decarboxylase inhibitors. 1. alpha- and beta-substituted histidine analogues.
Synthesis of a fragment of human parathyroid hormore, hPTH-(44-68).
Nonsteroidal antiinflammatory agents. 2. Synthesis and biological activity of 2-chloroindolecarboxylic acids.
Synthesis and -glucuronidase inhibitory activity of 2-arylquinazolin-4(3H)-ones.
Probing of primed and unprimed sites of calpains: Design, synthesis and evaluation of epoxysuccinyl-peptide derivatives as selective inhibitors.
Benzofuran derivatives as anticancer inhibitors of mTOR signaling.
New potent antibacterial oxazolidinone (MRX-I) with an improved class safety profile.
Aliphatic phenolic ethers from Trichobotrys effusa.
Antiviral C-25 epimers of 26-acetoxy steroids from the South China Sea gorgonian Echinogorgia rebekka.
Discovery of camphor-derived pyrazolones as 11-hydroxysteroid dehydrogenase type 1 inhibitors.
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
Novel hybrids of natural oridonin-bearing nitrogen mustards as potential anticancer drug candidates.
Phenolic Glycosides from the Twigs of Salix glandulosa.
An uncharged oxetanyl sulfoxide as a covalent modifier for improving aqueous solubility.
Hydroxybenzothiophene Ketones Are Efficient Pre-mRNA Splicing Modulators Due to Dual Inhibition of Dyrk1A and Clk1/4.
Liver x receptor agonists for the treatment of coronary heart disease and other disorders.
Synthesis and preliminary biological evaluation of new antiproliferative aromatic analogues of 1,25-dihydroxyvitamin D3.
Pyrrolopyrimidine Analogues as MKNK Inhibitors.
Chemically accessible hsp90 inhibitor that does not induce a heat shock response.
Lead optimization of imidazopyrazines: a new class of antimalarial with activity on Plasmodium liver stages.
Bicyclic tetrapeptides as potent HDAC inhibitors: effect of aliphatic loop position and hydrophobicity on inhibitory activity.
Structural Analysis of the Binding of Type I, I1/2, and II Inhibitors to Eph Tyrosine Kinases.
Nanomolar-Potency Small Molecule Inhibitor of STAT5 Protein.
3-Cyano-3-aza--amino Acid Derivatives as Inhibitors of Human Cysteine Cathepsins.
Substituted thieno[2,3-b]thiophenes and related congeners: Synthesis, -glucuronidase inhibition activity, crystal structure, and POM analyses.
Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response.
Selection of fragments for kinase inhibitor design: decoration is key.
Investigation of Cardiovascular Effects of Tetrahydro--carboline sstr3 antagonists.
Discovery of novel 1,5-benzodiazepine-2,4-dione derivatives as potential anticancer agents.
Cytotoxic vobasine, tacaman, and corynanthe-tryptamine bisindole alkaloids from Tabernaemontana and structure revision of tronoharine.
One-pot synthesis of polyunsaturated fatty acid amides with anti-proliferative properties.
Structure and Stereochemical Determination of Hypogeamicins from a Cave-Derived Actinomycete.
Discovery of a Negative Allosteric Modulator of GABAB Receptors.
Novel pyrazoline derivatives as bi-inhibitor of COX-2 and B-Raf in treating cervical carcinoma.
Prostaglandin Derivatives: Nonaromatic Phosphodiesterase-4 Inhibitors from the Soft Coral Sarcophyton ehrenbergi.
Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3--Oxyazetidine.
Cyclic Hexapeptides from the Deep South China Sea-Derived Streptomyces scopuliridis SCSIO ZJ46 Active Against Pathogenic Gram-Positive Bacteria.
Synthesis of benzopentathiepin analogs and their evaluation as inhibitors of the phosphatase STEP.
A coumarin lignanoid from the stems of Kadsura heteroclita.
Synthesis, anticandidal activity of N(3)-(4-methoxyfumaroyl)-(S)-2,3-diaminopropanoic amide derivatives--novel inhibitors of glucosamine-6-phosphate synthase.
Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity.
Molecular docking studies on analogues of quercetin with d-alanine:d-alanine ligase of Helicobacter pylori
SYNTHESIS AND CYTOTOXIC PROPERTIES OF NITRO- AND AMINOCHALCONES
Synthesis of quinolactacide via an acyl migration reaction and dehydrogenation with manganese dioxide, and its insecticidal activities.
Synthesis and Activity of Novel Acaricidal/Insecticidal 2, 4-Diphenyl-1, 3-oxazolines
Docking study on trametenolic acid B as a -glucosidase inhibitor
Synthesis and in vitro antiproliferative activity of novel (4-chloro- and 4-acyloxy-2-butynyl)thioquinolines.
Design, synthesis, and anticonvulsant activity of novel quinazolinone analogues
Synthesis, antioxidant, and antibacterial studies of phenolic esters and amides of 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acid
Evaluation of crude toxin and metabolite produced by Helminthosporium gramineum Rabenh for the control of rice sheath blight in paddy fields
Non-imidazole histamine H3 ligands: part V. synthesis and preliminary pharmacological investigation of 1-[2-thiazol-4-yl- and 1-[2-thiazol-5-yl-(2-aminoethyl)]-4-n-propylpiperazine derivatives.
Synthesis, characterisation, and antineoplastic cytotoxicity of hybrid naphthohydroquinonenucleic base mimic derivatives
Synthesis of some novel 2-substituted benzoxazoles as anticancer, antifungal, and antimicrobial agents
Synthesis of N-[3-(acetylthio)alkanoyl] and N-[3-mercaptoalkanoyl]-4-(s)-(phenylmethyl) pyroglutamic acids and prolines as potent ACE inhibitors
Synthesis of Some New Antimicrobial Thiadiazolyl and Oxadiazolyl Quinoline Derivatives
Microwave-assisted synthesis and pharmacological studies of novel 5-deazaalloxazine derivatives
Synthesis and Herbicidal Activity of 4-Thiazolone Derivatives and Their Effect on Plant Secretory Pathway
Synthesis and evaluation of new 1,2,3,4-tetrahydroisoquinoline analogs as antiglioma agents
Synthesis of some new indolo[2,3-c]isoquinolinyl pyrazoles, -1,3,4-oxadiazoles and their biological activities
Synthesis, characterisation and antimicrobial activities of novel 7,9-diphenyl-1,2,4-triaza-8-oxa-spiro[4.5]-decan-3-thiones
Insecticidal Activity of N-Acyl-N-(4-aryloxybenzyl)pyrazole-5-carboxamides
Anti-microbial benzimidazole derivatives: synthesis and in vitro biological evaluation
Synthesis of novel 2-(3-aryl-sydnon-4-ylidene)-5-substituted-[1,3,4]-thiadiazolylamines and [1,3,4]-thiadiazol-2-yl-3-oxo-[1,2,4]-triazoles as antimicrobial agents
Ligand-based drug design studies using predictive pharmacophore model generation on 4H-1,2,4-triazoles as AT1 receptor antagonists
Evaluation of rat kidney aldose reductase inhibitory activity of some N-acetyl dehydroalanine derivatives
Effectiveness of cyproconazole to control Armillaria root rot of apple, walnut and kiwifruit
2D and 3D QSAR analyses to predict favorable substitution sites in anilino-monoindolylmaleimides acting as PKCII selective inhibitors
CsFCelite catalyzed facile N-alkylation of 2(3H)-benzoxazolones and antimicrobial properties of 2-substituted benzoxazole and 3-substituted-2(3H)-benzoxazolone derivatives
Three-dimensional quantitative structureactivity relationship approach for the prediction of the antimycobacterial activity of 4-oxo-dihydroquinoline-3-carboxylic acid derivatives
Synthesis and in vitro and in vivo antimalarial activity of novel 4-anilinoquinoline Mannich base derivatives
Comprehensive structureactivity relationship analysis of substituted 5-(biphenyl-4-ylmethyl) pyrazoles derivatives as AT1 selective angiotensin II receptor antagonists: 2D and kNNMFA QSAR approach
Cytotoxic lipid esters from Peucedanum ledebourielloides
Thermal, kinetic, spectroscopic studies and anti-microbial, anti-tuberculosis, anti-oxidant properties of clioquinol and benzo-coumarin derivatives mixed complexes with copper ion
Synthesis of licochalcones and inhibition effects on radical-induced oxidation of DNA
Synthesis of new 3-aryl-4-(3-aryl-4,5-dihydro-1H-pyrazol-5-yl)-1-phenyl-1H-pyrazole derivatives as potential antimicrobial agents
Insect antifeedant and growth regulating activities of salannobutyrolactone and desacetylsalannobutyrolactone.
Fungicidal Properties of N-(3, 5-Dichlorophenyl)-N-methoxyformamidine and Computer Studies of Its Active Structures
Isolation and characterization of n-octacosanoic acid from Viburnum foetens: a novel antibiofilm agent against Streptococcus Mutans
Synthesis and pharmacological properties of some novel pyrazolidine and pyrazole derivatives
Substituted 2-[2-(pyridin-3-yl) phenyl] acetamides and ureas: design, synthesis, and anticonvulsant screening in mice
Insecticidal and Neuroblocking Activities toward American Cockroach (Periplaneta americana L.) of Imidacloprid Metabolites, 5-Hydroxy-, 4,5-Dihydroxy- and 4,5-Dehydroimidacloprid
Synthesis and antifungal activity of 2-chloromethyl-1H-benzimidazole derivatives against phytopathogenic fungi in vitro.
Fungicidal Activity of New Diphenylphosphinic Amide Derivatives
Synthesis, calcium-channel blocking activity, and conformational analysis of some novel 1,4-dihydropyridines: application of PM3 and DFT computational methods
Synthesis of novel 3-(5-sulfanyl-1,3,4-oxadiazol-2-yl)-2H-chromen-2-one condensed s-triazinyl piperazines and piperidines as antimicrobial agents
Synthesis, biopharmaceutical characterization, and antimicrobial study of novel azo dyes of 7-hydroxy-4-methylcoumarin
Synthesis and antimicrobial activity of some (3-phenyl-5-(1-phenyl-3-aryl-1H-pyrazol-4-yl)-4,5-dihydro-1H-pyrazol-1-yl)(pyridin-4-yl)methanones: new derivatives of 1,3,5-trisubstituted pyrazolines
Fungicidal Activity of Pyrazolylpyrimidines
Synthesis of some new thiazolopyrane and thiazolopyranopyrimidine derivatives bearing a sulfonamide moiety for evaluation as anticancer and radiosensitizing agents
Synthesis, physico-chemical properties, and antimicrobial evaluation of a new series of iron(III) hexadentate chelators
An efficient anticancer histone deacetylase inhibitor and its analogues for human HDAC8
Facile synthesis and herbicidal evaluation of 4H-3,1-benzoxazin-4-ones and 3H-quinazolin-4-ones with 2-phenoxymethyl substituents.
3D-QSAR and molecular docking studies of hydroxamic acids as peptide deformylase inhibitors
Synthesis of Mannich Bases of 2, 6-Disubstituted 2H-pyran-3(6H)-ones and their Miticidal Activity
Antibacterial and molecular docking studies of entagenic acid, a bioactive principle from seed kernel of Entada pursaetha DC
Cobalt mediated ring contraction reaction of lapachol and initial antibacterial evaluation of naphthoquinones derived from lapachol
Control of Greenhouse Whitefly (Trialeurodes vaporariorum) Using Visually Attractive Targets Impregnated with Pyriproxyfen
Synthesis and Fungicidal Activity of 6-Alkyl Six-membered Cyclic Thiophosphates.
Antithyroid agents and QSAR studies: inhibition of lactoperoxidase-catalyzed iodination reaction by isochromene-1-thiones
Antioxidant, cytotoxicity, and QSAR study of 1-adamantylthio derivatives of 3-picoline and phenylpyridines
Antioxidant activity and inhibition effect on the growth of human colon carcinoma (HT-29) cells of esculetin from Cortex Fraxini
Efficacy of Lawsonia inermis leaves extract and its phenolic compounds against olive knot and crown gall diseases
Tyrosinase inhibitor from black rice bran.
A novel and eco-friendly procedure for the synthesis of some pyrazolo-thiadiazolo-pyrimidinones and its in vitro anti-bacterial activity
Structural Modification of the 6-Chloropyridyl Moiety in the Imidacloprid, Skeleton: Introduction of a Five-membered Heteroaromatic Ring and the Resulting Insecticidal Activity.
Sideroxylin and 8-demethylsideroxylin from Eucalyptus saligna (Myrtaceae)
In silico ligand-based pharmacophore model generation for the identification of novel Pneumocystis carinii DHFR inhibitors
Design, synthesis, antifungal activity, and ADME prediction of functional analogues of terbinafine
Common binding requirements of PPAR-// pan agonists: quantitative structureactivity relationship analysis of indanylacetic acid derivatives carrying 4-thiazolyl-phenoxy tail group
Quantitative Structure-Activity Relationships of Fungicidal N-Phenylformamidoximes
Synthesis of a New 1, 2, 4-Oxadiazol-5-one Derivative, KC10017, and Its Controlling Activity against Rice Blast Disease Caused by Magnaporthe grisea
Bioactive xanthones with effect on P-glycoprotein and prediction of intestinal absorption
One pot synthesis of some novel coumarins containing 5-(substituted-2-hydroxybenzoyl) pyridine as a new class of antimicrobial and antituberculosis agents
Studies on arylfuran derivatives. Part XI. Synthesis, characterisation and biological studies on some Mannich bases carrying 2,4-dichlorophenylfurfural moiety.
Synthesis and evaluation of anti-proliferative activity of 1,4-disubstituted phthalazines
Synthesis of Both Enantiomers of Altholactone, Isoaltholactone and 5-Hydroxygoniothalamin from Tri-O-acetyl-D-glucal, and Their Biological Activities
Synthesis of novel 2-[4-(4-substitutedbenzamido/phenylacetamido)phenyl]benzothiazoles as antimicrobial agents
Potential anti-inflammatory activity and ulcerogenicity study of some novel pyrimido[4,5:4,5]pyrimido[1,6-a]azepine derivatives
Strategy for generation of new TACE inhibitors: pharmacophore and counter pharmacophore modeling to remove non-selective hits
Design and synthesis of some thieno[2,3-c]pyridazine derivatives of expected anticancer activity
Structure-Activity Relationships of Enantiomers of the Azole Fungicide Ipconazole and Its Related Compounds
Amide derivatives of [6-acyl-2-benzothiazolinon-3-yl] acetic acids as potential analgesic and anti-inflammatory compounds
Synthesis and structureactivity relationship of acylthiourea derivatives as inhibitors of microsomal epoxide hydrolase
Methyl jasmonate-induced suppression of anthracnose rot in tomato fruit
[1,2,4]Triazolo[4,3-a]quinoxaline: synthesis, antiviral, and antimicrobial activities
Microwave solvent-free condition synthesis and pharmacological evaluation of pyrano[3,2-c]quinolines
EGFR tyrosine kinase targeted compounds: synthesis, docking study, and in vitro antitumor activity of some new quinazoline and benzo[d]isothiazole derivatives
Sensitivity monitoring of powdery mildew pathogens to cyflufenamid and the evaluation of resistance risk
SYNTHESIS OF THE RIGID ANALOGUES OF AN SSRI BENZENEPROPANAMINE
4-Substitutedphthalazines and phthalazinones: synthesis, characterization and -adrenergic blocking activity
Effects of oleic acid on the tissue factor activity, blood lipids, antioxidant and oxidant parameters of streptozotocin induced diabetic rats fed a high-cholesterol diet
Synthesis and anti-inflammatory activity of 1-acetyl/propanoyl-5-aryl-3-(4-morpholinophenyl)-4,5-dihydro-1H-pyrazole derivatives
Synthesis of novel 1,4-naphthoquinone derivatives: antibacterial and antifungal agents
Tetracyclic spirooxindole blockers of hNaV1.7: activity in vitro and in CFA-induced inflammatory pain model
QSAR study of 5-arylidene-2,4-thiazolidinediones as aldose reductase inhibitors
Pharmacological screening for anti-inflammatory, analgesic activity of pyrazolyl derivatives along with molecular docking studies
[Drug-induced liver injury; fourteenth updated edition of the bibliographic database of liver injuries and related drugs].
Discovery of tetrahydroisoquinoline-based bivalent heterodimeric IAP antagonists.
The discovery of potent, selective, and reversible inhibitors of the house dust mite peptidase allergen Der p 1: an innovative approach to the treatment of allergic asthma.
Rational design, synthesis and anti-proliferative evaluation of novel 1,4-benzoxazine-[1,2,3]triazole hybrids.
Design, synthesis and biological evaluation of novel potent MDM2/p53 small-molecule inhibitors.
1,3,4-Oxadiazole-containing histone deacetylase inhibitors: anticancer activities in cancer cells.
Design, synthesis and biological evaluation of novel 5-phenyl-1H-pyrazole derivatives as potential BRAF(V600E) inhibitors.
Internalization and stability of a thymidylate synthase Peptide inhibitor in ovarian cancer cells.
4-Substituted quinazoline derivatives as novel EphA2 receptor tyrosine kinase inhibitors.
Structure-Based Design and Synthesis of Potent Cyclic Peptides Inhibiting the YAP-TEAD Protein-Protein Interaction.
In Vitro Antibacterial Activity of Prenylated Guanidine Alkaloids from Pterogyne nitens and Synthetic Analogues.
GnRH antagonists: the promise of treating sex-hormone-related diseases.
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.
Synthesis and structure-activity relationships of novel, potent, orally active hypoxia-inducible factor-1 inhibitors.
Allosteric modulation of the G protein-coupled US28 receptor of human cytomegalovirus: are the small-weight inverse agonist of US28 'camouflaged' agonists?
Structure-Based Design of a Potent, Selective, and Brain Penetrating PDE2 Inhibitor with Demonstrated Target Engagement.
Neutrophil elastase inhibitors as potential anti-inflammatory therapies.
Circumventing seizure activity in a series of G protein coupled receptor 119 (GPR119) agonists.
Impact of Stereochemistry on Ligand Binding: X-ray Crystallographic Analysis of an Epoxide-Based HIV Protease Inhibitor.
Novel Disubstituted Pyrimidines as Inhibitors of Bruton's Tyrosine Kinase.
Cytotoxic 1,5-diaryl-3-oxo-1,5-pentadienes: an assessment and comparison of membrane permeability using Caco-2 and MDCK monolayers.
Combination of novel imidazopyridazine mps-1 kinase inhibitors and bcl-2 family protein inhibitors.
Histone deacetylase inhibitors derived from 1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine and related heterocycles selective for the HDAC6 isoform.
LPM7 Inhibitors May Potentially Treat Autoimmune Diseases.
Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.
Development of a fluorometric microplate antiadhesion assay using uropathogenic Escherichia coli and human uroepithelial cells.
Tricyclic pyrazoles. Part 6. Benzofuro[3,2-c]pyrazole: a versatile architecture for CB2 selective ligands.
A fragment-based approach to identifying S-adenosyl-l-methionine -competitive inhibitors of catechol O-methyl transferase (COMT).
Graphite catalyzed solvent free synthesis of dihydropyrimidin-2(1H)-ones/thiones and their antidiabetic activity.
Cytotoxic alkylated hydroquinone, phenol, and cyclohexenone derivatives from Aspergillus violaceofuscus Gasperini.
Minor diterpene glycosides from the leaves of Stevia rebaudiana.
Constituents of the roots of Clausena lansium and their potential anti-inflammatory activity.
Synthesis, antibacterial and antitubercular activities of benzimidazole bearing substituted 2-pyridone motifs.
Synthesis and structure-activity relationship of cyclopentenone oximes as novel inhibitors of the production of tumor necrosis factor-.
Reactive oxygen species (ROS) inducible DNA cross-linking agents and their effect on cancer cells and normal lymphocytes.
Pyrimidinylpiperdinyloxypyridone Analogues as GPR119 Modulators.
Synthesis of isoquinolinone-based tricycles as novel poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors.
Preparation, anticholinesterase activity and molecular docking of new lupane derivatives.
Synthesis and biological evaluation of CHX-DAPYs as HIV-1 non-nucleoside reverse transcriptase inhibitors.
2,4-Bis(4-hydroxybenzyl)phenol inhibits heat shock transcription factor 1 and sensitizes lung cancer cells to conventional anticancer modalities.
Guanidinium-based derivatives: searching for new kinase inhibitors.
Piperazion[1,2-A]indol-1-ones and [1,4]Diazepino[1,2-A]indol-1-ones.
Synthesis and biological evaluation of novel naphthalene compounds as potential antidepressant agents.
Dammarane-type triterpenoids from Gentianella azurea.
Design, synthesis and biological evaluation of arylcinnamide hybrid derivatives as novel anticancer agents.
Oxirapentyns F-K from the marine-sediment-derived fungus Isaria felina KMM 4639.
Group A streptococcus inhibitors by high-throughput virtual screening.
Synthesis and antiproliferative activity of novobiocin analogues as potential hsp90 inhibitors.
2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
Synthesis and structure-activity relationship of non-phosphorus-based fructose-1,6-bisphosphatase inhibitors: 2,5-Diphenyl-1,3,4-oxadiazoles.
N-acylated sulfonamide congeners of fosmidomycin lack any inhibitory activity against DXR.
Design strategies to address kinetics of drug binding and residence time.
(+)- and (-)-liriodenol, a pair of novel enantiomeric lignans from Liriodendron hybrid.
Nucleobase modified neamines with a lysine as a linker, their inhibition specificity for TAR-Tat derived from HIV-1.
Loratadine analogues as MAGL inhibitors.
Synthesis and biological evaluation of novel HIV-1 protease inhibitors using tertiary amine as P2-ligands.
Discovery of a potent, orally available dual CysLT1 and CysLT2 antagonist with dicarboxylic acid.
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
New approaches to the synthesis of sildenafil analogues and their enzyme inhibitory activity.
Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.
Design and synthesis of novel 1,2,3-triazole-pyrimidine-urea hybrids as potential anticancer agents.
Design and synthesis of novel 1,2-dithiolan-4-yl benzoate derivatives as PTP1B inhibitors.
Selective inhibitors of protein methyltransferases.
Discovery of novel AHLs as potent antiproliferative agents.
Synthesis and antiproliferative activity of 3-(2-chloroethyl)-5-methyl-6-phenyl-8-(trifluoromethyl)-5,6-dihydropyrazolo[3,4-f][1,2,3,5]tetrazepin-4-(3H)-one.
Synthesis and anti-mycobacterial activity of 2-chloronicotinaldehydes based novel 1H-1,2,3-triazolylbenzohydrazides.
Synthesis, antimicrobial activity, and molecular modeling of novel 4-(3-(4-benzylpiperazin-1-yl)propoxy)-7-methoxy-3-substituted phenyl-2H-chromen-2-one
The synthesis, anti-inflammatory and antimicrobial activity evaluation of novel thioanalogs of 3,4-dihydrothiopyrimidin-2(1H)-one derivatives of N-aryl urea
Antimicrobial activity of thiazolyl benzenesulfonamide-condensed 2,4-thiazolidinediones derivatives
Peroxidizing Phytotoxic Activity of 1, 3, 4-Thiadiazolidine-2-thiones and 1, 2, 4-Triazolidine-3, 5-dithiones
Induction of Resistance against Rice Blast Disease by a Novel Class of Plant Activator, Pyrazolecarboxylic Acid Derivatives
Synthesis of 1, 2, 4-Triazolo[1, 5-a]-1, 3, 5-triazine Derivatives for Phytotoxic Activity
Synthesis and in vitro antitumor activity of new quinoline, pyrimido[4,5-b]quinoline, [1,2,3]triazino[4,5-b]quinoline, and [1,2,4]triazolo[2,3:3,4]pyrimido[6,5-b]quinoline analogs
Preparation and root growth-inhibitory activity of N-substituted 2-(2-chloroacetamido)-3-(furan-2-yl)propanamides.
Synthesis and Herbicidal Activity of 2-Benzylamino-4-methyl-6-trifluoromethyl-1, 3, 5-triazune Derivatives
Synthesis, characterization, and antimicrobial activity of some new coumarin derivatives
Antimicrobial, analgesic, DPPH scavenging activities and molecular docking study of some 1,3,5-triaryl-2-pyrazolines
Synthesis of novel pyrazolyl tetrazoles as selective COX-2 inhibitors
Insect antifeedants from Munronia henryi: structure of munroniamide.
Susceptibility of adult Trichogramma nubilale (Hymenoptera: Trichogrammatidae) to selected insecticides with different modes of action
Synthesis and evaluation of 4-(substituted)-acetylamino-3-mercapto-5-(4-substituted) phenyl-1,2,4-triazole derivatives as antimicrobial agents
Quinolinoneacetic acid derivatives as novel glutathione S-transferase P1-1 inhibitors: insights into the interaction modes by molecular modeling
Synthesis of fatty acid Schiff base esters as potential antimicrobial and chemotherapeutic agents
Study of the inactivation of copper, zinc superoxide dismutase by tetracycline analogues
Synthesis and antimicrobial screening of 5-(benzylidene)-3-phenylthiazolidin-4-one derivatives incorporating thiazole ring
Magnetic resonance assays of haloperidol in human serum albumin
Two novel trichothecenes from Myrothecium roridum
Potent limonoid insect antifeedant from Melia azedarach.
Discovery of a novel histone deacetylase 8 inhibitor by virtual screening
Microwave-assisted synthesis of 3-indolyl substituted 4H-chromenes catalyzed by DMAP and their antimicrobial activity
Growth retarding activity of lichen substances against the polyphagous herbivorous insect Spodoptera littoralis
Synthesis and Herbicidal Activities of the O-Syn and O-Anti Benzyl Epoxycyclopentyl Ethers
Synthesis of new derivatives of 2,2-dimethyl-2,3-dihydro-7-benzo[b]furanol with potential antimicrobial activity
High osmolar contrast medium causes mild oxidation in liver, bladder, and ovary tissues from rats: vitamin C has protective role
Differential effect of triazoles on mycelial growth and disease measurements of Monilinia fructicola isolates with reduced sensitivity to DMI fungicides
Insight into the structural requirement of aryltriazolinone derivatives as angiotensin II AT1 receptor: 2D and 3D-QSAR k-Nearest Neighbor Molecular Field Analysis approach
3-Aryl-2-{4-[4-(2,4-dioxothiazolidin-5-ylmethyl)phenoxy]-phenyl}-acrylic acid alkyl ester: synthesis and antihyperglycemic evaluation
Synthesis and antifungal activity of novel 7-O-substituted pyridyl-4-methyl coumarin derivatives
(+)-Cyclazosin Derivatives as 1-Adrenoceptor Antagonists
Comparative study of conventional and microwave-assisted synthesis of some Schiff bases and their potential as antimicrobial agents
Synthesis characterization and biological evaluation of some alkoxyphthalimide derivatives of 3-(4-substituted phenyl)-6,6-diphenyl-3,3a-dihydro-2H-imidazo[2,1-b]pyrazolo[3,4-d][1,3]thiazol-7(6H)-one
Synthesis, antimicrobial and antioxidant activities of 2-[1-{3,5-diaryl-4,5-dihydro-1H-pyrazolenyl}]-4-(4-nitrophenyl)-[1,3]-thiazoles
Application of pocket modeling and k-nearest neighbor molecular field analysis (kNN-MFA) for designing of some anticoagulants: potential factor IXa inhibitors
Antioxidant and -glucosidase inhibitory compounds from Pimpinella candolleana Wight et Arn.
Binding of Nicotinoids and the Related Compounds to the Insect Nicotinic Acetyicholine Receptor
Synthetic utility of sydnones: synthesis of pyrazolines derivatized with 1,2,4-triazoles as antihyperglymic, antioxidant agents and their DNA cleavage study
Predicting 3H-1,2,4-triazolinones as angiotensin II receptor antagonists: 2D and 3D QSAR by kNN-molecular field analysis approach
Experimental validation and docking studies of flavone derivatives on aldose reductase involved in diabetic retinopathy, neuropathy, and nephropathy
Efficacy evaluation of a neem (Azadirachta indica A. Juss) formulation against root-knot nematodes Meloidogyne incognita
Microwave-assisted solvent-free synthesis of biologically active novel heterocycles from 3-formylchromones
Mode of inhibition of acetylcholinesterase by monoterpenoids and implications for pest control
Effects of Pyridalyl, a Novel Insecticidal Agent, on Cultured Sf9 Cells
Design, synthesis, and in vitro antimicrobial activities of novel azetidinyl-3-quinazolin-4-one hybrids
Synthesis of limonoid CDE fragments related to limonin and nimbinim
Bifenthrin longevity at the termiticidal application rate.
ANTIPYRETIC, ANTINOCICEPTIVE AND ANTI-INFLAMMATORY ACTIVITIES OF CERTAIN -OXOBUTANOIC ACID DERIVATIVES
Synthesis antimicrobial and anticancer activity of N-arylmethylidene-piperazine-1-carbothiohydrazide
Weed control and sesame (Sesamum indicum L.) response to preplant incorporated herbicides and method of incorporation
Search for monoglyceride lipase inhibitors: synthesis and screening of arylthioamides derivatives
The effect of sodium bicarbonate alone or in combination with a reduced dose of tebuconazole on the control of apple scab
PRE-CLINICAL AND CLINICAL PHARMACOKINETICS OF THE DIASTEREOMERS OF ARTEETHER, A POTENT ANTIMALARIAL
The direct toxicity of BABA against grapevine ecosystem organisms
Synthesis and antitumor activity of new pyrido[2,3-d]pyrimidine derivatives
Synthesis, characterization, and antimicrobial evaluation of novel naphthalene-based 1,2,4-triazoles
Synthesis and antibacterial activities of para-alkoxy phenyl--ketoaldehyde derivatives
Some new thiazolyl thiazolidinedione derivatives as aldose reductase inhibitors
Synthesis, biological screening and ADME prediction of benzylindole derivatives as novel anti-HIV-1, anti-fungal and anti-bacterial agents
The Design and Synthesis of a Novel, Orally Active, Selective ETA Antagonist
Synthesis and anti-juvenile hormone activity of ethyl 4-(2-benzylalkyloxy)benzoates and their enantiomers
Design, synthesis, and biological evaluation studies of novel quinazolinone derivatives as anticonvulsant agents
Molecular modeling studies and synthesis of novel quinoxaline derivatives with potential anti-cancer activity as inhibitors of methionine synthase
Docking and quantitative structureactivity relationship studies for imidazo[1,2-a]pyrazines as inhibitors of checkpoint kinase-1
Effect of Insect Hormone Related Compounds on the Growth of Insect Cells
Isolation of long-chain esters from the rhizome of Polygonatum verticillatum by potent tyrosinase inhibition
(Hetero)aroyl esters of 2-(N-phthalimido)ethanol and analogues: parallel synthesis, anti-HIV-1 activity and cytotoxicity
Synthesis, characterization, anticancer, and antioxidant activity of some new thiazolidin-4-ones in MCF-7 cells
Evaluation of antileishmanial activities of triglycerides isolated from roots of Moringa stenopetala
Benzothiazole Schiff-bases as potential imaging agents for -amyloid plaques in Alzheimers disease
Synthesis and anticonvulsant activity of some N-(benzoyl)glycinanilide derivatives
Synthesis and anti-hypertensive activity of novel sulphadimidine derivatives
-Tubulins in Gibberella zeae: their characterization and contribution to carbendazim resistance.
3D QSAR ANALYSIS OF SOME HETEROCYCLIC COMPOUNDS AS CYCLOOXYGENASE-2 INHIBITORS
Effects of three neem-based insecticides on diamondback moth (lepidoptera: plutellidae)
Synthesis and evaluation of in vitro antimicrobial activity of novel 2,3-disubstituted-4-thiazolidinones from fatty acid hydrazides
QSAR analysis of N-myristoyltransferase inhibitors: antifungal activity of benzofurans
GLUTATHIONE SYNTHESIS IN FILARIAL WORMS: AN ATTRACTIVE TARGET FOR THE DESIGN AND SYNTHESIS OF NEW ANTIFILARIALS
Synthesis and enzyme inhibitory activities of some new pyrazole-based heterocyclic compounds
Synthesis of novel porphyrin-based lipids and their antibacterial activity
Bioactivity of compounds from Acmella oleracea against Tuta absoluta (Meyrick) (Lepidoptera: Gelechiidae) and selectivity to two non-target species.
Antioxidant phenolic compounds and flavonoids of Mitragyna rotundifolia (Roxb.) Kuntze in vitro
New asperxanthone and asperbiphenyl from the marine fungus Aspergillus sp.
Synthesis and antitubercular activity of nucleoside analogs based on L-ascorbic acid and bases
Actions of imidacloprid, clothianidin and related neonicotinoids on nicotinic acetylcholine receptors of American cockroach neurons and their relationships with insecticidal potency
Computational evaluation and experimental verification of antibacterial activity of some -lactams: advantages and limitations
Synthesis, AM1 calculation, and biological studies of thiopyran-4-one and their azine derivatives
Synthesis and evaluation of curcumin analogues as cytotoxic agents
LCMS/MS method for simultaneous analysis of cladrin and equol in rat plasma and its application in pharmacokinetics study of cladrin
Phenolic and iridoid glycosides from the rhizomes of Cyperus rotundus L.
Synthesis and antitumor studies of novel benzopyrano-1,2,3-selenadiazole and spiro[benzopyrano]-1,3,4-thiadiazoline derivatives
Novel molluscicide against Pomacea canaliculata based on quinoa (Chenopodium quinoa) saponins
Control of Contarinia nasturtii Keiffer (Diptera: Cecidomyiidea) by foliar sprays of acetamiprid on cauliflower transplants
Synthesis and cytotoxicity of novel chrysin derivatives
Response of dry bean to pre-plant incorporated and pre-emergence applications of S-metolachlor and fomesafen
Synthesis, characterization, biological evaluation and in silico screening of oxadiazinanones
Disease-controlling effect of a novel fungicide pyribencarb against Botrytis cinerea
Antifeedant activity of some diterpenoids
Synthesis and Acaricidal Activity of Pyrazole-5-carboxamide Derivatives
Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles as potential anticonvulsant agents
Using a selectivity index to evaluate logarithmic spraying in grass seed crops.
DNDi T. cruzi fenarimol series dataset from which preclinical candidate EPL-BS1246 was identified (see also related datasets CHEMBL2448688 and CHEMBL3137440)
Structure-Based Drug Design of Novel Potent and Selective Tetrahydropyrazolo[1,5-a]pyrazines as ATR Inhibitors.
Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
iNOS inhibitory activity of sesquiterpenoids and a monoterpenoid from the rhizomes of Curcuma wenyujin.
Podoimbricatin A, a cytotoxic diterpenoid with an unprecedented 6/6/5/6-fused tetracyclic ring system from the twigs and leaves of Podocarpus imbricatus.
Dual leucine zipper kinase inhibitors: potential treatments for neurodegenerative diseases.
Synthesis and biological evaluation of the [d-MeAla(11)]-epimer of coibamide A.
Bioactive diterpenoids and flavonoids from the aerial parts of Scoparia dulcis.
Repurposing cryptosporidium inosine 5'-monophosphate dehydrogenase inhibitors as potential antibacterial agents.
Identification and synthesis of quinolizidines with anti-influenza a virus activity.
Trimeric anthracenes from the endophytic fungus Stemphylium globuliferum.
Ralfuranone Is Produced by an Alternative Aryl-Substituted -Lactone Biosynthetic Route in Ralstonia solanacearum.
The effect of pK(a) on pyrimidine/pyridine-derived histamine H4 ligands.
Synthesis and antiproliferative evaluation of 2-hydroxylated (E)-stilbenes.
Inhibition of FAAH, TRPV1, and COX2 by NSAID-serotonin conjugates.
In search of next generation antimalarials.
Optimization of gefitinib analogues with potent anticancer activity.
RORt Modulators Are Potentially Useful for the Treatment of the Immune-Mediated Inflammatory Diseases.
A C-14 labeled Py-Im polyamide localizes to a subcutaneous prostate cancer tumor.
Anilinotriazoles as potent gamma secretase modulators.
Desmethyl macrolides: synthesis and evaluation of 4-desmethyl telithromycin.
Conformationally Restricted GABA with Bicyclo[3.1.0]hexane Backbone as the First Highly Selective BGT-1 Inhibitor.
Pro-apoptotic meiogynin A derivatives that target Bcl-xL and Mcl-1.
Design, synthesis and biological evaluation of novel arylpiperazine derivatives on human prostate cancer cell lines.
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
The next generation of phosphodiesterase inhibitors: structural clues to ligand and substrate selectivity of phosphodiesterases.
A new class of selective myocardial calcium channel modulators. 2. Role of the acetal chain in oxadiazol-3-one derivatives.
3-hydroxymethyl-7-(N-substituted aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline inhibitors of phenylethanolamine N-methyltransferase that display remarkable potency and selectivity.
Conformationally constrained analogues of diacylglycerol (DAG). 25. Exploration of the sn-1 and sn-2 carbonyl functionality reveals the essential role of the sn-1 carbonyl at the lipid interface in the binding of DAG-lactones to protein kinase C.
Uncharged AZT and D4T derivatives of phosphonoformic and phosphonoacetic acids as anti-HIV pronucleosides.
Carbonic anhydrase inhibitors: synthesis and inhibition of cytosolic/membrane-associated carbonic anhydrase isozymes I, II, and IX with sulfonamides incorporating hydrazino moieties.
Anchor-GRIND: filling the gap between standard 3D QSAR and the GRid-INdependent descriptors.
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
Synthesis and structure-activity relationship of novel 6-aryl-1,4-dihydrobenzo[d][1,3]oxazine-2-thiones as progesterone receptor modulators leading to the potent and selective nonsteroidal progesterone receptor agonist tanaproget.
Identification of 2-(4-benzyloxyphenyl)-N- [1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide, an orally efficacious melanin-concentrating hormone receptor 1 antagonist for the treatment of obesity.
Improving specificity vs bacterial thymidylate synthases through N-dansyl modulation of didansyltyrosine.
Non-nucleoside benzimidazole-based allosteric inhibitors of the hepatitis C virus NS5B polymerase: inhibition of subgenomic hepatitis C virus RNA replicons in Huh-7 cells.
New approaches toward anti-HIV chemotherapy.
Fluorescent photoaffinity probes for mitotic protein kinase Aurora A.
Synthesis and evaluation of novel prenylated chalcone derivatives as anti-leishmanial and anti-trypanosomal compounds.
Small-molecule phosphodiesterase probes: discovery of potent and selective CNS-penetrable quinazoline inhibitors of PDE1
A-ring substituted 17-arylsulfonamides of 17-aminoestra-1,3,5(10)-trien-3-ol as highly potent reversible inhibitors of steroid sulfatase.
Ligand efficient tetrahydro-pyrazolopyridines as inhibitors of ERK2 kinase.
Synthesis and biological evaluation of 9-N-oxamyl sialosides as Siglec-7 ligands.
A new small molecule inhibitor of soluble guanylate cyclase.
Tight binding enantiomers of pre-clinical drug candidates.
Chemical Biology of Leucine-Rich Repeat Kinase 2 (LRRK2) Inhibitors.
Discovery of thieno[3,2-c]pyridin-4-amines as novel Bruton's tyrosine kinase (BTK) inhibitors.
Discovery of 2-arylamino-4-(1-methyl-3-isopropylsulfonyl-4-pyrazol-amino)pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
Quinoline-based antimalarial hybrid compounds.
Heterocyclic chalcone activators of nuclear factor (erythroid-derived 2)-like 2 (Nrf2) with improved in vivo efficacy.
Hedgehog inhibitors from Withania somnifera.
Indole Glucocorticoid Receptor Antagonists Active in a Model of Dyslipidemia Act via a Unique Association with an Agonist Binding Site.
University of Dundee, Gates Library screen for HepG2 cell viability.
Kynurenine Monooxygenase (KMO) Inhibitors for the Treatment of Acute Pancreatitis and Neurodegenerative Disorders.
Discovery of (phenoxy-2-hydroxypropyl)piperidines as a novel class of voltage-gated sodium channel 1.7 inhibitors.
Synthesis of 17-membered azalides from a 16-membered macrolide utilizing amide-selective silane reduction
The use of porcupine inhibitors to target Wnt-driven cancers.
Structure-Guided Design of Novel l-Cysteine Derivatives as Potent KSP Inhibitors.
Nav1.7 Inhibitors: Potential Effective Therapy for the Treatment of Chronic Pain.
Structure-activity relationship of indoloquinoline analogs anti-MRSA.
Aspertetranones A-D, Putative Meroterpenoids from the Marine Algal-Associated Fungus Aspergillus sp. ZL0-1b14.
A solid- and solution-phase-based library of 2-methyl substituted penicillin derivatives and their effects on growth inhibition of tumor cell lines
Discovery and structural diversity of the hepatitis C virus NS3/4A serine protease inhibitor series leading to clinical candidate IDX320.
Anti-inflammatory Inositol Derivatives from the Whole Plant of Inula cappa.
Structural Optimization of Indole Derivatives Acting at Colchicine Binding Site as Potential Anticancer Agents.
Identification and SAR of Glycine Benzamides as Potent Agonists for the GPR139 Receptor.
RORc Modulators for the Treatment of Autoimmune Diseases.
Small molecules that promote regenerative repair for pancreatic and cardiovascular health.
The isolation and synthesis of a novel benzofuran compound from Tephrosia purpurea, and the synthesis of several related derivatives, which suppress histamine H1 receptor gene expression.
Discovery of Imidazo[1,2-][1,8]naphthyridine Derivatives as Potential HCV Entry Inhibitor.
Glucagon receptor antagonists, preparation and therapeutic uses
Amino tetrahydro-pyridopyrimidine PDE10 inhibitors
Compounds, pharmaceutical compositions and uses thereof
Aryl- or heteroaryl-substituted benzene compounds
Tetraline and indane derivatives, pharmaceutical compositions containing them, and their use in therapy
Androstane and pregnane steroids with potent allosteric GABA receptor chloride ionophore modulating properties
Purine and deazapurine derivatives as pharmaceutical compounds
Aryloxmethyl cyclopropane derivatives as PDE10 inhibitors
Pyrrolidine derivatives, pharmaceutical compositions and uses thereof
Pharmaceutical compositions comprising RET inhibitors and methods for the treatment of cancer
Scriptaid isosteres and their use in therapy
Fused heterocyclic compounds as orexin receptor modulators
Prostaglandin transporter inhibitors and uses thereof
Aminopyrimidines useful as inhibitors of protein kinases
Pyrrolo[2,3-d]pyrimidine tropomysin-related kinase inhibitors
Heteroaryl-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism
Anti-infective agents against intracellular pathogens
(EN) 3-sulfonyl-pyrazolo[1,5-a] pyrimidines / antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof
Hexahydrocyclopentapyrrolone, hexahydropyrrolopyrrolone, octahydropyrrolopyridinone and octahydropyridinone compounds
Compounds as cannabinoid receptor ligands
Dihydro-oxazolobenzodiazepinone compounds, a process for there preparation and pharmaceutical compositions containing them
Pyrrolopyrazoles, potent kinase inhibitors
Bridged bicyclic RHO kinase inhibitor compounds, composition and use
Preparation method of dihydroindene amide compounds, their pharmaceutical compositions containing compounds thereof and use as protein kinases inhibitor
Imidazo[1,5]naphthyridine compounds, their pharmaceutical use and compositions
4-aminoquinazoline derivatives and uses thereof
Substituted benzimidazole-type piperidine compounds and uses thereof
Identification of stabilizers of multimeric proteins
Pyridine compounds and the users thereof
Disubstituted azepan orexin receptor antagonists
7-membered ring compound and method of production and pharmaceutical application thereof
Compounds and compositions as protein kinase inhibitors
Hydroxyurea analogues as kinetic and mechanistic probes of the nitric oxide producing reactions of hydroxyurea and oxyhemoglobin.
Structure-activity relationship studies of gonadotropin-releasing hormone antagonists containing S-aryl/alkyl norcysteines and their oxidized derivatives.
(1S)-1,5-anhydro-1-[5-(4-ethoxybenzyl)-2-methoxy-4-methylphenyl]-1-thio-D-glucitol (TS-071) is a potent, selective sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for type 2 diabetes treatment.
N-(5-chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a novel, highly selective, orally available, dual-specific c-Src/Abl kinase inhibitor.
Hydroxamic acids as a novel family of serine racemase inhibitors: mechanistic analysis reveals different modes of interaction with the pyridoxal-5'-phosphate cofactor.
Synthesis of 1,1-[1-naphthyloxy-2-thiophenyl]-2-methylaminomethylcyclopropanes and their evaluation as inhibitors of serotonin, norepinephrine, and dopamine transporters.
Synthesis and structure-activity relationship studies for hydantoins and analogues as voltage-gated sodium channel ligands.
Complexes of alkylene-linked tacrine dimers with Torpedo californica acetylcholinesterase: Binding of Bis5-tacrine produces a dramatic rearrangement in the active-site gorge.
Tetrahydrobiopterin binding to aromatic amino acid hydroxylases. Ligand recognition and specificity.
Human beta-secretase (BACE) and BACE inhibitors.
Antimalarial peroxide dyads from natural artemisinin and hydroxyalkylated 1,2,4-trioxanes.
The role of intracellularly released formaldehyde and butyric acid in the anticancer activity of acyloxyalkyl esters.
CoMFA and CoMSIA investigations revealing novel insights into the binding modes of dopamine D3 receptor agonists.
Probing the subpockets of factor Xa reveals two binding modes for inhibitors based on a 2-carboxyindole scaffold: a study combining structure-activity relationship and X-ray crystallography.
Discovery of potent anilide inhibitors against the severe acute respiratory syndrome 3CL protease.
Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.
New potent P-glycoprotein inhibitors carrying a polycyclic scaffold.
Discovery of 1-(3'-aminobenzisoxazol-5'-yl)-3-trifluoromethyl-N-[2-fluoro-4- [(2'-dimethylaminomethyl)imidazol-1-yl]phenyl]-1H-pyrazole-5-carboxyamide hydrochloride (razaxaban), a highly potent, selective, and orally bioavailable factor Xa inhibitor.
Discovery of S-phase arresting agents derived from noscapine.
Synthesis, structure-activity relationship, and receptor pharmacology of a new series of quinoline derivatives acting as selective, noncompetitive mGlu1 antagonists.
Dopamine D3 receptor partial agonists and antagonists as potential drug abuse therapeutic agents.
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
Structure-activity relationship studies optimizing the antiproliferative activity of novel cyclic somatostatin analogues containing a restrained cyclic beta-amino acid.
Synthesis, DNA affinity, and antiprotozoal activity of fused ring dicationic compounds and their prodrugs.
Benzylated and prenylated flavonoids from the root barks of Cudrania tricuspidata with pancreatic lipase inhibitory activity.
Phenolic 4-hydroxy and 3,5-dihydroxy derivatives of 3-phenoxyquinoxalin-2(1H)-one as potent aldose reductase inhibitors with antioxidant activity.
Exploration of Pharmacophore in Chrysosplenol C as Activator in Ventricular Myocyte Contraction.
Inhibitors of the Epidermal Growth Factor Receptor (EGFR) May Provide Effective Treatment for Lung Adenocarcinoma.
Optimization of Novel Antagonists to the Neurokinin-3 Receptor for the Treatment of Sex-Hormone Disorders (Part II).
Optimization of a Dibenzodiazepine Hit to a Potent and Selective Allosteric PAK1 Inhibitor.
Exploring the Existing Drug Space for Novel pTyr Mimetic and SHP2 Inhibitors.
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
Dimeric Macrocyclic Antagonists of Inhibitor of Apoptosis Proteins for the Treatment of Cancer.
Indolylpiperidine derivatives as potent and selective 1B adrenoceptor antagonists.
Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors.
BRD4 Structure-Activity Relationships of Dual PLK1 Kinase/BRD4 Bromodomain Inhibitor BI-2536.
Carbonic Anhydrase Glycoinhibitors belonging to the Aminoxysulfonamide Series.
Lepidotol A from Mesua lepidota Inhibits Inflammatory and Immune Mediators in Human Endothelial Cells.
Triazole-Linked Glycolipids Enhance the Susceptibility of MRSA to -Lactam Antibiotics.
Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORt Inhibitors.
Design and synthesis of constrained analogs of LCRF-0004 as potent RON tyrosine kinase inhibitors.
Phenolic Compounds from the Leaves and Twigs of Osteomeles schwerinae That Inhibit Rat Lens Aldose Reductase and Vessel Dilation in Zebrafish Larvae.
Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.
Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.
Pyrrolopyridine or Pyrazolopyridine Derivatives.
Potential Treatment for the Respiratory Syncytial Virus Infections (HRSV).
Novel Chalcone-Thiazole Hybrids as Potent Inhibitors of Drug Resistant Staphylococcus aureus.
Discovery of 11-hydroxysteroid dehydrogenase type 1 inhibitor.
Synergistic activation of quorum sensing in Vibrio harveyi.
Going Out on a Limb: Delineating The Effects of -Branching, N-Methylation, and Side Chain Size on the Passive Permeability, Solubility, and Flexibility of Sanguinamide A Analogues.
Pandalisines A and B, novel indolizidine alkaloids from the leaves of Pandanus utilis.
Anti-proliferative activity of Monensin and its tertiary amide derivatives.
3-Propionyl-thiazolidine-4-carboxylic acid ethyl esters: a family of antiproliferative thiazolidines
Immunosuppressive effect of zhankuic acid C from Taiwanofungus camphoratus on dendritic cell activation and the contact hypersensitivity response.
Fatty Acid Synthase (FASN) Inhibitors as Potential Treatment for Cancer, Obesity, and Liver Related Disorders.
Recent progress on MAP kinase pathway inhibitors.
Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752).
MICE models: superior to the HERG model in predicting Torsade de Pointes.
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
Morpholinone compounds as factor IXA inhibitors
Tricyclic compounds and PBK inhibitors containing the same
Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonists
Substituted 3-heteroaroylamino-propionic acid derivatives and their use as pharmaceuticals
Identification and characterization of N-acetylcysteine conjugates of valproic acid in humans and animals.
Metabolic intermediate complex formation of human cytochrome P450 3A4 by lapatinib.
Pharmacokinetics and pharmacodynamics of sibrafiban (Ro 48-3657), an orally active IIb/IIIa antagonist, administered alone or in combination with heparin, aspirin, and recombinant tissue-type plasminogen activator in beagles.
Human cytochrome P450 3A4-catalyzed testosterone 6 beta-hydroxylation and erythromycin N-demethylation. Competition during catalysis.
CYP3A4-mediated hepatic metabolism of the HIV-1 protease inhibitor saquinavir in vitro.
Different in vitro metabolism of paclitaxel and docetaxel in humans, rats, pigs, and minipigs.
Studies on the role of metabolic activation in tyrosine kinase inhibitor-dependent hepatotoxicity: induction of CYP3A4 enhances the cytotoxicity of lapatinib in HepaRG cells.
CPY3A4-mediated -hydroxyaldehyde formation in saquinavir metabolism.
Relationship of glutathione S-transferase genotypes with side-effects of pulsed cyclophosphamide therapy in patients with systemic lupus erythematosus.
Quantitative determination of valproic acid and 14 metabolites in serum and urine by gas chromatography/mass spectrometry.
Quantification of docetaxel and its metabolites in human plasma by liquid chromatography/tandem mass spectrometry.
Combination of micellar electrokinetic and high-performance liquid chromatographies to assess age-related changes in the in vitro metabolism of Fischer 344 rat liver.
Discovery of potent and selective small-molecule PAR-2 agonists.
Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335).
Synthesis and resolution of cis-(+/-)-methyl (1R,2S/1S,2R)-2-[(4-hydroxy-4-phenylpiperidin-1-yl)methyl]-1-(4-methylphenyl)cyclopropanecarboxylate [(+/-)-PPCC)]: new sigma receptor ligands with neuroprotective effect.
Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity.
Effects of 7-O substitutions on estrogenic and anti-estrogenic activities of daidzein analogues in MCF-7 breast cancer cells.
Structure-activity relationship studies of spinorphin as a potent and selective human P2X(3) receptor antagonist.
New fluorinated 1,2,4-benzothiadiazine 1,1-dioxides: discovery of an orally active cognitive enhancer acting through potentiation of the 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid receptors.
Acridine-based agents with topoisomerase II activity inhibit pancreatic cancer cell proliferation and induce apoptosis.
Discovery of tetrasubstituted imidazolines as potent and selective neuropeptide Y Y5 receptor antagonists: reduced human ether-a-go-go related gene potassium channel binding affinity and potent antiobesity effect.
Influence of the linker in bispyridium compounds on the inhibition of human choline kinase.
Discovery of 4-substituted methoxybenzoyl-aryl-thiazole as novel anticancer agents: synthesis, biological evaluation, and structure-activity relationships.
Novel non-peptide nociceptin/orphanin FQ receptor agonist, 1-[1-(1-Methylcyclooctyl)-4-piperidinyl]-2-[(3R)-3-piperidinyl]-1H-benzimidazole: design, synthesis, and structure-activity relationship of oral receptor occupancy in the brain for orally potent antianxiety drug.
Synthesis, crystallization, and biological evaluation of an orally active prodrug of gemcitabine.
Discovery of potent and orally available malonyl-CoA decarboxylase inhibitors as cardioprotective agents.
Synthesis and structure-activity relationships of new benzodioxinic lactones as potential anticancer drugs.
Synthesis and in vitro antitumor activity of phenanthrolin-7-one derivatives, analogues of the marine pyridoacridine alkaloids ascididemin and meridine: structure-activity relationship.
Synthesis and structure-activity relationship of a new series of COX-2 selective inhibitors: 1,5-diarylimidazoles.
Structural determinants of Torpedo californica acetylcholinesterase inhibition by the novel and orally active carbamate based anti-alzheimer drug ganstigmine (CHF-2819).
Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.
Pyrrolo[1,2-b][1,2,5]benzothiadiazepines (PBTDs): A new class of agents with high apoptotic activity in chronic myelogenous leukemia K562 cells and in cells from patients at onset and who were imatinib-resistant.
Stereoselective preparation of N-[(R,R)-(E)-1-(3,4-dichlorobenzyl)-3- (2-oxoazepan-3-yl)carbamoyl]allyl-N-methyl-3,5-bis(trifluoromethyl)benzamide, a potent and orally active dual neurokinin NK(1)/NK(2) receptor antagonist.
Spirocyclopropyl beta-lactams as mechanism-based inhibitors of serine beta-lactamases. Synthesis by rhodium-catalyzed cyclopropanation of 6-diazopenicillanate sulfone.
FDA drug approval package for Ambrisentan
FDA drug approval package for Carisoprodol
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.
Carbocyclic[g]indole inhibitors of human nonpancreatic s-PLA2.
Novel indolylindazolylmaleimides as inhibitors of protein kinase C-beta: synthesis, biological activity, and cardiovascular safety.
Synthesis and cytotoxic evaluation of novel spirohydantoin derivatives of the dihydrothieno[2,3-b]naphtho-4,9-dione system.
Solid-phase total synthesis of kahalalide A and related analogues.
N-substituted piperidinyl alkyl imidazoles: discovery of methimepip as a potent and selective histamine H3 receptor agonist.
QSAR study of anticonvulsant negative allosteric modulators of the AMPA receptor.
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation.
First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication.
A nonpeptidic sulfonamide inhibits the p53-mdm2 interaction and activates p53-dependent transcription in mdm2-overexpressing cells.
Structure-based design, synthesis, and evaluation of conformationally constrained mimetics of the second mitochondria-derived activator of caspase that target the X-linked inhibitor of apoptosis protein/caspase-9 interaction site.
Dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
Stereoselective binding of indomethacin ethanolamide derivatives to cyclooxygenase-1.
Synthesis and biological evaluation of novel chloroethylaminoanthraquinones with potent cytotoxic activity against cisplatin-resistant tumor cells.
Pharmacological exploitation of the alpha1-adrenoreceptor antagonist doxazosin to develop a novel class of antitumor agents that block intracellular protein kinase B/Akt activation.
Probing a 3,4'-bis-guanidinium diaryl derivative as an allosteric inhibitor of the Ras pathway.
Discovery of Bivalent Kinase Inhibitors via Enzyme-Templated Fragment Elaboration.
Discovery of novel isatin-dehydroepiandrosterone conjugates as potential anticancer agents.
Design and synthesis of novel hydroxyanthraquinone nitrogen mustard derivatives as potential anticancer agents via a bioisostere approach.
Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold
Factors influencing the cytotoxicity of -methylene--hydroxy esters against pancreatic cancer.
Synthesis of chiral ND-322, ND-364 and ND-364 derivatives as selective inhibitors of human gelatinase.
Differential influence of 7 cations on 16 non-competitive NMDA receptor blockers.
Synthesis and in vitro antitumor evaluation of betulin acid ester derivatives as novel apoptosis inducers.
Structure-Affinity Relationship Analysis of Selective FKBP51 Ligands.
Pyrido- and benzisothiazolones as inhibitors of histone acetyltransferases (HATs)
Structural Insights Lead to a Negamycin Analogue with Improved Antimicrobial Activity against Gram-Negative Pathogens.
Imidazole derivatives show anticancer potential by inducing apoptosis and cellular senescence
Isoxazole derivatives of 6-fluoro-N-(6-methoxybenzo[d]thiazol-2-yl)benzo[d]thiazol-2-amine and N-(pyrimidin-2-yl)benzo[d]thiazol-2-amine: regulation of cell cycle and apoptosis by p53 activation via mitochondrial-dependent pathways
Mechanism of forming trimer, self-assembling nano-particle and inhibiting tumor growth of small molecule CIPPCT
Discovery of mitochondria-targeting berberine derivatives as the inhibitors of proliferation, invasion and migration against rat C6 and human U87 glioma cells
Multicomponent Synthesis and Biological Evaluation of a Piperazine-Based Dopamine Receptor Ligand Library.
Functional Profiling of 2-Aminopyrimidine Histamine H4 Receptor Modulators.
Discovery, SAR, and X-ray Binding Mode Study of BCATm Inhibitors from a Novel DNA-Encoded Library.
Structure-activity relationship studies of SETD8 inhibitors.
Synthesis and biological evaluation of a new class of quinazolinoneazoles as potential antimicrobial agents and their interactions with calf thymus DNA and human serum albumin
Novel isoniazid-amidoether derivatives: Synthesis, characterization and antimycobacterial activity evaluation
Bile acid amphiphiles with tunable head groups as highly selective antitubercular agents
Synthesis of hybrid anticancer agents based on kinase and histone deacetylase inhibitors
Synthesis, DNA binding, docking and photocleavage studies of quinolinyl chalcones
Pentafluorosulfanyl-containing flufenamic acid analogs: Syntheses, properties and biological activities.
Rational design of proteinprotein interaction inhibitors
Dehydroabietylamine derivatives as multifunctional agents for the treatment of Alzheimer's disease
Tetrazole regioisomers in the development of nitro group-containing antitubercular agents
Synthesis of -brominated phosphonates and their application as phosphate bioisosteres
Adamantane amine derivatives as dual acting NMDA receptor and voltage-gated calcium channel inhibitors for neuroprotection
Optimisation of a triazolopyridine based histone demethylase inhibitor yields a potent and selective KDM2A (FBXL11) inhibitor.
Discovery of Potent and Selective Inhibitors for ADAMTS-4 through DNA-Encoded Library Technology (ELT).
A step forward in the sigma enigma: a role for chirality in the sigma1 receptorligand interaction?
Structure-Based Design of Selective Janus Kinase 2 Imidazo[4,5-d]pyrrolo[2,3-b]pyridine Inhibitors.
Identification of death-associated protein kinases inhibitors using structure-based virtual screening.
Vaccinia virus virulence factor N1L is a novel promising target for antiviral therapeutic intervention.
Multiple and single binding modes of fragment-like kinase inhibitors revealed by molecular modeling, residue type-selective protonation, and nuclear overhauser effects.
1,1'-Disubstituted ferrocenes as molecular hinges in mono- and bivalent dopamine receptor ligands.
N-sulfonylanthranilic acid derivatives as allosteric inhibitors of dengue viral RNA-dependent RNA polymerase.
Hydration of drug-DNA complexes: greater water uptake for adriamycin compared to daunomycin.
Structure-activity relationships of 9-substituted-9-dihydroerythromycin-based motilin agonists: optimizing for potency and safety.
Discovery of 6alpha-ethyl-23(S)-methylcholic acid (S-EMCA, INT-777) as a potent and selective agonist for the TGR5 receptor, a novel target for diabesity.
Phenoxy herbicides and fibrates potently inhibit the human chemosensory receptor subunit T1R3.
Toward efficient drug screening by homogeneous assays based on the development of new fluorescent vasopressin and oxytocin receptor ligands.
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.
Novel bis- and tris-1,2,4-trioxanes: synthesis and antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice.
Synthesis and evaluation of 2'-hydroxyethyl trans-apovincaminate derivatives as antioxidant and cognitive enhancer agents.
Synthesis, radiosynthesis, and biological evaluation of fluorine-18-labeled 2beta-carbo(fluoroalkoxy)-3beta-(3'-((Z)-2-haloethenyl)phenyl)nortropanes: candidate radioligands for in vivo imaging of the serotonin transporter with positron emission tomography.
Synthesis, structure-activity relationships, and antitumor studies of 2-benzoxazolyl hydrazones derived from alpha-(N)-acyl heteroaromatics.
Synthesis and evaluation of [18F] labeled pyrimidine nucleosides for positron emission tomography imaging of herpes simplex virus 1 thymidine kinase gene expression.
Molecular-docking-guided design, synthesis, and biologic evaluation of radioiodinated quinazolinone prodrugs.
A pyridazine series of alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Design and synthesis of novel isoquinoline-3-nitriles as orally bioavailable Kv1.5 antagonists for the treatment of atrial fibrillation.
Dicarba analogues of the cyclic enkephalin peptides H-Tyr-c[D-Cys-Gly-Phe-D(or L)-Cys]NH(2) retain high opioid activity.
Alpha1-adrenoceptor antagonists. 6. Structural optimization of pyridazinone-arylpiperazines. Study of the influence on affinity and selectivity of cyclic substituents at the pyridazinone ring and alkoxy groups at the arylpiperazine moiety.
Discovery of a nanomolar inhibitor of the human murine double minute 2 (MDM2)-p53 interaction through an integrated, virtual database screening strategy.
HIV-1 protease mutations and inhibitor modifications monitored on a series of complexes. Structural basis for the effect of the A71V mutation on the active site.
Synthesis and antibacterial activity of 6-O-arylbutynyl ketolides with improved activity against some key erythromycin-resistant pathogens.
Synthesis and complement inhibitory activity of B/C/D-ring analogues of the fungal metabolite 6,7-diformyl-3',4',4a',5',6',7',8',8a'-octahydro-4,6',7'-trihydroxy- 2',5',5',8a'-tetramethylspiro[1'(2'H)-naphthalene-2(3H)-benzofuran].
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents.
Hydroxy-1,2,5-oxadiazolyl moiety as bioisoster of the carboxy function. Synthesis, ionization constants, and pharmacological characterization of gamma-aminobutyric acid (GABA) related compounds.
Discovery of a new family of inhibitors of human cytomegalovirus (HCMV) based upon lipophilic alkyl furano pyrimidine dideoxy nucleosides: action via a novel non-nucleosidic mechanism.
A novel somatostatin mimic with broad somatotropin release inhibitory factor receptor binding and superior therapeutic potential.
Predictive three-dimensional quantitative structure-activity relationship of cytochrome P450 1A2 inhibitors.
Determinants of retinoid X receptor transcriptional antagonism.
Syntheses, calcium channel agonist-antagonist modulation activities, and nitric oxide release studies of nitrooxyalkyl 1,4-dihydro-2,6-dimethyl-3-nitro-4-(2,1,3-benzoxadiazol-4-yl)pyridine-5-carboxylate racemates, enantiomers, and diastereomers.
Sulfonyl-containing aldophosphamide analogues as novel anticancer prodrugs targeted against cyclophosphamide-resistant tumor cell lines.
Design, synthesis, and biological evaluation of new cyclic disulfide decapeptides that inhibit the binding of AP-1 to DNA.
A non-peptide NK1 receptor agonist showing subpicomolar affinity.
Cyclic ADP-ribose analogues containing the methylenebisphosphonate linkage: effect of pyrophosphate modifications on Ca2+ release activity.
A phenylnorstatine inhibitor binding to HIV-1 protease: geometry, protonation, and subsite-pocket interactions analyzed at atomic resolution.
Novel benzophenones as non-nucleoside reverse transcriptase inhibitors of HIV-1.
Identification of 2,4-diamino-6,7-dimethoxyquinoline derivatives as G9a inhibitorsElectronic supplementary information (ESI) available. See DOI: 10.1039/c4md00274a.
Chemical Synthesis and Biological Activities of 20S,24S/R-Dihydroxyvitamin D3 Epimers and Their 1-Hydroxyl Derivatives.
Synthesis and evaluation of a bis-3-chloropiperidine derivative incorporating an anthraquinone pharmacophore.
Synthesis of imidazo[2,1-b][1,3,4]thiadiazolechalcones as apoptosis inducing anticancer agents
Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties.
Probing Mechanisms of CYP3A Time-Dependent Inhibition Using a Truncated Model System.
Computationally motivated synthesis and enzyme kinetic evaluation of N-(-d-glucopyranosyl)-1,2,4-triazolecarboxamides as glycogen phosphorylase inhibitors
Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists.
Repair of methyl lesions in RNA by oxidative demethylation
Virtual screening for novel Atg5Atg16 complex inhibitors for autophagy modulation
Modeling, synthesis and NMR characterization of novel chimera compounds targeting STAT3
8-Hydroxyquinoline: a privileged structure with a broad-ranging pharmacological potential
Identification and characterization of -sitosterol target proteins.
Current developments of coumarin-based anti-cancer agents in medicinal chemistry.
Macrocyclic derivatives of 6-methyluracil as ligands of the peripheral anionic site of acetylcholinesterase
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Design, synthesis, and biological and docking studies of novel epipodophyllotoxinchalcone hybrids as potential anticancer agents
Discovery of BMS-641988, a Novel Androgen Receptor Antagonist for the Treatment of Prostate Cancer.
Synthesis of imidazothiadiazolebenzimidazole conjugates as mitochondrial apoptosis inducers
Design of Potent and Orally Active GPR119 Agonists for the Treatment of Type II Diabetes.
An azumamide C analogue without the zinc-binding functionality
Highly Efficient Synthesis of 1,3-Dihydroxy-2-carboxycarbazole and Its Neuroprotective Effects.
Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis.
3,5-Diamino-1,2,4-triazoles as a novel scaffold for potent, reversible LSD1 (KDM1A) inhibitors.
The status of the lysophosphatidic acid receptor type 1 (LPA1R)
Discovery of Novel Isatin-Based p53 Inducers.
Design, synthesis and biological evaluation of novel 1,2,4-triazolo and 1,2,4-triazino[4,3-a]quinoxalines as potential anticancer and antimicrobial agents
Synthesis of new betulinic acidpeptide conjugates and in vivo and in silico studies of the influence of peptide moieties on the triterpenoid core activity
Discovery of an orally active subtype-selective HDAC inhibitor, chidamide, as an epigenetic modulator for cancer treatment
Virtual Screening and Biological Validation of Novel Influenza Virus PA Endonuclease Inhibitors.
Discovery of Triazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Synthesis, Structure-Activity Relationship, and Mechanistic Investigation of Lithocholic Acid Amphiphiles for Colon Cancer Therapy.
Elucidating new structural features of the triazole scaffold for the development of mPGES-1 inhibitors
Synthesis of tetrazole compounds as a novel type of potential antimicrobial agents and their synergistic effects with clinical drugs and interactions with calf thymus DNA
Evaluation of functional groups as acetyl-lysine mimetics for BET bromodomain inhibition
Modulation of the Interaction between a Peptide Ligand and a G Protein-Coupled Receptor by Halogen Atoms.
Styrylphenylphthalimides as Novel Transrepression-Selective Liver X Receptor (LXR) Modulators.
Prokineticin Receptor Modulators May Potentially Treat Psychiatric and Neurological Disorders.
Discovery and crystallography of bicyclic arylaminoazines as potent inhibitors of HIV-1 reverse transcriptase.
Naphthoquinone-based chalcone hybrids and derivatives: synthesis and potent activity against cancer cell lines
Design, synthesis and antitumor activity of non-camptothecin topoisomerase I inhibitors.
Novel Lobophorins Inhibit Oral Cancer Cell Growth and Induce Atf4- and Chop-Dependent Cell Death in Murine Fibroblasts.
Fused Morphlinopyrimidines and Methods of Use Thereof.
Novel anti-HIV-1 NNRTIs based on a pyrazolo[4,3-d]isoxazole backbone scaffold: design, synthesis and insights into the molecular basis of action
Analogues of the marine alkaloids oroidin, clathrodin, and hymenidin induce apoptosis in human HepG2 and THP-1 cancer cells
Design, synthesis, and preliminary bioactivity studies of substituted purine hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors
Probing cytochrome P450-mediated activation with a truncated azinomycin analogue
Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain
Suppression of Hepatocellular Carcinoma by Inhibition of Overexpressed Ornithine Aminotransferase.
Discovery and Structure Enabled Synthesis of 2,6-Diaminopyrimidin-4-one IRAK4 Inhibitors.
High-Throughput Screening of Patient-Derived Cultures Reveals Potential for Precision Medicine in Glioblastoma.
Tranylcypromine derivatives as inhibitors of histone demethylases LSD1 and/or LSD2
6-cyclylmethyl-and 6-alkylmethyl-substituted pyrazolepyrimidines
Botryllamides and method of inhibiting PGP in a mammal afflicted with cancer
Pyrazolopyrimidine JAK inhibitor compounds and methods
Prolyl hydroxylase inhibitors and method of use
(6-oxo-1,6-dihydropyrimidin-2-yl)amide derivatives, preparation thereof and pharmaceutical use thereof as AKT(PKB) phosphorylation inhibitors
Targeting NAD biosynthesis in bacterial pathogens
Adenosine derivatives, method for the synthesis thereof, and the pharmaceutical compositions for the prevention and treatment of the inflammatory diseases containing the same as an active ingredient
Methods of modifying amyloid Œ= oligomers using non-peptidic compounds
Thieno[3,2-C]pyridine kinase inhibitors with improved CYP safety profile
1,2,6-substituted benzimidazoles as FLAP modulators
Heterocyclic acrylamides and their use as pharmaceuticals
Bacterial thioredoxin reductase inhibitors and methods for use thereof
Acetic acid amide derivative having inhibitory activity on endothelial lipase
Cyclohexane-1,2‚Ä=-naphthalene-1‚Ä=,2‚Ä=-imidazol compounds and their use as BACE inhibitors
Spiropyrrolidine beta-secretase inhibitors for the treatment of alzheimer'S disease
Substituted 3-(1H-benzo[d]imidazol-2-yl)-1H-indazole analogs as inhibitors of the PDK1 kinase
Naphthalen-1-yl-(4-pentyloxynaphthalen-1-yl)methanone: a potent, orally bioavailable human CB1/CB2 dual agonist with antihyperalgesic properties and restricted central nervous system penetration.
Synthesis, flow cytometric evaluation, and identification of highly potent dipyridamole analogues as equilibrative nucleoside transporter 1 inhibitors.
7-Hydroxy-benzopyran-4-one derivatives: a novel pharmacophore of peroxisome proliferator-activated receptor alpha and -gamma (PPARalpha and gamma) dual agonists.
Synthesis and evaluation of structurally constrained quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
2-Amino-3,4-dihydroquinazolines as inhibitors of BACE-1 (beta-site APP cleaving enzyme): Use of structure based design to convert a micromolar hit into a nanomolar lead.
Solution kinetics measurements suggest HIV-1 protease has two binding sites for darunavir and amprenavir.
Design, synthesis, and in vivo SAR of a novel series of pyrazolines as potent selective androgen receptor modulators.
Allosteric modulation of the dopamine receptor by conformationally constrained type VI beta-turn peptidomimetics of Pro-Leu-Gly-NH2.
Whole structure-activity relationships of the fat-accumulation inhibitor (-)-ternatin: recognition of the importance of each amino acid residue.
Synthesis, cytotoxicity, and anti-Trypanosoma cruzi activity of new chalcones.
Noncovalent tripeptidyl benzyl- and cyclohexyl-amine inhibitors of the cysteine protease caspase-1.
New series of antiprion compounds: pyrazolone derivatives have the potent activity of inhibiting protease-resistant prion protein accumulation.
Characterization of tunable piperidine and piperazine carbamates as inhibitors of endocannabinoid hydrolases.
Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays.
Acylguanidines as small-molecule beta-secretase inhibitors.
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization.
Synthesis and pharmacological characterization of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonists.
Discovery of 6-N,N-bis(2,2,2-trifluoroethyl)amino- 4-trifluoromethylquinolin-2(1H)-one as a novel selective androgen receptor modulator.
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis.
Antitumor activity of substituted E-3-(3,4,5-trimethoxybenzylidene)-1,3-dihydroindol-2-ones1.
Peptide-mediated cell transport of water soluble porphyrin conjugates.
Replacement of the N-terminal tyrosine residue in opioid peptides with 3-(2,6-dimethyl-4-carbamoylphenyl)propanoic acid (Dcp) results in novel opioid antagonists.
Synthesis of adenophostin A analogues conjugating an aromatic group at the 5'-position as potent IP3 receptor ligands.
Dopamine/serotonin receptor ligands. 13: Homologization of a benzindoloazecine-type dopamine receptor antagonist modulates the affinities for dopamine D(1)-D(5) receptors.
Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109.
Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues. Novel nicotinic antagonist.
3,3-diaryl-1,3-dihydroindol-2-ones as antiproliferatives mediated by translation initiation inhibition.
Design, synthesis, and preliminary pharmacological evaluation of 4-aminopiperidine derivatives as N-type calcium channel blockers active on pain and neuropathic pain.
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.
A new simple and high-yield synthesis of suberoylanilide hydroxamic acid and its inhibitory effect alone or in combination with retinoids on proliferation of human prostate cancer cells.
Stereochemical studies of the monocyclic agouti-related protein (103-122) Arg-Phe-Phe residues: conversion of a melanocortin-4 receptor antagonist into an agonist and results in the discovery of a potent and selective melanocortin-1 agonist.
Identification of novel parasitic cysteine protease inhibitors using virtual screening. 1. The ChemBridge database.
Synthesis and evaluation of the affinity toward mu-opioid receptors of atypical, lipophilic ligands based on the sequence c[-Tyr-Pro-Trp-Phe-Gly-].
Novel azido and isothiocyanato analogues of [3-(4-phenylalkylpiperazin-1-yl)propyl]bis(4-fluorophenyl)amines as potential irreversible ligands for the dopamine transporter.
Synthesis and structure-activity relationships of a novel series of tricyclic dihydropyridine-based KATP openers that potently inhibit bladder contractions in vitro.
A method for designing conformationally restricted analogues based on allylic strain: synthesis of a novel class of noncompetitive NMDA receptor antagonists having the acrylamide structure.
A prodrug approach toward the development of water soluble fluoroquinolones and structure--activity relationships of quinoline-3-carboxylic acids.
Methods of using 4, 5, 6, 7-tetrahydroimidazo-[4,5-c]pyridine compounds
6-1H-imidazo-quinazoline and quinolines derivatives, new MAO inhibitors and imidazoline receptor ligands
Macrocyclic inhibitors of hepatitis C virus
Quinolin-4 (1H)-one derivatives as inhibitors of phosphatidylinositol 3-kinases
Substituted 2-amino-3-(sulfonyl)pyrazolo[1,5-a]pyrimidines - serotonin 5-HT6 receptor antagonists, method for use thereof
Fused pyrimidines and substituted quinazolines as inhibitors of p97
Benzimidazole derivatives and their use for modulating the GABAA receptor complex
Use of rosuvastatin lactols as medicaments
Substituted dipyridyl-dihydropyrazolones and use thereof
1,4-benzodiazepine-2,5-diones and related compounds with therapeutic properties
Apogossypolone derivatives as anticancer agents
Sulfamide derivative having an adamantyl group and its pharmaceutically acceptable salt
Cycloalkane carboxylic acid derivatives as CXCR3 receptor antagonists
Esters of (acyloxymethyl)acrylamide, a pharmaceutical composition containing them, and their use as inhibitors of the thioredoxin‚Äîthioredoxin reductase system
Heteroaromatic compounds and their use as dopamine D1 ligands
2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
5-substituted-2-phenylamino benzamides as MEK inhibitors
Heterocyclic substituted pyrimidine compound
Aminodihydrothiazine derivatives substituted with a cyclic group
Methods and compositions for sleep disorders and other disorders
Pyridopyrimidine derivatives and use thereof
Kinase inhibitors and methods of their use
Hexahydropyrrolo[3,4-b]pyrrole derivatives, preparation methods and pharmaceutical uses thereof
Unsaturated nitrogen heterocyclic compounds useful as PDE10 inhibitors
Compounds for the treatment of addiction
Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
Azinone-substituted azepino[b]indole and pyrido-pyrrolo-azepine MCH-1 antagonists, methods of making, and use thereof
Pyridine compounds as sodium channel blockers
Substituted spiro[cycloalkyl-1,3‚Ä=-indo]-2‚Ä=(1‚Ä=H)-one derivatives and their use as P38 mitogen-activated kinase inhibitors
2-PYRIDYLOXY-4-NITRILE OREXIN RECEPTOR ANTAGONISTS
Inhibitors of pyruvate kinase and methods of treating disease
Apoptosis signal-regulating kinase inhibitors
Therapeutic applications in the cardiovascular field of quinazolinedione derivatives
Small molecule antagonists of phosphatidylinositol-3,4,5-triphosphate (PIP3) and uses thereof
Compounds Useful as Inhibitors of ATR Kinase
Prokineticin receptor antagonists and uses thereof
4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors
Indazolyl-substituted dihydroisoxa-zolopyridines and methods of use thereof
Substituted indazole derivatives active as kinase inhibitors
Quinoxaline inhibitors of phosphoinositide-3-kinases (PI3Ks)
Activity based probes (ABPs) interacting with glycosidases
8-[3-amino-piperidin-1-yl]-xanthines, their preparation and their use as pharmaceutical compositions
Compounds, formulations, and methods of protein kinase C inhibition
Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
Pyridonemorphinan analogs and biological activity on opioid receptors
Pyridinedione carboxamide inhibitors of endothelial lipase
Amine substituted methanesulfonamide derivatives as vanilloid receptor ligands
2‚Ä=-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
Polysubstituted benzofurans and medicinal applications thereof
Aryl sulfamide and sulfamate derivatives as RORc modulators
Pyridine and pyrimidine derivatives as phosphodiesterase 10 inhibitors
Arylpiperazine-containing imidazole 4-carboxamide derivatives and pharmaceutical composition comprising same
1,5-naphthyridine derivatives and MELK inhibitors containing the same
Substituted 5,6,7,8-tetrahydro-1,6-naphthyridines as factor XIa inhibitors
Tetracycline compounds as tyrosyl-DNA phosphodiesterase I inhibitors
Oxazine derivatives and their use in the treatment of neurological disorders
Heterocyclic pyrazole compounds, method for preparing the same and use thereof
Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes
Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
Compounds for inhibiting semicarbazide-sensitive amine oxidase (SSAO)/vascular adhesion protein-1 (VAP-1) and uses thereof for treatment and prevention of diseases
Benzodioxole or benzodioxepine heterocyclic compounds as phosphodiesterase inhibitors
Resorcinol derivatives as HSP90 inhibitors
Imidazo[1,2-B][1,2,4]triazines as C-MET inhibitors
Substituted carbamoylmethylamino acetic acid derivatives as novel NEP inhibitors
2,3-disubstituted pyrazinesulfonamides as CRTH2 inhibitors
Alkoxy tetrahydro-pyridopyrimidine PDE10 inhibitors
Bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives and uses thereof
Nitrogen-containing heteroaryl derivatives
Substituted pyridinyl-pyrimidines and their use as medicaments
2,5-disubstituted thiomorpholine orexin receptor antagonists
Structural basis for platelet antiaggregation by angiotensin II type 1 receptor antagonist losartan (DuP-753) via glycoprotein VI.
Perspectives of P-glycoprotein modulating agents in oncology and neurodegenerative diseases: pharmaceutical, biological, and diagnostic potentials.
Enhancement of hydrophobic interactions and hydrogen bond strength by cooperativity: synthesis, modeling, and molecular dynamics simulations of a congeneric series of thrombin inhibitors.
Structural analogues of smoothened intracellular loops as potent inhibitors of Hedgehog pathway and cancer cell growth.
Discovery of dermorphin-based affinity labels with subnanomolar affinity for mu opioid receptors.
Nongenomic actions of bile acids. Synthesis and preliminary characterization of 23- and 6,23-alkyl-substituted bile acid derivatives as selective modulators for the G-protein coupled receptor TGR5.
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.
(S)-N-{3-[1-cyclopropyl-1-(2,4-difluoro-phenyl)-ethyl]-1H-indol-7-yl}-methanesulfonamide: a potent, nonsteroidal, functional antagonist of the mineralocorticoid receptor.
Discovery of low nanomolar and subnanomolar inhibitors of the mycobacterial beta-carbonic anhydrases Rv1284 and Rv3273.
Rational design, synthesis, and pharmacological properties of new 1,8-naphthyridin-2(1H)-on-3-carboxamide derivatives as highly selective cannabinoid-2 receptor agonists.
Discovery of inducible nitric oxide synthase (iNOS) inhibitor development candidate KD7332, part 1: Identification of a novel, potent, and selective series of quinolinone iNOS dimerization inhibitors that are orally active in rodent pain models.
Synthesis of novel 4,6-di(substituted)amino-1,2-dihydro-1,3,5-triazine derivatives as topical antiseptic agents.
Gamma-aminobutyric acid amides of nortriptyline and fluoxetine display improved pain suppressing activity.
Bivalent diketopiperazine-based tropomysin receptor kinase C (TrkC) antagonists.
IC50 data for the L-type calcium channel extracted from a set of literature articles
Structural investigation of the 7-chloro-3-hydroxy-1H-quinazoline-2,4-dione scaffold to obtain AMPA and kainate receptor selective antagonists. Synthesis, pharmacological, and molecular modeling studies.
Similar structure-activity relationships of quinoline derivatives for antiprion and antimalarial effects.
Effects of azaspiracid-1, a potent cytotoxic agent, on primary neuronal cultures. A structure-activity relationship study.
Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2'-C-methylcytidine.
Potent inhibitors of the Qi site of the mitochondrial respiration complex III.
Design and synthesis of novel 2-amino-5-hydroxyindole derivatives that inhibit human 5-lipoxygenase.
Synthesis and mixed lineage kinase activity of pyrrolocarbazole and isoindolone analogs of (+)K-252a.
Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding.
Molecular tongs containing amino acid mimetic fragments: new inhibitors of wild-type and mutated HIV-1 protease dimerization.
Metabolically stabilized benzothiazoles for imaging of amyloid plaques.
Novel methylenephosphophosphonate analogues of mycophenolic adenine dinucleotide. Inhibition of inosine monophosphate dehydrogenase.
Divalent and trivalent alpha-ketocarboxylic acids as inhibitors of protein tyrosine phosphatases.
Identification of a nonsteroidal liver X receptor agonist through parallel array synthesis of tertiary amines.
Design, synthesis, and structure-activity relationship of 6-alkynylpyrimidines as potent adenosine kinase inhibitors.
Design and synthesis of tricyclic compounds with enone functionalities in rings A and C: a novel class of highly active inhibitors of nitric oxide production in mouse macrophages.
A new generation of N-aryl-N'-(1-alkyl-2-chloroethyl)ureas as microtubule disrupters: synthesis, antiproliferative activity, and beta-tubulin alkylation kinetics.
Discovery of 8-hydroxyadenines as a novel type of interferon inducer.
Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding.
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.
In vitro and in vivo antitumor properties of tetrakis((trishydroxy- methyl)phosphine)gold(I) chloride.
Development of potential antitumor agents. Synthesis and biological evaluation of a new set of sulfonamide derivatives as histone deacetylase inhibitors.
Interactive SAR studies: rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists.
Enantioselective responses to a phosphorothioate analogue of lysophosphatidic acid with LPA3 receptor-selective agonist activity.
Structure-activity relationship of imidazo[1,2-a]pyridines as ligands for detecting beta-amyloid plaques in the brain.
Pyrazolopyrrolidine derivatives and their use in the treatment of disease
Substituted heteroarylamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
Pyrid-2yl fused heterocyclic compounds, and compositions and uses thereof
Fused heterocyclic derivative, medicinal composition containing the same, and medicinal use thereof
Isonicotinamide orexin receptor antagonists
Substituted 2-aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment
Heteroaromatic compounds as BTK inhibitors
Substituted 6,6-fused nitrogenous heterocyclic compounds and uses thereof
Benzomorphan analogs and the use thereof
Nitrogen-containing spirocyclic compounds and pharmaceutical uses thereof
Substituted pyrazolo-quinazoline derivatives, process for their preparation and their use as kinase inhibitors
Pyridone amides as modulators of sodium channels
Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
Substituted 2-[2-(phenyl) ethylamino] alkaneamide derivatives and their use as sodium and/or calcium channel modulators
Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
Benzofuran derivatives for the treatment of hepatitis C
Inhibitors of human EZH2 and methods of use thereof
Dimethylarginine dimethylaminohydrolase inhibitors and methods of use thereof
Inhibitors of dimethylarginine dimethylaminohydrolase
Substituted imidazopyr- and imidazotri-azines
Substituted imidazolones, compositions containing such compounds and methods of use
Substituted 2-azabicycles and their use as orexin receptor modulators
Azaindolylphenyl sulfonamides as serine/threonine kinase inhibitors
4-carboxybenzylamino derivatives as histone deacetylase inhibitors
9-(pyrazol-3-yl)-9H-purine-2-amine and 3-(pyrazol-3-yl) -3H-imidazo[4,5-B] pyridin-5-amine derivatives and their use for the treatment of cancer
Carbamoyloxy arylalkan arylpiperazine analgesics
Imidazopyridines and imidazopyrimidines as HIV-1 reverse transcriptase inhibitors
Cyclic inhibitors of 11Œ=-hydroxysteroid dehydrogenase 1 based on the 1,3-oxazinan-2-one structure
Triazole compounds that modualte HSP90 activity
Pyrolinone derivative and pharmaceutical composition comprising the same
Imidazo[1,2-a]pyridine derivatives: preparation and pharmaceutical applications
Estrogen receptor ligands and methods of use thereof
Phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy
N-substituted benzamides and methods of use thereof
1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders
Substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs as tyrosine receptor kinase BTK inhibitors
Cycloalkyl-substituted imidazole derivative
Piperidinyl derivative as a modulator of chemokine receptor activity
N-substituted aminobenzocycloheptene, aminotetraline, aminoindane and phenalkylamine derivatives, pharmaceutical compositions containing them, and their use in therapy
Selective glycosidase inhibitors and uses thereof
Substituted tricyclic compounds and methods of use thereof
Tricyclic compounds and methods of use therefor
Method of using substituted 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
3-Oxo-2,3-dihydro-1H-indazole-4-carboxamide derivatives as PARP-1 inhibitors
2-aminopyrimidin-4-one and 2-aminopyridine derivatives both having BACE1-inhibiting activity
Picolinamido-propanoic acid derivatives useful as glucagon receptor antagonists
Quinazoline compounds as kinase inhibitors
Substituted dihydropteridin-6-one derivatives, process for their preparation and their use as kinase inhibitors
Imaging diagnostic agent and extracorporeal diagnostic agent for incurable neurological diseases
Benzenesulfonamide compounds, method for synthesizing same, and use thereof in medicine as well as in cosmetics
Aminopyridines useful as inhibitors of protein kinases
Thieno [2, 3-B] pyridine derivatives as viral replication inhibitors
Thienopyrimidines containing a substituted alkyl group for pharmaceutical compositions
Pyrrole compounds, a process for their preparation and pharmaceutical compositions containing them
C-aryl glucoside SGLT2 inhibitors and pharmaceutical compositions comprising same
Azabiphenylaminobenzoic acid derivatives as DHODH inhibitors
2-carboxamide-7-piperazinyl-benzofuran derivatives
Pyrimidine-substituted pyrrolidine derivatives, pharmaceutical compositions and uses thereof
Arylamino purine derivatives, preparation method and pharmaceutical use thereof
Heterocyclic substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
Compounds and compositions as kinase inhibitors
Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
Inhibition of memapsin 1 cleavage in the treatment of diabetes
5-membered ring heteroaromatic derivatives having NPY Y5 receptor antagonistic activity
Phenyl and benzodioxinyl substituted indazoles derivatives
Tricyclic derivative or pharmaceutically acceptable salts thereof, preparation method thereof, and pharmaceutical composition containing the same
Imidazo[4,5-c]quinolines as DNA-PK inhibitors
3- and 6-quinolines with N-attached heterocyclic CGRP receptor antagonists
Substituted heteroarylamine carboxamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
PARP inhibitor compounds, compositions and methods of use
Neuroprotective and neuro-restorative iron chelators and monoamine oxidase inhibitors and uses thereof
Novel cambinol analogs as sirtuin inhibitors: synthesis, biological evaluation, and rationalization of activity.
Novel indazole non-nucleoside reverse transcriptase inhibitors using molecular hybridization based on crystallographic overlays.
Discovery of N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide (BMS-777607), a selective and orally efficacious inhibitor of the Met kinase superfamily.
Design, synthesis, and estrogenic activity of a novel estrogen receptor modulator--a hybrid structure of 17beta-estradiol and vitamin E in hippocampal neurons.
Discovery of potent competitive inhibitors of indoleamine 2,3-dioxygenase with in vivo pharmacodynamic activity and efficacy in a mouse melanoma model.
Radiosynthesis and bioimaging of the tuberculosis chemotherapeutics isoniazid, rifampicin and pyrazinamide in baboons.
2009 Claude S. Hudson Award in Carbohydrate Chemistry. Carbohydrates: a frontier in medicinal chemistry.
Bis(dialkylaminethiocarbonyl)disulfides as potent and selective monoglyceride lipase inhibitors.
Pharmacophore modeling and molecular docking led to the discovery of inhibitors of human immunodeficiency virus-1 replication targeting the human cellular aspartic acid-glutamic acid-alanine-aspartic acid box polypeptide 3.
Identification of 4-aminopyrazolylpyrimidines as potent inhibitors of Trk kinases.
Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from cryptosporidium.
Novel triazole ribonucleoside down-regulates heat shock protein 27 and induces potent anticancer activity on drug-resistant pancreatic cancer.
Phosphonated carbocyclic 2'-oxa-3'-azanucleosides as new antiretroviral agents.
FDA drug approval package for Simvastatin
FDA drug approval package for Aliskiren hemifumarate
FDA drug approval package for Aspirin (clinical pharmacology review, Ref:ID 3227827)
FDA drug approval package for diclofenac acid (NDA 22-202 CP, Ref ID: 3374276)
Deepening the Topology of the Translocator Protein Binding Site by Novel N,N-Dialkyl-2-arylindol-3-ylglyoxylamides.
Anti-bacterial glycosyl triazoles - Identification of an N-acetylglucosamine derivative with bacteriostatic activity against Bacillus.
Design of glycosyltransferase inhibitors targeting human O-GlcNAc transferase (OGT)
Sulfonium ions as inhibitors of the mycobacterial galactofuranosyltransferase GlfT2
Discovery of novel guanidinophenylpyrazole human acrosin inhibitors by molecular hybridization
Conformational analysis of peramivir reveals critical differences between free and enzyme-bound states
Naphthalene and 2,3-dihydrobenzo[b][1,4]dioxine derivatives with extended side chains as new scaffolds of CB2-selective ligands
Identification of pyrazine-based TrkA inhibitors: design, synthesis, evaluation, and computational modeling studies.
Discovery of substituted 1,4-dihydroquinolines as novel promising class of P-glycoprotein inhibitors: First structure-activity relationships and bioanalytical studies.
Design, synthesis and molecular docking of novel bipyrazolyl thiazolone scaffold as a new class of antibacterial agents
Osthol and curcumin as inhibitors of human Pgp and multidrug efflux pumps of Staphylococcus aureus: reversing the resistance against frontline antibacterial drugs
Discovery and structural analyses of S-adenosyl-L-homocysteine hydrolase inhibitors based on non-adenosine analogs.
A critical evaluation of pyrrolo[2,3-d]pyrimidine-4-amines as Plasmodium falciparum apical membrane antigen 1 (AMA1) inhibitors
A double effect molecular switch leads to a novel potent negative allosteric modulator of metabotropic glutamate receptor 5
N-Arylalkylbenzo[d]thiazole-2-carboxamides as anti-mycobacterial agents: design, new methods of synthesis and biological evaluation
Recent trends in orexin research--2010 to 2015.
Identification of tanshinone IIA as a natural monoacylglycerol lipase inhibitor by combined in silico and in vitro approach
Synthesis of 1-O-acetylbritannilactone analogues from Inula britannica and in vitro evaluation of their anticancer potential
Synthesis and bioevaluation of heterocyclic derivatives of Cleistanthin-A.
Exploring the substrate promiscuity of an antibiotic inactivating enzyme
Beyond substrate analogues: new inhibitor chemotypes for glycosyltransferases
From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.
Branched -d-mannopyranosides: a new class of potent FimH antagonists
Investigation on the sucrose binding pocket of HIV-1 Integrase by molecular dynamics and synergy experiments.
Diversity-Oriented Synthesis for Novel, Selective and Drug-like Inhibitors for a Phosphatase from Mycobacterium Tuberculosis.
Optimization of the anti-cancer activity of phosphatidylinositol-3 kinase pathway inhibitor PITENIN-1: switching a thiourea with 1,2,3-triazole.
Identification and optimisation of 7-azaindole PAK1 inhibitors with improved potency and kinase selectivity
Cytoprotective effects of hydrogen sulfide-releasing N-methyl-D-aspartate receptor antagonists are mediated by intracellular sulfane sulfur.
Combining Mass Spectrometric Metabolic Profiling with Genomic Analysis: A Powerful Approach for Discovering Natural Products from Cyanobacteria.
Design and synthesis of membrane-targeting antibiotics: from peptides- to aminosugar-based antimicrobial cationic amphiphiles
Non-classical -carbonic anhydrase inhibitors-towards novel anti-mycobacterials
Novel cajaninstilbene acid derivatives as antibacterial agents.
The discovery of ezetimibe: a view from outside the receptor.
Design, synthesis, and biological activity of a difluoro-substituted, conformationally rigid vigabatrin analogue as a potent gamma-aminobutyric acid aminotransferase inhibitor.
Small molecule mitochondrial F1F0 ATPase hydrolase inhibitors as cardioprotective agents. Identification of 4-(N-arylimidazole)-substituted benzopyran derivatives as selective hydrolase inhibitors.
Formation of water-soluble pincer silver(I)-carbene complexes: a novel antimicrobial agent.
Carbon isosteres of the 4-aminopyridine substructure of chloroquine: effects on pK(a), hematin binding, inhibition of hemozoin formation, and parasite growth.
(2R,1'S,2'R,3'S)-2-(2'-Carboxy-3'-phenylcyclopropyl)glycine (PCCG-13), the first potent and selective competitive antagonist of phospholipase D-coupled metabotropic glutamate receptors: asymmetric synthesis and preliminary biological properties.
Pharmacophore and quantitative structure-activity relationship modeling: complementary approaches for the rationalization and prediction of UDP-glucuronosyltransferase 1A4 substrate selectivity.
Bisphosphonate prodrugs: synthesis and in vitro evaluation of novel clodronic acid dianhydrides as bioreversible prodrugs of clodronate.
Benzodiazepine receptor ligands. 4. Synthesis and pharmacological evaluation of 3-heteroaryl-8-chloropyrazolo[5,1-c][1,2,4] benzotriazine 5-oxides.
(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.
Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3- hydroxymethyl-4-piperidyl]-3-ethyl-1, 3-dihydro-2H-benzimidazol-2-one (J-113397).
5-Amino-1-(chloromethyl)-1,2-dihydro-3H-benz[e]indoles: relationships between structure and cytotoxicity for analogues bearing different DNA minor groove binding subunits.
Asymmetric synthesis and antiviral activities of L-carbocyclic 2', 3'-didehydro-2',3'-dideoxy and 2',3'-dideoxy nucleosides.
(2S,1'S,2'R,3'R)-2-(2'-Carboxy-3'-hydroxymethylcyclopropyl) glycine is a highly potent group 2 and 3 metabotropic glutamate receptor agonist with oral activity.
FDA drug approval package for saquinavir mesylate (NDA: 21-785)
Compounds having TRPV1 antagonistic activity and uses thereof
Use of azaphilone compounds for the modulation of the activity of a nuclear hormone receptor
Amino nicotinic and isonicotinic acid derivatives as DHODH inhibitors
Cyclohexane derivative having NPY Y5 receptor antagonism
Amino-indolyl-substituted imidazolyl-pyrimidines and their use as medicaments
N-hydroxy-benzamids for the treatment of cancer
Compounds as hypoxia mimetics, and compositions and uses thereof
Tetrahydrocyclopenta[c]acridine derivatives as kinase inhibitors and biological
Aminopyrimidine derivatives as LRRK2 modulators
Azetidine and piperidine compounds useful as PDE10 inhibitors
Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds
Adenosine receptor ligands and uses thereof
Substituted pyrido[3,2-E][1,2,4]-triazolo[4,3-A]pyrazines for the treatment of central nervous system disorders
Anti-cancer compound and pharmaceutical composition containing the same
Uracil compound or salt thereof having human deoxyuridine triphosphatase inhibitory activity
Oxazole and thiazole compounds as KSP inhibitors
Piperidine derivatives as modulators of chemokine receptor activity
Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use
Aminoalcohol substituted 2,3-dihydroimidazo[1,2-c]quinazoline derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
Substituted oxazolidinones and their use in the field of blood coagulation
Thiophene compounds for inflammation and immune-related uses
Nitrogen-containing heterocyclic compound and use of same
1,3,5-triazine-2-amine derivatives, preparation thereof and diagnostic and therapeutic use thereof
Cyclohexane-1,2‚Ä=-indene-1‚Ä=,2‚Ä=-imidazol compounds and their use as BACE inhibitors
Benzoxazepin compounds selective for PI3K P110 delta and methods of use
Morpholinyl derivatives useful as MOGAT-2 inhibitors
3-pyrimidin-4-yl-oxazolidin-2-ones as inhibitors of mutant IDH
Substituted imidazo[1,2-a]pyrimidines and ‚Äîpyridines
Compounds and their administration for treating a neurodegenerative disease as well as a method for identifying a compound capable of inhibiting a kinase, such as LRRK
Bivalent ligands for the treatment of neurological disorders
3-(heteroaryl-amino)-1,2,3,4-tetrahydro-9H-carbazole derivatives and their use as prostaglandin D2 receptor modulators
Imidazo[1,2-Œ±]pyridine sulfonamides as TRPM8 modulators
Pyrimidinyl-piperazines useful as D3/D2 receptor ligands
Disubstituted heteroaryl-fused pyridines
Chromane derivatives as TRPV3 modulators
Pyrido-, pyrazo- and pyrimido-pyrimidine derivatives as mTOR inhibitors
Agents for reversing epigenetic silencing of genes
Cycloalkylnitrile pyrazole carboxamides as janus kinase inhibitors
Pyrimidinecarboxamide derivatives as inhibitors of Syk kinase
Substituted bicyclic 1-carboxylic-acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin C
Tricyclic compound and pharmaceutical use thereof
5-HT3 receptor modulators, methods of making, and use thereof
Trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease
Substituted phenylureas and phenylamides as vanilloid receptor ligands
Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators
Substituted benzamide analogs as mGluR5 negative allosteric modulators and methods of making and using the same
2-arylimidazole derivatives as PDE10A enzyme inhibitors
Alicyclic[c] benzopyrone derivatives and uses thereof
2,3,4,5-tetrahydro-benzo{B}{1,4}diazepine-comprising compounds of formula(III) for treating pain
Substituted 2-(chroman-6-yloxy)-thiazoles and their use as pharmaceuticals
ALDH-2 inhibitors in the treatment of addiction
Bicyclic heterocyclic compounds as FGFR inhibitors
17-(1‚Ä=propenyl)-17-3‚Ä=-oxidoestra-4-en-3-one derivative, use thereof, and medicament containing said derivative
Substituted aminopropionic derivatives as neprilysin inhibitors
Combination therapy with MDM2 and EFGR inhibitors
Bicyclic compounds and their uses as dual c-SRC/JAK inhibitors
4-substituted-cyclohexylamino-4-piperidinyl-acetamide antagonists of CCR2
4-aminopyrimidine derivatives and their as as adenosine A2a receptor antagonists
Method of treating human skin and a skin care composition for use in such a method
N-biphenylmethylindole modulators of PPARG
Primary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
Substituted indanes, method for the production thereof, and use thereof as drugs
Quinoline derivatives and MELK inhibitors containing the same
Pyrazole compound and pharmaceutical use thereof
Sulfonamide compounds having TRPM8 antagonistic activity
Fluorene compound and pharmaceutical use thereof
Substituted (E)-N‚Ä=-(1-phenylethylidene)benzohydrazide analogs as histone demethylase inhibitors
Pyridazine carboxamide orexin receptor antagonists
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
Structure-based optimization of pyrazolo[3,4-d]pyrimidines as Abl inhibitors and antiproliferative agents toward human leukemia cell lines.
Synthesis and biological evaluation of the mitochondrial complex 1 inhibitor 2-[4-(4-fluorobutyl)benzylsulfanyl]-3-methylchromene-4-one as a potential cardiac positron emission tomography tracer.
Design, synthesis, and testing of non-nephrotoxic desazadesferrithiocin polyether analogues.
Betulinic acid derivatives as human immunodeficiency virus type 2 (HIV-2) inhibitors.
Design, synthesis, and evaluation of tricyclic, conformationally constrained small-molecule mimetics of second mitochondria-derived activator of caspases.
Highly potent 4-amino-indolo[2,3-c]azepin-3-one-containing somatostatin mimetics with a range of sst receptor selectivities.
Computer-aided identification of Trypanosoma brucei uridine diphosphate galactose 4'-epimerase inhibitors: toward the development of novel therapies for African sleeping sickness.
Estrogen receptor dependent inhibitors of NF-kappaB transcriptional activation-1 synthesis and biological evaluation of substituted 2-cyanopropanoic acid derivatives: pathway selective inhibitors of NF-kappaB, a potential treatment for rheumatoid arthritis.
Facile stereospecific synthesis and biological evaluation of (S)- and (R)-2-amino-2-methyl-4-[123I]iodo-3-(E)-butenoic acid for brain tumor imaging with single photon emission computerized tomography.
Synthesis and biological evaluation of (hetero)arylmethyloxy- and arylmethylamine-phenyl derivatives as potent P-glycoprotein modulating agents.
Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity.
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.
Discovery of a potent, selective, and orally active human epidermal growth factor receptor-2 sheddase inhibitor for the treatment of cancer.
Design, synthesis, and evaluation of novel boronic-chalcone derivatives as antitumor agents.
Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Rationally designed nucleoside antibiotics that inhibit siderophore biosynthesis of Mycobacterium tuberculosis.
Synthesis and biological evaluation of purealin and analogues as cytoplasmic dynein heavy chain inhibitors.
Selective antiproliferative activity of hydroxynaphthyl-beta-D-xylosides.
A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.
SAR by MS: discovery of a new class of RNA-binding small molecules for the hepatitis C virus: internal ribosome entry site IIA subdomain.
Mono- or diphenylpyridazines connected to N-(2,4-difluorophenyl)-N'-heptylurea as acyl-CoA:cholesterol acyltransferase inhibitors.
Rapid synthesis of triazole-modified resveratrol analogues via click chemistry.
Identification from a positional scanning peptoid library of in vivo active compounds that neutralize bacterial endotoxins.
Identification of isoflavone derivatives as effective anticryptosporidial agents in vitro and in vivo.
Jatrophane diterpenes as P-glycoprotein inhibitors. First insights of structure-activity relationships and discovery of a new, powerful lead.
Restriction of a peptide turn conformation and conformational analysis of guanidino group using arginine-proline fused amino acids: application to mini atrial natriuretic peptide on binding to the receptor.
Phosphinic pseudo-tripeptides as potent inhibitors of matrix metalloproteinases: a structure-activity study.
Synthesis and biological evaluation of iodinated and fluorinated 9-(2-hydroxypropyl) and 9-(2-hydroxyethoxy)methyl purine nucleoside analogues.
Identification of a potent and selective 5-HT(6) antagonist: one-step synthesis of (E)-3-(benzenesulfonyl)-2- (methylsulfanyl)pyrido[1,2-a]pyrimidin-4-ylidenamine from 2-(benzenesulfonyl)-3,3-bis(methylsulfanyl)acrylonitrile.
Combined effect of platination and intercalation upon DNA binding of novel cytotoxic Pt-bis(naphthalimide) complexes.
Identification of (3R)-7-hydroxy-N-((1S)-1-[[(3R,4R)-4-(3-hydroxyphenyl)- 3,4-dimethyl-1-piperidinyl]methyl]-2-methylpropyl)-1,2,3,4-tetrahydro- 3-isoquinolinecarboxamide as a novel potent and selective opioid kappa receptor antagonist.
Syntheses and structure-activity relationships of 5,6,7, 8-tetrahydro-5,5,8,8-tetramethyl-2-quinoxaline derivatives with retinoic acid receptor alpha agonistic activity.
A potential melanoma tracer: synthesis, radiolabeling, and biodistribution in mice of a new nitridotechnetium bis(aminothiol) derivative pharmacomodulated by a N-(diethylaminoethyl)benzamide.
Selective ET(A) antagonists. 5. Discovery and structure-activity relationships of phenoxyphenylacetic acid derivatives.
Design, synthesis, and evaluation of analogues of 3,3,3-trifluoro-2-hydroxy-2-phenyl-propionamide as orally available general anesthetics.
[1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
Compositions and methods for treatment of leukemia
Imidazo-, pyrazolopyrazines and imidazotriazines and their use
Pyrazolylbenzothiazole derivatives and their use as therapeutic agents
Substituted 6,7-dialkoxy-3-isoquinolinol derivatives as inhibitors of phosphodiesterase 10 (PDE10A)
Substituted dihydropyrazolones for treating cardiovascular and hematological diseases
Fused heterocyclic derivative and pharmaceutical use thereof
Epiminocycloalkyl[b] indole derivatives as serotonin sub-type 6 (5-HT6) modulators and uses thereof
Inhibitors of histone deacetylase and prodrugs thereof
Proline sulfonamide derivatives as orexin receptor antagonists
Carbazole and carboline kinase inhibitors
Substituted imidazopyridines as HDM2 inhibitors
C-linked hydroxamic acid derivatives useful as antibacterial agents
Substituted indole compounds having NOS inhibitory activity
6-fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-quinazolin-4-one as an inhibitor of human phosphatidylinositol 3-kinase delta
Bryostatin analogues, synthetic methods and uses
Pyrrolopyridazine JAK3 inhibitors and their use for the treatment of inflammatory and autoimmune diseases
Cancer targeting using carbonic anhydrase isoform IX inhibitors
Heteroaryl substituted indole compounds useful as MMP-13 inhibitors
Conformationally restricted urea inhibitors of soluble epoxide hydrolase
Substituted aminobutyric derivatives as neprilysin inhibitors
Intramolecular hydrogen-bonded nitric oxide synthase inhibitors
Medical composition for treatment or prophylaxis of glaucoma
Aminotetraline derivatives, pharmaceutical compositions containing them, and their use in therapy
Azabenzothiazole compounds, compositions and methods of use
Methods and compositions of treating a flaviviridae family viral infection
Spiro-amino-imidazo-fused heterocyclic compounds as beta-secretase modulators and methods of use
Soft protease inhibitors and pro-soft forms thereof
Seven-membered ring compound and pharmaceutical use therefor
Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
Benzimidazole inhibitors of leukotriene production
Pyrazole-amide compounds and pharmaceutical use thereof
Tetrahydro-azacarboline MCH-1 antagonists, methods of making, and uses thereof
Tetrahydroquinoxaline urea derivatives as modulators of 11-B-hydroxysteroid dehydrogenase type I
Selective caspase inhibitors and uses thereof
Pyridazinones, method of making, and method of use thereof
Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides inhibitors of cathepsin C
Purine derivatives as adenosine A1 receptor agonists and methods of use thereof
1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors
Methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds
Compounds and their use as BACE inhibitors
(aza)indole derivative and use thereof for medical purposes
1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derivatives
Cyclohexyl amide derivatives and their use as CRF-1 receptor antagonists
Complement pathway modulators and uses thereof
Dipeptidyl peptidase-IV inhibiting compounds, methods of preparing the same, and pharmaceutical compositions containing the same as active agent
Benzonitrile derivatives as kinase inhibitors
Bicyclic dihydroimidazolone CGRP receptor antagonists
Management and treatment of benign prostatic hyperplasia
Fused bicyclic oxazolidinone CETP inhibitor
Phenylcyclopropylamine derivatives and their medical use
Benzoxazines, benzothiazines, and related compounds having NOS inhibitory activity
Compounds effective as xanthine oxidase inhibitors, method for preparing the same, and pharmaceutical composition containing the same
Substituted quinolines and their use as medicaments
3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivatives as kinase inhibitors
Indazole compounds useful as ketohexokinase inhibitors
Heterocyclic compounds as S1P1 agonists for the treatment of autoimmune and vascular diseases
Nitrogen-containing heterocyclic compound and use thereof
Method of reducing intraocular pressure in humans
Quinazoline derivatives as a multiplex inhibitor and method for the preparation thereof
Imidazopyridine derivatives as inhibitors of receptor tyrosine kinases
Preparation and uses of 1,2,4-triazolo [1,5a] pyridine derivatives
2H-imidazol-4-amine compounds and their use as BACE inhibitors
Nitrogen-containing condensed heterocyclic compound
Spiro-amino-imidazolone and spiro-amino-dihydro-pyrimidinone compounds as beta-secretase modulators and methods of use
Treatment of liver disorders with PI3K inhibitors
In pursuit of natural product leads: synthesis and biological evaluation of 2-[3-hydroxy-2-[(3-hydroxypyridine-2-carbonyl)amino]phenyl]benzoxazole-4-carboxylic acid (A-33853) and its analogues: discovery of N-(2-benzoxazol-2-ylphenyl)benzamides as novel antileishmanial chemotypes.
Modulation of cellular apoptosis with apoptotic protease-activating factor 1 (Apaf-1) inhibitors.
Dual-action lipophilic iminosugar improves glycemic control in obese rodents by reduction of visceral glycosphingolipids and buffering of carbohydrate assimilation.
Selective angiotensin II AT2 receptor agonists: arylbenzylimidazole structure-activity relationships.
Thiophene bioisosteres of spirocyclic sigma receptor ligands. 1. N-substituted spiro[piperidine-4,4'-thieno[3,2-c]pyrans].
Identification of inhibitors of drug-resistant Candida albicans strains from a library of bicyclic peptidomimetic compounds.
(Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators.
Structure-activity relationships of a novel series of urotensin II analogues: identification of a urotensin II antagonist.
Dopamine receptor ligands. Part 18: (1) modification of the structural skeleton of indolobenzazecine-type dopamine receptor antagonists.
Extra binding region induced by non-zinc chelating inhibitors into the S1' subsite of matrix metalloproteinase 8 (MMP-8).
Urotensin-II receptor modulators as potential drugs.
4-Oxo-beta-lactams (azetidine-2,4-diones) are potent and selective inhibitors of human leukocyte elastase.
Novel peptidomimetic cysteine protease inhibitors as potential antimalarial agents.
Scaffold hopping with molecular field points: identification of a cholecystokinin-2 (CCK2) receptor pharmacophore and its use in the design of a prototypical series of pyrrole- and imidazole-based CCK2 antagonists.
Design, synthesis, and biological evaluation of dual binding site acetylcholinesterase inhibitors: new disease-modifying agents for Alzheimer's disease.
A selective estrogen receptor modulator designed for the treatment of uterine leiomyoma with unique tissue specificity for uterus and ovaries in rats.
Novel tricyclic compounds having acetylene groups at C-8a and cyano enones in rings A and C: highly potent anti-inflammatory and cytoprotective agents.
7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine: a functionally selective gamma-aminobutyric acid(A) (GABA(A)) alpha2/alpha3-subtype selective agonist that exhibits potent anxiolytic activity but is not sedating in animal models.
Mapping the melatonin receptor. 7. Subtype selective ligands based on beta-substituted N-acyl-5-methoxytryptamines and beta-substituted N-acyl-5-methoxy-1-methyltryptamines.
Discovery of iodinated somatostatin analogues selective for hsst2 and hsst5 with excellent inhibition of growth hormone and prolactin release from rat pituitary cells.
Synthesis and biological evaluation of new pentaphyrin macrocycles for photodynamic therapy.
Virtual screening of novel CB2 ligands using a comparative model of the human cannabinoid CB2 receptor.
Synthesis and structure-activity relationships of linear and conformationally constrained peptide analogues of CIYKYY as Src tyrosine kinase inhibitors.
Biological mechanisms of action of novel C-10 non-acetal trioxane dimers in prostate cancer cell lines.
Synthesis and structure-activity relationships of parasiticidal thiosemicarbazone cysteine protease inhibitors against Plasmodium falciparum, Trypanosoma brucei, and Trypanosoma cruzi.
3-Alkylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides as ATP-sensitive potassium channel openers: effect of 6,7-disubstitution on potency and tissue selectivity.
Synthesis of 2',5'-dideoxy-2-fluoroadenosine and 2',5'-dideoxy-2,5'-difluoroadenosine: potent P-site inhibitors of adenylyl cyclase.
Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.
Hydrophobic acetal and ketal derivatives of mannopeptimycin-alpha and desmethylhexahydromannopeptimycin-alpha: semisynthetic glycopeptides with potent activity against Gram-positive bacteria.
Synthesis and use of novel ether phospholipid enantiomers to probe the molecular basis of the antitumor Effects of alkyllysophospholipids: correlation of differential activation of c-Jun NH(2)-terminal protein kinase with antiproliferative effects in neuronal tumor cells.
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
Exploring structure-activity relationships of transition state analogues of human purine nucleoside phosphorylase.
4-[(Alkylamino)methyl]furo[3,2-c]pyridines: a new series of selective kappa-receptor agonists.
Synthesis and antitumor activity of novel O-carbamoylmethyloxime derivatives of radicicol.
Thioamides: synthesis, stability, and immunological activities of thioanalogues of Imreg. Preparation of new thioacylating agents using fluorobenzimidazolone derivatives.
Novel prodrug approach for tertiary amines: synthesis and preliminary evaluation of N-phosphonooxymethyl prodrugs.
N-((3-benzyl)-2,2-(bis-phenyl)-propan-1-amine derivatives as CETP inhibitors for the treatment of atherosclerosis and cardiovascular diseases
Furo[3, 2-B] pyrrol-3-ones as cathespin S inhibitors
Histone deacetylase inhibitors based simultaneously on trisubstituted 1H-pyrroles and aromatic and heteroaromatic spacers
Derivatives of azaindoles as inhibitors of protein kinases ABL and SRC
Pyruvamide compounds as inhibitors of dust mite group 1 peptidase allergen and their use
Inhibition of small ubiquitin-like modifier enzymes with substituted pyrrolo[2,3-b]quinoxalines
Sulfoximine-substituted pyrimidines as CDK- and/or VEGF inhibitors, their production and use as pharmaceutical agents
Tropomyosin-related kinase (TRK) inhibitors
PIM kinase inhibitors and methods of their use
Quinoline carboxamide derivatives as protein tyrosine kinase inhibitors
Pyrazolopyrimidine compounds and their use as PDE10 inhibitors
Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
Compounds from Antrodia cinnamomea and use thereof
Pharmaceutical composition comprising estetrol derivatives for use in cancer therapy
Heterocyclic compounds as ERK inhibitors
7-deazapurine modulators of histone methyltransferase, and methods of use thereof
Thiophenecarboxamide derivatives as EP4 receptor ligands
Cyclic inhibitors of 11BETA-hydroxysteroid dehydrogenase 1
Method of using 4,5,6,7-tetrahydroimidazo[4,5-C]pyridine compounds
Triazolones as fatty acid synthase inhibitors
3-amido-pyrrolo[3,4-C]pyrazole-5(1H, 4H,6H) carbaldehyde derivatives
Aryl- and heteroaryl-substituted tetrahydroisoquinolines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
Azole derivatives in the form of lipase and phospholipase inhibitors
Urokinase inhibitors, production and use thereof
(3-aryl-piperazin-1-yl), (2-aryl-morpholin-4-yl) and (2-aryl-thiomorpholin-4-yl) derivatives of 6,7-dialkoxy-quinazoline, 6,7-dialkoxyphtalazine and 6,7-dialkoxyisoquinoline as PDE10A enzyme inhibitors
Substituted piperidine compounds and their use as orexin receptor modulators
Pyridone and pyridazinone derivatives as anti-obesity agents
Processes and intermediates for preparing substituted hexahydrofuro [2,3-b] furans
Acylpiperazinones and their use as pharmaceuticals
Compositions and methods for treating cancer
Substituted pyrrolotriazines as protein kinase inhibitors
Benzenesulfonyl-chromane, thiochromane, tetrahydronaphthalene and related gamma secretase inhibitors
Phenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
Pyrazole oxadiazole derivatives as S1P1 agonists
2,3-dihydro-1H-indene-2-yl urea derivative and pharmaceutical application of same
Nitrogenous-ring acylguanidine derivative
Sulfonamide compounds useful as CYP17 inhibitors
Non-ATP dependent inhibitors of extracellular signal-regulated kinase (ERK)
Heteroaromatic phenylimidazole derivatives as PDE10A enzyme inhibitors
Compound of a reverse-turn mimetic and a production method and use therefor
Pyrrolopyrimidine compounds and their uses
Pyrazol-4-yl-heterocyclyl-carboxamide compounds and methods of use
Cyclic P1 linkers as factor XIa inhibitors
Triazole derivatives with improved receptor activity and bioavailability properties as ghrelin antagonists of growth hormone secretagogue receptors
4-phenylpiperazine derivatives with functionalized linkers as dopamine D3 receptor selective ligands and methods of use
Compounds for the treatment of inflammatory disorders
3-oxo-2,3-dihydro-1H-isoindole-4-carboxamides with selective PARP-1 inhibition
Phenylpropionamide compounds and the use thereof
Tricyclic compounds, compositions, and methods
1,3-oxazines as BACE1 and/or BACE2 inhibitors
Pyrimido [5,4-D] pyrimidine derivatives for the inhibition of tyrosine kinases
Compounds and methods for treating bacterial infections
Sulfur-containing heterocyclic derivative having beta secretase inhibitory activity
Phenylimidazole derivatives as PDE10A enzyme inhibitors
Tetrahydro-pyrido-pyrimidine derivatives
Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
Na/K-ATPase ligands, ouabain antagonists, assays and uses thereof
Imidazo [2, 1-B] [1, 3, 4] thiadiazole derivatives
Quinoxaline carboxamide derivatives as protein tyrosine kinase inhibitors
Compounds for the treatment of CNS disorders
1,4-diaryl-pyrimidopyridazine-2,5-diones and their use
Inhibitors of syk and JAK protein kinases
Thienopyrazole derivative having PDE7 inhibitory activity
Derivatives of 7-alkynyl-1,8-naphthyridones, preparation method thereof and use of same in therapeutics
S1P3 receptor inhibitors for treating pain
Pyridine-2-derivatives as smoothened receptor modulators
Methods of using cycloalkylmethylamine derivatives
Thienopyrimidines for pharmaceutical compositions
Substituted pyrazolo[1,5-a]pyrimidine compounds as Trk kinase inhibitors
Process for preparing a compound useful for producing an optically active diazabicyclooctane compound
Histone deacetylase inhibitor of benzamides and use thereof
Methods for treating or preventing cancer and neurodegenerative diseases
Diamide compounds having muscarinic receptor antagonist and Œ=2 adrenergic receptor agonist activity
Non-peptide macrocyclic histone deacetylese (HDAC) inhibitors and methods of making and using thereof
In vitro structure-activity relationship and in vivo characterization of 1-(aryl)-3-(4-(amino)benzyl)urea transient receptor potential vanilloid 1 antagonists.
Synthesis, antitubulin, and antiproliferative SAR of analogues of 2-methoxyestradiol-3,17-O,O-bis-sulfamate.
Lead optimization of N-3-substituted 7-morpholinotriazolopyrimidines as dual phosphoinositide 3-kinase/mammalian target of rapamycin inhibitors: discovery of PKI-402.
Macrocyclic pyridyl polyoxazoles: selective RNA and DNA G-quadruplex ligands as antitumor agents.
Inhibitors of the hepatitis C virus NS3 protease with basic amine functionality at the P3-amino acid N-terminus: discovery and optimization of a new series of P2-P4 macrocycles.
Validation of diacyl glycerolacyltransferase I as a novel target for the treatment of obesity and dyslipidemia using a potent and selective small molecule inhibitor.
Fructose-1,6-bisphosphatase Inhibitors. 2. Design, synthesis, and structure-activity relationship of a series of phosphonic acid containing benzimidazoles that function as 5'-adenosinemonophosphate (AMP) mimics.
Antiviral potential and molecular insight into neuraminidase inhibiting diarylheptanoids from Alpinia katsumadai.
N-hydroxybenzimidazole inhibitors of the transcription factor LcrF in Yersinia: novel antivirulence agents.
Identification of novel falcipain-2 inhibitors as potential antimalarial agents through structure-based virtual screening.
Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells.
Novel peptidomimetics containing a vinyl ester moiety as highly potent and selective falcipain-2 inhibitors.
Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors.
Novel synthesis, cytotoxic evaluation, and structure-activity relationship studies of a series of alpha-alkylidene-gamma-lactones and lactams.
Microwave-accelerated synthesis of P1'-extended HIV-1 protease inhibitors encompassing a tertiary alcohol in the transition-state mimicking scaffold.
Probing the pharmacophore of ginkgolides as glycine receptor antagonists.
Total synthesis of two novel subpicomolar sarco/endoplasmatic reticulum Ca2+-ATPase inhibitors designed by an analysis of the binding site of thapsigargin.
1-(5-Chloro-2-alkoxyphenyl)-3-(5-cyanopyrazin-2-yl)ureas [correction of cyanopyrazi] as potent and selective inhibitors of Chk1 kinase: synthesis, preliminary SAR, and biological activities.
N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
1-Benzhydryl-3-phenylurea and 1-benzhydryl-3-phenylthiourea derivatives: new templates among the CB1 cannabinoid receptor inverse agonists.
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Indol-1-yl acetic acids as peroxisome proliferator-activated receptor agonists: design, synthesis, structural biology, and molecular docking studies.
Conversion of the potent delta-opioid agonist H-Dmt-Tic-NH-CH(2)-bid into delta-opioid antagonists by N(1)-benzimidazole alkylation(1).
Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists.
Synthesis and biological activity of 7-phenyl-6,9-dihydro-3H-pyrrolo[3,2-f]quinolin-9-ones: a new class of antimitotic agents devoid of aromatase activity.
Indolin-2-ones with high in vivo efficacy in a model for multiple sclerosis.
Development of irreversible diphenyl phosphonate inhibitors for urokinase plasminogen activator.
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Design, synthesis, structural studies, biological evaluation, and computational simulations of novel potent AT(1) angiotensin II receptor antagonists based on the 4-phenylquinoline structure.
A ligand-based approach to identify quantitative structure-activity relationships for the androgen receptor.
Synthesis and biological evaluation of 2-phenylpyran-4-ones: a new class of orally active cyclooxygenase-2 inhibitors.
Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.
Novel S-substituted aminoalkylamino ethanethiols as potential antidotes against sulfur mustard toxicity.
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
Progesterone receptor ligand binding pocket flexibility: crystal structures of the norethindrone and mometasone furoate complexes.
Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
In vitro and in vivo evaluation of ruthenium(II)-arene PTA complexes.
Comparative molecular active site analysis (CoMASA). 1. An approach to rapid evaluation of 3D QSAR.
MMV Malaria Box gametocyte standard membrane feeding assay screening.
Substituted 3-arylsulfonyl-pyrazolo[1,5-A]pyrimidines, serotonin 5-HT6 receptor antagonists and methods for the production and use thereof
Modulators of calcium release-activated calcium channel
Technetium- and rhenium-bis(heteroaryl) complexes and methods of use thereof
Bicyclic aryl and heteroaryl sodium channel inhibitors
2-amino-3-sulphonyl-tetrahydro-pyrazolo[1,5-A]pyrido-pyrimidine antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof
Dihydropyrimidin-2(1H)-one compounds as neurokinin-3 receptor antagonists
Benzofuro[3,2-c] pyridines and related analogs as serotonin sub-type 6 (5-HT6) modulators for the treatment of obesity, metabolic syndrome, cognition and schizophrenia
5 oxo-5,8-dihydropyrido[2,3-d]pyrimidine derivatives as CaMKII kinase inhibitors for treating cardiovascular diseases
3,5-disubstituted alkynylbenzene compound and salt thereof
Azaindazoles as kinase inhibitors and use thereof
Histone deacetylase inhibitors, process for preparation and uses thereof
Substituted pyrimidines for the treatment of diseases such as cancer
Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
Selective phosphodiesterase 9A inhibitors as medicaments for improving cognitive processes
Tetrahydroisoquinolines, pharmaceutical compositions containing them, and their use in therapy
Acyclic amine inhibitors of nucleoside phosphorylases and hydrolases
Substituted pyrimidine compounds and their use as SYK inhibitors
Biphenyl derivatives useful as glucagon receptor antagonists
Compound useful for the treatment of degenerative and inflammatory diseases
Imidazo[5,1-f][1,2,4]triazines for the treatment of neurological disorders
Imidazole derivatives and their use as modulators of cyclin dependent kinases
Anti-inflammatory compound having inhibitory activity against multiple tyrosine kinases and pharmaceutical composition containing same
Method for enhancing anti-tumor effect of a microtubule-targeting drug, and a method for treatment of tumor
Tetrahydro-pyrazolo[1,5-a]pyrido-pyrimidines as antagonists of serotonin 5-HT6 receptors, methods for the production and use thereof
Aryl glycoside compound, preparation method and use thereof
Substituted 4-(indazolyl)-1,4-dihydropyridines and methods of use thereof
Heteroarylcarboxylic acid ester derivative
Heterocyclic modulators of lipid synthesis
Imidazo[1,2-a]pyridines and imidazo[1,2-b]pyridazines as mark inhibitors
1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds
Substituted benzo-pyrido-triazolo-diazepine compounds
1‚Ä=-substituted pyrimidine N-nucleoside analogs for antiviral treatment
Indole derivative or pharmaceutically acceptable salt thereof
Lithocholic acid analogues that inhibit sialyltransferase
Substituted 3-phenyl-1,2,4-Oxadiazole compounds
Spirocyclic nitriles as protease inhibitors
Triazole compounds that modulate HSP90 activity
(4-{4-[5-(benzooxazol-2-ylamino)-pyridin-2-yl]-phenyl}-cyclohexyl)-acetic acid useful for treating or preventing conditions or disorders associated with DGAT1 activity
Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
Tricyclic derivatives, process for their preparation and their use as kinase inhibitors
Pyrazine derivatives and use as PI3K inhibitors
Amide, urea or sulfone amide linked benzothiazole inhibitors of endothelial lipase
Azetidine derivatives, pharmaceutical compositions and uses thereof
Cycloalkyl ether compounds and their use as BACE inhibitors
Bicyclo[3.2.1]octyl amide derivatives and uses of same
Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds for use in the treatment of chemokine-mediated pathologies
Synthesis of bicyclic compounds and method for their use as therapeutic agents
17Beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of hormone-related diseases
Substituted imidazo[1,5-A]quinoxalines as phosphodiesterase 9 inhibitors
C-aryl glucoside derivatives, preparation process and pharmaceutical use thereof
Heteroaryloxycarbocyclyl compounds as PDE10 inhibitors
Substituted pyrazolone compounds and methods of use
SGLT-2 inhibitors, methods of making them, and uses thereof
Oxime-based compound, pharmaceutical composition containing the same and method for preparing the same
Cyclohexyl amide derivatives as CRF receptor antagonists
Pyridopyrazines as highly selective ras-Raf-Mek-Erk signal transduction pathway inhibitors
Triazolium salts as PAR1 inhibitors, production thereof, and use as medicaments
Cyclic ether DGAT1 inhibitorscyclic ether DGAT1 inhibitors
Aza- and diaza-phthalazine compounds as P38 map kinase modulators and methods of use thereof
Dual action inhibitors against histone deacetylases and 3-hydroxy-3-methylglutaryl coenzyme a reductase
Adenosine compounds and their use thereof
Thiazolyl mGluR5 antagonists and methods for their use
Targeting the fatty acid biosynthesis enzyme, beta-ketoacyl-acyl carrier protein synthase III (PfKASIII), in the identification of novel antimalarial agents.
Complementary three-dimensional quantitative structure-activity relationship modeling of binding affinity and functional potency: a study on alpha4beta2 nicotinic ligands.
Role of the hydrogen bonding heteroatom-Lys53 interaction between the p38alpha mitogen-activated protein (MAP) kinase and pyridinyl-substituted 5-membered heterocyclic ring inhibitors.
Cyclic sulfones as novel P3-caps for hepatitis C virus NS3/4A (HCV NS3/4A) protease inhibitors: synthesis and evaluation of inhibitors with improved potency and pharmacokinetic profiles.
14beta-Arylpropiolylamino-17-cyclopropylmethyl-7,8-dihydronormorphinones and related opioids. Further examples of pseudoirreversible mu opioid receptor antagonists.
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
Short antisense oligonucleotides with novel 2'-4' conformationaly restricted nucleoside analogues show improved potency without increased toxicity in animals.
Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1).
Design, synthesis and biological evaluation of glutathione peptidomimetics as components of anti-Parkinson prodrugs.
Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes.
Irreversible inhibition of dipeptidyl peptidase 8 by dipeptide-derived diaryl phosphonates.
Modeling of the aryl hydrocarbon receptor (AhR) ligand binding domain and its utility in virtual ligand screening to predict new AhR ligands.
Conformational analysis and receptor docking of N-[(1S,2S)-3-(4-chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (taranabant, MK-0364), a novel, acyclic cannabinoid-1 receptor inverse agonist.
Limonoids with Anti-HIV Activity from Cipadessa cinerascens.
Deconins A-E: Cuparenic and Mevalonic or Propionic Acid Conjugates from the Basidiomycete Deconica sp. 471.
Antagonism/Agonism modulation to build novel antihypertensives selectively triggering i1-imidazoline receptor activation.
N-(3-Ethynyl-2,4-difluorophenyl)sulfonamide Derivatives as Selective Raf Inhibitors.
Cytotoxic and antiviral nitrobenzoyl sesquiterpenoids from the marine-derived fungus Aspergillus ochraceus Jcma1F17
Discovery of small molecule inhibitors targeting the SUMOSIM interaction using a protein interface consensus approach
N1-linked melatonin dimers as bivalent ligands targeting dimeric melatonin receptors
Inhibitors of the PD-1/PD-L1 Pathway Can Mobilize the Immune System: An Innovative Potential Therapy for Cancer and Chronic Infections.
Design, Synthesis, and Biological Evaluation of Novel Imidazo[1,2-a]pyridine Derivatives as Potent c-Met Inhibitors.
Design and Validation of FRESH, a Drug Discovery Paradigm Resting on Robust Chemical Synthesis.
Novel N-Acetyl Bioisosteres of Melatonin: Melatonergic Receptor Pharmacology, Physicochemical Studies, and Phenotypic Assessment of Their Neurogenic Potential.
Design and synthesis of close analogs of LCRF-0004, a potent and selective RON receptor tyrosine kinase inhibitor.
Discovery and SAR study of a sulfonamide hydroxamic acid inhibitor for the botulinum neurotoxin serotype A light chain
Bis-arylidene oxindole-betulinic Acid conjugate: a fluorescent cancer cell detector with potent anticancer activity.
Synthesis of mixed opioid affinity cyclic endomorphin-2 analogues with fluorinated phenylalanines.
Monocarboxylate transporter 1 inhibitors as potential anticancer agents.
Novel azoles as potent and selective cannabinoid CB2 receptor agonists.
Design of Pyridopyrazine-1,6-dione -Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability.
Inhibitors of the PAR-2 Signaling Pathway May Treat Pain and Inflammation.
Discovery of Quinazoline-Based Fluorescent Probes to 1-Adrenergic Receptors.
Combretastatin A-4 inspired novel 2-aryl-3-arylamino-imidazo-pyridines/pyrazines as tubulin polymerization inhibitors, antimitotic and anticancer agents
Design, synthesis and biological evaluation of novel trimethylpyrazine-2-carbonyloxy-cinnamic acids as potent cardiovascular agents
Design, Synthesis, and Evaluation of 4- and 5-Substituted o-(Octanesulfonamido)benzoic Acids as Inhibitors of Glycerol-3-Phosphate Acyltransferase.
Discovery of a Potent Parenterally Administered Factor XIa Inhibitor with Hydroxyquinolin-2(1H)-one as the P2' Moiety.
Iminolactones from Schizophyllum commune.
Optimizing glucokinase activator binding kinetics to lower in vivo hypoglycemia risk
Novel phthalimide derivatives with TNF- and IL-1 expression inhibitory and apoptotic inducing properties
Design, Synthesis, and Pharmacological Evaluation of Fused -Homophenylalanine Derivatives as Potent DPP-4 Inhibitors.
Top-down Targeted Metabolomics Reveals a Sulfur-Containing Metabolite with Inhibitory Activity against Angiotensin-Converting Enzyme in Asparagus officinalis.
Isolation and Characterization of Dammarane-Type Saponins from Gynostemma pentaphyllum and Their Inhibitory Effects on IL-6-Induced STAT3 Activation.
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
The antimalarial drug atovaquone binds to saposin B with comparable affinity to coenzyme Q10
Minor Structural Change to Tertiary Sulfonamide RORc Ligands Led to Opposite Mechanisms of Action.
The synthesis and functional evaluation of a mitochondria-targeted hydrogen sulfide donor, (10-oxo-10-(4-(3-thioxo-3H-1,2-dithiol-5-yl)phenoxy)decyl)triphenylphosphonium bromide (AP39)
Scaffold hopping of potential anti-tumor agents by WEGA: a shape-based approach
Dibenzazepines and dibenzoxazepines as sodium channel blockers.
Introduction of polar groups on the naphthalene scaffold of molecular tongs inhibiting wild-type and mutated HIV-1 protease dimerization
Benzoxaborole antimalarial agents. Part 4. Discovery of potent 6-(2-(alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles.
Discovery of a Potent Class of PI3K Inhibitors with Unique Binding Mode via Encoded Library Technology (ELT).
Selective Inhibition of Bacterial Topoisomerase I by alkynyl-bisbenzimidazoles.
Bioactive Limonoid Constituents of Munronia henryi.
SAR and Structural Analysis of Siderophore-Conjugated Monocarbam Inhibitors of Pseudomonas aeruginosa PBP3.
Synthesis and Initial in Vivo Studies with [(11)C]SB-216763: The First Radiolabeled Brain Penetrative Inhibitor of GSK-3.
Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes.
Chrodrimanins I and J from the Antarctic Moss-Derived Fungus Penicillium funiculosum GWT2-24.
Design and Evaluation of 3-(Benzylthio)benzamide Derivatives as Potent and Selective SIRT2 Inhibitors.
(R)-2-Phenylpyrrolidine Substituted Imidazopyridazines: A New Class of Potent and Selective Pan-TRK Inhibitors.
Synthesis and Pharmacology of /(3)-Peptides Based on the Melanocortin Agonist Ac-His-dPhe-Arg-Trp-NH2 Sequence.
Two diseases, one approach: multitarget drug discovery in Alzheimer's and neglected tropical diseases
Synthesis and antiproliferative evaluation of 9-methoxy-6-(piperazin-1-yl)-11H-indeno[1,2-c]quinoline-11-one derivatives. Part 4
University of Dundee Gates Library Compound Collection
Emerging molecular approaches to pain therapy.
Prediction of ligand-receptor binding thermodynamics by free energy force field three-dimensional quantitative structure-activity relationship analysis: applications to a set of glucose analogue inhibitors of glycogen phosphorylase.
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
Anti-Helicobacter pylori agents. 3. 2-[(Arylalkyl)guanidino]-4-furylthiazoles.
5-Fluorinated L-lysine analogues as selective induced nitric oxide synthase inhibitors.
2-Substituted 4-(thio)chromenone 6-O-sulfamates: potent inhibitors of human steroid sulfatase.
Imidazole inhibitors of cytokine release: probing substituents in the 2 position.
Discovery of the first N-substituted 4beta-methyl-5-(3-hydroxyphenyl)morphan to possess highly potent and selective opioid delta receptor antagonist activity.
Discovery of potent, nonsteroidal, and highly selective glucocorticoid receptor antagonists.
Novel 2-oxoamide inhibitors of human group IVA phospholipase A(2).
Discovery of tyrosine-based potent and selective melanocortin-1 receptor small-molecule agonists with anti-inflammatory properties.
Identification of potent and selective small-molecule inhibitors of caspase-3 through the use of extended tethering and structure-based drug design.
Influence of the 5-HT6 receptor on acetylcholine release in the cortex: pharmacological characterization of 4-(2-bromo-6-pyrrolidin-1-ylpyridine-4-sulfonyl)phenylamine, a potent and selective 5-HT6 receptor antagonist.
Discovery of gamma-lactam hydroxamic acids as selective inhibitors of tumor necrosis factor alpha converting enzyme: design, synthesis, and structure-activity relationships.
1-Benzyl-3-(5'-hydroxymethyl-2'-furyl)indazole (YC-1) derivatives as novel inhibitors against sodium nitroprusside-induced apoptosis.
FDA drug approval package for Epirubicin (NDA: 21-010 and 50-778)
HDAC inhibitors and therapeutic methods of using same
Œ=-Secretase substrates and methods of use
Nitrogen heterocycle derivatives, preparation thereof and application thereof in human therapeutics
Compounds and methods for kinase modulation, and indications therefor
Azolopyridin-3-one derivatives as inhibitors of lipases and phospholipases
Hydroxymethylaryl-substituted pyrrolotriazines as ALK1 inhibitors
Azinone-substituted azapolycycle MCH-1 antagonists, methods of making, and use thereof
Substituted pyrrolo[3,4-D]imidazoles for the treatment of MDM2/4 mediated diseases
7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives and their use as prostaglandin D2 receptor modulators
Pyrido [5, 4-D] pyrimidines as cell proliferation inhibitors
Pyrrolopyrimidine compounds as inhibitors of CDK4/6
Derivatives of [1,3]Oxazin-2-one useful for the treatment of metabolic diseases such as lipid disorders
4-Cyano-1H-imidazole-2-carboxylic acid [2-cyclohex-1-enyl-4-(2,6-dioxo-piperidin-4-yl)-phenyl]-amide; tyrosine kinase inhibitor; autoimmune diseases, antiinflammatory, anticarcinogenic agent
Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases
Substituted pyrido[2,3-d]pyrimidin-7(8H)-ones and therapeutic uses thereof
Phytoestrogenic formulations for alleviation or prevention of neurodegenerative diseases
Substituted imidazopyridinyl-aminopyridine compounds
Trypsin-like serine protease inhibitors, and their preparation and use
Fused pyridine, pyrimidine and triazine compounds as cell cycle inhibitors
Small molecule inhibitors of RGS proteins
Respiratory formulations and compounds for use therein
Synthesis and use of dual tyrosyl-DNA phosphodiesterase I (TDP1)- topoisomerase I (TOP1) inhibitors
1,2,5-substituted benzimidazoles as FLAP modulators
Substituted pyrimido[1,2-b]indazoles and their use as modulators of the Pi3K/Akt pathway
Pyrimidine derivatives that inhibit FAK/PTK2
2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives and use thereof to block reuptake of norepinephrine, dopamine, and serotonin
Fluoro-substituted 2-aryl-3,5-dicyano-4-indazolyl-6-methyl-1,4-dihydropyridines and uses thereof
Tricyclic compounds as modulators of TNF-Œ± synthesis and as PDE4 inhibitors
Tricyclic pyrrolo derivatives, process for their preparation and their use as kinase inhibitors
Compounds and compositions as Syk kinase inhibitors
Aminopyridine and carboxypyridine compounds as phosphodiesterase 10 inhibitors
Tetrahydropyrido-pyridine and tetrahydropyrido-pyrimidine compounds and use thereof as C5a receptor modulators
Substituted 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of Cathepsin C
Triazolopyridazines as PAR1 inhibitors, production thereof, and use as medicaments
Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
Piperazine compound capable of inhibiting prostaglandin D synthase
Co-crystals and salts of CCR3-inhibitors
Cytoskeletal active rho kinase inhibitor compounds, composition and use
Synthetic compounds and methods to decrease nicotine self-administration
Small molecule inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase
Compounds for treatment of Alzheimer's disease
19-nor-steroid derivatives with a 15Œ±,16Œ±-methylene group and a saturated 17,17-spirolactone ring, use thereof, and medicaments containing said derivatives
Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof
Heterocyclic derivatives and their use in the treatment of neurological disorders
Substituted bicyclic heteroaryl compounds
Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use
Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer
6,7-unsaturated-7-carbamoyl substituted morphinan derivative
Heterocyclic analogs of propargyl-linked inhibitors of dihydrofolate reductase
Ring-substituted N-pyridinyl amides as kinase inhibitors
Azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
Specific nNOS inhibitors for the therapy and prevention of human melanoma
Macrocyclic compounds and their use as kinase inhibitors
6-amino quinazoline or 3-cyano quinoline derivatives, preparation methods and pharmaceutical uses thereof
Bivalent inhibitors of IAP proteins and therapeutic methods using the same
2-aryl imidazo[1,2-a]pyridine-3-acetamide derivatives, preparation methods and uses thereof
Aminoheteroaryl compounds and preparation method and use thereof
Substituted imidazo[2,1-A]isoindoles as PDE10 inhibitors
Inhibitors of epoxide hydrolases for the treatment of inflammation
Disubstituted octahydropyrrolo[3,4-c]pyrroles as orexin receptor modulators
Diamino heterocyclic carboxamide compound
Dioxa-bicyclo[3.2.1]octane-2,3,4-triol derivatives
5,6,7,8,9,10-hexahydro-6,10-epimino[1,2,4]triazolo[4,3-a]azocines as P2X7 modulators
Imidazotriazinecarbonitriles useful as kinase inhibitors
Substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
Modulators of calcium release-activated calcium channel and methods for treatment of non-small cell lung cancer
3-oxo-2,3-dihydro-1H-isoindole-4-carboxamides as PARP inhibitors
Pyridone analogs useful as melanin concentrating hormone receptor-1 antagonists
Inhibitors of cyclophilins and uses thereof
Optimization of ADME Properties for Sulfonamides Leading to the Discovery of a T-Type Calcium Channel Blocker, ABT-639.
Synthesis of iminosugar derivatives presenting naphthyl and alkyl amine interacting groups and binding to somatostatin receptors
A practical glycosyltransferase assay for the identification of new inhibitor chemotypes
Discovery of 5-Amino-N-(1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide Inhibitors of IRAK4.
Inhibitors of the human neuraminidase enzymes
Acetate-Derived Metabolites from the Brown Alga Lobophora variegata.
HPLC-NMR and HPLC-MS Profiling and Bioassay-Guided Identification of Secondary Metabolites from the Australian Plant Haemodorum spicatum.
Synthesis, antiribosomal and antibacterial activity of 4-O-glycopyranosyl paromomycin aminoglycoside antibiotics
Prostaglandin EP3 Receptor Antagonists May Provide Novel Treatment for Diabetes.
Identification of Jumonji AT-Rich Interactive Domain 1A Inhibitors and Their Effect on Cancer Cells.
Selective Acetamidine-Based Nitric Oxide Synthase Inhibitors: Synthesis, Docking, and Biological Studies.
Discovery of LRRK2 inhibitors using sequential in silico joint pharmacophore space (JPS) and ensemble docking.
Generation of Broad-Spectrum Antifungal Drug Candidates from the Natural Product Compound Aureobasidin A.
New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure.
Bioactive Diterpenoids from the Leaves of Callicarpa macrophylla.
Identification of Oxaphenalenone Ketals from the Ascomycete Fungus Neonectria sp.
A new class of ghrelin O-acyltransferase inhibitors incorporating triazole-linked lipid mimetic groups.
A Selective, Cell-Permeable Nonphosphorylated Bicyclic Peptidyl Inhibitor against Peptidyl-Prolyl Isomerase Pin1.
Dehydro--proline Containing 41 Integrin Antagonists: Stereochemical Recognition in Ligand-Receptor Interplay.
The biology and synthesis of -hydroxytropolones.
Discovery and Optimization of Selective Nav1.8 Modulator Series That Demonstrate Efficacy in Preclinical Models of Pain.
Towards bacterial adhesion-based therapeutics and detection methods
Development and validation of a novel assay to identify radiosensitizers that target nucleophosmin 1.
A full conformational characterization of antiandrogen cortexolone-17-propionate and related compounds through theoretical calculations and nuclear magnetic resonance spectroscopy
Species differences in drug plasma protein binding
Synthesis of C-5 and C-6-modified -GalCer analogues as iNKT-cell agonists.
Discovery of A-893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2.
Aryl Pyrazoles as Potent Inhibitors of Arginine Methyltransferases: Identification of the First PRMT6 Tool Compound.
Multivalent Amino Sugars to Recognize Different TAR RNA Conformations.
Structure activity relationship study of Mezzettiasides natural products and their four new disaccharide analogues for anticancer/antibacterial activity.
Trifluoromethoxyl substituted phenylethylene diamines as high affinity sigma receptor ligands with potent anti-cocaine actions.
Tetracycline analogues with a selective inhibitory effect on HIF-1
Synthesis and structural characterization of natural benzofuranoids.
Structure-Activity Relationship Studies of 3-epi-Deoxynegamycin Derivatives as Potent Readthrough Drug Candidates.
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.
Bioactivity of surface tethered Osteogenic Growth Peptide motifs
Treatment of Cancer with NAMPT Inhibitors.
Syntheses and Antibacterial Activity of N-Acylated Ciprofloxacin Derivatives Based on the Trimethyl Lock.
Novel 2,5-disubtituted-1,3,4-oxadiazoles with benzimidazole backbone: a new class of -glucuronidase inhibitors and in silico studies.
Synthesis and evaluation of a series of quinolinyl trans-cyanostilbene analogs as anticancer agents
Amino Acid Thioester Derivatives: A Highly Promising Scaffold for the Development of Metallo--lactamase L1 Inhibitors.
Synthesis, characterization and evaluation of the substituent effect on the amoebicide activity of new hydrazone derivatives
Potent and Selective Amidopyrazole Inhibitors of IRAK4 That Are Efficacious in a Rodent Model of Inflammation.
Synthesis and biological evaluation of novel bivalent -carbolines as potential antitumor agents
Pyridinonaphthyridinone Inhibitors of Type 2 Methionine Aminopeptidase.
Anti-dormant mycobacterial activity and target analysis of nybomycin produced by a marine-derived Streptomyces sp.
LAT Transport Inhibitors from Pittosporum venulosum Identified by NMR Fingerprint Analysis.
Synthesis and discovery of (I-3,II-3)-biacacetin as a novel non-zinc binding inhibitor of MMP-2 and MMP-9.
Flavonoids from Perovskia atriplicifolia and Their in Vitro Displacement of the Respective Radioligands for Human Opioid and Cannabinoid Receptors.
Inhibition of Cathepsin K: A Novel and Promising Treatment for Osteoporosis.
Synthesis and evaluation of artesunateindoloquinoline hybrids as antimalarial drug candidates
Effect of water solvation on the lipophilicity of isomeric pyrimidine-carboxamides.
Synthesis, enantiomeric separation and docking studies of spiropiperidine analogues as ligands of the nociceptin/orphanin FQ receptor
Investigation of novel ropinirole analogues: synthesis, pharmacological evaluation and computational analysis of dopamine D2 receptor functionalized congeners and homobivalent ligands
Cafestol-Type Diterpenoids from the Twigs of Tricalysia fruticosa with Potential Anti-inflammatory Activity.
-Heteroarylalkylcarbamates as inhibitors of fatty acid amide hydrolase (FAAH)
Thiazole-based aminopyrimidines and N-phenylpyrazolines as potent antimicrobial agents: synthesis and biological evaluation
MLN8054 and Alisertib (MLN8237): Discovery of Selective Oral Aurora A Inhibitors.
Synthesis and structure-activity relationships of novel anti-hepatitis C agents: N3,5'-cyclo-4-(beta-D-ribofuranosyl)-vic-triazolo[4,5-b]pyridin-5-one derivatives.
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities.
Multivalent antimicrobial peptides from a reactive polymer scaffold.
Structure-based design of spiro-oxindoles as potent, specific small-molecule inhibitors of the MDM2-p53 interaction.
Sabadinine: a potential non-peptide anti-severe acute-respiratory-syndrome agent identified using structure-aided design.
New class of corticotropin-releasing factor (CRF) antagonists: small peptides having high binding affinity for CRF receptor.
Design, synthesis, and activity of a series of pyrrolidine-3-carboxylic acid-based, highly specific, orally active ET(B) antagonists containing a diphenylmethylamine acetamide side chain.
Quantitative structure-activity relationship modeling of dopamine D(1) antagonists using comparative molecular field analysis, genetic algorithms-partial least-squares, and K nearest neighbor methods.
Synthesis and structure-activity relationship of alpha-sulfonylhydroxamic acids as novel, orally active matrix metalloproteinase inhibitors for the treatment of osteoarthritis.
Allosteric modulation of the adenosine A(1) receptor. Synthesis and biological evaluation of novel 2-amino-3-benzoylthiophenes as allosteric enhancers of agonist binding.
Drug rings database with web interface. A tool for identifying alternative chemical rings in lead discovery programs.
Pharmacophoric requirements for the cannabinoid side chain. Probing the cannabinoid receptor subsite at C1'.
Molecular docking studies of natural cholinesterase-inhibiting steroidal alkaloids from Sarcococca saligna.
Discovery of 1,6-naphthyridines as a novel class of potent and selective human cytomegalovirus inhibitors.
A novel acetylated analogue of dynorphin A-(1-11) amide as a kappa-opioid receptor antagonist.
Synthesis and in vitro evaluation of new 8-amino-1,4-benzoxazine derivatives as neuroprotective antioxidants.
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
Nonpeptide luteinizing hormone-releasing hormone antagonists derived from erythromycin A: design, synthesis, and biological activity of cladinose replacement analogues.
Certain compounds, compositions and methods
Pyridone and aza-pyridone compounds and methods of use
Pharmaceutically active compounds as Axl inhibitors
Oxadiazole inhibitors of leukotriene production
1,4-oxazepines as BACE1 and/or BACE2 inhibitors
Substituted cis- and trans-stilbenes as therapeutic agents
Apoptosis signal-regulating kinase 1 inhibitors
Aryl or N-heteroaryl substituted methanesulfonamide derivatives as vanilloid receptor ligands
Compounds having CRTH2 antagonist activity
Thiophene derivative as SGLT2 inhibitor and pharmaceutical composition comprising same
Compounds and methods useful for directing stem cell differentiation
Diphenylmethane derivatives as SGLT2 inhibitors
Dihydropyrimidin-2(1H)-one compounds as S-nitrosoglutathione reductase inhibitors
3H-imidazo [4, 5-C] pyridine-6-carboxamides as anti-inflammatory agents
2,7-substituted thieno[3,2-d] pyrimidine compounds as protein kinase inhibitors
Naphthyridine derivatives as inhibitors of hypoxia inducible factor (HIF) hydroxylase
Method of treating contrast-induced nephropathy
NMDA receptor antagonists for neuroprotection
Method for the treatment of neurological disorders by enhancing the activity of beta-glucocerebrosidase
Pyrrolopyrimidines as janus kinase inhibitors
[1,3,4] oxadiazole derivative and application thereof
Imidazolothiazole compounds and methods of use thereof
Furopyridinyl-substituted 1,4-dihydropyridine derivatives and methods of use thereof
Substituted isoquinolinones and quinazolinones
5-lipoxygenase-activating protein inhibitor
4-substituted-2-amino-pyrimidine derivatives
Substituted 2,3,5,9,9B-pentaazacyclopenta[a]naphthalenes and uses thereof
Compounds for the inhibition of integrins and use thereof
Benzoic acid derivative MDM2 inhibitor for the treatment of cancer
Compositions for preventing and/or treating degenerative disorders of the central nervous system
Substituted piperidinyl-pyridazinyl derivatives useful as SCD 1 inhibitors
Heteroaryloxyheterocyclyl compounds as PDE10 inhibitors
Pyrazolo[3,4-d]pyrimidine compounds and their use as PDE2 inhibitors and/or CYP3A4 inhibitors
Prolyl hydroxylase inhibitors and methods of use
Carboxy isatin hydrazones and their esters as Shp2 inhibitors
Use of PDE7 inhibitors for the treatment of movement disorders
Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
4-(pyridin-3-yl)-2(pyridin-2yl)-1,2-dihydro-3H-pyrazol-3-one derivatives as specific HIF-pyrolyl-4-hydroxylase inhibitors for treating cardiovascular and haematological diseases
Aryl, heteroaryl, and heterocycle substituted tetrahydroisoquinolines and use thereof
Kinase inhibitors and methods of use thereof
Triazolo and tetrazolo pyrimidine derivatives as HNE inhibitors for treating COPD
Substituted cycloalcano[e and d] pyrazolo [1,5-a]pyrimidines/antagonists of serotonin 5-HT6 receptors and methods for production and the use thereof
Nitrogen containing heteroaryl compounds
Compounds for the treatment of hepatitis C
Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as cFMS inhibitors
Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors
Non-amidic linkers with branched termini as CGRP receptor antagonists
Benzimidazole derivatives: preparation and pharmaceutical applications
Peptidomimetic sulfamide compounds and antiviral uses thereof
Tricyclic imidazole compounds as PDE10 inhibitors
Substituted piperidines as Par-1 antagonists
Monoacylglycerol lipase inhibitors for the treatment of metabolic diseases and related disorders
Methods for increasing the stabilization of hypoxia inducible factor-1 alpha
Macrocyclic indoles as hepatitis C virus inhibitors
Substituted 7-azabicyles and their use as orexin receptor modulators
Substituted oxazolidinones and their use
Pyrrolo[2,3-B]pyridine CDK9 kinase inhibitors
Pyridyl piperidine orexin receptor antagonists
Indolecarboxylic acid derivative having PGD2 receptor antagonistic activity
Pyrazolopyrimidines as metabotropic glutamate 5 receptor antagonists
Substituted pyrazolo[1,5-a]pyrimidine compounds as mTOR inhibitors
Dipeptidyl-peptidase-IV inhibitors for treatment of type 2 diabetes complex with hypertension
2,5-disubstituted piperidine orexin receptor antagonists
Piperazine compound having a PGDS inhibitory effect
Compounds and method for treatment of HIV
Bicyclic heterocycle compounds and their uses in therapy
N-[2-hydroxycarbamoyl-2-(piperazinyl) ethyl] benzamide compounds, their preparation and their use as TACE inhibitors
Indanyl-substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-C]pyridines, their use as medicament, and pharmaceutical preparations comprising them
Substituted piperidine spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof
Pyrimidine compounds as inhibitors of protein kinases IKK epsilon and/or TBK-1, processes for their preparation, and pharmaceutical compositions containing them
Amino-pyridine-containing spleen tyrosine kinase (SYK) inhibitors
Identification of a novel pyrazolo[3,4-d]pyrimidine able to inhibit cell proliferation of a human osteogenic sarcoma in vitro and in a xenograft model in mice.
First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.
Structure-based optimization of protein tyrosine phosphatase 1B inhibitors: from the active site to the second phosphotyrosine binding site.
Discovery of 4-amino and 4-hydroxy-1-aroylindoles as potent tubulin polymerization inhibitors.
Engineered apoptosis-inducing peptides with enhanced mitochondrial localization and potency.
Inhibition of the signal transducer and activator of transcription-3 (STAT3) signaling pathway by 4-oxo-1-phenyl-1,4-dihydroquinoline-3-carboxylic acid esters.
3-amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases.
The importance of micelle-bound states for the bioactivities of bifunctional peptide derivatives for delta/mu opioid receptor agonists and neurokinin 1 receptor antagonists.
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.
Putative bioactive conformations of amide linked cyclic myelin basic protein peptide analogues associated with experimental autoimmune encephalomyelitis.
Design and development of water-soluble curcumin conjugates as potential anticancer agents.
Influence of selective fluorination on the biological activity and proteolytic stability of glucagon-like peptide-1.
Improved angiostatic activity of dasatinib by modulation with hydrophobic chains.
Discovery of piperidin-4-yl-aminopyrimidine derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometries.
Synthesis, biological evaluation and modeling studies of terphenyl topoisomerase II inhibitors as anticancer agents.
Design, synthesis and antitumor activity of triterpenoid pyrazine derivatives from 23-hydroxybetulinic acid.
Structure-activity studies in the development of a hydrazone based inhibitor of adipose-triglyceride lipase (ATGL).
Positron emission tomography to elucidate pharmacokinetic differences of regioisomeric retinoid x receptor agonists.
Approved Drugs Containing Thiols as Inhibitors of Metallo--lactamases: Strategy To Combat Multidrug-Resistant Bacteria.
Discovery of imidazopyridine derivatives as highly potent respiratory syncytial virus fusion inhibitors.
Synthesis of New DPP-4 Inhibitors Based on a Novel Tricyclic Scaffold.
Biphenyl-ethyl-pyrrolidine derivatives as histamine h3 receptor modulators for the treatment of cognitive disorders.
-Carbonic Anhydrases Possess Thioesterase Activity.
Novel N-benzenesulfonyl sophocarpinol derivatives as coxsackie B virus inhibitors.
Activity of lipo-cyclic -AApeptides against biofilms of Staphylococcus epidermidis and Pseudomonas aeruginosa.
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.
Dual high-resolution -glucosidase and radical scavenging profiling combined with HPLC-HRMS-SPE-NMR for identification of minor and major constituents directly from the crude extract of Pueraria lobata.
Synthesis and Evaluation of Quinazolines as Inhibitors of the Bacterial Cell Division Protein FtsZ.
Lead optimization of spiropyrazolopyridones: a new and potent class of dengue virus inhibitors.
Selected hybrid natural products as tubulin modulators.
Discovery of potent hexapeptide agonists to human neuromedin u receptor 1 and identification of their serum metabolites.
Synthesis and biological evaluation of aminopolyamines.
The first potent inhibitors for human glutaminyl cyclase: synthesis and structure-activity relationship.
Parallel solution-phase and microwave-assisted synthesis of new S-DABO derivatives endowed with subnanomolar anti-HIV-1 activity.
Novel 4-oxo-1,4-dihydroquinoline-3-carboxamide derivatives as new CB2 cannabinoid receptors agonists: synthesis, pharmacological properties and molecular modeling.
Bisguanidine, bis(2-aminoimidazoline), and polyamine derivatives as potent and selective chemotherapeutic agents against Trypanosoma brucei rhodesiense. Synthesis and in vitro evaluation.
Benzoyl ring halogenated classical 2-amino-6-methyl-3,4-dihydro-4-oxo-5-substituted thiobenzoyl-7H-pyrrolo[2,3-d]pyrimidine antifolates as inhibitors of thymidylate synthase and as antitumor agents.
Identification of 4-(1H-imidazol-4(5)-ylmethyl)pyridine (immethridine) as a novel, potent, and highly selective histamine H(3) receptor agonist.
Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein.
Predicting the cell differentiation activity of 1 alpha,25-dihydroxyvitamin D3 side chain analogues from docking simulations.
A novel class of inhibitors of peptide deformylase discovered through high-throughput screening and virtual ligand screening.
A cyclopent-2-enecarbonyl group mimics proline at the P2 position of prolyl oligopeptidase inhibitors.
Anti-HIV activity of (-)-(2R,4R)-1- (2-hydroxymethyl-1,3-dioxolan-4-yl)-thymine against drug-resistant HIV-1 mutants and studies of its molecular mechanism.
Structure-activity study on a novel series of macrocyclic inhibitors of the hepatitis C virus NS3 protease leading to the discovery of BILN 2061.
Pyrazolo[3,4-d]pyrimidines endowed with antiproliferative activity on ductal infiltrating carcinoma cells.
Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays.
Design, synthesis, and biological evaluation of 1,2,3,7-tetrahydro-6h-purin-6-one and 3,7-dihydro-1h-purine-2,6-dione derivatives as corticotropin-releasing factor(1) receptor antagonists.
Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
Compositions and methods for inhibition of cathepsins
Derivatives of propargylamine having neuroprotective capacity for the treatment of Alzheimer's and Parkinson's diseases
Solid forms of gyrase inhibitor (R)-1-ethyl-3-[6-fluoro-5-[2-(1-hydroxy-1-methyl-ethyl)pryimidin-5-yl]-7-(tetrahydrofuran-2-yl)-1H-benzimidazol-2-yl]urea
Vanilloid receptor ligands, pharmaceutical compositions containing them, process for making them, and use thereof for treating pain and other conditions
Imidazo-oxazine compound or salt thereof
Pyrrolo[2,3-a] carbazoles and use thereof as PIM kinase inhibitors
Sulfone-substituted anilinopyrimidine derivatives as CDK inhibitors, the production thereof, and use as a medicine
Nitrogen containing morphinan derivatives and the use thereof
N1/N2-lactam acetyl-CoA carboxylase inhibitors
1-pyrazolyl-3-(4-((2-anilinopyrimidin-4-yl)oxy)napththalen-1-yl) ureas as p38 MAP kinase inhibitors
4-(azacycloalkyl)benzene-1,3-diol compounds as tyrosinase inhibitors, process for the preparation thereof and use thereof in human medicine and in cosmetics
Oxadiazole derivative having endothelial lipase inhibitory activity
Ethers, secondary amines and derivatives thereof as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto
Crystalline forms of a prolyl hydroxylase inhibitor
Multifunctional radical quenchers and their uses
6-substituted indole-3-carboxylic acid amide compounds having sphingosine-1-phosphate (S1P) receptor antagonist biological activity
5-fluoro-3-phenyl-2[1-(9H-purin-6-ylamino)propyl]-3H-quinazolin-4-one and 6-fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)ethyl]-3H-quinazolin-4-one as inhibitors of human phosphatidylinositol 3-kinase delta
Substituted aminotetrahydrothiopyrans and derivatives thereof as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
Pyrimidinecarboxamides as CXCR2 modulators
Bivalent diazo bicyclic Smac mimetics and the uses thereof
Inhibition of Shp2/PTPN11 protein tyrosine phosphatase by NSC-87877, NSC-117199 and their analogs
Reverse amide compounds as protein deacetylase inhibitors and methods of use thereof
Benzothiazoles having histamine H3 receptor activity
5-membered nitrogen containing heterocyclic derivatives and pharmaceutical compositions comprising the same
Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
Diazabenzo[de] anthracen-3-one compounds and methods for inhibiting PARP
17Œ±-hydroxylase/C17,20-lyase inhibitors
Fused heterocyclic derivatives and methods of use
Imidazole derivatives used as TAFIa inhibitors
Derivatives of N-acyl-N‚Ä=-phenylpiperazine useful (inter alia) for the prophylaxis or treatment of diabetes
Compounds for the treatment of neurodegenerative diseases
Tetrazole compounds for reducing uric acid
Oxadiazole fused heterocyclic derivatives useful for the treatment of multiple sclerosis
Oxadiazole beta carboline derivatives as antidiabetic compounds
Dibenzothiazepine derivatives and uses thereof‚Äî424
2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole and estrogen formulations
Naphthalene-based inhibitors of anti-apoptotic proteins
Pyrazolylaminopyridine derivatives useful as kinase inhibitors
Substituted fused imidazoles and pyrazoles and use thereof
3-substituted-2-(arlyalkyl)-1-azabicycloalkanes and methods of use thereof
HIV protease inhibitors and methods for using
Thienopyrimidine derivatives, processes for the preparation thereof and therapeutic uses thereof
Quinoline-carboxamide derivatives as P2Y12 antagonists
Thiazolidinedione derivative and use thereof
17-hydroxy-19-nor-21-carboxylic acid-steroid Œ=-lactone derivative, use thereof, and medicament containing the derivative
Heterocyclic compounds, processes for their preparation, medicaments comprising these compounds, and the use thereof
Spiropiperidine prolylcarboxypeptidase inhibitors
7-azoniabicyclo[2.2.1]heptane derivatives, methods of production, and pharmaceutical uses thereof
Pyrazolopyrimidine compounds as kinase inhibitors
Rosuvastatin and atorvastatin derivatives
Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
Modified macrophage migration inhibitory factor inhibitors
Substituted naphthyridines and their use as medicaments
Antimalarial agents that are inhibitors of dihydroorotate dehydrogenase
Substituted dihydropyrazolones and their use
Cyclohexyl-azetidinyl antagonists of CCR2
Azinone-substituted azabicycloalkane-indole and azabicycloalkane-pyrrolo-pyridine MCH-1 antagonists, methods of making, and use thereof
Fused bicyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
Methotrexate adjuvants to reduce toxicity and methods for using the same
Triazolopyridine compounds as PIM kinase inhibitors
O-GlcNAc transferase inhibitors and uses thereof
Meta-substituted phenyl sulfonyl amides of secondary amino acid amides, the production thereof, and use thereof as matriptase inhibitors
Fused tricyclic dual inhibitors of CDK 4/6 and FLT3
Substituted dihydropyrazolones and use thereof as HIF-prolyl-4-hydroxylase inhibitors
Design, synthesis, and structure-activity relationship studies of novel 2,4,6-trisubstituted-5-pyrimidinecarboxylic acids as peroxisome proliferator-activated receptor gamma (PPARgamma) partial agonists with comparable antidiabetic efficacy to rosiglitazone.
Investigations on the 4-quinolone-3-carboxylic acid motif. 1. Synthesis and structure-activity relationship of a class of human immunodeficiency virus type 1 integrase inhibitors.
The potential of transient receptor potential vanilloid type 1 channel modulators for the treatment of pain.
Second generation tetrahydroquinoline-based protein farnesyltransferase inhibitors as antimalarials.
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.
Synthesis and structure-activity relationships of dimeric peptide antagonists of the human immunoglobulin G-human neonatal Fc receptor (IgG-FcRn) interaction.
Enhancing the intestinal absorption of molecules containing the polar guanidino functionality: a double-targeted prodrug approach.
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
Discovery and optimization of p38 inhibitors via computer-assisted drug design.
Synthesis and biological evaluation of guanidino compounds endowed with subnanomolar affinity as competitive inhibitors of maize polyamine oxidase.
Design, synthesis, and melatoninergic activity of new azido- and isothiocyanato-substituted indoles.
Potential neuroprotective drugs in cerebral ischemia: new saturated and polyunsaturated lipids coupled to hydrophilic moieties: synthesis and biological activity.
Synthesis and biological evaluation of a novel series of "ortho-nitrated" inhibitors of catechol-O-methyltransferase.
PABA/NO as an anticancer lead: analogue synthesis, structure revision, solution chemistry, reactivity toward glutathione, and in vitro activity.
Dopamine/serotonin receptor ligands. 10: SAR Studies on azecine-type dopamine receptor ligands by functional screening at human cloned D1, D2L, and D5 receptors with a microplate reader based calcium assay lead to a novel potent D1/D5 selective antagonist.
Potent and selective mitogen-activated protein kinase kinase (MEK) 1,2 inhibitors. 1. 4-(4-bromo-2-fluorophenylamino)-1- methylpyridin-2(1H)-ones.
Synthesis and characterization of a platinum(II) complex tethered to a ligand of the peripheral benzodiazepine receptor.
Overlapping, nonidentical binding sites of different classes of nonpeptide antagonists for the human gonadotropin-releasing hormone receptor.
Cyclopropylamino acid amide as a pharmacophoric replacement for 2,3-diaminopyridine. Application to the design of novel bradykinin B1 receptor antagonists.
Synthesis, biological evaluation, and molecular modeling investigation of new chiral fibrates with PPARalpha and PPARgamma agonist activity.
Synthesis and biological evaluation of 11-substituted 6-aminobenzo[c]phenanthridine derivatives, a new class of antitumor agents.
Heterocyclic and phenyl double-bond-locked combretastatin analogues possessing potent apoptosis-inducing activity in HL60 and in MDR cell lines.
Modifications to the tetracaine scaffold produce cyclic nucleotide-gated channel blockers with widely varying efficacies.
Metabolism and quantification of [(18)F]DPA-714, a new TSPO positron emission tomography radioligand.
Pharmacogenomics of gemcitabine metabolism: functional analysis of genetic variants in cytidine deaminase and deoxycytidine kinase.
Identification of the cytochrome P450 and other enzymes involved in the in vitro oxidative metabolism of a novel antidepressant, Lu AA21004.
Microdialysis evaluation of clozapine and N-desmethylclozapine pharmacokinetics in rat brain.
Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods.
Effect of structural variation on aldehyde oxidase-catalyzed oxidation of zoniporide.
Brain distribution and bioavailability of elacridar after different routes of administration in the mouse.
A comprehensive assessment of repaglinide metabolic pathways: impact of choice of in vitro system and relative enzyme contribution to in vitro clearance.
Chronic doxorubicin cardiotoxicity modulates cardiac cytochrome P450-mediated arachidonic acid metabolism in rats.
Pharmacokinetics of oral D-serine in D-amino acid oxidase knockout mice.
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
Metabolism-dependent inhibition of CYP3A4 by lapatinib: evidence for formation of a metabolic intermediate complex with a nitroso/oxime metabolite formed via a nitrone intermediate.
Induction of hepatic multidrug resistance-associated protein 3 by ethynylestradiol is independent of cholestasis and mediated by estrogen receptor.
Species difference in the mechanism of nonlinear pharmacokinetics of E2074, a novel sodium channel inhibitor, in rats, dogs, and monkeys.
Utility of drug depletion-time profiles in isolated hepatocytes for accessing hepatic uptake clearance: identifying rate-limiting steps and role of passive processes.
Potent inhibition of human sulfotransferase 1A1 by 17-ethinylestradiol: role of 3'-phosphoadenosine 5'-phosphosulfate binding and structural rearrangements in regulating inhibition and activity.
Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes.
Significance of reductive metabolism in human intestine and quantitative prediction of intestinal first-pass metabolism by cytosolic reductive enzymes.
Cytochrome P450 3A-mediated microsomal biotransformation of 1,25-dihydroxyvitamin D3 in mouse and human liver: drug-related induction and inhibition of catabolism.
In vitro studies on the oxidative metabolism of 20(s)-ginsenoside Rh2 in human, monkey, dog, rat, and mouse liver microsomes, and human liver s9.
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
Comparison of metabolism of sesamin and episesamin by drug-metabolizing enzymes in human liver.
Metabolism and pharmacokinetics of mangiferin in conventional rats, pseudo-germ-free rats, and streptozotocin-induced diabetic rats.
Characterization of human cytochrome P450s involved in the bioactivation of clozapine.
Inhibition of P-glycoprotein leads to improved oral bioavailability of compound K, an anticancer metabolite of red ginseng extract produced by gut microflora.
Metabolic chiral inversion of brivanib and its relevance to safety and pharmacology.
Potential role of UGT1A4 promoter SNPs in anastrozole pharmacogenomics.
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.
Autoinhibition of CYP3A4 leads to important role of CYP2C8 in imatinib metabolism: variability in CYP2C8 activity may alter plasma concentrations and response.
Evaluation of hepatic disposition of paroxetine using sandwich-cultured rat and human hepatocytes.
Characterization of efflux transporters involved in distribution and disposition of apixaban.
Novel bioactivation mechanism of reactive metabolite formation from phenyl methyl-isoxazoles.
Disposition and metabolism of LY2452473, a selective androgen receptor modulator, in humans.
Compartmental and enzyme kinetic modeling to elucidate the biotransformation pathway of a centrally acting antitrypanosomal prodrug.
Quantitative prediction of human intestinal glucuronidation effects on intestinal availability of UDP-glucuronosyltransferase substrates using in vitro data.
Acetylenic linkers in lead compounds: a study of the stability of the propargyl-linked antifolates.
Preferred binding orientations of phenacetin in CYP1A1 and CYP1A2 are associated with isoform-selective metabolism.
Compartmentalization and antiviral effect of efavirenz metabolites in blood plasma, seminal plasma, and cerebrospinal fluid.
Metabolism and pharmacokinetics of indacaterol in humans.
Evidence for substrate-dependent inhibition profiles for human liver aldehyde oxidase.
Regiospecificity and stereospecificity of human UDP-glucuronosyltransferases in the glucuronidation of estriol, 16-epiestriol, 17-epiestriol, and 13-epiestradiol.
Nicotinamide N-oxidation by CYP2E1 in human liver microsomes.
Assessment of exposure of metabolites in preclinical species and humans at steady state from the single-dose radiolabeled absorption, distribution, metabolism, and excretion studies: a case study.
Delayed elimination of SN-38 in cancer patients with severe renal failure.
Organic anion transporter 3 interacts selectively with lipophilic -lactam antibiotics.
Metabolic transformation of antitumor acridinone C-1305 but not C-1311 via selective cellular expression of UGT1A10 increases cytotoxic response: implications for clinical use.
Identification of multiple binding sites for substrate transport in bovine organic anion transporting polypeptide 1a2.
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
Metabolism of saikosaponin a in rats: diverse oxidations on the aglycone moiety in liver and intestine in addition to hydrolysis of glycosidic bonds.
In vivo biliary clearance should be predicted by intrinsic biliary clearance in sandwich-cultured hepatocytes.
Tissue distribution and identification of radioactivity components at elimination phase after oral administration of [14C]CS-1036, an -amylase inhibitor, to rats.
Interaction of silymarin flavonolignans with organic anion-transporting polypeptides.
Metabolite profiling of bendamustine in urine of cancer patients after administration of [14C]bendamustine.
The inactivation of human CYP2E1 by phenethyl isothiocyanate, a naturally occurring chemopreventive agent, and its oxidative bioactivation.
Breast cancer resistance protein (ABCG2) determines distribution of genistein phase II metabolites: reevaluation of the roles of ABCG2 in the disposition of genistein.
Pharmacokinetics, biotransformation, and mass balance of edoxaban, a selective, direct factor Xa inhibitor, in humans.
Metabolic activation of mefenamic acid leading to mefenamyl-S-acyl-glutathione adduct formation in vitro and in vivo in rat.
Metabolism of (2S)-pterosin A: identification of the phase I and phase II metabolites in rat urine.
Metabolism of the c-Fos/activator protein-1 inhibitor T-5224 by multiple human UDP-glucuronosyltransferase isoforms.
Interaction of lapatinib with cytochrome P450 3A5.
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity.
Significance of peptide transporter 1 in the intestinal permeability of valacyclovir in wild-type and PepT1 knockout mice.
NADPH-cytochrome P450 oxidoreductase: roles in physiology, pharmacology, and toxicology.
Function of the blood-brain barrier and restriction of drug delivery to invasive glioma cells: findings in an orthotopic rat xenograft model of glioma.
Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects.
Brain efflux index to investigate the influence of active efflux on brain distribution of pemetrexed and methotrexate.
Disposition and metabolism of GSK2251052 in humans: a novel boron-containing antibiotic.
Mechanistic studies on the absorption and disposition of scutellarin in humans: selective OATP2B1-mediated hepatic uptake is a likely key determinant for its unique pharmacokinetic characteristics.
In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitor.
Role of the intestinal peptide transporter PEPT1 in oseltamivir absorption: in vitro and in vivo studies.
Evaluation of the relationship between sex, polymorphisms in CYP2C8 and CYP2C9, and pharmacokinetics of angiotensin receptor blockers.
The role of a basolateral transporter in rosuvastatin transport and its interplay with apical breast cancer resistance protein in polarized cell monolayer systems.
Antineoplastic agents. 599. Total synthesis of dolastatin 16.
Modification of amphipathic non-opioid dynorphin A analogues for rat brain bradykinin receptors.
Synthesis and Biological Activities of 5-Thio--GalCers.
Fibroblast Growth Factor Receptor 3 (FGF-R3): A Promising Therapeutic Target for the Treatment of Bladder Cancer.
Dactylomelane diterpenes from the sea hare Aplysia depilans.
Indole based peptidomimetics as anti-inflammatory and anti-hyperalgesic agents: Dual inhibition of 5-LOX and COX-2 enzymes.
Azolylthioacetamide: A Highly Promising Scaffold for the Development of Metallo--lactamase Inhibitors.
Rational Design of a Novel AMPA Receptor Modulator through a Hybridization Approach.
Decaprenylphosphoryl--d-ribose 2'-Epimerase 1 (DprE1): A Novel Therapeutic Target for the Treatment of Tuberculosis.
Pyridopyrimidinone Derivatives as Potent and Selective c-Jun N-Terminal Kinase (JNK) Inhibitors.
Discovery of a Potent and Orally Bioavailable Dual Antagonist of CC Chemokine Receptors 2 and 5.
Discovery of a Dual PRMT5-PRMT7 Inhibitor.
Design and synthesis of novel arctigenin analogues for the amelioration of metabolic disorders.
Rho kinase inhibitors: potentially versatile therapy for the treatment of cardiovascular diseases and more.
N (1)-Fluoroalkyltryptophan Analogues: Synthesis and in vitro Study as Potential Substrates for Indoleamine 2,3-Dioxygenase.
Tankyrase 1 Inhibitors with Drug-like Properties Identified by Screening a DNA-Encoded Chemical Library.
Synthesis and Evaluation of Conjugates of Novel TLR7 Inert Ligands as Self-Adjuvanting Immunopotentiators.
Discovery of benzimidazole oxazolidinediones as novel and selective nonsteroidal mineralocorticoid receptor antagonists.
Phenolic diterpenoid derivatives as anti-influenza a virus agents.
Exploiting the Polypharmacology of -Carbolines to Disrupt O. volvulus Molting.
Discovery of a Selective TRPM8 Antagonist with Clinical Efficacy in Cold-Related Pain.
First Crystal Structures of Mycobacterium tuberculosis 6-Oxopurine Phosphoribosyltransferase: Complexes with GMP and Pyrophosphate and with Acyclic Nucleoside Phosphonates Whose Prodrugs Have Antituberculosis Activity.
Design and Synthesis of Acetylenyl Benzamide Derivatives as Novel Glucokinase Activators for the Treatment of T2DM.
N-Aryl azacycles as novel sodium channel blockers.
Helical Antimicrobial Sulfono--AApeptides.
Neopetrocyclamines A and B, polycyclic diamine alkaloids from the sponge Neopetrosia cf exigua.
Melanin-concentrating hormone receptor 1 antagonists for treatment of obesity.
Discovery of Novel Multiacting Topoisomerase I/II and Histone Deacetylase Inhibitors.
Switch in Site of Inhibition: A Strategy for Structure-Based Discovery of Human Topoisomerase II Catalytic Inhibitors.
Membrane-Targeting DCAP Analogues with Broad-Spectrum Antibiotic Activity against Pathogenic Bacteria.
Novel benzamide-based histamine h3 receptor antagonists: the identification of two candidates for clinical development.
Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors.
Peptidic inhibitors for in vitro pentamer formation of human papillomavirus capsid protein l1.
Structural requirements for bisphosphonate binding on hydroxyapatite: NMR study of bisphosphonate partial esters.
Discovery of a Cyclic Boronic Acid -Lactamase Inhibitor (RPX7009) with Utility vs Class A Serine Carbapenemases.
Discovery of a Novel Series of Thienopyrimidine as Highly Potent and Selective PI3K Inhibitors.
Design, synthesis and biological characterization of selective LIMK inhibitors.
Structure-activity relationships in 1,4-benzodioxan-related compounds. 9. From 1,4-benzodioxane to 1,4-dioxane ring as a promising template of novel alpha1D-adrenoreceptor antagonists, 5-HT1A full agonists, and cytotoxic agents.
Synthesis and SAR of novel 4-morpholinopyrrolopyrimidine derivatives as potent phosphatidylinositol 3-kinase inhibitors.
Design, synthesis, and biological evaluation of 16-substituted 4-azasteroids as tissue-selective androgen receptor modulators (SARMs).
Design, synthesis, and pharmacological effects of a cyclization-activated steroid prodrug for colon targeting in inflammatory bowel disease.
18F stilbenes and styrylpyridines for PET imaging of A beta plaques in Alzheimer's disease: a miniperspective.
A class of 3S-2-aminoacyltetrahydro-beta-carboline-3-carboxylic acids: their facile synthesis, inhibition for platelet activation, and high in vivo anti-thrombotic potency.
Optimizing cell permeation of an antibiotic resistance inhibitor for improved efficacy.
Design and synthesis of novel diaminoquinazolines with in vivo efficacy for beta-catenin/T-cell transcriptional factor 4 pathway inhibition.
Fluorescently labeled analogues of dofetilide as high-affinity fluorescence polarization ligands for the human ether-a-go-go-related gene (hERG) channel.
Design, synthesis, and biological evaluation of (2R,alphaS)-3,4-dihydro-2-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]-5-[3-(trifluoromethoxy)-phenyl]-alpha-(trifluoromethyl)-1(2H)-quinolineethanol as potent and orally active cholesteryl ester transfer protein inhibitor.
Coordination chemistry based approach to lipophilic inhibitors of 1-deoxy-D-xylulose-5-phosphate reductoisomerase.
Antimalarial activity of novel 1,2,5,6-tetraoxacycloalkanes and 1,2,5-trioxacycloalkanes.
Synthesis and structure-activity relationships of a new model of arylpiperazines. 8. Computational simulation of ligand-receptor interaction of 5-HT(1A)R agonists with selectivity over alpha1-adrenoceptors.
Discovery of a fluoroindolo[2,3-a]carbazole clinical candidate with broad spectrum antitumor activity in preclinical tumor models superior to the marketed oncology drug, CPT-11.
Design and synthesis of N-[(4-methoxyphenoxy)carbonyl]-N-[[4-[2-(5- methyl-2-phenyl-4-oxazolyl)ethoxy]phenyl]methyl]glycine [Muraglitazar/BMS-298585], a novel peroxisome proliferator-activated receptor alpha/gamma dual agonist with efficacious glucose and lipid-lowering activities.
High-affinity epidermal growth factor receptor (EGFR) irreversible inhibitors with diminished chemical reactivities as positron emission tomography (PET)-imaging agent candidates of EGFR overexpressing tumors.
Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA.
Biaryl ureas as potent and orally efficacious melanin concentrating hormone receptor 1 antagonists for the treatment of obesity.
Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations.
New pyrrolo[2,1-f]purine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives as potent and selective human A3 adenosine receptor antagonists.
From 1-acyl-beta-lactam human cytomegalovirus protease inhibitors to 1-benzyloxycarbonylazetidines with improved antiviral activity. A straightforward approach to convert covalent to noncovalent inhibitors.
From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Major effect of pyrrolic N-benzylation in norbinaltorphimine, the selective kappa-opioid receptor antagonist.
Fancy bioisosteres: metallocene-derived G-protein-coupled receptor ligands with subnanomolar binding affinity and novel selectivity profiles.
1,3,4-thiadiazole derivatives. Synthesis, structure elucidation, and structure-antituberculosis activity relationship investigation.
Mechanism-based inactivation of cytochrome P450 2B6 by methadone through destruction of prosthetic heme.
The role of aldehyde oxidase and xanthine oxidase in the biotransformation of a novel negative allosteric modulator of metabotropic glutamate receptor subtype 5.
Characterization of SAGE Mdr1a (P-gp), Bcrp, and Mrp2 knockout rats using loperamide, paclitaxel, sulfasalazine, and carboxydichlorofluorescein pharmacokinetics.
Elucidation of the metabolic pathways and the resulting multiple metabolites of almorexant, a dual orexin receptor antagonist, in humans.
Biocatalytic synthesis and structure elucidation of cyclized metabolites of the deacetylase inhibitor panobinostat (LBH589).
Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.
Species-dependent uptake of glycylsarcosine but not oseltamivir in Pichia pastoris expressing the rat, mouse, and human intestinal peptide transporter PEPT1.
Investigating the enteroenteric recirculation of apixaban, a factor Xa inhibitor: administration of activated charcoal to bile duct-cannulated rats and dogs receiving an intravenous dose and use of drug transporter knockout rats.
Reversible inhibition of human carboxylesterases by acyl glucuronides.
Impact of hydrolysis-mediated clearance on the pharmacokinetics of novel anaplastic lymphoma kinase inhibitors.
Role of human UDP-glucuronosyltransferases in the biotransformation of the triazoloacridinone and imidazoacridinone antitumor agents C-1305 and C-1311: highly selective substrates for UGT1A10.
Metabolism and pharmacokinetics of JM6 in mice: JM6 is not a prodrug for Ro-61-8048.
Sequential metabolism of AMG 487, a novel CXCR3 antagonist, results in formation of quinone reactive metabolites that covalently modify CYP3A4 Cys239 and cause time-dependent inhibition of the enzyme.
Metabolism of bis(4-fluorobenzyl)trisulfide and its formation of hemoglobin adduct in rat erythrocytes.
Predicting phenolic acid absorption in Caco-2 cells: a theoretical permeability model and mechanistic study.
Hydralazine as a selective probe inactivator of aldehyde oxidase in human hepatocytes: estimation of the contribution of aldehyde oxidase to metabolic clearance.
Metabolism of the active metabolite of quetiapine, N-desalkylquetiapine in vitro.
Glutaredoxin is involved in the formation of the pharmacologically active metabolite of clopidogrel from its GSH conjugate.
Identification of metabolites of ganoderic acid D by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry.
Selective mechanism-based inactivation of CYP3A4 by CYP3cide (PF-04981517) and its utility as an in vitro tool for delineating the relative roles of CYP3A4 versus CYP3A5 in the metabolism of drugs.
Pharmacokinetic mechanism involved in the prolonged high retention of laninamivir in mouse respiratory tissues after intranasal administration of its prodrug laninamivir octanoate.
Pharmacokinetics, metabolism, and excretion of the glycogen synthase kinase-3 inhibitor LY2090314 in rats, dogs, and humans: a case study in rapid clearance by extensive metabolism with low circulating metabolite exposure.
Oxidative ipso substitution of 2,4-difluoro-benzylphthalazines: identification of a rare stable quinone methide and subsequent GSH conjugate.
Methadone N-demethylation by the common CYP2B6 allelic variant CYP2B6.6.
Characterization of the in vitro and in vivo metabolism and disposition and cytochrome P450 inhibition/induction profile of saxagliptin in human.
Species differences in biliary clearance and possible relevance of hepatic uptake and efflux transporters involvement.
Metabolism of triethylenetetramine and 1,12-diamino-3,6,9-triazadodecane by the spermidine/spermine-N(1)-acetyltransferase and thialysine acetyltransferase.
Discovery and characterization of novel, potent, and selective cytochrome P450 2J2 inhibitors.
Biotransformation of two -secretase inhibitors including ring opening and contraction of a pyrimidine ring.
Cytochrome P450-mediated oxidative metabolism of abused synthetic cannabinoids found in K2/Spice: identification of novel cannabinoid receptor ligands.
Cytochrome P450 regulation by -tocopherol in Pxr-null and PXR-humanized mice.
In vivo-formed versus preformed metabolite kinetics of trans-resveratrol-3-sulfate and trans-resveratrol-3-glucuronide.
Preclinical evaluation of the metabolism and disposition of RRx-001, a novel investigative anticancer agent.
In vitro hepatotoxicity and cytochrome P450 induction and inhibition characteristics of carnosic acid, a dietary supplement with antiadipogenic properties.
Evaluation of inhibition selectivity for human cytochrome P450 2A enzymes.
Pharmacokinetics, bioavailability, tissue distribution, excretion, and metabolite identification of methoxyflavones in Kaempferia parviflora extract in rats.
Hepatobiliary disposition of 17-OHPC and taurocholate in fetal human hepatocytes: a comparison with adult human hepatocytes.
Optimized experimental design for the estimation of enzyme kinetic parameters: an experimental evaluation.
P-glycoprotein increases portal bioavailability of loperamide in mouse by reducing first-pass intestinal metabolism.
Amide hydrolysis of a novel chemical series of microsomal prostaglandin E synthase-1 inhibitors induces kidney toxicity in the rat.
Absorption, elimination, and metabolism of CS-1036, a novel -amylase inhibitor in rats and monkeys, and the relationship between gastrointestinal distribution and suppression of glucose absorption.
Covalent modification and time-dependent inhibition of human CYP2E1 by the meta-isomer of acetaminophen.
An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations.
Involvement of organic anion-transporting polypeptides in the hepatic uptake of dioscin in rats and humans.
Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone.
Excretion and metabolism of milnacipran in humans after oral administration of milnacipran hydrochloride.
Clinical pharmacokinetics, metabolism, and drug-drug interaction of carfilzomib.
Characterization of human liver enzymes involved in the biotransformation of boceprevir, a hepatitis C virus protease inhibitor.
Pulmonary metabolism of resveratrol: in vitro and in vivo evidence.
Metabolism, excretion, and pharmacokinetics of ((3,3-difluoropyrrolidin-1-yl)((2S,4S)-4-(4-(pyrimidin-2-yl)piperazin-1-yl)pyrrolidin-2-yl)methanone, a dipeptidyl peptidase inhibitor, in rat, dog and human.
Reversible disulfide formation of the glutamate carboxypeptidase II inhibitor E2072 results in prolonged systemic exposures in vivo.
Bioactivation of the cancer chemopreventive agent tamoxifen to quinone methides by cytochrome P4502B6 and identification of the modified residue on the apoprotein.
Unique metabolic pathway of [(14)C]lenvatinib after oral administration to male cynomolgus monkey.
Orally active ghrelin receptor inverse agonists and their actions on a rat obesity model.
Structure-Based Design of Macrocyclic Coagulation Factor VIIa Inhibitors.
Design and discovery of 2-(4-(1H-tetrazol-5-yl)-1H-pyrazol-1-yl)-4-(4-phenyl)thiazole derivatives as cardiotonic agents via inhibition of PDE3.
Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity.
Novel inhibitors targeting PPM1D phosphatase potently suppress cancer cell proliferation.
Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
Discovery of a Potent and Selective ROMK Inhibitor with Pharmacokinetic Properties Suitable for Preclinical Evaluation.
Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors.
Identification of amino acid appended acridines as potential leads to anti-cancer drugs.
Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
Synthesis of novel compounds containing morpholine and 5(4H)-oxazolone rings as potent tyrosinase inhibitors.
Synthesis of a novel series of 2,3,4-trisubstituted oxazolidines designed by isosteric replacement or rigidification of the structure and cytotoxic evaluation
Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents.
Design, synthesis, and biological evaluation of aminopyrazine derivatives as inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2).
Muscarinic acetylcholine receptor binding affinities of pethidine analogs.
Synthesis of potent urease inhibitors based on disulfide scaffold and their molecular docking studies.
Mixed up minor groove binders: Convincing AT specific compounds to recognize a GC base pair.
2-Arylquinazolin-4(3H)-ones: A new class of -glucosidase inhibitors.
Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.
Ligand-Orientation Based Fragment Selection in STD NMR Screening.
(1-(4-(Naphthalen-2-yl)pyrimidin-2-yl)piperidin-4-yl)methanamine: a wingless beta-catenin agonist that increases bone formation rate.
Dihydropyrrole[2,3-d]pyridine derivatives as novel corticotropin-releasing factor-1 antagonists: mapping of the receptor binding pocket by in silico docking studies.
Synthesis and biological characterization of B-ring amino analogues of potent benzothiadiazine hepatitis C virus polymerase inhibitors.
Structure-based design of a macrocyclic inhibitor for peptide deformylase.
2-Oxotetrahydroquinoline-based antimalarials with high potency and metabolic stability.
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
2-Thiazolylimino/heteroarylimino-5-arylidene-4-thiazolidinones as new agents with SHP-2 inhibitory action.
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
Determination of the microscopic equilibrium dissociation constants for risedronate and its analogues reveals two distinct roles for the nitrogen atom in nitrogen-containing bisphosphonate drugs.
In vitro analysis of stable, receptor-selective neurotensin[8-13] analogues.
Photodynamic molecular beacon triggered by fibroblast activation protein on cancer-associated fibroblasts for diagnosis and treatment of epithelial cancers.
Inhibitors of Src homology-2 domain containing protein tyrosine phosphatase-2 (Shp2) based on oxindole scaffolds.
Prediction of Thorough QT study results using action potential simulations based on ion channel screens.
Simulation of multiple ion channel block provides improved early prediction of compounds' clinical torsadogenic risk.
Discovery of the first potent, selective 5-hydroxytryptamine1D receptor antagonist.
CoMFA and CoMSIA analyses of Pneumocystis carinii dihydrofolate reductase, Toxoplasma gondii dihydrofolate reductase, and rat liver dihydrofolate reductase.
Discovery of a new series of centrally active tricyclic isoxazoles combining serotonin (5-HT) reuptake inhibition with alpha2-adrenoceptor blocking activity.
Dicarboxylic acid azacycle l-prolyl-pyrrolidine amides as prolyl oligopeptidase inhibitors and three-dimensional quantitative structure-activity relationship of the enzyme-inhibitor interactions.
Discovery of bicycloalkyl urea melanin concentrating hormone receptor antagonists: orally efficacious antiobesity therapeutics.
Synthesis of new quinoxaline-2-carboxylate 1,4-dioxide derivatives as anti-Mycobacterium tuberculosis agents.
Novel alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration.
A positron emission tomography radioligand for the in vivo labeling of metabotropic glutamate 1 receptor: (3-ethyl-2-[11C]methyl-6-quinolinyl)(cis- 4-methoxycyclohexyl)methanone.
Amino acid ester prodrugs of the antiviral agent 2-bromo-5,6-dichloro-1-(beta-D-ribofuranosyl)benzimidazole as potential substrates of hPEPT1 transporter.
Structure-based drug discovery using GPCR homology modeling: successful virtual screening for antagonists of the alpha1A adrenergic receptor.
[Nalpha-benzylTyr1,cyclo(D-Asp5,Dap8)]- dynorphin A-(1-11)NH2 cyclized in the "address" domain is a novel kappa-opioid receptor antagonist.
Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.
Phytochemical Investigation of the Constituents Derived from the Australian Plant Macropidia fuliginosa.
Polycyclic Polyprenylated Xanthones from Symphonia globulifera: Isolation and Biomimetic Electrosynthesis.
Kadcoccinic Acids A-J, Triterpene Acids from Kadsura coccinea.
Discovery of 3,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridin-2(1H)-one derivatives as novel JAK inhibitors.
Imidazole clubbed 1,3,4-oxadiazole derivatives as potential antifungal agents.
Isolation of a Cyclic Depsipetide, Aspergillicin F, and Synthesis of Aspergillicins with Innate Immune-Modulating Activity.
Discovery of small molecules with vasodilating characteristics and adjustable hydrolytic behavior.
Selenorhodamine photosensitizers with the Texas-red core for photodynamic therapy of cancer cells.
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.
Discovery of novel, potent, selective and cellular active ADC type PTP1B inhibitors via fragment-docking-oriented de novel design.
Design, synthesis and preliminary bioactivity evaluations of substituted quinoline hydroxamic acid derivatives as novel histone deacetylase (HDAC) inhibitors.
Cytotoxic triterpene saponins from Cercodemas anceps.
Structure activity relationship study of burkholdine analogues toward simple antifungal agents.
Discovery of potent 1L-adrenoceptor agonists: Design and synthesis of bicyclic derivatives.
Ionic derivatives of betulinic acid exhibit antiviral activity against herpes simplex virus type-2 (HSV-2), but not HIV-1 reverse transcriptase.
Peptide HIV fusion inhibitors: modifications and conjugations
Modification of cellular DNA by synthetic aziridinomitosenes.
Discovery of wrightiadione as a novel template for the TrkA kinase inhibitors.
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
Scaffold-Hopping and Structure-Based Discovery of Potent, Selective, And Brain Penetrant N-(1H-Pyrazol-3-yl)pyridin-2-amine Inhibitors of Dual Leucine Zipper Kinase (DLK, MAP3K12).
Design, synthesis and biological evaluation of 3-aryl-rhodanine benzoic acids as anti-apoptotic protein Bcl-2 inhibitors.
Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents
Discovery and optimisation studies of antimalarial phenotypic hits.
Bastadins, brominated-tyrosine derivatives, suppress accumulation of cholesterol ester in macrophages.
Design, synthesis and biological evaluation of imidazopyridine/imidazopyrimidine-benzimidazole conjugates as potential anticancer agents
Design, synthesis and anticancer mechanistic studies of linked azoles
Novel 2-Carbonylbenzo[b]thiophene 1,1-Dioxide Derivatives as Potent Inhibitors of STAT3 Signaling Pathway.
Insights into Structure-Activity Relationships of Bacterial RNA Polymerase Inhibiting Corallopyronin Derivatives.
Developing structure-activity relationships from an HTS hit for inhibition of the Cks1-Skp2 protein-protein interaction.
Synthesis and biological evaluation of pentanedioic acid derivatives as farnesyltransferase inhibitors
Oxopyrido[2,3-d]pyrimidines as Covalent L858R/T790M Mutant Selective Epidermal Growth Factor Receptor (EGFR) Inhibitors.
Synthesis of donepezil-based multifunctional agents for the treatment of Alzheimer's disease.
Radiolabelling and positron emission tomography of PT70, a time-dependent inhibitor of InhA, the Mycobacterium tuberculosis enoyl-ACP reductase.
A study of ad-proline peptidomimetic inhibitor of melanoma and endothelial cell invasion through activity towards MMP-2 and MMP-9
Evaluation of Improved Glycogen Synthase Kinase-3 Inhibitors in Models of Acute Myeloid Leukemia.
3-(2,6-Dichloro-benzyloxy)-11-oxo-olean-12-ene-29-oic acid, a semisynthetic derivative of glycyrrhetic acid: synthesis, antiproliferative, apoptotic and anti-angiogenesis activity
Decorated 6,6,7,7-tetrahydro-1H,1H-2,3-biindole scaffold as promising candidate for recognition of the CDK2 allosteric site
Beyond the affinity for protein kinase C: exploring 2-phenyl-3-hydroxypropyl pivalate analogues as C1 domain-targeting ligands
O-Benzoyl pyridine aldoxime and amidoxime derivatives: novel efficient DNA photo-cleavage agents
Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.
Novel Fluorinated 8-Hydroxyquinoline Based Metal Ionophores for Exploring the Metal Hypothesis of Alzheimer's Disease.
Identification of Bidentate Salicylic Acid Inhibitors of PTP1B.
Synthesis and antiviral activity of the carbocyclic analogue of the highly potent and selective anti-VZV bicyclo furano pyrimidines.
HCV NS5b RNA-dependent RNA polymerase inhibitors: from alpha,gamma-diketoacids to 4,5-dihydroxypyrimidine- or 3-methyl-5-hydroxypyrimidinonecarboxylic acids. Design and synthesis.
Benzothiophene selective estrogen receptor modulators with modulated oxidative activity and receptor affinity.
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists.
Smallest peptoids with antiproliferative activity on human neoplastic cells.
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Rational design and synthesis of an orally active indolopyridone as a novel conformationally constrained cannabinoid ligand possessing antiinflammatory properties.
Design and synthesis of novel N-acetylgalactosamine-terminated glycolipids for targeting of lipoproteins to the hepatic asialoglycoprotein receptor.
N-substituted 3-acetyltetramic acid derivatives as antibacterial agents.
Second-generation lymphocyte function-associated antigen-1 inhibitors: 1H-imidazo[1,2-alpha]imidazol-2-one derivatives.
Entry into a new class of potent proteasome inhibitors having high antiproliferative activity by structure-based design.
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method.
N-benzylnaltrindoles as long-acting delta-opioid receptor antagonists.
Synthesis and in vitro evaluation of 4-substituted N-(1,1-dimethylethyl)-3-oxo-4-androstene-17 beta-carboxamides as 5 alpha-reductase inhibitors and antiandrogens.
Synthesis and serotonergic activity of arylpiperazide derivatives of serotonin: potent agonists for 5-HT1D receptors.
Effects of log P and phenyl ring conformation on the binding of 5-phenylhydantoins to the voltage-dependent sodium channel.
New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent.
Phosphinic acid analogues of GABA. 1. New potent and selective GABAB agonists.
Tricyclic heteroaromatic systems. Synthesis and A1 and A2a adenosine binding activities of some 1-aryl-1,4-dihydro-3-methyl[1]benzopyrano[2,3-c] pyrazol-4-ones, 1-aryl-4,9-dihydro-3-methyl-1H-pyrazolo[3,4-b]quinolin-4- ones, and 1-aryl-1H-imidazo[4,5-b]quinoxalines.
Synthesis and structure-activity relationships of side-chain-substituted analogs of the allylamine antimycotic terbinafine lacking the central amino function.
Novel NMDA antagonists: replacement of the pyridinium ring of 6,11-ethanobenzo[b]quinolizinium cations with heteroisoquinolinium cations.
Structure-activity relationships of lactone ring-opened analogs of the antimalarial 1,2,4-trioxane artemisinin.
Mercaptoacyl amino acid inhibitors of atriopeptidase. 1. Structure-activity relationship studies of methionine and S-alkylcysteine derivatives.
Antitumor agents. 166. Synthesis and biological evaluation of 5,6,7,8-substituted-2-phenylthiochromen-4-ones.
Synthesis of novel trans-4-(substituted-benzamido)-3,4-dihydro-2H-benzo[b]-pyran-3-ol derivatives as potential anticonvulsant agents with a distinctive binding profile.
Design, synthesis, and evolution of a novel, selective, and orally bioavailable class of thrombin inhibitors: P1-argininal derivatives incorporating P3-P4 lactam sulfonamide moieties.
3-substituted thieno[2,3-b][1,4]thiazine-6-sulfonamides. A novel class of topically active carbonic anhydrase inhibitors.
Analogues of the muscarinic agent 2'-methylspiro[1-azabicyclo[2.2.2]octane-3,4'-[1,3]dioxolane]: synthesis and pharmacology.
A molecular modeling study of the interactions between the antiestrogen drug tamoxifen and several derivatives, and the calcium-binding protein calmodulin.
Synthesis and structure-activity relationships of cephalosporins with C-3' catechol-containing residues.
Studies on pyridonecarboxylic acids. 1. Synthesis and antibacterial evaluation of 7-substituted-6-halo-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3- carboxylic acids.
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.
Potential antitumor agents. 21. Structure determination and antitumor activity of imidazo[2,1-b]thiazole guanylhydrazones.
Synthesis and biochemical evaluation of the CBI-PDE-I-dimer, a benzannelated analog of (+)-CC-1065 that also produces delayed toxicity in mice.
A homologous series of permanently charged 1,4-dihydropyridines: novel probes designed to localize drug binding sites on ion channels.
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
Anthracene-9,10-diones as potential anticancer agents. Synthesis, DNA-binding, and biological studies on a series of 2,6-disubstituted derivatives.
Preparation and in vitro and in vivo evaluation of quinolones with selective activity against gram-positive organisms.
Discovery and structure-activity relationship of a series of 1-carba-1-dethiacephems exhibiting activity against methicillin-resistant Staphylococcus aureus.
New N alpha-guanidinobenzoyl derivatives of hirudin-54-65 containing stabilized carboxyl or phosphoryl groups on the side chain of phenylalanine-63.
Comparative molecular field analysis of anticoccidial triazines.
3-[4-[1-(6-Fluorobenzo[b]thiophen-3-yl)-4-piperazinyl]butyl]- 2,5,5-trimethyl-4-thiazolidinone: a new atypical antipsychotic agent for the treatment of schizophrenia.
Anti-AIDS agents 49. Synthesis, anti-HIV, and anti-fusion activities of IC9564 analogues based on betulinic acid.
Probing the ATP ribose-binding domain of cyclin-dependent kinases 1 and 2 with O(6)-substituted guanine derivatives.
Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1.
Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues.
Guanidino N-substituted and N,N-disubstituted derivatives of the kappa-opioid antagonist GNTI.
In silico and NMR identification of inhibitors of the IGF-I and IGF-binding protein-5 interaction.
5-HT4 receptor ligands: applications and new prospects.
An algorithm-directed two-component library synthesized via solid-phase methodology yielding potent and orally bioavailable p38 MAP kinase inhibitors.
Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide.
Phenoxypropoxybiguanides, prodrugs of DHFR-inhibiting diaminotriazine antimalarials.
Spectral and crystallographic study of pyridinic analogues of nimesulide: determination of the active form of methanesulfonamides as COX-2 selective inhibitors.
Soluble tetraarylporphyrin-platinum conjugates as cytotoxic and phototoxic antitumor agents.
Indanylidenes. 2. Design and synthesis of (E)-2-(4-chloro-6-fluoro-1-indanylidene)-N-methylacetamide, a potent antiinflammatory and analgesic agent without centrally acting muscle relaxant activity.
Indanylidenes. 1. Design and synthesis of (E)-2-(4,6-difluoro-1-indanylidene)acetamide, a potent, centrally acting muscle relaxant with antiinflammatory and analgesic activity.
Potent, selective, and systemically-available inhibitors of acyl-coenzyme A:cholesterol acyl transferase (ACAT).
Applications of combinatorial technologies to drug discovery. 1. Background and peptide combinatorial libraries.
Novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 7. 8-Arylethyldipyridodiazepinones as potent broad-spectrum inhibitors of wild-type and mutant enzymes.
Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene.
Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.
Structure-activity relationship studies of central nervous system agents. 13. 4-[3-(Benzotriazol-1-yl)propyl]-1-(2-methoxyphenyl)piperazine, a new putative 5-HT1A receptor antagonist, and its analogs.
Preparation, characterization, DNA binding, and in vitro cytotoxicity of the enantiomers of the platinum(II) complexes N-methyl-, N-ethyl- and N,N-dimethyl-(R)- and -(S)-3-aminohexahydroazepinedichloroplatinum(II).
Novel benzothiazolin-2-one and benzoxazin-3-one arylpiperazine derivatives with mixed 5HT1A/D2 affinity as potential atypical antipsychotics.
A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).
Synthesis and biological evaluation of 2-acyl analogues of paclitaxel (Taxol).
Novel cyclic compounds as potent phosphodiesterase 4 inhibitors.
2-Iminopyrrolidines as potent and selective inhibitors of human inducible nitric oxide synthase.
2-[N-Acylamino(C1-C3)alkyl]indoles as MT1 melatonin receptor partial agonists, antagonists, and putative inverse agonists.
Synthesis, acid-base behavior, and binding properties of 6-modified myo-inositol 1,4,5-tris(phosphate)s.
5,6-Cis-penems: broad-spectrum anti-methicillin-resistant Staphylococcus aureus beta-lactam antibiotics.
(1 alpha, 2 beta, 3 beta, 4 alpha)-1,2-bis[N-propyl-N-(4-phenoxybenzyl) amino]carbonyl]cyclobutane-3,4-dicarboxylic acid (A-87049): a novel potent squalene synthase inhibitor.
Synthesis and biological activity of conformationally restricted analogues of milnacipran: (1S, 2R)-1-phenyl-2-[(R)-1-amino-2-propynyl]-N,N- diethylcyclopropanecarboxamide is a novel class of NMDA receptor channel blocker.
Functionally selective M1 muscarinic agonists. 3. Side chains and azacycles contributing to functional muscarinic selectivity among pyrazinylazacycles.
Flexible 1-[(2-aminoethoxy)alkyl]-3-ar(o)yl(thio)ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation.
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
Novel inhibitors of the nuclear factor of activated T cells (NFAT)-mediated transcription of beta-galactosidase: potential immunosuppressive and antiinflammatory agents.
Correlation of antimalarial activity of artemisinin derivatives with binding affinity with ferroprotoporphyrin IX.
Substituted (1,2-diarylethyl)amide acyl-CoA:cholesterol acyltransferase inhibitors: effect of polar groups on in vitro and in vivo activity.
Antidiabetic agents: a new class of reversible carnitine palmitoyltransferase I inhibitors.
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Design, synthesis, biology, and conformations of bicyclic alpha-melanotropin analogues.
Structural modifications of thalidomide produce analogs with enhanced tumor necrosis factor inhibitory activity.
(Piperidinylalkoxy)chromones: novel antihistamines with additional antagonistic activity against leukotriene D4.
Synthesis and protein kinase C inhibitory activities of balanol analogs with replacement of the perhydroazepine moiety.
Synthesis, chemical, and biological properties of vinylogous hydroxamic acids: dual inhibitors of 5-lipoxygenase and IL-1 biosynthesis.
(R)-1,2,3,4-tetrahydro[1]benzothieno[2,3-c]pyridines: novel optically active compounds with strong 5-HT1A receptor binding ability exhibiting anticonflict activity and lessening of memory impairment.
Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor.
Isopropyl and phenyl esters of 3 beta-(4-substituted phenyl)tropan-2 beta-carboxylic acids. Potent and selective compounds for the dopamine transporter.
Synthesis of 2,4-disubstituted thiazoles and selenazoles as potential antifilarial and antitumor agents. 2. 2-Arylamido and 2-alkylamido derivatives of 2-amino-4-(isothiocyanatomethyl)thiazole and 2-amino-4-(isothiocyanatomethyl)selenazole.
Synthesis and antibacterial activity of a series of basic amides of teicoplanin and deglucoteicoplanin with polyamines.
N-(5,5-diacetoxypent-1-yl)doxorubicin: a new intensely potent doxorubicin analogue.
Reversible inhibitors of the gastric (H+/K+)-ATPase. 2. 1-Arylpyrrolo[3,2-c]quinolines: effect of the 4-substituent.
The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives.
Dibenz[b,e]oxepin derivatives: novel antiallergic agents possessing thromboxane A2 and histamine H1 dual antagonizing activity. 1.
Benzothiazole hydroxy ureas as inhibitors of 5-lipoxygenase: use of the hydroxyurea moiety as a replacement for hydroxamic acid.
Benzoquinazoline inhibitors of thymidylate synthase: enzyme inhibitory activity and cytotoxicity of some sulfonamidobenzoylglutamate and related derivatives.
Quinolinecarboxylic acids. 3. Synthesis and antibacterial evaluation of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de] [1,4]benzothiazine-6-carboxylic acids related to rufloxacin.
HIV-1 protease inhibitors based on hydroxyethylene dipeptide isosteres: an investigation into the role of the P1' side chain on structure-activity.
Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety.
2a-[4-(Tetrahydropyridoindol-2-yl)butyl]tetrahydrobenzindole derivatives: new selective antagonists of the 5-hydroxytryptamine7 receptor.
Hybrid-designed inhibitors of p38 MAP kinase utilizing N-arylpyridazinones.
Discovery of 2-phenylamino-imidazo[4,5-h]isoquinolin-9-ones: a new class of inhibitors of lck kinase.
Discovery and biological evaluation of a new family of potent modulators of multidrug resistance: reversal of multidrug resistance of mouse lymphoma cells by new natural jatrophane diterpenoids isolated from Euphorbia species.
Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
Design and synthesis of plasmepsin I and plasmepsin II inhibitors with activity in Plasmodium falciparum-infected cultured human erythrocytes.
Array-based structure and gene expression relationship study of antitumor sulfonamides including N-[2-[(4-hydroxyphenyl)amino]-3-pyridinyl]-4-methoxybenzenesulfonamide and N-(3-chloro-7-indolyl)-1,4-benzenedisulfonamide.
Cysteine derivatives as inhibitors for carboxypeptidase A: synthesis and structure-activity relationships.
Synthesis and in vivo antitumor activity of poly(l-glutamic acid) conjugates of 20S-camptothecin.
Synthesis and notable antimalarial activity of acyclic peroxides, L-(alkyldioxy)-L-(methyldioxy)cyclododecanes.
Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones.
Alkoxypsoralens, novel nonpeptide blockers of Shaker-type K+ channels: synthesis and photoreactivity.
Nucleosides and nucleotides. 177. 9-(6,7-dideoxy-beta-D-allo-hept-5- ynofuranosyl)adenine: a selective and potent ligand for P3 purinoceptor-like protein.
1,4- and 2,6-disubstituted amidoanthracene-9,10-dione derivatives as inhibitors of human telomerase.
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.
Enhancement of oral absorption in selective 5-HT1D receptor agonists: fluorinated 3-[3-(piperidin-1-yl)propyl]indoles.
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Modified ibogaine fragments: synthesis and preliminary pharmacological characterization of 3-ethyl-5-phenyl-1,2,3,4,5, 6-hexahydroazepino[4,5-b]benzothiophenes.
TROTEC-1: a new high-affinity ligand for labeling of the dopamine transporter.
Molecular modeling of phenothiazines and related drugs as multidrug resistance modifiers: a comparative molecular field analysis study.
Dual inhibition of phosphodiesterase 4 and matrix metalloproteinases by an (arylsulfonyl)hydroxamic acid template.
1-aryl-4-[(5-methoxy-1,2,3, 4-tetrahydronaphthalen-1-yl)alkyl]piperazines and their analogues: influence of the stereochemistry of the tetrahydronaphthalen-1-yl nucleus on 5-HT1A receptor affinity and selectivity versus alpha1 and D2 receptors. 5.
Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.
Structure-based design and synthesis of high affinity tripeptide ligands of the Grb2-SH2 domain.
Synthesis of potent cyclic hexapeptide NK-1 antagonists. Use of a minilibrary in transforming a peptidal somatostatin receptor ligand into an NK-1 receptor ligand via a polyvalent peptidomimetic.
First examples of peptidomimetic inhibitors of interleukin-1 beta converting enzyme.
(S)-(-)-4-[4-[2-(isochroman-1-yl)ethyl]-piperazin-1-yl] benzenesulfonamide, a selective dopamine D4 antagonist.
Potent inhibitors of acyl-CoA:cholesterol acyltransferase. 2. Structure-activity relationships of novel N-(2,2-dimethyl-2,3-dihydrobenzofuran-7-yl)amides.
Structure-activity relationship studies on benzofuran analogs of propafenone-type modulators of tumor cell multidrug resistance.
N-acylated alpha-amino acids as novel oral delivery agents for proteins.
Novel non-nucleoside inhibitors of HIV-1 reverse transcriptase. 3. Dipyrido[2,3-b:2',3'-e]diazepinones.
[125I/127I]iodoHoechst 33342: synthesis, DNA binding, and biodistribution.
Ribose-modified adenosine analogues as potential partial agonists for the adenosine receptor.
Synthesis and selective monoamine oxidase B-inhibiting properties of 1-methyl-1,2,3,6-tetrahydropyrid-4-yl carbamate derivatives: potential prodrugs of (R)- and (S)-nordeprenyl.
Computation of brain-blood partitioning of organic solutes via free energy calculations.
Novel N6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A3 adenosine receptors.
Antiandrogenic steroidal sulfonyl heterocycles. Utility of electrostatic complementarity in defining bioisosteric sulfonyl heterocycles.
Discovery of new non-phospholipid inhibitors of the secretory phospholipases A2.
Antiviral enantiomeric preference for 5'-noraristeromycin.
Adenosine deaminase inhibitors: synthesis and structure-activity relationships of 2-hydroxy-3-nonyl derivatives of azoles.
New hexahydroxybiphenyl derivatives as inhibitors of protein kinase C.
(H+,K+)-ATPase inhibiting 2-[(2-pyridylmethyl)sulfinyl]benzimidazoles. 4. A novel series of dimethoxypyridyl-substituted inhibitors with enhanced selectivity. The selection of pantoprazole as a clinical candidate.
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.
6-Azasteroids: potent dual inhibitors of human type 1 and 2 steroid 5 alpha-reductase.
Synthesis and optical resolution of (R)- and (S)-trans-7-Hydroxy-2-[N-propyl-N-(3'-iodo-2'-propenyl)amino]tetralin: a new D3 dopamine receptor ligand.
Structure-activity relationships of the antimalarial agent artemisinin. 1. Synthesis and comparative molecular field analysis of C-9 analogs of artemisinin and 10-deoxoartemisinin.
Synthesis and antiviral activity of acyclic nucleosides with a 3(S),5-dihydroxypentyl or 4(R)-methoxy-3(S),5-dihydroxypentyl side chain.
5-(Aminomethyl)-3-aryldihydrofuran-2(3H)-ones, a new class of monoamine oxidase-B inactivators.
New nonpeptide angiotensin II receptor antagonists. 1. Synthesis, biological properties, and structure-activity relationships of 2-alkyl benzimidazole derivatives.
Design and synthesis of trans-N-[4-[2-(6-cyano-1,2,3, 4-tetrahydroisoquinolin-2-yl)ethyl]cyclohexyl]-4-quinolinecarboxamide (SB-277011): A potent and selective dopamine D(3) receptor antagonist with high oral bioavailability and CNS penetration in the rat.
Synthesis of novel, potent, diol-based HIV-1 protease inhibitors via intermolecular pinacol homocoupling of (2S)-2-benzyloxymethyl-4-phenylbutanal.
Synthesis, antitumor cytotoxicity, and DNA-binding of novel N-5,2-di(omega-aminoalkyl)-2,6-dihydropyrazolo[3,4,5-kl]acridine-5-carboxamides.
Carbocyclic dinucleoside polyphosphonates: interaction with HIV reverse transcriptase and antiviral activity.
Relationships between structure and interaction kinetics for HIV-1 protease inhibitors.
Novel selective PDE4 inhibitors. 1. Synthesis, structure-activity relationships, and molecular modeling of 4-(3,4-dimethoxyphenyl)-2H-phthalazin-1-ones and analogues.
3-(4-Fluoropiperidin-3-yl)-2-phenylindoles as high affinity, selective, and orally bioavailable h5-HT(2A) receptor antagonists.
Synthesis and activity of substituted 2-phenylquinolin-4-amines, antagonists of immunostimulatory CpG-oligodeoxynucleotides.
Design, synthesis, and biological activities of classical N-[4-[2-(2-amino-4-ethylpyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-l-glutamic acid and its 6-methyl derivative as potential dual inhibitors of thymidylate synthase and dihydrofolate reductase and as potential antitumor agents.
Specific inhibition of a family 1A dihydroorotate dehydrogenase by benzoate pyrimidine analogues.
Synthesis, structure-activity relationship, and evaluation of SR141716 analogues: development of central cannabinoid receptor ligands with lower lipophilicity.
Noncalcemic, antiproliferative, transcriptionally active, 24-fluorinated hybrid analogues of the hormone 1alpha, 25-dihydroxyvitamin D3. Synthesis and preliminary biological evaluation.
Halogenated chalcones with high-affinity binding to P-glycoprotein: potential modulators of multidrug resistance.
Synthesis and evaluation of 7 alpha-iodo-5 alpha-dihydrotestosterone as a potential radioligand for androgen receptor.
Identification of a dihydropyridine as a potent alpha1a adrenoceptor-selective antagonist that inhibits phenylephrine-induced contraction of the human prostate.
S-(N-aryl-N-hydroxycarbamoyl)glutathione derivatives are tight-binding inhibitors of glyoxalase I and slow substrates for glyoxalase II.
Selective inhibitors of human lactate dehydrogenases and lactate dehydrogenase from the malarial parasite Plasmodium falciparum.
Mutational evidence for a common kappa antagonist binding pocket in the wild-type kappa and mutant mu[K303E] opioid receptors.
(+)-4-[2-[4-(8-Chloro-3,10-dibromo-6,11-dihydro-5H-benzo[5, 6]cyclohepta[1,2-b]- pyridin-11(R)-yl)-1-piperidinyl]-2-oxo-ethyl]-1-piperidinecarboxamid e (SCH-66336): a very potent farnesyl protein transferase inhibitor as a novel antitumor agent.
N-[omega-(Tetralin-1-yl)alkyl] derivatives of 3,3-dimethylpiperidine are highly potent and selective sigma1 or sigma2 ligands.
32-Ascomycinyloxyacetic acid derived immunosuppressants. Independence of immunophilin binding and immunosuppressive potency.
Orally active non-peptide fibrinogen receptor (GpIIb/IIIa) antagonists: identification of 4-[4-[4-(aminoiminomethyl)phenyl]-1-piperazinyl]-1-piperidineacetic acid as a long-acting, broad-spectrum antithrombotic agent.
Synthesis, cocaine receptor affinity, and dopamine uptake inhibition of several new 2 beta-substituted 3 beta-phenyltropanes.
(-)-11-Hydroxy-7'-isothiocyanato-1',1'-dimethylheptyl-delta 8-THC: a novel, high-affinity irreversible probe for the cannabinoid receptor in the brain.
Synthesis and anti-HIV-1 activity of 4,5,6,7-tetrahydro-5-methylimidazo-[4,5,1-jk][1,4]benzodiazepin- 2(1H)-one (TlBO) derivatives. 4.
Synthesis and biological activity of certain 4'-thio-D-arabinofuranosylpurine nucleosides.
5-(4-Chlorophenyl)-4-methyl-3-(1-(2-phenylethyl)piperidin-4-yl)isoxazole: a potent, selective antagonist at human cloned dopamine D4 receptors.
Dicarboxylic acid dipeptide neutral endopeptidase inhibitors.
Molecular similarity from atomic electrostatic multipole comparisons. Application to anti-HIV drugs.
Synthesis and evaluation of phorboid 20-homovanillates: discovery of a class of ligands binding to the vanilloid (capsaicin) receptor with different degrees of cooperativity.
Drug delivery systems. 2. Camptothecin 20-O-poly(ethylene glycol) ester transport forms.
Potent human immunodeficiency virus type 1 protease inhibitors that utilize noncoded D-amino acids as P2/P3 ligands.
Synthesis of novel 2,4-diaminopyrrolo-[2,3-d]pyrimidines with antioxidant, neuroprotective, and antiasthma activity.
Alkane-6,8-diol: inhibitor of tumor promotion in two-stage carcinogenesis in mouse skin.
Probing the hydrophobic pocket of the active site of aromatase with 4-phenoxy-7 alpha-(phenylthio)-4-androstene-3,17-dione.
(Aryloxy)methylsilane derivatives as new cholesterol biosynthesis inhibitors: synthesis and hypocholesterolemic activity of a new class of squalene epoxidase inhibitors.
4-Aza-3-oxo-5 alpha-androst-1-ene-17 beta-N-aryl-carboxamides as dual inhibitors of human type 1 and type 2 steroid 5 alpha-reductases. Dramatic effect of N-aryl substituents on type 1 and type 2 5 alpha-reductase inhibitory potency.
Potent 6-desfluoro-8-methylquinolones as new lead compounds in antibacterial chemotherapy.
Simultaneous pharmacokinetic screening of a mixture of compounds in the dog using API LC/MS/MS analysis for increased throughput.
Peptidyl alpha-ketoheterocyclic inhibitors of human neutrophil elastase. 3. In vitro and in vivo potency of a series of peptidyl alpha-ketobenzoxazoles.
Halogenated mazindol analogs as potential inhibitors of the cocaine binding site at the dopamine transporter.
Mononucleoside phosphotriester derivatives with S-acyl-2-thioethyl bioreversible phosphate-protecting groups: intracellular delivery of 3'-azido-2',3'-dideoxythymidine 5'-monophosphate.
Design of 5-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,3,4-thiadiazoles, -1,3,4-oxadiazoles, and -1,2,4-triazoles as orally-active, nonulcerogenic antiinflammatory agents.
2,3-Epoxy-10-aza-10,11-dihydrosqualene, a high-energy intermediate analogue inhibitor of 2,3-oxidosqualene cyclase.
Computer-aided mapping of the beta-adrenoceptor. 1. Explanation for effect of para substitution on blocking activity at the beta-1-adrenoceptor.
Structure-activity studies on benzhydrol-containing nipecotic acid and guvacine derivatives as potent, orally-active inhibitors of GABA uptake.
Effect of N-alkylation on the affinities of analogues of spiperone for dopamine D2 and serotonin 5-HT2 receptors.
Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere.
Design and synthesis of some substrate analogue inhibitors of phospholipase A2 and investigations by NMR and molecular modeling into the binding interactions in the enzyme-inhibitor complex.
6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: structure-activity relationships for the AMPA-type non-NMDA receptor.
Secondary metabolites by chemical screening. 17. Nigericinol derivatives: synthesis, biological activities, and modeling studies.
Synthesis and anti-HIV activity of 9-[c-4,t-5-bis(hydroxymethyl)cyclopent-2-en-r-1-yl]-9H-adenine.
Nonpeptide angiotensin II receptor antagonists. 1. Synthesis and in vitro structure-activity relationships of 4-[[[(1H-pyrrol-1-ylacetyl)amino]phenyl]methyl]imidazole derivatives as angiotensin II receptor antagonists.
The synthesis of novel GABA uptake inhibitors. 1. Elucidation of the structure-activity studies leading to the choice of (R)-1-[4,4-bis(3-methyl-2-thienyl)-3-butenyl]-3-piperidinecarboxylic acid (tiagabine) as an anticonvulsant drug candidate.
Synthesis and conformational analysis of fusidic acid side chain derivatives in relation to antibacterial activity.
Rational design, discovery, and synthesis of a novel series of potent growth hormone secretagogues.
Design, synthesis, computational prediction, and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii.
A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents.
Experimental precedent for the need to involve the primary hydration layer of DNA in lead drug design.
Combinatorial lead optimization of a neuropeptide FF antagonist.
Novel tricyclic-alpha-alkyloxyphenylpropionic acids: dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity.
Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Secretase targets for Alzheimer's disease: identification and therapeutic potential.
Exploration of novel aryl binding sites of farnesyltransferase using molecular modeling and benzophenone-based farnesyltransferase inhibitors.
Fluorescent tricyclic analogues of acyclovir and ganciclovir. A structure-antiviral activity study.
Synthesis and cytotoxicity on sensitive and doxorubicin-resistant cell lines of new pyrrolo[2,1-c][1,4]benzodiazepines related to anthramycin.
Design, synthesis, and tripeptidyl peptidase II inhibitory activity of a novel series of (S)-2,3-dihydro-2-(4-alkyl-1H-imidazol-2-yl)-1H-indoles.
Design, synthesis and biological evaluation of novel arachidonic acid derivatives as highly potent and selective endocannabinoid transporter inhibitors.
Isosteric analogues of nicotinamide adenine dinucleotide derived from furanfurin, thiophenfurin, and selenophenfurin as mammalian inosine monophosphate dehydrogenase (type I and II) inhibitors.
Design and synthesis of hydrazinopeptides and their evaluation as human leukocyte elastase inhibitors.
Structure-based design of beta-lactamase inhibitors. 2. Synthesis and evaluation of bridged sulfactams and oxamazins.
New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: candidates for clinical development.
Studies on quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides. 8.1, 2 synthesis and pharmacological evaluation of tricyclic fused quinazolines and 1,2,4-benzothiadiazine 1,1-dioxides as potential alpha1-adrenoceptor antagonists.
Peptidomimetic growth hormone secretagogues. Design considerations and therapeutic potential.
Synthesis and biological evaluation of a new series of sterols as potential hypocholesterolemic agents.
Synthesis, activity, and molecular modeling of new 2, 4-dioxo-5-(naphthylmethylene)-3-thiazolidineacetic acids and 2-thioxo analogues as potent aldose reductase inhibitors.
Binding affinities for sulfonamide inhibitors with human thrombin using Monte Carlo simulations with a linear response method.
Nitrogen-carbon-linked (azolylphenyl)oxazolidinones with potent antibacterial activity against the fastidious gram-negative organisms Haemophilus influenzae and Moraxella catarrhalis.
Use of papain as a model for the structure-based design of cathepsin K inhibitors: crystal structures of two papain-inhibitor complexes demonstrate binding to S'-subsites.
Synthesis and antitumor activity of novel 6-alkyl-6-demethylmitomycins.
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
Synthesis and immunostimulating properties of lipophilic ester and ether muramyl peptide derivatives.
(2S,4S)-2-amino-4-(4,4-diphenylbut-1-yl)- pentane-1,5-dioic acid: a potent and selective antagonist for metabotropic glutamate receptors negatively linked to adenylate cyclase.
Structure-activity relationships of cysteine-lacking pentapeptide derivatives that inhibit ras farnesyltransferase.
Inhibitors of acyl-CoA: cholesterol O-acyl transferase (ACAT) as hypocholesterolemic agents. CI-1011: an acyl sulfamate with unique cholesterol-lowering activity in animals fed noncholesterol-supplemented diets.
Synthesis and in vitro evaluation of new wortmannin esters: potent inhibitors of phosphatidylinositol 3-kinase.
Synthesis of some 2-aryl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-ones as tools to define the essential pharmacophoric descriptors of a benzodiazepine receptor ligand.
2-[2'-(Dimethylamino)ethyl]-1,2-dihydro- 3H-dibenz[de,h]isoquinoline-1,3-diones with substituents at positions 4, 8, 9, 10, and 11. Synthesis, antitumor activity, and quantitative structure-activity relationships.
Studies on disease-modifying antirheumatic drugs: synthesis of novel quinoline and quinazoline derivatives and their anti-inflammatory effect.
Synthesis and modeling studies with monocyclic analogues of mycophenolic acid.
Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of (R*,R*)-(+/-)-methyl 3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3-methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase.
5,7-Dimethoxy-3-(4-pyridinyl)quinoline is a potent and selective inhibitor of human vascular beta-type platelet-derived growth factor receptor tyrosine kinase.
Dual antagonists of platelet activating factor and histamine. Identification of structural requirements for dual activity of N-Acyl-4-(5,6-dihydro-11H-benzo [5,6]cyclohepta-[1,2-b]pyridin-11-ylidene)piperidines.
Nonsteroidal antiinflammatory drug hydroxamic acids. Dual inhibitors of both cyclooxygenase and 5-lipoxygenase.
Methylsulfamic acid esters. A new chemical class of oral antiarthritic agents.
Synthesis and evaluation of multisubstrate inhibitors of an oncogene-encoded tyrosine-specific protein kinase. 1.
2-Chloro-1-(2,4-dichlorophenyl)-3-(1H-imidazol-1-yl)-2-phenylpropan-1-one hydrochloride, a novel, nonmutagenic antibacterial with specific activity against anaerobic bacteria.
Probing the bradykinin receptor: mapping the geometric topography using ethers of hydroxyproline in novel peptides.
Tertiary 2-haloethylamine derivatives of the muscarinic agent McN-A-343, [4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]trimethylammonium chloride.
Assessment of the in vivo and in vitro opioid activity of bridged hexahydroaporphine and isoquinoline molecules.
Syntheses and 5-HT2 antagonist activity of bicyclic 1,2,4-triazol-3(2H)-one and 1,3,5-triazine-2,4(3H)-dione derivatives.
Synthesis and immunosuppressive activity of some side-chain variants of mycophenolic acid.
Atrial natriuretic peptide receptor modulators: effects of disubstituted quinazolines on receptor binding and in vitro biological activity.
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.
Conformationally constrained congeners of 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones active on the cardiovascular system: conformational studies by molecular mechanics calculations and 1H NMR spectroscopy.
Preparation and anticonvulsant activity of a series of functionalized alpha-heteroatom-substituted amino acids.
Stereospecific synthesis of (R)- and (S)-S-adenosyl-1,8-diamino-3-thiooctane, a potent inhibitor of polyamine biosynthesis. Comparison of asymmetric induction vs enantiomeric synthesis.
Novel erythromycin derivatives with aryl groups tethered to the C-6 position are potent protein synthesis inhibitors and active against multidrug-resistant respiratory pathogens.
Synthesis, molecular modeling, and structure-activity relationship of benzophenone-based CAAX-peptidomimetic farnesyltransferase inhibitors.
Rationally based efficacy tuning of selective dopamine d4 receptor ligands leading to the complete antagonist 2-[4-(4-chlorophenyl)piperazin-1-ylmethyl]pyrazolo[1,5-a]pyridine (FAUC 213).
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Synthesis and antibacterial evaluation of certain quinolone derivatives.
S-acyl-2-thioethyl aryl phosphotriester derivatives of AZT: synthesis, antiviral activity, and stability study.
Oxidation of N(omega)-hydroxyarginine analogues by NO-synthase: the simple, non amino acid N-butyl N'-hydroxyguanidine is almost as efficient an NO precursor as N(omega)-hydroxyarginine.
Reversible carnitine palmitoyltransferase inhibitors with broad chemical diversity as potential antidiabetic agents.
Hydrophilic, pro-drug analogues of T138067 are efficacious in controlling tumor growth in vivo and show a decreased ability to cross the blood brain barrier.
Synthesis and antiviral activity of novel erythrofuranosyl imidazo[1,2-a]pyridine C-nucleosides constructed via palladium coupling of iodoimidazo[1,2-a]pyridines and dihydrofuran.
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
Quinazolin-4-one alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonists: structure-activity relationship of the C-2 side chain tether.
2002 Alfred Burger Award Address in Medicinal Chemistry. Natural products and design: interrelated approaches in drug discovery.
3-Deoxy-D-myo-inositol 1-phosphate, 1-phosphonate, and ether lipid analogues as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth.
Inhibition of human neutrophil elastase. 4. Design, synthesis, X-ray crystallographic analysis, and structure-activity relationships for a series of P2-modified, orally active peptidyl pentafluoroethyl ketones.
Improved binding affinity for cyclophilin A by a cyclosporin derivative singly modified at its effector domain.
Design, synthesis, and study of 9-substituted ellipticine and 2-methylellipticinium analogues as potential CNS-selective antitumor agents.
Structural features important for sigma 1 receptor binding.
Isochroman-6-carboxamides as highly selective 5-HT1D agonists: potential new treatment for migraine without cardiovascular side effects.
Spiro[1H-indene-1,4'-piperidine] derivatives as potent and selective non-peptide human somatostatin receptor subtype 2 (sst2) agonists.
The frontier orbital phase angles: novel QSAR descriptors for benzene derivatives, applied to phenylalkylamine hallucinogens.
5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors.
Structure-activity requirements for flavone cytotoxicity and binding to tubulin.
Novel acyl-CoA:cholesterol acyltransferase inhibitors. Synthesis and biological activity of 3-quinolylurea derivatives.
Antineoplastic agents. 278. Isolation and structure of axinastatins 2 and 3 from a western Caroline Island marine sponge.
Antiviral activities of methylated nordihydroguaiaretic acids. 1. Synthesis, structure identification, and inhibition of tat-regulated HIV transactivation.
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib).
Synthesis and nicotinic acetylcholine receptor binding properties of exo-2-(2'-fluoro-5'-pyridinyl)-7-azabicyclo-[2.2.1]heptane: a new positron emission tomography ligand for nicotinic receptors.
Synthesis and cytotoxic evaluation of substituted sulfonyl-N-hydroxyguanidine derivatives as potential antitumor agents.
Synthesis and antitumor activity of a new class of pyrazolo[4,3-e]pyrrolo[1,2-a][1,4]diazepinone analogues of pyrrolo[1,4][2,1-c]benzodiazepines.
N-phosphoryl derivatives of bisantrene. Antitumor prodrugs with enhanced solubility and reduced potential for toxicity.
Cyclic enkephalin analogs with exceptional potency at peripheral delta opioid receptors.
Nitrobenzyl mustard quaternary salts: a new class of hypoxia-selective cytotoxins showing very high in vitro selectivity.
Concepts and progress in the development of peptide mimetics.
N-(acyloxyalkyl)pyridinium salts as soluble prodrugs of a potent platelet activating factor antagonist.
Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.
Anti-HIV michellamines from Ancistrocladus korupensis.
Synthesis and characterization of [125I]-N-(N-benzylpiperidin-4-yl)-4- iodobenzamide, a new sigma receptor radiopharmaceutical: high-affinity binding to MCF-7 breast tumor cells.
Synthesis and biological evaluation of 14-alkoxymorphinans. 11. 3-Hydroxycyprodime and analogues: opioid antagonist profile in comparison to cyprodime.
Antitumor agents. 150. 2',3',4',5',5,6,7-substituted 2-phenyl-4-quinolones and related compounds: their synthesis, cytotoxicity, and inhibition of tubulin polymerization.
Presynaptic cholinergic modulators as potent cognition enhancers and analgesic drugs. 1. Tropic and 2-phenylpropionic acid esters.
Synthesis and biological evaluation of 5-[[3,5-bis(1,1-dimethylethyl)- 4-hydroxyphenyl]methylene]oxazoles, -thiazoles, and -imidazoles: novel dual 5-lipoxygenase and cyclooxygenase inhibitors with antiinflammatory activity.
Synthesis and biological evaluation of novel C-4 aziridine-bearing paclitaxel (taxol) analogs.
N-[(1-butyl-4-piperidinyl)methyl]-3,4dihydro-2H-[1,3]oxazino[3,2- a]indole10-carboxamide hydrochloride: the first potent and selective 5-HT4 receptor antagonist amide with oral activity.
New drug developments for opportunistic infections in immunosuppressed patients: Pneumocystis carinii.
Bioisosteric replacement of the alpha-amino carboxylic acid functionality in 2-amino-5-phosphonopentanoic acid yields unique 3,4-diamino-3-cyclobutene-1,2-dione containing NMDA antagonists.
1-Naphthylpiperazine derivatives as potential atypical antipsychotic agents.
Naphtho and benzo analogues of the kappa opioid agonist trans-(+/-)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl] benzeneacetamide.
Synthesis and antiretrovirus properties of 5'-isocyano-5'-deoxythymidine, 5'-isocyano-2',5'-dideoxyuridine, 3'-azido-5'-isocyano-3',5'-dideoxythymidine, and 3'-azido-5'-isocyano-2',3',5'-trideoxyuridine.
Adenosine deaminase inhibitors. Synthesis and biological evaluation of C1' and nor-C1' derivatives of (+)-erythro-9-(2(S)-hydroxy-3(R)-nonyl)adenine.
Novel non-cross resistant diaminoanthraquinones as potential chemotherapeutic agents.
Incorporation of a novel conformationally restricted tyrosine analog into a cyclic, delta opioid receptor selective tetrapeptide (JOM-13) enhances delta receptor binding affinity and selectivity.
DNA-directed alkylating agents. 4. 4-anilinoquinoline-based minor groove directed aniline mustards.
Antidopaminergic effects of the stereoisomers of N-[(1-alkyl-2- pyrrolidinyl)methyl]-5-sulfamoylbenzamides and -2,3-dihydrobenzofuran-7-carboxamides.
Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors.
Fluoronaphthyridines as antibacterial agents. 4. Synthesis and structure-activity relationships of 5-substituted-6-fluoro-7-(cycloalkylamino)-1,4-dihydro-4-oxo-1,8- naphthyridine-3-carboxylic acids.
Synthesis and antitumor activity of 2-beta-D-ribofuranosyloxazole-4-carboxamide (oxazofurin).
Heterosubstituted anthracene-9,10-dione analogues. The synthesis and antitumor evaluation of 5,8-bis[(aminoalkyl)amino]naphtho[2,3-b] thiophene-4,9-diones.
Synthesis and antitumor activity of 3- and 5-hydroxy-4-methylpyridine-2-carboxaldehyde thiosemicarbazones.
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 1. Receptor interactions.
Hypoxia-selective antitumor agents. 16. Nitroarylmethyl quaternary salts as bioreductive prodrugs of the alkylating agent mechlorethamine.
Syntheses and structure-activity relationships of nonnatural beta-C-nucleoside 5'-triphosphates bearing an aromatic nucleobase with phenolic hydroxy groups: inhibitory activities against DNA polymerases.
Synthesis and biological evaluation of non-peptidic cyclophilin ligands.
Design, synthesis, and biological activity of a novel non-cisplatin-type platinum-acridine pharmacophore.
Enantioselective syntheses of potent retinoid X receptor ligands: differential biological activities of individual antipodes.
Rapid enantiomeric quantification of an antiviral nucleoside agent (D,L-FMAU, 2'-fluoro-5-methyl-beta,D,L-arabinofurano-syluracil) by mass spectrometry.
trans-1-[(2-Phenylcyclopropyl)methyl]-4-arylpiperazines: mixed dopamine D(2)/D(4) receptor antagonists as potential antipsychotic agents.
Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Orally-effective, long-acting sorbitol dehydrogenase inhibitors: synthesis, structure-activity relationships, and in vivo evaluations of novel heterocycle-substituted piperazino-pyrimidines.
Designing non-peptide peptidomimetics in the 21st century: inhibitors targeting conformational ensembles.
4'-Arylpyrrolomorphinans: effect of a pyrrolo-N-benzyl substituent in enhancing delta-opioid antagonist activity.
Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.
Synthesis and biological evaluation of s-triazine substituted polyamines as potential new anti-trypanosomal drugs.
Synthesis and structure-activity relationship of (lactamylvinyl)cephalosporins exhibiting activity against staphylococci, pneumococci, and enterococci.
Synthesis of 1-substituted 3-(chloromethyl)-6-aminoindoline (6-amino-seco-CI) DNA minor groove alkylating agents and structure-activity relationships for their cytotoxicity.
5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.
2,4-Diamino-6,7-dihydro-5H-cyclopenta[d]pyrimidine analogues of trimethoprim as inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.
Opioid antagonist activity of naltrexone-derived bivalent ligands: importance of a properly oriented molecular scaffold to guide "address" recognition at kappa opioid receptors.
Hypoglycemic prodrugs of 4-(2,2-dimethyl-1-oxopropyl)benzoic acid.
Nonsymmetric P2/P2' cyclic urea HIV protease inhibitors. Structure-activity relationship, bioavailability, and resistance profile of monoindazole-substituted P2 analogues.
Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition.
Novel heterocyclic-fused pyridazinones as potent and selective phosphodiesterase IV inhibitors.
Antineoplastic agents. 410. Asymmetric hydroxylation of trans-combretastatin A-4.
Nonsymmetrically substituted cyclic urea HIV protease inhibitors.
Structure-activity relationships of N2-aryl-3-(isoxazolylsulfamoyl)-2-thiophenecarboxamides as selective endothelin receptor-A antagonists.
Antiviral and anti-inflammatory diterpenoids from the soft coral Sinularia gyrosa.
Rearranged diterpenoids from the biotransformation of ent-trachyloban-18-oic acid by Rhizopus arrhizus.
Selective type IV phosphodiesterase inhibitors as antiasthmatic agents. The syntheses and biological activities of 3-(cyclopentyloxy)-4-methoxybenzamides and analogues.
Synthesis and antimicrobial and toxicological studies of amino acid and peptide derivatives of kanamycin A and netilmicin.
Betulinic acid derivatives: a new class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action.
A new arylpiperazine antipsychotic with high D2/D3/5-HT1A/alpha 1A-adrenergic affinity and a low potential for extrapyramidal effects.
Studies of the active conformation of a novel series of benzamide dopamine D2 agonists.
Synthesis and structure-activity relationships of N-propyl-N-(4-pyridinyl)-1H-indol-1-amine (besipirdine) and related analogs as potential therapeutic agents for Alzheimer's disease.
Synthesis and biological activity of novel quaternary ammonium derivatives of alkylglycerols as potent inhibitors of protein kinase C.
5-Methyl-6-phenyl-1,3,5,6-tetrahydro-3,6-methano-1,5-benzodiazocine-2,4-dione (BA 41899): representative of a novel class of purely calcium-sensitizing agents.
Inhibition of the EGF-stimulated cellular proliferation of ER 22 cells by hydroxybiphenyl derivatives.
Vinblastine and vincristine are inhibitors of monoamine oxidase B.
Synthesis and evaluation of N,N-di-n-propyltetrahydrobenz[f]indol-7-amine and related congeners as dopaminergic agonists.
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
New anticancer agents: alterations of the carbamate group of ethyl (5-amino-1,2-dihydro-3-phenylpyrido[3,4-b]pyrazin-7-yl)car bamates.
Cryptosphaerolide, a cytotoxic Mcl-1 inhibitor from a marine-derived ascomycete related to the genus Cryptosphaeria.
Fluoronaphthyridines and quinolones as antibacterial agents. 1. Synthesis and structure-activity relationships of new 1-substituted derivatives.
The 2-desamino and 2-desamino-2-methyl analogues of aminopterin do not inhibit dihydrofolate reductase but are potently toxic to tumor cells in culture.
Antitumor agents. 111. New 4-hydroxylated and 4-halogenated anilino derivatives of 4'-demethylepipodophyllotoxin as potent inhibitors of human DNA topoisomerase II.
5-OHKF and NorKA, depsipeptides from a Hawaiian collection of Bryopsis pennata: binding properties for NorKA to the human neuropeptide Y Y1 receptor.
The binding of benzenesulfonamides to carbonic anhydrase enzyme. A molecular mechanics study and quantitative structure-activity relationships.
Styrylpyrazoles, styrylisoxazoles, and styrylisothiazoles. Novel 5-lipoxygenase and cyclooxygenase inhibitors.
Structure-activity relationship of antiestrogens: a study using triarylbutenone, benzofuran, and triarylfuran analogues as models for triarylethylenes and triarylpropenones.
Is there a case for P-450 inhibitors in cancer treatment?
LH-RH antagonists: design and synthesis of a novel series of peptidomimetics.
Synthesis and biological evaluation of 4,6-diethyl-1,3,4,5-tetrahydropyrano[4,3-b]indole-4-acetic acid, an isomer of etodolac.
Evidence for nitroxyl in the catalase-mediated bioactivation of the alcohol deterrent agent cyanamide.
Synthesis and antiarrhythmic activity of cis-2,6-dimethyl-alpha,alpha-diaryl-1-piperidinebutanols.
Antitumor properties of tetrahydrobenz[a]anthraquinone derivatives.
6-Substituted-4-(3-bromophenylamino)quinazolines as putative irreversible inhibitors of the epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor (HER-2) tyrosine kinases with enhanced antitumor activity.
4-(Phenylsulfonyl)piperidines: novel, selective, and bioavailable 5-HT(2A) receptor antagonists.
Structure-based de novo design, synthesis, and biological evaluation of non-azole inhibitors specific for lanosterol 14alpha-demethylase of fungi.
Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.
Phenanthroindolizidine alkaloids as cytotoxic substances in a Danaid butterfly, Ideopsis similis, against human cancer cells.
4-(4-cycloalkyl/aryl-oxazol-5-yl)benzenesulfonamides as selective cyclooxygenase-2 inhibitors: enhancement of the selectivity by introduction of a fluorine atom and identification of a potent, highly selective, and orally active COX-2 inhibitor JTE-522(1).
A novel series of 2,6,7-substituted 2,3-dihydro-1,4-benzodioxin and 2,6,7-substituted 1,4-benzodioxin derivatives as lipid peroxidation inhibitors. Structure-activity relationships for high inhibition of human low-density lipoprotein peroxidation.
(-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor.
Bisphosphonates inhibit the growth of Trypanosoma brucei, Trypanosoma cruzi, Leishmania donovani, Toxoplasma gondii, and Plasmodium falciparum: a potential route to chemotherapy.
Antitumor polycyclic acridines. 8.(1) Synthesis and telomerase-inhibitory activity of methylated pentacyclic acridinium salts.
2-amino-2-oxazolines as subtype selective alpha(2) adrenoceptor agonists.
Synthesis, anti-human immunodeficiency virus and anti-hepatitis B virus activities of novel oxaselenolane nucleosides.
Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy.
Synthesis and voltage-clamp studies of methyl 1,4-dihydro-2, 6-dimethyl-5-nitro-4-(benzofurazanyl)pyridine-3-carboxylate racemates and enantiomers and of their benzofuroxanyl analogues.
A facile, alternative synthesis of 4'-thioarabinonucleosides and their biological activities.
Synthesis of carboranes containing an azulene framework and in vitro evaluation as boron carriers.
Synthesis and dopaminergic properties of benzo-fused analogues of quinpirole and quinelorane.
Studies of pyrrolo[1,2-alpha]benzimidazolequinone DT-diaphorase substrate activity, topoisomerase II inhibition activity, and DNA reductive alkylation.
3-[2-(Pyrrolidin-1-yl)ethyl]indoles and 3-[3-(piperidin-1-yl)propyl]indoles: agonists for the h5-HT1D receptor with high selectivity over the h5-HT1B subtype.
Search for DNA repair inhibitors: selective binding of nucleic bases-acridine conjugates to a DNA duplex containing an abasic site.
Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 4. Incorporation of P1 lactam moieties as L-glutamine replacements.
Potent antagonists of somatostatin: synthesis and biology.
Thromboxane modulating agents. 3. 1H-imidazol-1-ylalkyl- and 3-pyridinylalkyl-substituted 3-[2-[(arylsulfonyl)amino]ethyl]benzenepropanoic acid derivatives as dual thromboxane synthase inhibitor/thromboxane receptor antagonists.
Investigation of the configurational and conformational influences on the hormonal activity of 1,2-bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamines and of their platinum(II) complexes. 1. Synthesis, estradiol receptor affinity, and estrogenic activity of diastereomeric [N-alkyl- and N,N'-dialkyl-1,2- bis(2,6-dichloro-4-hydroxyphenyl)ethylenediamine]dichloroplatinum(II) complexes.
High-affinity partial agonist imidazo[1,5-a]quinoxaline amides, carbamates, and ureas at the gamma-aminobutyric acid A/benzodiazepine receptor complex.
Dithiolopyrrolone antibiotic formation induced by adding valeric acid to the culture broth of Saccharothrix algeriensis.
Novel 3-hydroxy-2(1H)-pyridinones. Synthesis, iron(III)-chelating properties, and biological activity.
Polyamine analogues with antitumor activity.
Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors.
Ocular delivery of the beta-adrenergic antagonist alprenolol by sequential bioactivation of its methoxime analogue.
N-substituted dibenzoxazepines as analgesic PGE2 antagonists.
Decapeptide agonists of human C5a: the relationship between conformation and spasmogenic and platelet aggregatory activities.
Potential antitumor agents. 58. Synthesis and structure-activity relationships of substituted xanthenone-4-acetic acids active against the colon 38 tumor in vivo.
Antitumor and DNA-binding properties of a group of oligomeric complexes of Pt(II) and Pt(IV).
Azole endothelin antagonists. 3. Using delta log P as a tool to improve absorption.
Guanine, pyrazolo[3,4-d]pyrimidine, and triazolo[4,5-d]pyrimidine (8-azaguanine) phosphonate acyclic derivatives as inhibitors of purine nucleoside phosphorylase.
Conformationally restricted analogues of the muscarinic agent N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide.
Structure-activity relationships of estrogenic ligands: synthesis and evaluation of (17 alpha, 20E)- and (17 alpha, 20Z)-21-halo-19-norpregna-1,3,5(10),20-tetraene-3,17 beta-diols.
2-Pyridinone derivatives: a new class of nonnucleoside, HIV-1-specific reverse transcriptase inhibitors.
3-Alkyl-4-aminobutyric acids: the first class of anticonvulsant agents that activates L-glutamic acid decarboxylase.
Tetrahydrothiadiazoloisoquinolines: synthesis and inhibition of phenylethanolamine-N-methyltransferase.
Renin inhibitors based on dipeptide analogues. Incorporation of the hydroxyethylene isostere at the P2/P3 sites.
Alpha-diketone and alpha-keto ester derivatives of N-protected amino acids and peptides as novel inhibitors of cysteine and serine proteinases.
Synthesis and structure-activity relationships of a novel class of 5-lipoxygenase inhibitors. 2-(Phenylmethyl)-4-hydroxy-3,5-dialkylbenzofurans: the development of L-656,224.
Diels-Alder adducts of vinyl porphyrins: synthesis and in vivo photodynamic effect against a rat bladder tumor.
A new series of tricyclic (aryloximino)propanolamines displaying very high selective beta 2-blocking properties.
Synthesis and structure-activity relationships of 5-substituted 6,8-difluoroquinolones, including sparfloxacin, a new quinolone antibacterial agent with improved potency.
Activity of acyclic 6-(phenylselenenyl)pyrimidine nucleosides against human immunodeficiency viruses in primary lymphocytes.
beta-Resorcylic acid lactones from a Paecilomyces fungus.
Synthesis and pharmacological evaluation of 1-(aminomethyl)-3,4-dihydro-5-hydroxy-1H-2-benzopyrans as dopamine D1 selective ligands.
Histamine H3 ligands: just pharmacological tools or potential therapeutic agents?
Benzodiazepine receptor binding activity of 8-substituted-9-(3-substituted-benzyl)-6-(dimethylamino)-9H-purines.
Structure-activity studies for a novel series of tricyclic substituted hexahydrobenz[e]isoindole alpha(1A) adrenoceptor antagonists as potential agents for the symptomatic treatment of benign prostatic hyperplasia (BPH).
Reporter affinity labels: an o-phthalaldehyde derivative of beta-naltrexamine as a fluorogenic ligand for opioid receptors.
Rational design, synthesis, and biological activity of novel conformationally restricted vitamin D analogues, (22R)- and (22S)-22-ethyl-1,25-dihydroxy-23,24-didehydro-24a,24b-dihomo-20-epivitamin D(3).
'3+1' mixed-ligand oxotechnetium(V) complexes with affinity for melanoma: synthesis and evaluation in vitro and in vivo.
Conformationally constrained analogues of diacylglycerol (DAG). 17. Contrast between sn-1 and sn-2 DAG lactones in binding to protein kinase C.
Design, synthesis, and biological evaluation of a series of lavendustin A analogues that inhibit EGFR and Syk tyrosine kinases, as well as tubulin polymerization.
Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor.
Design, synthesis, and structure-activity relationships of novel non-imidazole histamine H(3) receptor antagonists.
Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis.
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors.
Antineoplastic agents. 443. Synthesis of the cancer cell growth inhibitor hydroxyphenstatin and its sodium diphosphate prodrug.
Pyrrolomorphinans as delta opioid receptor antagonists. The role of steric hindrance in conferring selectivity.
Bisquaternary ligands of the common allosteric site of M2 acetylcholine receptors: search for the minimum essential distances between the pharmacophoric elements.
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydropyridono[5,6-g]quinolines.
Synthesis and stereochemical structure-activity relationships of 1,3-dioxoperhydropyrido[1,2-c]pyrimidine derivatives: potent and selective cholecystokinin-A receptor antagonists.
3 Beta-(4-ethyl-3-iodophenyl)nortropane-2 beta-carboxylic acid methyl ester as a high-affinity selective ligand for the serotonin transporter.
NMR-based discovery of lead inhibitors that block DNA binding of the human papillomavirus E2 protein.
Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity.
Potent and selective inhibition of neuronal nitric oxide synthase by N omega-propyl-L-arginine.
Design, synthesis, and biochemical evaluation of phosphonate and phosphonamidate analogs of glutathionylspermidine as inhibitors of glutathionylspermidine synthetase/amidase from Escherichia coli.
A novel series of 2,5-substituted tryptamine derivatives as vascular 5HT1B/1D receptor antagonists.
Effect of modifications of the alkylpiperazine moiety of trazodone on 5HT2A and alpha1 receptor binding affinity.
A new single-photon emission computed tomography imaging agent for serotonin transporters: [123I]IDAM, 5-iodo-2-((2-((dimethylamino)methyl)phenyl)thio)benzyl alcohol.
Conformational studies of paclitaxel analogs modified at the C-2' position in hydrophobic and hydrophilic solvent systems.
The C-32 triacetyl-L-rhamnose derivative of ascomycin: a potent, orally active macrolactone immunosuppressant.
Hypoxia-selective antitumor agents. 11. Chlorambucil N-oxide: a reappraisal of its synthesis, stability, and selective toxicity for hypoxic cells.
3-and 4-substituted 4H-pyrido[4,3-e]-1,2,4-thiadiazine 1,1-dioxides as potassium channel openers: synthesis, pharmacological evaluation, and structure-activity relationships.
Correlation of anti-HIV potency with lipophilicity in a series of cosalane analogs having normal alkenyl and phosphodiester chains as cholestane replacements.
Synthesis and biological activity of 3-substituted imidazo[1,2-a]pyridines as antiulcer agents.
Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.
Investigation of (Oxodioxolenyl)methyl carbamates as nonchiral bioreversible prodrug moieties for chiral amines.
Renin inhibitors. Synthesis of transition-state analogue inhibitors containing phosphorus acid derivatives at the scissile bond.
New anticancer agents: chiral isomers of ethyl 5-amino-1,2-dihydro-2-methyl-3-phenylpyrido[3,4-b]pyrazine-7-car bamate .
Synthesis and anthelmintic activity of a series of pyrazino[2,1-a][2]benzazepine derivatives.
(R)-methanandamide: a chiral novel anandamide possessing higher potency and metabolic stability.
(Acyloxy)alkyl carbamate prodrugs of norfloxacin.
Relationship between tissue selectivity and lipophilicity for inhibitors of HMG-CoA reductase.
Folic acid analogues lacking the 2-carbon are substrates for folylpolyglutamate synthetase and inhibit cell growth.
trans-3-n-propyl-L-proline is a highly favorable, conformationally restricted replacement for methionine in the C-terminal tetrapeptide of cholecystokinin. Stereoselective synthesis of 3-allyl- and 3-n-propyl-L-proline derivatives from 4-hydroxy-L-proline.
Function of negative charge in the "address domain" of deltorphins.
Nucleosides and nucleotides. 95. Improved synthesis of 1-(2-azido-2-deoxy-beta-D-arabinofuranosyl)cytosine (cytarazid) and -thymine. Inhibitory spectrum of cytarazid on the growth of various human tumor cells in vitro.
Synthesis and biological evaluation of 5-deazaisofolic acid, 5-deaza-5,6,7,8-tetrahydroisofolic acid, and their N9-substituted analogues.
Synthesis and biological activity of novel folic acid analogues: pteroyl-S-alkylhomocysteine sulfoximines.
Improvements in the minimum binding sequence of C5a: examination of His-67.
The first mechanism-based inactivators for angiotensin-converting enzyme.
Synthesis and antitumor activity of structural analogues of the epipodophyllotoxins.
Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.
Synthesis and structure-activity relationship of some 5-[[[(dialkylamino)alkyl]-1-piperidinyl]acetyl]-10,11-dihydro-5H- benzo[b,e][1,4]diazepin-11-ones as M2-selective antimuscarinics.
Antimycobacterial activity of a series of pyrazinoic acid esters.
Synthesis of 20-hydroxy-, 20-amino-, and 20-nitro-14-hydroxy-21-nor-5 beta,14 beta-pregnane C-3 glycosides and related derivatives: structure-activity relationships of pregnanes that bind to the digitalis receptor.
Synthesis and opioid receptor affinity of a series of 2, 4-diaryl-substituted 3,7-diazabicylononanones.
Structural aspects of isozyme selectivity in the binding of inhibitors to carbonic anhydrases II and IV.
Optimization of substituted N-3-benzylimidazoquinazolinone sulfonamides as potent and selective PDE5 inhibitors.
Design, synthesis, and preliminary pharmacological evaluation of N-acyl-3-aminoglutarimides as broad-spectrum chemokine inhibitors in vitro and anti-inflammatory agents in vivo.
Preparation and characterization of novel trans-[PtCl(2)(amine)(isopropylamine)] compounds: cytotoxic activity and apoptosis induction in ras-transformed cells.
Synthesis and biological evaluation of 2'-carbamate-linked and 2'-carbonate-linked prodrugs of paclitaxel: selective activation by the tumor-associated protease plasmin.
Synthesis and hypolipidemic and antiplatelet activities of alpha-asarone isomers in humans (in vitro), mice (in vivo), and rats (in vivo).
Synthesis and pharmacological evaluation of new pyrazolidine-3, 5-diones as AT(1) angiotensin II receptor antagonists.
Fenchylamine sulfonamide inhibitors of amyloid beta peptide production by the gamma-secretase proteolytic pathway: potential small-molecule therapeutic agents for the treatment of Alzheimer's disease.
Modeling cyclooxygenase inhibition. Implication of active site hydration on the selectivity of ketoprofen analogues.
Conceptually new low-calcemic oxime analogues of the hormone 1 alpha,25-dihydroxyvitamin D(3): synthesis and biological testing.
Role of hydrophobic interactions in binding S-(N-aryl/alkyl-N-hydroxycarbamoyl)glutathiones to the active site of the antitumor target enzyme glyoxalase I.
3,5-Disubstituted-4-hydroxyphenyls linked to 3-hydroxy-2-methyl-4(1H)-pyridinone: potent inhibitors of lipid peroxidation and cell toxicity.
Novel agonists of 5HT2C receptors. Synthesis and biological evaluation of substituted 2-(indol-1-yl)-1-methylethylamines and 2-(indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder.
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain.
Viracept (nelfinavir mesylate, AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease.
Synthesis and evaluation of novel fluorinated methotrexate derivatives for application to rheumatoid arthritis treatment.
17 beta-(3-furyl)-5 beta-androstane-3 beta, 14 beta, 17 alpha-triol (PST 2238). A very potent antihypertensive agent with a novel mechanism of action.
NAcSDKP analogues resistant to angiotensin-converting enzyme.
Cyclic enkephalin analogues with exceptional potency and selectivity for delta-opioid receptors.
Novel non-nucleoside inhibitors of human immunodeficiency virus type 1 reverse transcriptase. 6. 2-Indol-3-yl- and 2-azaindol-3-yl-dipyridodiazepinones.
A novel series of [2-[methyl(2-phenethyl)amino]-2-oxoethyl] benzene-containing leukotriene B4 antagonists: initial structure-activity relationships.
Design and synthesis of phosphinamide-based hydroxamic acids as inhibitors of matrix metalloproteinases.
Identification of highly potent retinoic acid receptor alpha-selective antagonists.
Emerging therapies for the prevention or treatment of postmenopausal osteoporosis.
Enantiospecific semisynthesis of (+)-almuheptolide-A, a novel natural heptolide inhibitor of the mammalian mitochondrial respiratory chain.
Depsides and depsidones as inhibitors of HIV-1 integrase: discovery of novel inhibitors through 3D database searching.
Hexestrol-linked cytotoxic agents: synthesis and binding affinity for estrogen receptors.
Synthesis of naphthalenesulfonic acid small molecules as selective inhibitors of the DNA polymerase and ribonuclease H activities of HIV-1 reverse transcriptase.
Cardioselective antiischemic ATP-sensitive potassium channel openers. 4. Structure-activity studies on benzopyranylcyanoguanidines: replacement of the benzopyran portion.
A novel, picomolar inhibitor of human immunodeficiency virus type 1 protease.
Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.
Aspartyl alpha-((diphenylphosphinyl)oxy)methyl ketones as novel inhibitors of interleukin-1 beta converting enzyme. Utility of the diphenylphosphinic acid leaving group for the inhibition of cysteine proteases.
Non-peptidic inhibitors of human leukocyte elastase. 4. Design, synthesis, and in vitro and in vivo activity of a series of beta-carbolinone-containing trifluoromethyl ketones.
Structure-activity relationships of the antimalarial agent artemisinin. 2. Effect of heteroatom substitution at O-11: synthesis and bioassay of N-alkyl-11-aza-9-desmethylartemisinins.
Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity.
5-[(3-nitropyrid-2-yl)amino]indoles: novel serotonin agonists with selectivity for the 5-HT1D receptor. Variation of the C3 substituent on the indole template leads to increased 5-HT1D receptor selectivity.
Structure-based design of HIV-1 protease inhibitors: replacement of two amides and a 10 pi-aromatic system by a fused bis-tetrahydrofuran.
4-Amidinoindan-1-one 2'-amidinohydrazone: a new potent and selective inhibitor of S-Adenosylmethionine decarboxylase.
Novel binding mode of highly potent HIV-proteinase inhibitors incorporating the (R)-hydroxyethylamine isostere.
Structure-function studies in a series of carboxyl-terminal octapeptide analogues of anaphylatoxin C5a.
Renal vasodilators. The role of the 4-substituent in isoquinolin-3-ol cardiovascular agents: 4-ureido derivatives of isoquinolin-3-ol with selective renal vasodilator properties.
3-(5-Alkyl-4-hydroxy-3-methoxy-1-naphthalenyl)-2-methyl-2-propenoic acids as orally active inhibitors of IL-1 generation.
KDR Kinase Inhibitor Isolated from the Mushroom Boletopsis leucomelas.
Synthesis and antiviral activity of the enantiomeric forms of carba-5-iodo-2'-deoxyuridine and carba-(E)-5-(2-bromovinyl)-2'-deoxyuridine.
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 11. Quinolylmethyl analogues with basic substituents conveying specificity.
Dimethylsulfonium analogues of the muscarinic agent McN-A-343: [4-[[N-(3- or 4-halophenyl)carbamoyl]oxy]-2-butynyl] dimethylsulfonium perchlorates.
Synthesis and dopaminergic activity of 2-substituted octahydrobenzo[f]quinolines.
Synthesis and evaluation of the pharmacological activity of rigid analogues of sympathomimetic catecholamines derived from bicyclo[2.2.1]heptane.
(1-Pyrenylmethyl)amino alcohols, a new class of antitumor DNA intercalators. Discovery and initial amine side chain structure-activity studies.
N5-acetyl-N5-hydroxy-L-ornithine-derived siderophore-carbacephalosporin beta-lactam conjugates: iron transport mediated drug delivery.
New inhibitors of renin that contain novel phosphostatine Leu-Val replacements.
New 1-(heterocyclylalkyl)-4-(propionanilido)-4-piperidinyl methyl ester and methylene methyl ether analgesics.
Antimalarials. 16. Synthesis of 2-substituted analogues of 8-[(4-amino-1-methylbutyl)amino]-6-methoxy-4-methyl-5-[3- (trifluoromethyl)phenoxy]quinoline as candidate antimalarials.
BCX-1812 (RWJ-270201): discovery of a novel, highly potent, orally active, and selective influenza neuraminidase inhibitor through structure-based drug design.
bis-Quinolinium cyclophanes: 8,14-diaza-1,7(1, 4)-diquinolinacyclotetradecaphane (UCL 1848), a highly potent and selective, nonpeptidic blocker of the apamin-sensitive Ca(2+)-activated K(+) channel.
(S)-4-Methyl-2-(methylamino)pentanoic acid [4, 4-bis(4-fluorophenyl)butyl]amide hydrochloride, a novel calcium channel antagonist, is efficacious in several animal models of pain.
Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Synthesis, molecular modeling, and opioid receptor affinity of 9, 10-diazatricyclo[4.2.1.1(2,5)]decanes and 2,7-diazatricyclo[4.4.0. 0(3,8)]decanes structurally related to 3,8-diazabicyclo[3.2. 1]octanes.
New tetracyclic analogues of photochemotherapeutic drugs 5-MOP and 8-MOP: synthesis, DNA interaction, and antiproliferative activity.
Design, synthesis, and preliminary pharmacological evaluation of 1, 4-diazabicyclo[4.3.0]nonan-9-ones as a new class of highly potent nootropic agents.
A new class of potential chloroquine-resistance reversal agents for Plasmodia: syntheses and biological evaluation of 1-(3'-diethylaminopropyl)-3-(substituted phenylmethylene)pyrrolidines.
Anti-Helicobacter pylori agents. 4. 2-(Substituted guanidino)-4-phenylthiazoles and some structurally rigid derivatives.
GABA-Activated ligand gated ion channels: medicinal chemistry and molecular biology.
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.
Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
Protection against oxidative damage by iron chelators: effect of lipophilic analogues and prodrugs of N,N'-bis(3,4,5-trimethoxybenzyl)ethylenediamine- N,N'-diacetic acid (OR10141).
Antimitotic antitumor agents: synthesis, structure-activity relationships, and biological characterization of N-aryl-N'-(2-chloroethyl)ureas as new selective alkylating agents.
Synthesis and in vitro antitumor activity of new deaza analogues of the nonpolyglutamatable antifolate N(alpha)-(4-amino-4-deoxypteroyl)-N(delta)-hemiphthaloyl-L-ornithine (PT523).
New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring.
2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease.
Synthesis and in vitro pharmacology of a series of new chiral histamine H3-receptor ligands: 2-(R and S)-Amino-3-(1H-imidazol-4(5)-yl)propyl ether derivatives.
Structure-activity relationships of 2'-deoxy-2',2'-difluoro-L-erythro-pentofuranosyl nucleosides.
H3-receptor antagonists: synthesis and structure-activity relationships of para- and meta-substituted 4(5)-phenyl-2-[[2-[4(5)-imidazolyl]ethyl]thio]imidazoles.
Discovery of 3-aminobenzyloxycarbonyl as an N-terminal group conferring high affinity to the minimal phosphopeptide sequence recognized by the Grb2-SH2 domain.
Thermodynamic aspects of hydrophobicity and the blood-brain barrier permeability studied with a gel filtration chromatography.
Sustained decrease in cocaine-maintained responding in rhesus monkeys with 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-hydroxy-3-phenylpropyl) piperazinyl decanoate, a long-acting ester derivative of GBR 12909.
Structure-activity relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.
A new candidate for an anti-HIV-1 agent: modified cyclodextrin sulfate (mCDS71).
N-(carboxymethyl)-N-[3,5-bis(decyloxy)-phenyl]glycine (Ro 23-9358): a potent inhibitor of secretory phospholipases A2 with antiinflammatory activity.
Inhibition of herpes simplex virus type 1 ribonucleotide reductase by substituted tetrapeptide derivatives.
(3SR,4aRS,6RS,8aRS)-6-[2-(1H-tetrazol-5-yl)ethyl]decahydroisoquinoline-3 - carboxylic acid: a structurally novel, systemically active, competitive AMPA receptor antagonist.
Preparation and pharmacological evaluation of enantiomers of certain nonoxygenated aporphines: (+)- and (-)-aporphine and (+)- and (-)-10-methylaporphine.
Bis(heteroaryl)piperazine (BHAP) reverse transcriptase inhibitors: structure-activity relationships of novel substituted indole analogues and the identification of 1-[(5-methanesulfonamido-1H-indol-2-yl)-carbonyl]-4-[3- [(1-methylethyl)amino]-pyridinyl]piperazine monomethanesulfonate (U-90152S), a second-generation clinical candidate.
Synthesis of 2-imidazolidinylidenepropanedinitrile derivatives as stimulators of gastrointestinal motility.
Synthesis of oxadiazolidinedione derivatives as quisqualic acid analogues and their evaluation at a quisqualate-sensitized site in the rat hippocampus.
Synthesis, NMDA receptor antagonist activity, and anticonvulsant action of 1-aminocyclobutanecarboxylic acid derivatives.
Rational modification of human synovial fluid phospholipase A2 inhibitors.
The discovery of sulfonamide endothelin antagonists and the development of the orally active ETA antagonist 5-(dimethylamino)-N-(3,4-dimethyl-5-isoxazolyl)-1-naphthalenesulf onamide.
3-Substituted, 3-(4-pyridinylmethyl)-1,3-dihydro-1-phenyl-2H-indol-2-ones as acetylcholine release enhancers: synthesis and SAR.
Toward a novel metal-based chemotherapy against tropical diseases. 1. Enhancement of the efficacy of clotrimazole against Trypanosoma cruzi by complexation to ruthenium in RuCl2(clotrimazole)2.
Novel [2-(4-piperidinyl)ethyl](thio)ureas: synthesis and antiacetylcholinesterase activity.
Tetrapeptide CCK agonists: structure-activity studies on modifications at the N-terminus.
A structure-activity study of four dopamine D-1 and D-2 receptor antagonists, representing the phenylindan, -indene, and -indole structural classes of compounds.
Dibenzoxepin derivatives: thromboxane A2 synthase inhibition and thromboxane A2 receptor antagonism combined in one molecule.
N-(4-Isoxazolylthiazol-2-yl)oxamic acid derivatives as potent orally active antianaphylactic agents.
Carboxyalkyl dipeptides with atrial natriuretic factor potentiating and antihypertensive activity.
2 beta-substituted analogues of cocaine. Synthesis and inhibition of binding to the cocaine receptor.
Synthesis and antibacterial activity of 1-(substituted pyrrolyl)-7-(substituted amino)-6-fluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids.
Terpenoids and a flavonoid glycoside from Acacia pennata leaves as hedgehog/GLI-mediated transcriptional inhibitors.
Phosphorus-containing inhibitors of HMG-CoA reductase. 2. Synthesis and biological activities of a series of substituted pyridines containing a hydroxyphosphinyl moiety.
Structural studies on bioactive compounds. 8. Synthesis, crystal structure, and biological properties of a new series of 2,4-diamino-5-aryl-6-ethylpyrimidine dihydrofolate reductase inhibitors with in vivo activity against a methotrexate-resistant tumor cell line.
Perfluorinated analogues of poison ivy allergens. Synthesis and skin tolerogenic activity in mice.
Design and conformational analysis of several highly potent bradykinin receptor antagonists.
Peptide to glycopeptide: glycosylated oligopeptide renin inhibitors with attenuated in vivo clearance properties.
Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent.
HIV protease: a novel chemotherapeutic target for AIDS.
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 4. Addition of chromone moiety enhances leukotriene D4 receptor binding affinity.
Using theoretical descriptors in quantitative structure-activity relationships: some toxicological indices.
Synthesis and siderophore activity of albomycin-like peptides derived from N5-acetyl-N5-hydroxy-L-ornithine.
Boron-containing thiouracil derivatives for neutron-capture therapy of melanoma.
Cysteine protease inhibition by azapeptide esters.
Discovery of novel and potent retinoic acid receptor alpha agonists: syntheses and evaluation of benzofuranyl-pyrrole and benzothiophenyl-pyrrole derivatives.
Design, synthesis, and biological evaluation of potent and selective amidino bicyclic factor Xa inhibitors.
Design, synthesis, SAR, and biological evaluation of highly potent benzimidazole-spaced phosphono-alpha-amino acid competitive NMDA antagonists of the AP-6 type.
A novel series of 4-piperidinopyridine and 4-piperidinopyrimidine inhibitors of 2,3-oxidosqualene cyclase-lanosterol synthase.
Inhibition of protein-protein association by small molecules: approaches and progress.
Synthesis of new dihydroindeno[1,2-c]isoquinoline and indenoisoquinolinium chloride topoisomerase I inhibitors having high in vivo anticancer activity in the hollow fiber animal model.
Biarylpropylsulfonamides as novel, potent potentiators of 2-amino-3- (5-methyl-3-hydroxyisoxazol-4-yl)- propanoic acid (AMPA) receptors.
Inhibition of protein synthesis by didemnins: cell potency and SAR.
Discovery of (2S)-1-(4-amino-2,3,5- trimethylphenoxy)-3-[4-[4-(4- fluorobenzyl)phenyl]-1-piperazinyl]-2-propanol dimethanesulfonate (SUN N8075): a dual Na(+) and Ca(2+) channel blocker with antioxidant activity.
Caspases as targets for anti-inflammatory and anti-apoptotic drug discovery.
Nonnucleoside human cytomegalovirus inhibitors: synthesis and antiviral evaluation of (chlorophenylmethyl)benzothiadiazine dioxide derivatives.
Bioactive pseudopeptidic analogues and cyclostereoisomers of osteogenic growth peptide C-terminal pentapeptide, OGP(10-14).
Antitumor agents. 207. Design, synthesis, and biological testing of 4beta-anilino-2-fluoro-4'-demethylpodophyllotoxin analogues as cytotoxic and antiviral agents.
Design, synthesis, and evaluation of opioid analogues with non-peptidic beta-turn scaffold: enkephalin and endomorphin mimetics.
Design, synthesis, and discovery of novel trans-stilbene analogues as potent and selective human cytochrome P450 1B1 inhibitors.
The squalestatins: inhibitors of squalene synthase. Enzyme inhibitory activities and in vivo evaluation of C3-modified analogues.
Monoaryl- and bisaryldihydroxytropolones as potent inhibitors of inositol monophosphatase.
Structure-activity studies on anticonvulsant sugar sulfamates related to topiramate. Enhanced potency with cyclic sulfate derivatives.
Synthesis, molecular modeling, and K+ channel-blocking activity of dequalinium analogues having semirigid linkers.
Thrombus imaging using technetium-99m-labeled high-potency GPIIb/IIIa receptor antagonists. Chemistry and initial biological studies.
Synthesis of C3 heteroatom-substituted azetidinones that display potent cholesterol absorption inhibitory activity.
Synthesis of 3 beta-aryl-8-azabicyclo[3.2.1]octanes with high binding affinities and selectivities for the serotonin transporter site.
Development of a high specific activity sulfur-35-labeled sulfonamide radioligand that allowed the identification of a new growth hormone secretagogue receptor.
Synthesis of acyclo-C-nucleosides in the imidazo[1,2-a]pyridine and pyrimidine series as antiviral agents.
Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.
Synthesis, activity, and structure--activity relationship studies of novel cationic lipids for DNA transfer.
Design and synthesis of 2',3'-dideoxy-2',3'-didehydro-beta-L-cytidine (beta-L-d4C) and 2',3'-dideoxy 2',3'-didehydro-beta-L-5-fluorocytidine (beta-L-Fd4C), two exceptionally potent inhibitors of human hepatitis B virus (HBV) and potent inhibitors of human immunodeficiency virus (HIV) in vitro.
Synthesis and activity against multidrug resistance in Chinese hamster ovary cells of new acridone-4-carboxamides.
Studies directed toward the design of orally active renin inhibitors. 2. Development of the efficacious, bioavailable renin inhibitor (2S)-2-benzyl-3- [[(1-methylpiperazin-4-yl)sulfonyl]propionyl]-3-thiazol-4-yl-L-alanine amide of (2S,3R,4S)-2-amino-1-cyclohexyl-3,4-dihydroxy-6-methylheptane (A-72517).
Solvent-dependent conformation and hydrogen-bonding capacity of cyclosporin A: evidence from partition coefficients and molecular dynamics simulations.
Synthesis and structure-activity relationships of naphthalene-substituted derivatives of the allylamine antimycotic terbinafine.
Synthesis of phosphocholine and quaternary amine ether lipids and evaluation of in vitro antineoplastic activity.
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
Enantioselectivity of cocaine recognition sites: binding of (1S)- and (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)tropane (beta-CIT) to monoamine transporters.
Estrone sulfamates: potent inhibitors of estrone sulfatase with therapeutic potential.
Design and synthesis of peptidomimetic inhibitors of HIV-1 protease and renin. Evidence for improved transport.
Leukotriene B4 (LTB4) receptor antagonists: a series of (hydroxyphenyl)pyrazoles.
Synthesis and metabotropic receptor activity of the novel rigidified glutamate analogues (+)- and (-)-trans-azetidine-2,4-dicarboxylic acid and their N-methyl derivatives.
Plant antitumor agents. 30. Synthesis and structure activity of novel camptothecin analogs.
Quantitative structure-activity relationships of the inhibition of Pneumocystis carinii dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(X-phenyl)-s-triazines.
4-Deacetyltaxol and 10-acetyl-4-deacetyltaxotere: synthesis and biological evaluation.
8-Substituted O6-benzylguanine, substituted 6(4)-(benzyloxy)pyrimidine, and related derivatives as inactivators of human O6-alkylguanine-DNA alkyltransferase.
Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: orally active iron chelators with clinical potential.
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
Dopamine autoreceptor agonists as potential antipsychotics. 2. (Aminoalkoxy)-4H-1-benzopyran-4-ones.
Positional effects of sulfation in hirudin and hirudin PA related anticoagulant peptides.
Enzymatic synthesis and comparative biological evaluation of a phosphonate analogue of the lipid A precursor.
Potent inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Asp-carboxylate of RGDX mimetics and the platelet GP IIb-IIIa receptor.
Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics.
Ester and amide derivatives of E64c as inhibitors of platelet calpains.
Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists.
Nucleosides and nucleotides. 100. 2'-C-cyano-2'-deoxy-1-beta-D-arabinofuranosyl-cytosine (CNDAC): design of a potential mechanism-based DNA-strand-breaking antineoplastic nucleoside.
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases.
Synthesis and estrogen receptor binding of novel 11 beta-substituted estra-1,3,5(10)-triene-3,17 beta-diols.
Analogues of natural phloroglucinols as antagonists against both thromboxane A2 and leukotriene D4.
Molecular determinants of MAO selectivity in a series of indolylmethylamine derivatives: biological activities, 3D-QSAR/CoMFA analysis, and computational simulation of ligand recognition.
Structure-activity relationships of (E)-5-(2-bromovinyl)uracil and related pyrimidine nucleosides as antiviral agents for herpes viruses.
Design and synthesis of potent C(2)-symmetric diol-based HIV-1 protease inhibitors: effects of fluoro substitution.
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
New neplanocin analogues. 12. Alternative synthesis and antimalarial effect of (6'R)-6'-C-methylneplanocin A, a potent AdoHcy hydrolase inhibitor.
Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
Hunting the emesis and efficacy targets of PDE4 inhibitors: identification of the photoaffinity probe 8-(3-azidophenyl)-6- [(4-iodo-1H-1-imidazolyl)methyl]quinoline (APIIMQ).
5-[1'-(2'-N-Arylsulfonyl-1',2',3',4'-tetrahydroisoquinolyl)]-4, 5-dihydro-2(3H)-furanones: positive allosteric modulators of the GABA(A) receptor with a new mode of action.
Development of novel quinone phosphorodiamidate prodrugs targeted to DT-diaphorase.
Non-amidine-containing 1,2-dibenzamidobenzene inhibitors of human factor Xa with potent anticoagulant and antithrombotic activity.
Synthesis of 1-(3,4-dihydroxy-5-nitrophenyl)-2-phenyl-ethanone and derivatives as potent and long-acting peripheral inhibitors of catechol-O-methyltransferase.
Synthesis of 2-amino-5-sulfanyl-1,3,4-thiadiazole derivatives and evaluation of their antidepressant and anxiolytic activity.
Crystal structure of human cyclin-dependent kinase 2 in complex with the adenine-derived inhibitor H717.
4-Amino-2-[4-[1-(benzyloxycarbonyl)-2(S)- [[(1,1-dimethylethyl)amino]carbonyl]-piperazinyl]-6, 7-dimethoxyquinazoline (L-765,314): a potent and selective alpha1b adrenergic receptor antagonist.
Structure-based design of HIV protease inhibitors: sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors.
Design and synthesis of histidine analogues of folic acid and methotrexate as potential folylpolyglutamate synthetase inhibitors.
Homology modeling of metabotropic glutamate receptors. (mGluRs) structural motifs affecting binding modes and pharmacological profile of mGluR1 agonists and competitive antagonists.
Design and synthesis of enantiomers of 3,5-dinitro-o-tyrosine: alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonists.
HIV protease inhibitory bis-benzamide cyclic ureas: a quantitative structure-activity relationship analysis.
Design and synthesis of malonic acid-based inhibitors of human neutrophil collagenase (MMP8).
3 alpha-(4'-substituted phenyl)tropane-2 beta-carboxylic acid methyl esters: novel ligands with high affinity and selectivity at the dopamine transporter.
Comparative molecular field analysis of haptens docked to the multispecific antibody IgE(Lb4)
Potent and selective ligands for the dopamine transporter (DAT): structure-activity relationship studies of novel 4-[2-(diphenylmethoxy)ethyl]-1-(3-phenylpropyl)piperidine analogues.
Effects of alpha- and beta-galactosylated C2-ceramides on the immune system.
Synthesis and in vitro characterization of N-[5-(4,5-dihydro-1H-imidazol-2-yl)-2-hydroxy-5,6,7,8- tetrahydronaphthalen-1-yl]methanesulfonamide and its enantiomers: a novel selective alpha 1A receptor agonist.
Mapping the aspartic acid binding site of Escherichia coli asparagine synthetase B using substrate analogs.
Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors.
Synthesis, chemical reactivity, and antitumor evaluation of congeners of carmethizole hydrochloride, an experimental "acylated vinylogous carbinolamine" tumor inhibitor.
Structure-activity relationship within a series of pyrazolidinone antibacterial agents. 2. Effect of side-chain modification on in vitro activity and pharmacokinetic parameters.
Bis-catechol-substituted redox-reactive analogues of hexamethonium and decamethonium: stimulated affinity-dependent reactivity through iron peroxide catalysis.
(S)-N-tert-butyl-3-(4-(2-methoxyphenyl)-piperazin-1-yl)-2-phenylpropanamide [(S)-WAY-100135]: a selective antagonist at presynaptic and postsynaptic 5-HT1A receptors.
Orally active water-soluble N,O-acyl transfer products of a beta,gamma-bishydroxyl amide containing renin inhibitor.
Structure-based design of inhibitors of purine nucleoside phosphorylase. 2. 9-Alicyclic and 9-heteroalicyclic derivatives of 9-deazaguanine.
Synthesis and antineoplastic activity of 1a-formyl and 1a-thioformyl derivatives of mitomycin C and 2-methylaziridine.
N-omega-fluoroalkyl analogs of (1R)-2 beta-carbomethoxy-3 beta-(4-iodophenyl)-tropane (beta-CIT): radiotracers for positron emission tomography and single photon emission computed tomography imaging of dopamine transporters.
2-(3,4-Dichlorophenyl)-N-methyl-N-[(1S)-1-(3-isothiocyanatophenyl)-2-(1-pyrrolidinyl)ethyl]acetamide: an opioid receptor affinity label that produces selective and long-lasting kappa antagonism in mice.
Derivatives of cis-2-amino-8-hydroxy-1-methyltetralin: mixed 5-HT1A-receptor agonists and dopamine D2-receptor antagonists.
Cyclic GMP phosphodiesterase inhibitors. 1. The discovery of a novel potent inhibitor, 4-((3,4-(methylenedioxy)benzyl)amino)-6,7,8-trimethoxyquinazoline.
Synthesis and anti-HIV evaluation of D4T and D4T 5'-monophosphate prodrugs.
Anticonvulsant activities of some arylsemicarbazones displaying potent oral activity in the maximal electroshock screen in rats accompanied by high protection indices.
Benzisoxazole- and benzisothiazole-3-carboxamides as potential atypical antipsychotic agents.
Homodimeric and heterodimeric bis(amino thiol) oxometal complexes with rhenium(V) and technetium(V). Control of heterodimeric complex formation and an approach to metal complexes that mimic steroid hormones.
Synthesis and pharmacological evaluation of a series of dibenzo[a,d]cycloalkenimines as N-methyl-D-aspartate antagonists.
Reversible inhibitors of the gastric (H+/K+)-ATPase. 1. 1-Aryl-4-methylpyrrolo[3,2-c]quinolines as conformationally restrained analogues of 4-(arylamino)quinolines.
Potential antimitotic agents. Synthesis of some ethyl benzopyrazin-7-ylcarbamates, ethyl pyrido[3,4-b]pyrazin-7-ylcarbamates, and ethyl pyrido[3,4-e]-as-triazin-7-ylcarbamates.
Aldosterone antagonists. 3. Synthesis and activities of steroidal 7 alpha-(alkoxycarbonyl)-15,16-methylene spirolactones.
Synthesis and antirhinovirus activity of 8-substituted analogues of 6-(dimethylamino)-9-(4-methylbenzyl)-2-(trifluoromethyl)-9H-purine.
Potential antitumor agents. 59. Structure-activity relationships for 2-phenylbenzimidazole-4-carboxamides, a new class of "minimal" DNA-intercalating agents which may not act via topoisomerase II.
2,4-Dihydro-3H-1,2,4-triazol-3-ones as anticonvulsant agents.
Phosphorus-containing inhibitors of HMG-CoA reductase. 1. 4-[(2-arylethyl)hydroxyphosphinyl]-3-hydroxy-butanoic acids: a new class of cell-selective inhibitors of cholesterol biosynthesis.
Mechanism and inhibition of cytochrome P-450 aromatase.
Relaxant activity of 4-amido-3,4-dihydro-2H-1-benzopyran-3-ols and 4-amido-2H-1-benzopyrans on guinea pig isolated trachealis.
Receptor ligands which bind the oxytocin receptor with selectivity and high affinity. Chemical modification of a Streptomyces silvensis derived cyclic hexapeptide.
Total synthesis of the four stereoisomers of dihexadecanoyl phosphatidylinositol and the substrate stereospecificity of human erythrocyte membrane phosphatidylinositol 4-kinase.
Synthesis and receptor binding of enantiomeric N-substituted cis-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexylamines as high-affinity sigma receptor ligands.
Cyclization-activated prodrugs. Basic carbamates of 4-hydroxyanisole.
Prodrugs for amidines: synthesis and anti-Pneumocystis carinii activity of carbamates of 2,5-bis(4-amidinophenyl)furan.
(4-[18F]fluoro-3-iodobenzyl)guanidine, a potential MIBG analogue for positron emission tomography.
Alpha(2) adrenoceptor agonists as potential analgesic agents. 3. Imidazolylmethylthiophenes.
Nucleosides and nucleotides. 175. Structural requirements of the sugar moiety for the antitumor activities of new nucleoside antimetabolites, 1-(3-C-ethynyl-beta-D-ribo-pentofuranosyl)cytosine and -uracil1.
Synthesis and structure-activity relationships of peptidyl alpha-keto heterocycles as novel inhibitors of prolyl endopeptidase.
A ureido-thioisobutyric acid (GW9578) is a subtype-selective PPARalpha agonist with potent lipid-lowering activity.
Discovery and optimization of a novel series of thrombin receptor (par-1) antagonists: potent, selective peptide mimetics based on indole and indazole templates.
Inhibition of topoisomerase I by anthracycline antibiotics: evidence for general inhibition of topoisomerase I by DNA-binding agents.
ATP-Citrate lyase as a target for hypolipidemic intervention. 2. Synthesis and evaluation of (3R,5S)-omega-substituted-3-carboxy-3, 5-dihydroxyalkanoic acids and their gamma-lactone prodrugs as inhibitors of the enzyme in vitro and in vivo.
Design and synthesis of lipophilic phosphoramidate d4T-MP prodrugs expressing high potency against HIV in cell culture: structural determinants for in vitro activity and QSAR.
Novel antidiabetic and hypolipidemic agents. 5. Hydroxyl versus benzyloxy containing chroman derivatives.
Structure-activity relationships and molecular modeling analysis of flavonoids binding to the benzodiazepine site of the rat brain GABA(A) receptor complex.
Derivatives of (R)- and (S)-5-fluoro-8-hydroxy-2-(dipropylamino)tetralin: synthesis and interactions with 5-HT1A receptors.
Buspirone analogues as ligands of the 5-HT1A receptor. 1. The molecular structure of buspirone and its two analogues.
Highly selective aldose reductase inhibitors. 1. 3-(Arylalkyl)-2,4,5-trioxoimidazolidine-1-acetic acids.
Design, synthesis, and biological evaluation of conformationally constrained aci-reductone mimics of arachidonic acid.
Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
Synthesis, physicochemical properties, and biological evaluation of hydroxypyranones and hydroxypyridinones: novel bidentate ligands for cell-labeling.
Toward a novel metal-based chemotherapy against tropical diseases. 3. Synthesis and antimalarial activity in vitro and in vivo of the new gold-chloroquine complex [Au(PPh3)(CQ)]PF6.
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles.
d-Fused [1]benzazepines with selective in vitro antitumor activity: synthesis and structure-activity relationships.
Synthesis and evaluation of N-(phenylacetyl)trifluoromethanesulfonamides as anticonvulsant agents.
Design, synthesis, and evaluation of the multidrug resistance-reversing activity of D-glucose mimetics of hapalosin.
Synthesis of a photoaffinity analog of taxol as an approach to identify the taxol binding site on microtubules.
Benzoxazolamines and benzothiazolamines: potent, enantioselective inhibitors of leukotriene biosynthesis with a novel mechanism of action.
Specific inhibitors of ileal bile acid transport.
Mechanism-based isocoumarin inhibitors for human leukocyte elastase. Effect of the 7-amino substituent and 3-alkoxy group in 3-alkoxy-7-amino-4-chloroisocoumarins on inhibitory potency.
Novel heterocyclic analogues of the new potent class of calcium entry blockers: 1-[[4-(aminoalkoxy)phenyl]sulfonyl]indolizines.
Application of a conformationally restricted Phe-Leu dipeptide mimetic to the design of a combined inhibitor of angiotensin I-converting enzyme and neutral endopeptidase 24.11.
Synthesis and kappa-opioid antagonist selectivity of a norbinaltorphimine congener. Identification of the address moiety required for kappa-antagonist activity.
Synthesis and biological activity of spirocyclic benzopyran imidazolone potassium channel openers.
Discovery of a potent, peripherally selective trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonist for the treatment of gastrointestinal motility disorders.
Novel 3 alpha-(diphenylmethoxy)tropane analogs: potent dopamine uptake inhibitors without cocaine-like behavioral profiles.
X-ray crystal structure, partitioning behavior, and molecular modeling study of piracetam-type nootropics: insights into the pharmacophore.
Anti-human immunodeficiency virus and anti-hepatitis-B virus activities and toxicities of the enantiomers of 2'-deoxy-3'-oxa-4'-thiocytidine and their 5-fluoro analogues in vitro.
Structure-activity relationship studies at the benzodiazepine receptor (BZR): a comparison of the substitutent effects of pyrazoloquinolinone analogs.
Novel potassium channel openers: synthesis and pharmacological evaluation of new N-(substituted-3-pyridyl)-N'-alkylthioureas and related compounds.
Cardioselective anti-ischemic ATP-sensitive potassium channel openers.
Three-dimensional quantitative structure-activity relationship (QSAR) of HIV integrase inhibitors: a comparative molecular field analysis (CoMFA) study.
Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships.
5-(5-Bromothien-2-yl)-2'-deoxyuridine and 5-(5-chlorothien-2-yl)-2'-deoxyuridine are equipotent to (E)-5-(2-bromovinyl)-2'-deoxyuridine in the inhibition of herpes simplex virus type I replication.
Synthesis and antimalarial activity of 2-aziridinyl- and 2,3-bis(aziridinyl)-1,4-naphthoquinonyl sulfonate and acylate derivatives.
Structure-activity study of hCGRP8-37, a calcitonin gene-related peptide receptor antagonist.
A new class of acyclic phosphonate nucleotide analogues: phosphonate isosteres of acyclovir and ganciclovir monophosphates as antiviral agents.
7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4-dihydro-8- propyl-2H-1-benzopyran-2-carboxylic acid: an orally active selective leukotriene B4 receptor antagonist.
Synthesis and biological activity of 2'-deoxy-4'-thio pyrimidine nucleosides.
Targeting renal dipeptidase (dehydropeptidase I) for inactivation by mechanism-based inactivators.
Isoprenyl phosphinylformates: new inhibitors of squalene synthetase.
The synthesis and potassium channel blocking activity of some (4-methanesulfonamidophenoxy)propanolamines as potential class III antiarrhythmic agents.
On the optimization of hydrophobic and hydrophilic substituent interactions of 2,4-diamino-5-(substituted-benzyl)pyrimidines with dihydrofolate reductase.
Stereospecific synthesis, assignment of absolute configuration, and biological activity of the enantiomers of 3-[[[3-[2-(7-chloroquinolin-2-yl)-(E)-ethenyl]phenyl] [[3-(dimethylamino)-3-oxopropyl]thio]methyl]thio]propionic acid, a potent and specific leukotriene D4 receptor antagonist.
3',3'-Difluoro-3'-deoxythymidine: comparison of anti-HIV activity to 3'-fluoro-3'-deoxythymidine.
Synthesis and antiviral activity of 5-heteroaryl-substituted 2'-deoxyuridines.
Novel synthesis and biochemical properties of an [125I]-labeled photoaffinity probe for thromboxane A2/prostaglandin H2 receptors.
Synthesis and resolution of (+-)-7-chloro-8-hydroxy-1-(3'-iodophenyl)-3-methyl-2,3,4,5-tetrahydro- 1H-3- benzazepine (TISCH): a high affinity and selective iodinated ligand for CNS D1 dopamine receptor.
4-Aryl-2,4-dioxobutanoic acid inhibitors of HIV-1 integrase and viral replication in cells.
Synthesis of apicidin-derived quinolone derivatives: parasite-selective histone deacetylase inhibitors and antiproliferative agents.
Heteroaryl-fused 2-phenylisothiazolone inhibitors of cartilage breakdown.
Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation.
Cyclic HIV protease inhibitors: design and synthesis of orally bioavailable, pyrazole P2/P2' cyclic ureas with improved potency.
Synthesis and evaluation of 4-(2'-methoxyphenyl)-1-[2'-[N-(2"-pyridinyl)-p- iodobenzamido]ethyl]piperazine (p-MPPI): a new iodinated 5-HT1A ligand.
Studies on the mechanism of decomposition and structural factors affecting the aqueous stability of 1,2-bis(sulfonyl)-1-alkylhydrazines.
4-[5-Methyl-3-phenylisoxazol-4-yl]- benzenesulfonamide, valdecoxib: a potent and selective inhibitor of COX-2.
Dual function glutamate-related ligands: discovery of a novel, potent inhibitor of glutamate carboxypeptidase II possessing mGluR3 agonist activity.
Heterodimeric tacrine-based acetylcholinesterase inhibitors: investigating ligand-peripheral site interactions.
Synthesis, binding properties, and 18F labeling of fluorocarazolol, a high-affinity beta-adrenergic receptor antagonist.
Urea-PETT compounds as a new class of HIV-1 reverse transcriptase inhibitors. 3. Synthesis and further structure-activity relationship studies of PETT analogues.
Discovery of chiral N,N-disubstituted trifluoro-3-amino-2-propanols as potent inhibitors of cholesteryl ester transfer protein.
New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: synthesis and anti-HIV evaluation.
High-resolution X-ray crystallography reveals precise binding interactions between human nonpancreatic secreted phospholipase A2 and a highly potent inhibitor (FPL67047XX).
Synthesis and pharmacology of a very potent cannabinoid lacking a phenolic hydroxyl with high affinity for the CB2 receptor.
New neplanocin analogues. 7. Synthesis and antiviral activity of 2-halo derivatives of neplanocin A.
Potent inhibition of tumor necrosis factor-alpha production by tetrafluorothalidomide and tetrafluorophthalimides.
Identification of a retinoic acid receptor alpha subtype specific agonist.
Ryanodine action at calcium release channels. 1. importance of hydroxyl substituents.
Chromophore-modified bis-naphthalimides: synthesis and antitumor activity of bis-dibenz[de,h]isoquinoline-1,3-diones.
Modulators of leukotriene biosynthesis and receptor activation.
Antimicrobial alpha, alpha-dialkylated amino acid rich peptides with in-vivo activity against an intracellular pathogen.
The chemistry of pseudomonic acid. 17. Dual-action C-1 oxazole derivatives of pseudomonic acid having an extended spectrum of antibacterial activity.
Structure-activity relationships for acridine-substituted analogues of the mixed topoisomerase I/II inhibitor N-[2-(dimethylamino)ethyl]acridine-4-carboxamide.
Structure-activity relationships in a series of substituted indolocarbazoles: topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties.
Synthesis and evaluation of aryl-substituted N-(arylethyl)-N-methyl-2-(1-pyrrolidinyl)ethylamines and corresponding arylacetamides for sigma receptor affinity.
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.
New non-peptide endothelin-A receptor antagonists: synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-,-N-pyrimidinyl-,-N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides.
Potent quinoxaline-spaced phosphono alpha-amino acids of the AP-6 type as competitive NMDA antagonists: synthesis and biological evaluation.
Active site-directed synthetic thrombin inhibitors: synthesis, in vitro and in vivo activity profile of BMY 44621 and analogs. An examination of the role of the amino group in the D-Phe-Pro-Arg-H series.
3-Tetrahydrofuran and pyran urethanes as high-affinity P2-ligands for HIV-1 protease inhibitors.
Antitumor agents. 3. Synthesis and biological activity of 4 beta-alkyl derivatives containing hydroxy, amino, and amido groups of 4'-O-demethyl-4-desoxypodophyllotoxin as antitumor agents.
N-(1-methyl-5-indolyl)-N'-(3-methyl-5-isothiazolyl)urea: a novel, high-affinity 5-HT2B receptor antagonist.
Cosalane analogues with enhanced potencies as inhibitors of HIV-1 protease and integrase.
Deoxygenated inositol 1,4,5-trisphosphate analogues and their interaction with metabolic enzymes. (1R,2R,4R)-cyclohexane-1,2,4-tris(methylenesulfonate): a potent selective 5-phosphatase inhibitor.
Effects of solvation on the ionization and conformation of raclopride and other antidopaminergic 6-methoxysalicylamides: insight into the pharmacophore.
Synthesis and antitumor activity of isodoxorubicin analogues.
Synthesis and biological activity of thiazolylindolequinones, analogues of the natural product BE 10988.
Inhibition of human neutrophil elastase with peptidyl electrophilic ketones. 2. Orally active PG-Val-Pro-Val pentafluoroethyl ketones.
Design of thymidylate synthase inhibitors using protein crystal structures: the synthesis and biological evaluation of a novel class of 5-substituted quinazolinones.
Amidinium cation as a mimic of allylic carbocation: synthesis and squalene synthetase inhibitory activity of an amidinium analog of a carbocation intermediate.
GC sequence specific recognition by an N-formamido, C-terminus-modified and imidazole-containing analogue of netropsin.
1,2,3-Triazole-[2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D- ribofuranosyl]-3'-spiro-5"-(4"-amino-1",2"-oxathiole 2",2"-dioxide) (TSAO) analogues: synthesis and anti-HIV-1 activity.
Alfred Burger Award address. A half century in medicinal chemistry with major emphasis on pain-relieving drugs and their antagonists.
Reevaluating equilibrium and kinetic binding parameters for lipophilic drugs based on a structural model for drug interaction with biological membranes.
Effect of hydroxyl group configuration in hydroxyethylamine dipeptide isosteres on HIV protease inhibition. Evidence for multiple binding modes.
Synthesis and biological activity of 5-alkyl-1,7,8-trisubstituted-6-fluoroquinoline-3-carboxylic acids.
Synthesis and cytotoxicity studies of 8-amino-6-methyl-2-beta-D-ribofuranosyl-1,2,3,5,6,7-hexaazaacenaphthyle ne (7-aza-TCN) and the corresponding 2'-deoxy- and arabinonucleoside analogues.
Studies on neurokinin antagonists. 1. The design of novel tripeptides possessing the glutaminyl-D-tryptophylphenylalanine sequence as substance P antagonists.
Synthesis and serotonergic pharmacology of the enantiomers of 3-[(N-methylpyrrolidin-2-yl)methyl]-5-methoxy-1H-indole: discovery of stereogenic differentiation in the aminoethyl side chain of the neurotransmitter serotonin.
Carbohydrate materials bearing neuraminidase-resistant C-glycosides of sialic acid strongly inhibit the in vitro infectivity of influenza virus.
Iodinated tomoxetine derivatives as selective ligands for serotonin and norepinephrine uptake sites.
7,8-Dihydro-8-ethyl-2-(3-noradamantyl)-4-propyl-1H-imidazo[2,1-i]purin-5(4H)-one: a potent and water-soluble adenosine A1 antagonist.
A dideazatetrahydrofolate analogue lacking a chiral center at C-6, N-[4-[2-(2-amino-3,4-dihydro-4-oxo-7H-pyrrolo[2,3-d]pyrimidin-5- yl)ethyl]benzoyl]-L-glutamic acid, is an inhibitor of thymidylate synthase.
3-(2-carboxyindol-3-yl)propionic acid derivatives: antagonists of the strychnine-insensitive glycine receptor associated with the N-methyl-D-aspartate receptor complex.
Stereospecificity of amino acid side chains in deltorphin defines binding to opioid receptors.
Adenosine receptors: pharmacology, structure-activity relationships, and therapeutic potential.
4-Oxospiro[benzopyran-2,4'-piperidines] as class III antiarrhythmic agents. Pharmacological studies on 3,4-dihydro-1'-[2-(benzofurazan-5-yl)- ethyl]-6-methanesulfonamidospiro[(2H)-1-benzopyran-2,4'-piperidin]-4-on e (L-691,121).
Nonpeptide angiotensin II antagonists: N-phenyl-1H-pyrrole derivatives are angiotensin II receptor antagonists.
A remarkable change of opioid receptor selectivity on the attachment of a peptidomimetic kappa address element to the delta antagonist, natrindole: 5'-[N2-alkylamidino)methyl]naltrindole derivatives as a novel class of kappa opioid receptor antagonists.
Chemistry and pharmacology of the non-benzodiazepine anxiolytic enciprazine and related compounds.
Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of [beta-(Aroylamino)ethyl]piperazines and -piperidines and [2-[(Arylamino)carbonyl]ethyl]piperazines, -pyrazinopyridoindoles, and -pyrazinoisoquinolines. A new class of potent H1 antagonists.
(1R,3S)-1-(aminomethyl)-3,4-dihydro-5,6-dihydroxy-3-phenyl-1H-2-benzopyran: a potent and selective D1 agonist.
3-Phenyl analogues of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]-methyl]-1,4-benzodioxan (WB 4101) as highly selective alpha 1-adrenoceptor antagonists.
Anti-AIDS agents. 42. Synthesis and anti-HIV activity of disubstituted (3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone analogues.
X-Ray structure of citrate bound to Src SH2 leads to a high-affinity, bone-targeted Src SH2 inhibitor.
Synthesis and biological evaluation of the first N-alkyl cage dimeric 4-aryl-1,4-dihydropyridines as novel nonpeptidic HIV-1 protease inhibitors.
Structure-activity relationships of novel 2-substituted quinazoline antibacterial agents.
Synthesis of new cyclitol compounds that influence the activity of phosphatidylinositol 4-kinase isoform, PI4K230.
seco-Cyclothialidines: new concise synthesis, inhibitory activity toward bacterial and human DNA topoisomerases, and antibacterial properties.
Synthesis and pharmacological evaluation of some 8-cyanopyrido[3', 2':4,5]thieno[3,2-d]triazine derivatives as inhibitors of nitric oxide and eicosanoid biosynthesis.
N4-(omega-Aminoalkyl)-1-[(omega-aminoalkyl)amino]-4- acridinecarboxamides: novel, potent, cytotoxic, and DNA-binding agents.
Nonpeptide cholecystokinin-2 receptor agonists.
Nonsteroidal progesterone receptor ligands. 1. 3-Aryl-1-benzoyl-1,4,5,6-tetrahydropyridazines.
Synthesis and antiviral activity of novel anti-VZV 5-substituted uracil nucleosides with a cyclopropane sugar moiety.
N-3-substituted imidazoquinazolinones: potent and selective PDE5 inhibitors as potential agents for treatment of erectile dysfunction.
Synthesis and immunosuppressive activity of 2-substituted 2-aminopropane-1,3-diols and 2-aminoethanols.
Two-stage method for protein-ligand docking.
Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase.
Synthesis of non-nucleoside analogs of toyocamycin, sangivamycin, and thiosangivamycin: the effect of certain 4- and 4,6-substituents on the antiviral activity of pyrrolo[2,3-d]pyrimidines.
Active site directed inhibition of estrone sulfatase by nonsteroidal coumarin sulfamates.
2-substituted piperazines as constrained amino acids. Application to the synthesis of potent, non carboxylic acid inhibitors of farnesyltransferase.
Studies on selectin blocker. 1. Structure-activity relationships of sialyl Lewis X analogs.
Synthesis and structure-activity relationships of a new model of arylpiperazines. 3.1 2-[omega-(4-arylpiperazin-1-yl)alkyl]perhydropyrrolo- [1,2-c]imidazoles and -perhydroimidazo[1,5-a]pyridines: study of the influence of the terminal amide fragment on 5-HT1A affinity/selectivity.
Octanol-, chloroform-, and propylene glycol dipelargonat-water partitioning of morphine-6-glucuronide and other related opiates.
Preparation of phenolic paclitaxel metabolites.
Novel selective PDE IV inhibitors as antiasthmatic agents. Synthesis and biological activities of a series of 1-aryl-2,3-bis(hydroxymethyl)naphthalene lignans.
Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents.
Synthesis and biological activity of aromatic amino acid phosphoramidates of 5-fluoro-2'-deoxyuridine and 1-beta-arabinofuranosylcytosine: evidence of phosphoramidase activity.
Synthesis and biochemical evaluation of adenosylspermidine, a nucleoside-polyamine adduct inhibitor of spermidine synthase.
Prodrugs of nitroxyl as potential aldehyde dehydrogenase inhibitors vis-a-vis vascular smooth muscle relaxants.
Synthesis and binding properties of 2-amino-5-phosphono-3-pentenoic acid photoaffinity ligands as probes for the glutamate recognition site of the NMDA receptor.
Activity of N6-substituted 2-chloroadenosines at A1 and A2 adenosine receptors.
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters.
Novel inhibitors of prolyl 4-hydroxylase. 2. 5-Amide substituted pyridine-2-carboxylic acids.
Inhibitors of sterol synthesis. 3 beta,25-dihydroxy-5 alpha-cholest-8(14)-en-15-one, an active metabolite of 3 beta-hydroxy-5 alpha-cholest-8(14)-en-15-one.
Inactivation of calpain by peptidyl fluoromethyl ketones.
Inhibition of pig kidney L-aromatic amino acid decarboxylase by 2,3-methano-m-tyrosines.
Second-generation benzodiazepine CCK-B antagonists. Development of subnanomolar analogs with selectivity and water solubility.
High-affinity and potent, water-soluble 5-amino-1,4-benzodiazepine CCKB/gastrin receptor antagonists containing a cationic solubilizing group.
Antitumor agents. 123. Synthesis and human DNA topoisomerase II inhibitory activity of 2'-chloro derivatives of etoposide and 4 beta-(arylamino)-4'-O-demethylpodophyllotoxins.
3'-Spiro nucleosides, a new class of specific human immunodeficiency virus type 1 inhibitors: synthesis and antiviral activity of [2'-5'-bis-O-(tert-butyldimethylsilyl)-beta-D-xylo- and -ribofuranose]-3'-spiro-5"-[4"-amino-1",2"-oxathiole 2",2"-dioxide] (TSAO) pyrimidine nucleosides.
SC-53116: the first selective agonist at the newly identified serotonin 5-HT4 receptor subtype.
Synthesis and antimalarial properties of 1-imino derivatives of 7-chloro-3-substituted-3,4-dihydro-1,9(2H,10H)-acridinediones and related structures.
Rationally designed "dipeptoid" analogues of CCK. A Free-Wilson/Fujita-Ban analysis of some alpha-methyltryptophan derivatives as CCK-B antagonists.
Synthesis of N-glyoxyl prolyl and pipecolyl amides and thioesters and evaluation of their in vitro and in vivo nerve regenerative effects.
Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.
1-[2-[(5-Cyanopyridin-2-yl)amino]ethylamino]acetyl-2-(S)-pyrrolidinecarbonitrile: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties.
Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors.
Formaldehyde-induced DNA cross-link of indolizino[1,2-b]quinolines derived from the A-D rings of camptothecin.
Antiestrogens and selective estrogen receptor modulators as multifunctional medicines. 2. Clinical considerations and new agents.
A new aliphatic amino prodrug system for the delivery of small molecules and proteins utilizing novel PEG derivatives.
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach.
Design, synthesis, and biological evaluation of thio-containing compounds with serum HDL-cholesterol-elevating properties.
N-[3-(1H-imidazol-4-ylmethyl)phenyl]ethanesulfonamide (ABT-866, 1),(1) a novel alpha(1)-adrenoceptor ligand with an enhanced in vitro and in vivo profile relative to phenylpropanolamine and midodrine.
Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
Design of novel chimeric melanotropin-deltorphin analogues. Discovery of the first potent human melanocortin 1 receptor antagonist.
Synthesis and diuretic activity of alkyl- and arylguanidine analogs of N,N'-dicyclohexyl-4-morpholinecarboxamidine in rats and dogs.
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents.
Development of new carboxylic acid-based MMP inhibitors derived from functionalized propargylglycines.
Novel antiarthritic agents with 1,2-isothiazolidine-1,1-dioxide (gamma-sultam) skeleton: cytokine suppressive dual inhibitors of cyclooxygenase-2 and 5-lipoxygenase.
Medicinal chemistry of neuronal voltage-gated sodium channel blockers.
Pharmacophore models of group I and group II metabotropic glutamate receptor agonists. Analysis of conformational, steric, and topological parameters affecting potency and selectivity.
A structure-affinity relationship study on derivatives of N-[2-[4-(4-Chlorophenyl)piperazin-1-yl]ethyl]-3-methoxybenzamide, a high-affinity and selective D(4) receptor ligand.
Novel lipoamino acid- and liposaccharide-based system for peptide delivery: application for oral administration of tumor-selective somatostatin analogues.
Design of adenosine kinase inhibitors from the NMR-based screening of fragments.
1-(2-Nitrophenyl)thiosemicarbazides: a novel class of potent, orally active non-peptide antagonist for the bradykinin B(2) receptor.
Solid-phase synthesis and inhibitory effects of some pyrido[1,2-c]pyrimidine derivatives on leukocyte formations and experimental inflammation.
L-735,524: the design of a potent and orally bioavailable HIV protease inhibitor.
Synthesis and evaluation of the anti-HIV activity of aza and deaza analogues of isoddA and their phosphates as prodrugs.
Eucalmaidins A-E, (+)-oleuropeic acid derivatives from the fresh leaves of Eucalyptus maideni.
Apoptosis-inducing galactolipids from a cultured marine diatom, Phaeodactylum tricornutum.
Aplysinoplides A-C, cytotoxic sesterterpenes from the marine sponge Aplysinopsis digitata.
Pronounced pharmacological differences arising from minor structural changes in conformationally defined amphetamine analogues. Comparative evaluation of endo- and exo-2-amino- and endo- and exo-2-(methylamino)benzobicyclo[2.2.1]heptene and -benzobicylco[2.2.2]octene analogues. Conformationally defined adrenergic agents. 4.
Quantitative structure-activity relationships for N-[N',N'-disubstituted-amino)acetyl]arylamines for local anesthetic activity and acute toxicity.
New triterpenoid sulfates from the red alga Tricleocarpa fragilis.
New cembranes from the soft coral sarcophyton species
Secobotrytriendiol and related sesquiterpenoids: new phytotoxic metabolites from Botrytis cinerea.
Cycloartane triterpenoids from Kleinhovia hospita.
Biscarpamontamines A and B, an aspidosperma-iboga bisindole alkaloid and an aspidosperma-aspidosperma bisindole alkaloid, from Tabernaemontana sphaerocarpa.
[5-(N4,N4-Dimethylasparagine),8-lysine]vasopressin: the first 5-position neurohypophyseal hormone analogue to retain to retain significant antidiuretic potency.
Potential organ- or tumor-imaging agents. 21. Acyl-labeled esters of cholesterol.
Nonsteroidal antiinflammatory agents. 2. Synthesis of 4',5-disubstituted 3-biphenylylacetic acids and their derivatives with antiinflammatory and analgesic activities.
Oblongolides from the endophytic fungus Phomopsis sp. BCC 9789.
Antineoplastic agents. 565. Synthesis of combretastatin D-2 phosphate and dihydro-combretastatin D-2.
Neuroleptic activity in 5-aryltetrahydro-gamma-carbolines.
Bioactive guanidine alkaloids from two Caribbean marine sponges.
Synthesis and antibacterial activity of new 1-oxa-1-dethiacephalosporins.
General behavior, toxicity, and cytotoxic activity of elenoside, a lignan from Justicia hyssopifolia.
Sesquiterpene quinols/quinones from the Micronesian sponge Petrosaspongia metachromia.
Isolation and structure determination of novamethymycin, a new bioactive metabolite of the methymycin biosynthetic pathway in Streptomyces venezuelae.
Nagelamides A-H, new dimeric bromopyrrole alkaloids from marine sponge Agelas species.
Isolation, structure, absolute stereochemistry, and HIV-1 integrase inhibitory activity of integrasone, a novel fungal polyketide.
Spongiadioxins A and B, two new polybrominated dibenzo-p-dioxins from an Australian marine sponge Dysidea dendyi.
Two new lactones with mosquito larvicidal activity from three Hortonia species.
3-Acetoxyspathulenol, a new aromadendrane-type natural product from the soft Coral Parerythropodium fulvum.
Phenotypic and genotypic characterization of Enterobacteriaceae with decreased susceptibility to carbapenems: results from large hospital-based surveillance studies in China.
Verbalactone, a new macrocyclic dimer lactone from the roots of Verbascum undulatum with antibacterial activity.
Iridoids as allelochemicals and DNA polymerase inhibitors.
New lipopeptides from the Caribbean cyanobacterium Lyngbya majuscula.
Isoterchebulin and 4,6-O-isoterchebuloyl-D-glucose, novel hydrolyzable tannins from Terminalia macroptera.
Coumarins isolated from Angelica gigas inhibit acetylcholinesterase: structure-activity relationships.
Acetylated analogues of the microtubule-stabilizing agent discodermolide: preparation and biological activity.
Glanvillic acids A and B and methyl capucinoate A, new metabolites isolated from the Caribbean sponges Plakortis halichondrioides and Plakinastrella onkodes.
Massarinolins A-C: new bioactive sesquiterpenoids from the aquatic fungus massarina tunicata
Antimicrobial and cytotoxic phenolic glycoside esters from the New Zealand tree Toronia toru.
Cacofurans A and B, new furanoditerpenes from a marine sponge.
A new dimeric stilbene with tyrosinase inhibitiory activity from Artocarpus gomezianus.
Pachycladins A-E, prostate cancer invasion and migration inhibitory Eunicellin-based diterpenoids from the red sea soft coral Cladiella pachyclados.
Synthesis, antiretrovirus effects, and phosphorylation kinetics of 3'-isocyano-3'-deoxythymidine and 3'-isocyano-2',3'-dideoxyuridine.
Synthesis and anticonvulsant properties of 2,3,3a,4-tetrahydro-1H-pyrrolo[1,2-a]benzimidazol-1-ones.
N6-bicycloalkyladenosines with unusually high potency and selectivity for the adenosine A1 receptor.
Acyclic analogues of 3'-azido-3'-deoxythymidine as potential antiviral agents. Nucleoside synthesis by Michael addition.
6- and 8-hydroxy-3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans. Dopamine agonists with autoreceptor selectivity.
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 9. Lipophilic trimethoprim analogues as antigonococcal agents.
Synthesis and cardiotonic activity of a series of substituted 4-alkyl-2(1H)-quinazolinones.
Potential antitumor agents. 54. Chromophore requirements for in vivo antitumor activity among the general class of linear tricyclic carboxamides.
N-sulfonyl imidates as a novel prodrug form for an ester function or a sulfonamide group.
Synthesis and pharmacology of trans-4-n-propyl-3,4,4a,10b-tetrahydro-2H,5H-1-benzopyrano[4,3-b ]-1,4-oxazin-7- and -9-ols: the significance of nitrogen pKa values for central dopamine receptor activation.
Carbamate ester derivatives as potential prodrugs of the presynaptic dopamine autoreceptor agonist (-)-3-(3-hydroxyphenyl)-N-propylpiperidine.
Conformation-activity relationship study of 5-HT3 receptor antagonists and a definition of a model for this receptor site.
Potent, low molecular weight renin inhibitors containing a C-terminal heterocycle: hydrogen bonding at the active site.
Synthesis and pharmacological activity of angiotensin converting enzyme inhibitors: N-(mercaptoacyl)-4-substituted-(S)-prolines.
Synthesis, binding studies, and structure-activity relationships of 1-aryl-and 2-aryl[1]benzopyranopyrazol-4-ones, central benzodiazepine receptor ligands.
6-(Alkylamino)-9-benzyl-9H-purines. A new class of anticonvulsant agents.
Synthesis of 7,12-dihydropyrido[3,4-b:5,4-b']diindoles. A novel class of rigid, planar benzodiazepine receptor ligands.
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
Chemical differentiating agents. Differentiation of HL-60 cells by hexamethylenebis[acetamide] analogues.
Stereospecific synthesis of chiral metabolites of ifosfamide and their determination in the urine.
Cardiotonic agents. 1. 4,5-Dihydro-6-[4-(1H-imidazol-1-yl)phenyl]-3 (2H)-pyridazinones: novel positive inotropic agents for the treatment of congestive heart failure.
Crystal structures and pharmacological activity of calcium channel antagonists: 2,6-dimethyl-3,5-dicarbomethoxy-4-(unsubstituted, 2-methyl-, 4-methyl-, 3-nitro-, 4-nitro-, and 2,4-dinitrophenyl)-1,4-dihydropyridine.
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors.
Synthesis and psychoanaleptic properties of new compounds structurally related to diphenhydramine.
Synthesis and biological activity of 5-(trifluoromethyl)- and 5-(pentafluoroethyl)pyrimidine nucleoside analogues.
Synthesis and antibacterial activity of some ester, amides, and hydrazides of 3-carboxyrifamycin S. Relationship between structure and activity of ansamycins.
gamma-Aminobutyric acid agonists, antagonists, and uptake inhibitors. Design and therapeutic aspects.
Syntheses and diuretic activity of 1,2-dihydro-2-(3-pyridyl)-3H-pyrido[2,3-d]pyrimidin-4-one and related compounds.
2-(Aminomethyl)phenols, a new class of saluretic agents. 5. Fused-ring analogues.
synthesis and antitumor activity of 2-deoxyribofuranosides of 3-deazaguanine.
Peptide sweeteners. 4. Hydroxy and methoxy substitution of the aromatic ring in L-aspartyl-L-phenylalanine methyl ester. Structure-taste relationships.
Scalarane and homoscalarane compounds from the nudibranchs Glossodoris sedna and Glossodoris dalli: chemical and biological properties.
Diterpenoid sweeteners. Synthesis and sensory evaluation of stevioside analogues nondegradable to steviol.
Inhibition of human acrosin by monosaccharides and related compounds: structure-activity relationships.
Synthesis and pharmacology of metabolically stable tert-butyl ethers of morphine and levorphanol.
Species- or isozyme-specific enzyme inhibitors. 8. Synthesis of disubstituted two-substrate condensation products as inhibitors of rat adenylate kinases.
Constituents of the leaves of Magnolia ovata.
Inhibitors of osteoclast formation from rhizomes of Cibotium barometz.
Synthesis and antiarrhythmic activity of alpha, alpha-bis[(dialkylamino)alkyl]phenylacetamides.
Fluoroprostaglandins: synthesis and biological evaluation of the methyl esters of (+)-12-fluoro-, (-)-ent-12-fluoro-, (+)-15-epi-fluoro-, and (-)-ent-15 epi-12-fluoroprostaglandin F2 alpha.
Acylthioxanthenes: agents which selectively reduce decerebrate rigidity in the cat.
Anthoptilides A-E, new Briarane diterpenes from the Australian sea pen Anthoptilum cf. kukenthali.
Triterpenoids from the leaves of Diospyros kaki (persimmon) and their inhibitory effects on protein tyrosine phosphatase 1B.
Maleimide and maleic anhydride derivatives from the mycelia of Antrodia cinnamomea and their nitric oxide inhibitory activities in macrophages.
Saponins and polyphenols from Fadogia ancylantha (makoni tea).
Synthesis and stereochemistry of 7-phenyl-2-propionanilidobenzo[a]quinolizidine derivatives. Structural probes of fentanyl analgesics.
Separation of potent central and renal dopamine agonist activity in substituted 6-chloro-2,3,4,5-tetrahydro-7,8-dihydroxy-1-phenyl-1H-3-benzazepines.
Biologically active secondary metabolites from fungi. 12.(1) oidiolactones A-F, labdane diterpene derivatives isolated from oidiodendron truncata
Three new antibacterial alkaloids from a marine sponge Stelletta species.
Schweinfurthins I and J from Macaranga schweinfurthii.
Minor furanocoumarins and coumarins in grapefruit peel oil as inhibitors of human cytochrome P450 3A4.
Acremolides A-D, lipodepsipeptides from an Australian marine-derived fungus, Acremonium sp.
Synthesis and beta-adrenergic blocking activity of new aliphatic oxime ethers.
Further membranolide diterpenes from the antarctic sponge dendrilla membranosa.
Monanchorin, a bicyclic alkaloid from the sponge Monanchora ungiculata.
Isolation and structure determination of nostocyclopeptides A1 and A2 from the terrestrial cyanobacterium Nostoc sp. ATCC53789.
In vitro pharmacodynamics of levofloxacin and other aerosolized antibiotics under multiple conditions relevant to chronic pulmonary infection in cystic fibrosis.
Cytotoxic dolabellane diterpenes from the Formosan soft coral Clavularia inflata.
Synthetic analogues of the microtubule-stabilizing agent (+)-discodermolide: preparation and biological activity.
A cyclohexanonyl bromophenol from the red alga Symphyocladia latiuscula.
Triterpene saponins and lignans from the roots of Pulsatilla chinensis and their cytotoxic activity against HL-60 cells.
A cytotoxic lobane diterpene from the formosan soft coral Sinularia inelegans.
Montipyridine, a new pyridinium alkaloid from the stony coral montipora species.
Seco[D-Asp3]microcystin-RR and [D-Asp3,D-Glu(OMe)6]microcystin-RR, two new microcystins from a toxic water bloom of the cyanobacterium planktothrixrubescens.
Euplectin and coneuplectin, new naphthopyrones from the lichen Flavoparmelia euplecta.
Cyclotheonamide E4 and E5, new potent tryptase inhibitors from an Ircinia species of sponge.
Characterization of an anti-tuberculosis resin glycoside from the prairie medicinal plant Ipomoea leptophylla.
Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities.
Aurantosides D, E, and F: new antifungal tetramic acid glycosides from the marine sponge Siliquariaspongia japonica.
2,4,5-trimethoxystyrene, a bioactive component of the bark of Duguetia panamensis.
AMP-activated protein kinase (AMPK) activation by benzofurans and coumestans isolated from Erythrina abyssinica.
A bastadin with potent and selective delta-opioid receptor binding affinity from the Australian sponge Ianthella flabelliformis.
Synthesis and pharmacological studies of N-[4-[2-hydroxy-3-[[2-[4-(1H-imidazol-1- yl)phenoxy]ethyl]amino]propoxy]phenyl]methanesulfonamide, a novel antiarrhythmic agent with class II and class III activities.
Synthesis of the tumorigenic 3,4-dihydrodiol metabolites of dibenz[a,j]anthracene and 7,14-dimethyldibenz[a,j]anthracene.
7-substituted 5-amino-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3- quinolinecarboxylic acids: synthesis and biological activity of a new class of quinolone antibacterials.
9-(trans-2',trans-3'-dihydroxycyclopent-4'-enyl) derivatives of adenine and 3-deazaadenine: potent inhibitors of bovine liver S-adenosylhomocysteine hydrolase.
Conformationally constrained renin inhibitory peptides: gamma-lactam-bridged dipeptide isostere as conformational restriction.
Cytotoxic nor-chamigrane and chamigrane endoperoxides from a basidiomycetous fungus.
Synthesis and thromboxane synthetase inhibitory activity of di- or tetrahydrobenzo[b]thiophenecarboxylic acid derivatives.
Cyclobut-A and cyclobut-G: broad-spectrum antiviral agents with potential utility for the therapy of AIDS.
Retinobenzoic acids. 1. Structure-activity relationships of aromatic amides with retinoidal activity.
[(6,7-Dichlorobenzo[b]thien-5-yl)oxy]acetic acids and 1,1-dioxides. 1. A structurally novel class of diuretics with hypotensive activity.
Synthesis and renin inhibitory activity of angiotensinogen analogues having dehydrostatine, Leu psi [CH2S]Val, or Leu psi [CH2SO]Val at the P1-P1' cleavage site.
Thrombin inhibitors. 3. Carboxyl-containing amide derivatives of N alpha-substituted L-arginine.
Phenylethanoid glycosides from Lantana fucata with in vitro anti-inflammatory activity.
3-Carbonylacrylic derivatives as potential antimicrobial agents. Correlations between activity and reactivity toward cysteine.
Synthesis and biological activity of carboxylic acid replacement analogues of the potent angiotensin converting enzyme inhibitor 5(S)-benzamido-4-oxo-6-phenylhexanoyl-L-proline.
Reductive amination of 3-ketoanguidin and antitumor activity of the products.
Comparative biological activities of highly potent active-site analogues of alpha-melanotropin.
Aporphines. 39. Synthesis, dopamine receptor binding, and pharmacological activity of (R)-(-)- and (S)-(+)-2-hydroxyapomorphine.
Imidodisulfamides. 1. A novel class of antagonists of slow-reacting substance of anaphylaxis.
Synthesis and preliminary antitumor evaluation of 5-iminodoxorubicin.
Antiinflammatory agents. 2. Syntheses and antiinflammatory activity of substituted 2-aminophenylacetic acid derivatives.
Synthesis and biological activity of structural analogues of the anticancer benzophenanthridine alkaloid nitidine chloride.
2,3-Dimethyl-1,4-naphthoquinone derivatives as bioreductive alkylating agents with cross-linking potential.
Structural requirements of olefinic 5-substituted deoxyuridines for antiherpes activity.
Synthesis and antileukemic activity of fluorinated analogues of 2,3-dihydro-5-phenyl-6,7-bis(hydroxymethyl)-1H-pyrrolizine biscarbamate.
Quantitative structure-activity relationship by distance geometry: quinazolines as dihydrofolate reductase inhibitors.
Synthesis, decomposition kinetics, and preliminary toxicological studies of pure N-acetyl-p-benzoquinone imine, a proposed toxic metabolite of acetaminophen.
Aporphines. 58. N-(2-chloroethyl) [8,9-2H]norapomorphine, an irreversible ligand for dopamine receptors: synthesis and application.
Synthesis and biological evaluation of radiolabeled beta-ruthenocenylalanine.
Synthesis of 3,6-bis(aminoalkoxy)acridines and their effect on the immune System.
Studies on the synthesis of chemotherapeutics. 12. Synthesis and antitumor activity of N-phthalidyl-5-fluorouracil derivatives.
Carbon-7 substituted actinomycin D analogues as improved antitumor agents: synthesis and DNA-binding and biological properties.
Use of (S)-(trifloxymethyl)oxirane in the synthesis of a chiral beta-adrenoceptor antagonist, (R)- and (S)-9-[[3-(tert-butylamino)-2-hydroxypropyl]oximino]fluorene.
Cardenolide glycosides of Thevetia peruviana and triterpenoid saponins of Sapindus emarginatus as TRAIL resistance-overcoming compounds.
Scalarane-based sesterterpenoid RCE-protease inhibitors isolated from the Indonesian marine sponge Carteriospongia foliascens.
Brartemicin, an inhibitor of tumor cell invasion from the actinomycete Nonomuraea sp.
Synthesis and biological activity of flavipucine analogues.
synthesis and biological evaluation of fully functionalized seco-pancratistatin analogues.
Phenolic constituents of the rhizomes of the Thai medicinal plant Belamcanda chinensis with proliferative activity for two breast cancer cell lines.
Perspective on the design and biochemical pharmacology of inhibitors of thymidylate synthetase.
Structure and antibacterial activity ofp6 new labdane diterpenoid from Salvia leriaefolia.
Oxygenated cembranoids from a Formosan soft coral Sinularia gibberosa.
Cinnamic ester derivatives from Oxalis pes-caprae (Bermuda buttercup).
Bioactive compounds from Bauhinia purpurea possessing antimalarial, antimycobacterial, antifungal, anti-inflammatory, and cytotoxic activities.
Pim2 inhibitors from the Papua New Guinean plant Cupaniopsis macropetala.
Chinikomycins A and B: isolation, structure elucidation, and biological activity of novel antibiotics from a marine Streptomyces sp. isolate M045.
Chemistry and structure-activity relationship of HIV-1 integrase inhibitor integracide B and related natural products.
Noreupenifeldin, a tropolone from an unidentified ascomycete.
Erythrina alkaloids and a pterocarpan from the bark of Erythrina subumbrans.
Quassinoid inhibition of AP-1 function does not correlate with cytotoxicity or protein synthesis inhibition.
S-alkenyl cysteine sulfoxide and its antioxidant properties from Allium cepa var. tropeana (red onion) seeds.
Chemical and pharmaceutical studies on medicinal plants in Paraguay. Geraniin, an angiotensin-converting enzyme inhibitor from "paraparai mi," Phyllanthus niruri.
Antipruritic dinaphthofuran-7,12-dione derivatives from the pericarp of Impatiens balsamina.
Two new mono-tetrahydrofuran ring acetogenins, annomuricin E and muricapentocin, from the leaves of Annona muricata.
Novel marine di-Z-carotenoids: cucumariaxanthins A, B, and C from the sea cucumber Cucumaria japonica.
Terezines A-D: new amino acid-derived bioactive metabolites from the coprophilous fungus Sporormiella teretispora.
The arenarans, sesquiterpene ethers from the marine sponge Dysidea arenaria.
Isolation and bioactivities of constitutents of the roots of Garcinia atroviridis.
Isolation and structure elucidation of a novel antimalarial macrocyclic polylactone, menisporopsin A, from the fungus Menisporopsis theobromae.
Acylated flavonol glycosides from the flower of Inula britannica.
Hydrachine A, a novel alkaloid from the roots of Hydrangea chinensis.
Prunioside A: a new terpene glycoside from Spiraea prunifolia.
Periconicins, two new fusicoccane diterpenes produced by an endophytic fungus Periconia sp. with antibacterial activity.
New xenicane diterpenoids from the gorgonian Acalycigorgia inermis.
Immunomodulatory constituents from an Ascomycete, Eupenicillium crustaceum, and revised absolute structure of macrophorin D.
Anti-HIV prenylated flavonoids from Monotes africanus.
Microxine, a new cdc2 kinase inhibitor from the Australian marine sponge Microxina species.
Reversal of fluconazole resistance in multidrug efflux-resistant fungi by the Dysidea arenaria sponge sterol 9alpha,11alpha-epoxycholest-7-ene-3beta,5alpha,6alpha,19-tetrol 6-acetate.
New antihepatotoxic cerebroside from Lycium chinense fruits.
Chemical studies on mexican plants used in traditional medicine, VI. Additional new 4-phenylcoumarins from Exostema caribaeum.
Structure and absolute configuration of palmonine F, a new eunicellin-based diterpene from the gorgonian Eunicella verrucosa.
Potential tumor- or organ-imaging agents. 29. Radioiodinated esters and amides of 20-hydroxy- and 20-aminopregn-5-en-3 beta-ols.
Synthesis and structure-activity relationships of a new series of antiarrhythmic agents: monobasic derivatives of disobutamide.
Apoptotic effects of polyprenylated benzoylphloroglucinol derivatives from the twigs of Garcinia multiflora.
Synthesis and analgesic activity of pemedolac (cis-1-ethyl-1,3,4,9-tetrahydro-4-(phenylmethyl)pyrano[3,4-b]ind ole-1- acetic acid).
Molecular basis for bleomycin amplification: conformational and stereoelectronic effects in unfused amplifiers.
[1,2,4]Triazolo[4,3-a]quinoxalin-4-amines: a new class of A1 receptor selective adenosine antagonists.
Monophosphoric acid diesters of 7 beta-hydroxycholesterol and of pyrimidine nucleosides as potential antitumor agents: synthesis and preliminary evaluation of antitumor activity.
Neuroprotective xanthone glycosides from Swertia punicea.
Lactonecembranoids from Croton laevigatus.
Derivatives of 2-methylenepropane-1,3-diol as new antagonists of platelet activating factor.
Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor.
Fluorinated pyrimidine nucleosides. 4. Synthesis and antitumor testing of a series of 2',5'-dideoxy- and 2',3',5'-trideoxynucleosides of 5-fluorouracil.
N6-[2-(3,5-dimethoxyphenyl)-2-(2-methylphenyl)ethyl]adenosine and its uronamide derivatives. Novel adenosine agonists with both high affinity and high selectivity for the adenosine A2 receptor.
Phloroglucinols from the argentine ferns Elaphoglossum gayanum and E. piloselloides.
New chiral and isomeric cyclopropyl ketoxime propanolamine derivatives with potent beta-adrenergic blocking properties.
Synthesis of 5-aryl-2H-tetrazoles, 5-aryl-2H-tetrazole-2-acetic acids, and [(4-phenyl-5-aryl-4H-1,2,4-triazol-3-yl)thio]acetic acids as possible superoxide scavengers and antiinflammatory agents.
Cyclopentenyluridine and cyclopentenylcytidine analogues as inhibitors of uridine-cytidine kinase.
Hypolipidemic 4,5-dihydro-4-oxo-5,5-disubstituted-2-furancarboxylic acids.
Antiallergy agents. 2. 2-Phenyl-5-(1H-tetrazol-5-yl)pyrimidin-4(3H)-ones.
Two clonidine-like compounds with substituents at the 2-, 3-, and 6-position of the phenyl ring possessing pronounced hypotensive potencies.
2-Acetylpyridine thiosemicarbazones. 4. Complexes with transition metals as antimalarial and antileukemic agents.
Receptor-based design of dihydrofolate reductase inhibitors: comparison of crystallographically determined enzyme binding with enzyme affinity in a series of carboxy-substituted trimethoprim analogues.
Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin.
Steroidogenesis inhibitors. 1. Adrenal inhibitory and interceptive activity of trilostane and related compounds.
Preparation of 20-(hydroxymethyl)-4-methyl-4-aza-2-oxa-5 alpha-pregnan-3-one as an inhibitor of testosterone 5 alpha-reductase.
2-[[[2-(2,6-Dimethoxyphenoxy)ethyl]amino]-methyl] -1,4-benzoxathian: a new antagonist with high potency and selectivity toward alpha 1-adrenoreceptors.
Resolution of etodolac and antiinflammatory and prostaglandin synthetase inhibiting properties of the enantiomers.
A dipeptide derived from kainic and L-glutamic acids: a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties.
Design, synthesis, and testing of potential antisickling agents. 4. Structure-activity relationships of benzyloxy and phenoxy acids.
Phosphorus-nitrogen compounds. 26. Phosphaminimides. 2. 2,2'-Phosphinylidenebis(1,1,1-trimethylhydrazinium) iodide inner salts as agents affecting ganglionic transmission.
Imidazo[1,5-d][1,2,4]triazines as potential antiasthma agents.
Trequinsin, a potent new antihypertensive vasodilator in the series of 2-(arylimino)-3-alkyl-9,10-dimethoxy-3,4,6,7-tetrahydro-2H-py rim ido [6,1-a]isoquinolin-4-ones.
Synthesis of certain hydroxy analogues of the antimalarial drug primaquine and their in vitro methemoglobin-producing and glutathione-depleting activity in human erythrocytes.
Structure--activity relationships for and potentiation of the antimitogenic activity of 2-5A core derived from 2-5A, a mediator of interferon action.
Improved synthesis and antitumor evaluation of 5,8-dideazaisofolic acid and closely related analogues.
Aurantiomides A-C, quinazoline alkaloids from the sponge-derived fungus Penicillium aurantiogriseum SP0-19.
Makaluvic acids from the South African latrunculid sponge Strongylodesma aliwaliensis.
Cytotoxic staurosporines from the marine ascidian Cystodytes solitus.
Sorocenols G and H, anti-MRSA oxygen heterocyclic Diels-Alder-type adducts from Sorocea muriculata roots.
ent-kaurane diterpenoids from the liverwort Jungermannia atrobrunnea.
Pinpointing pseurotins from a marine-derived Aspergillus as tools for chemical genetics using a synthetic lethality yeast screen.
Cyclic peroxides derived from the marine sponge Plakortis simplex.
Cytotoxic diterpenoids and sesquiterpenoids from Pteris multifida.
Induction of apoptosis by diterpenes from the soft coral Xenia elongata.
Chromones from the endophytic fungus Pestalotiopsis sp. isolated from the chinese mangrove plant Rhizophora mucronata.
Cyclic depsipeptides, ichthyopeptins A and B, from Microcystis ichthyoblabe.
Antineoplastic agents. 550. Synthesis of 10b(s)-epipancratistatin from (+)-narciclasine.
Dendronpholides A-R, cembranoid diterpenes from the chinese soft coral Dendronephthya sp.
(Iso)-quinoline alkaloids from fungal fruiting bodies of Cortinarius subtortus.
Octanorcucurbitane and cucurbitane triterpenoids from the tubers of Hemsleya endecaphylla with HIV-1 inhibitory activity.
Bioactive sulfated sesterterpene alkaloids and sesterterpene sulfates from the marine sponge Fasciospongia sp.
Limonoids showing selective toxicity to DNA repair-deficient yeast and other constituents of Trichilia emetica.
Antineoplastic agents. 362. Isolation and X-ray crystal structure of dibromophakellstatin from the Indian ocean sponge Phakellia mauritiana.
Isolation of two flavonoids from Tanacetum microphyllum as PMA-induced ear edema inhibitors.
Oscillapeptin G, a tyrosinase inhibitor from toxic Oscillatoria agardhii.
Isolation of the furan fatty acid, (8Z,11Z,14Z,17Z)-3,6-epoxyeicos-3,5,8,11,14,17-hexenoic acid from the New Zealand sponge Hymeniacidon hauraki.
HIV inhibitory natural products. 26. Quinoline alkaloids from Euodia roxburghiana.
Bastadin 20 and bastadin O-sulfate esters from Ianthella basta: novel modulators of the Ry1R FKBP12 receptor complex.
A new flavonol glycoside gallate ester from Acer okamotoanum and its inhibitory activity against human immunodeficiency virus-1 (HIV-1) integrase.
Friedelane triterpenoids from Maytenus macrocarpa.
Bruceosides D, E, and F, three new cytotoxic quassinoid glucosides from Brucea javanica.
Bis(sulfato)-cyclosiphonodictyol A, a new disulfated sesquiterpene-hydroquinone from a deep water collection of the Marine sponge Siphonodictyon coralliphagum.
Six lignans from Phyllanthus myrtifolius.
Structure-activity relationship of in vitro antiviral and cytotoxic activity of semisynthetic analogues of scopadulane diterpenes.
Three new bistetrahydrofuran acetogenins from the seeds of Annona spinescens.
Bioactive diterpenoids from Octocorallia, 2. Deoxyxeniolide B, a novel ichthyotoxic diterpenoid from the soft coral Xenia elongata.
Structural revisions of some non-adjacent bis-tetrahydrofuran annonaceous acetogenins.
Two new bioactive carbazole alkaloids from the root bark of Clausena harmandiana.
Bioactive constituents of the roots of Licania intrapetiolaris.
Discorhabdin P, a new enzyme inhibitor from a deep-water Caribbean sponge of the genus Batzella.
(Imidazo[1,2-a]pyrimidin-2-yl)phenylmethanones and related compounds as potential nonsedative anxiolytics.
Synthesis and pharmacological evaluation of CNS activities of [1,2,3]triazolo[4,5-b][1,5]-, imidazolo[4,5-b][1,5]-, and pyrido[2,3-b][1,5]benzodiazepines. 10-Piperazinyl-4H-1,2,3-triazolo[4,5-b][1,5]benzodiazepines with neuroleptic activity.
Resolved 6,7,8,9-tetrahydro-N,N-dimethyl-3H-benz[e]indol-8-amine: central dopamine and serotonin receptor stimulating properties.
Mutagenicity of substituted (o-phenylenediamine)platinum dichloride in the Ames test. A quantitative structure-activity analysis.
Syntheses and gastric acid antisecretory properties of the H2-receptor antagonist. N-[3-[3-(1-piperidinylmethyl)phenoxy]propyl]thieno[3,4-d]isot hiazol-3-amine 1,1-dioxide and related derivatives.
Graphics computer-aided receptor mapping as a predictive tool for drug design: development of potent, selective, and stereospecific ligands for the 5-HT1A receptor.
Synthesis of antimicrobial agents. 1. Syntheses and antibacterial activities of 7-(azole substituted)quinolones.
(+/-)-4-tert-butyl-3-cyano-1-(4-ethynylphenyl)-2,6,7-trioxabi cyclo[2.2.2]octane: synthesis of a remarkably potent GABAA receptor antagonist.
Excitatory amino acid agonists. Enzymic resolution, X-ray structure, and enantioselective activities of (R)- and (S)-bromohomoibotenic acid.
Octahydrobenzo[g]quinolines: potent dopamine agonists which show the relationship between ergolines and apomorphine.
Design, synthesis, and antineoplastic activity of 2'-deoxy-2'-methylidenecytidine.
Synthesis and biological evaluations of certain 2-halo-2'-substituted derivatives of 9-beta-D-arabinofuranosyladenine.
Cytotoxic ent-kaurane diterpenoids from Isodon rubescens var. lushiensis.
Leucoridines A-D, cytotoxic Strychnos-Strychnos bisindole alkaloids from Leuconotis.
Synthesis and hypolipidemic activity of 2-substituted isobutyric acid derivatives.
Selective opioid receptor agonists and antagonists: research tools and potential therapeutic agents.
Binding of steroids to the progestin and glucocorticoid receptors analyzed by correspondence analysis.
A novel peptide delivery system involving peptidase activated prodrugs as antimicrobial agents. Synthesis and biological activity of peptidyl derivatives of 5-fluorouracil.
N-(1,3,4,6,7,12b-hexahydro-2H-benzo[b]furo[2,3-a]quinolizin -2-yl)-N- methyl-2-hydroxyethane-sulfonamide: a potent and selective alpha 2-adrenoceptor antagonist.
Synthesis and antiarrhythmic activity of new 1-[1-[2-[3-(alkylamino)-2-hydroxypropoxy]phenyl]vinyl]-1 H-imidazoles and related compounds.
Synthesis and neuroleptic activity of N-[(1-ethyl-2-pyrrolidinyl)methyl]-2-methoxy-5-sulfonamidobenzamide s.
Adenosine deaminase inhibitors. Conversion of a single chiral synthon into erythro- and threo-9-(2-hydroxy-3-nonyl)adenines.
Synthetic CNS agents. 1. (+/-)-1,2,3,4,4a,5,10,10a-Octahydro-5,10[1',2'] -benzenobenz[g]isoquinoline hydrochloride. A new, highly potent, potential antidepressant.
Antitumor imidazotetrazines. 1. Synthesis and chemistry of 8-carbamoyl-3-(2-chloroethyl)imidazo[5,1-d]-1,2,3,5-tetrazin-4(3 H)-one , a novel broad-spectrum antitumor agent.
Pyrazolodiazepines. 3. 4-Aryl-1,6,7,8-tetrahydro-1,3-dialkylpyrazolo[3,4-e][1,4]diazepines as antidepressant agents.
In vitro antiplasmodial, antiamoebic, and cytotoxic activities of some monomeric isoquinoline alkaloids.
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
Synthesis and evaluation of 24-(isopropyl[75Se]seleno)chol-5-en-3 beta-ol.
[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action.
Studies on 4(1H)-quinazolinones. 5. Synthesis and antiinflammatory activity of 4(1H)-quinazolinone derivatives.
Study on the inhibition of adenosine deaminase.
Analogues of platelet activating factor. 3. Replacement of the phosphate moiety with a sulfonylbismethylene group.
Sulfonyliminoimidazolidines. A new class of oral hypoglycemic agents. 1. 1-[[p-[2-(acylamino)ethyl]phenyl]sulfonyl]-2-iminoimidazolidines.
Bile acids with a cyclopropyl-containing side chain. 1. Preparation and properties of 3 alpha, 7 beta-dihydroxy-22,23-methylene-5 beta-cholan-24-oic acid.
Sulfated steroids: ptilosteroids A-C and ptilosaponosides A and B from the Solomon Islands marine sponge Ptilocaulis spiculifer.
Phenalenone-type compounds from Musa acuminata var. "Yangambi km 5" (AAA) and their activity against Mycosphaerella fijiensis.
Itosides J-N from Itoa orientalis and structure - anti-COX-2 activity relationship of phenolic glycosides.
Total synthesis and biological evaluation of the marine bromopyrrole alkaloid dispyrin: elucidation of discrete molecular targets with therapeutic potential.
Epicoccins A-D, epipolythiodioxopiperazines from a Cordyceps-colonizing isolate of Epicoccum nigrum.
5-Bromo-8-methoxy-1-methyl-beta-carboline, an alkaloid from the New Zealand marine bryozoan Pterocella vesiculosa.
Unprecedented hemiketal cembranolides with anti-inflammatory activity from the soft coral Lobophytum durum.
Strongylophorine-26, an inhibitor of cancer cell Invasion: SAR revealed by synthesis of analogues.
A dimeric lactone from Ardisia japonica with inhibitory activity for HIV-1 and HIV-2 ribonuclease H.
Stellettins L and M, cytotoxic isomalabaricane-type triterpenes, and sterols from the marine sponge Stelletta tenuis.
Halichonadin F and the Cu(I) complex of halichonadin C from the sponge Halichondria sp.
Guaiane sesquiterpene lactones and amino acid-sesquiterpene lactone conjugates from the aerial parts of Saussurea pulchella.
Cytotoxic withanolides from the flowers of Datura metel.
C-geranylated chalcones from the stems of Angelica keiskei with superoxide-scavenging activity.
Antibacterial C-geranylflavonoids from Paulownia tomentosa Fruits.
Bacillamides from a hypersaline microbial mat bacterium.
Micropeptins from the freshwater cyanobacterium Microcystis aeruginosa (NIES-100).
A direct bioautographic tlc assay for compounds possessing antibacterial activity.
SB-202742, a novel beta-lactamase inhibitor isolated from Spondias mombin.
Pyrazolopyrimidinediones are selective agents for Helicobacter pylori that suppress growth through inhibition of glutamate racemase (MurI).
Rapamycin protects mice from staphylococcal enterotoxin B-induced toxic shock and blocks cytokine release in vitro and in vivo.
Isolation and structure elucidation of 34-sulfatobastadin 13, an inhibitor of the endothelin A receptor, from a marine sponge of the genus Ianthella.
Selligueain A, a novel highly sweet proanthocyanidin from the rhizomes of Selliguea feei.
Identification and characterization of CTX-M-producing Shigella isolates in the United States.
Pharmacokinetics of chloroquine and monodesethylchloroquine in pregnancy.
1H- and 13C-nmr assignments of phyllanthin and hypophyllanthin: lignans that enhance cytotoxic responses with cultured multidrug-resistant cells.
Cytotoxic and antimalarial bisbenzylisoquinoline alkaloids from Stephania erecta.
In vitro activity of ACH-702, a new isothiazoloquinolone, against Nocardia brasiliensis compared with econazole and the carbapenems imipenem and meropenem alone or in combination with clavulanic acid.
Comparison of anidulafungin MICs determined by the clinical and laboratory standards institute broth microdilution method (M27-A3 document) and Etest for Candida species isolates.
(-)-agelasidine C and (-)-agelasidine D, two new hypotaurocyamine diterpenoids from the Caribbean sea sponge Agelas clathrodes.
Baseline genotypic and phenotypic susceptibilities of HIV-1 group O to enfuvirtide.
Antimalarial asexual stage-specific and gametocytocidal activities of HIV protease inhibitors.
First report of plasmid-mediated quinolone resistance determinant qnrS1 in an Escherichia coli strain of animal origin in Italy.
1,2-Bis(sulfonyl)hydrazines. 3. Effects of structural modification on antineoplastic activity.
Alkaloids from the bark of Guatteria hispida and their evaluation as antioxidant and antimicrobial agents.
Thiodiketopiperazines produced by the endophytic fungus Epicoccum nigrum.
Pre- and postsynaptic dopaminergic activities of indolizidine and quinolizidine derivatives of 3-(3-hydroxyphenyl)-N-(n-propyl)piperidine (3-PPP). Further developments of a dopamine receptor model.
Renin inhibitors containing isosteric replacements of the amide bond connecting the P3 and P2 sites.
Resolution of the nonsteroidal antiandrogen 4'-cyano-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-3'- (trifluoromethyl)-propionanilide and the determination of the absolute configuration of the active enantiomer.
A new class of nonhormonal pregnancy-terminating agents. Synthesis and contragestational activity of 3,5-diaryl-s-triazoles.
A new 2D-TLC bioautography method for the discovery of novel antifungal agents To control plant pathogens.
An unusual nitrogenous terphenyl derivative from fruiting bodies of the basidiomycete Sarcodon leucopus.
Inhibition of vertebrate squalene epoxidase by extended and truncated analogues of trisnorsqualene alcohol.
5-Isoquinolinesulfonamide derivatives. 2. Synthesis and vasodilatory activity of N-(2-aminoethyl)-5-isoquinolinesulfonamide derivatives.
Synthesis and evaluation of 4-(substituted thio)-4-androstene-3,17-dione derivatives as potential aromatase inhibitors.
Synthesis of thyrotropin-releasing hormone analogues. 2. Tripeptides structurally greatly differing from TRH with high central nervous system activity.
(Acyloxy)alkyl carbamates as novel bioreversible prodrugs for amines: increased permeation through biological membranes.
Antiallergic agents. 3. N-(1H-tetrazol-5-yl)-2-pyridinecarboxamides.
Synthesis and antitumor activity of cis-dichloroplatinum (II)-N-aminated nucleoside complexes.
Synthesis of 3,4-dihydro-4-oxoquinazoline derivatives as potential anticonvulsants.
Synthesis and in vitro pharmacology of 7-oxabicyclo[2.2.1]heptane analogues of thromboxane A2/PGH2.
Synthesis and pharmacological characterization of 5-(2-dodecylphenyl)-4,6-dithianonanedioic acid and 5-[2-(8-phenyloctyl)phenyl]-4,6-dithianonanedioic acid: prototypes of a novel class of leukotriene antagonists.
Stereostructure-activity relationship of opioid agonist and antagonist bivalent ligands. Evidence for bridging between vicinal opioid receptors.
Inhibition of human dihydrofolate reductase by 4,6-diamino-1,2-dihydro-2,2-dimethyl-1-(substituted-phenyl)-s-triazine s. A quantitative structure-activity relationship analysis.
Synthesis and antiinflammatory activity of [(cycloalkylmethyl)phenyl]acetic acids and related compounds.
Synthesis of 2-(2,3-dihydro-2-oxo-1,3,4-oxadiazol-5-yl) benzo heterocycles. A novel series of orally active antiallergic agents.
Potential tissue-imaging agents: 23-(trimethyl [117mSn]stannyl)-24-nor-5 alpha-cholan-3 beta-ol.
Synthesis of 3-hydroxy-2- and -4-pyridone nucleosides as potential antitumor agents.
Synthesis and pharmacological activity of partially modified retro-inverso dermorphin tetrapeptides.
Inhibition by 5-(substituted-benzyl)-2,4-diaminopyrimidines of murine tumor (L5178Y) cell cultures sensitive to and resistant to methotrexate. Further evidence for the sensitivity of resistant cells to hydrophobic drugs.
Synthesis of prostanoids with bicyclo[2.2.1]heptane, bicyclo[3.1.1]heptane, and bicyclo[2.2.2]octane ring systems. Activities of 15-hydroxy epimers on human platelets.
Syntheses and anthelmintic activity of alkyl 5(6)-(substituted-carbamoyl)- and 5(6)-(disubstituted-carbamoyl)benzimidazole-2-carbamates and related compounds.
Molluscicidal Phloroglucinols from the Fern Elaphoglossum piloselloides.
Ambuic acid and torreyanic acid derivatives from the endolichenic fungus Pestalotiopsis sp.
Triterpene saponins from Bacopa monnieri and their antidepressant effects in two mice models.
New phenylpropenoids, bis(1-phenylethyl)phenols, bisquinolinone alkaloid, and anti-inflammatory constituents from Zanthoxylum integrifoliolum.
Nuttingins A-F and malonganenones D-H, tetraprenylated alkaloids from the Tanzanian gorgonian Euplexaura nuttingi.
Antiproliferative triterpenes from Melaleuca ericifolia.
Biotransformation of polymethoxylated flavonoids: access to their 4'-O-demethylated metabolites.
Sesquiterpenoids and phenylpropanoids from pericarps of Illicium oligandrum.
Subinhibitory concentrations of antibiotics induce phenazine production in a marine Streptomyces sp.
Lipoxygenase inhibitory constituents of the fruits of noni (Morinda citrifolia) collected in Tahiti.
Cytotoxic and antibacterial sesquiterpenes from Thespesia populnea.
Brianodins A-D, briarane-type diterpenoids from soft coral Pachyclavularia sp.
Flavonoids as opioid receptor ligands: identification and preliminary structure-activity relationships.
Tetradehydrohalicyclamine A and 22-hydroxyhalicyclamine A, new cytotoxic bis-piperidine alkaloids from a marine sponge Amphimedon sp.
Cytotoxic C47-polyacetylene carboxylic acids from a marine sponge Pertrosia sp.
Pestalotheols A-D, bioactive metabolites from the plant endophytic fungus Pestalotiopsis theae.
Antimicrobial prenylated anthracene derivatives from the leaves of Harungana madagascariensis.
Thiomycalolides: new cytotoxic trisoxazole-containing macrolides isolated from a marine sponge Mycale sp.
Purpurediolin and purpurenin, two new cytotoxic adjacent bis-tetrahydrofuran annonaceous acetogenins from the seeds of Annona purpurea.
Activity-guided isolation of constituents of Tephrosia purpurea with the potential to induce the phase II enzyme, quinone reductase.
Bioactive ent-kaurene diterpenoids from Annona senegalensis.
Facile total synthesis and antimicrobial activity of the marine fatty acids (Z)-2-methoxy-5-hexadecenoic acid and (Z)-2-methoxy-6-hexadecenoic acid.
Maprouneacin, a new daphnane diterpenoid with potent antihyperglycemic activity from Maprounea africana.
Rubrobramide, a cytotoxic and phytotoxic metabolite from Cladobotyrum rubrobrunnescens.
Carmabins A and B, new lipopeptides from the Caribbean cyanobacterium Lyngbya majuscula.
Isolation and characterization of a new triterpene from Iris missouriensis.
Isolation and identification of "diazepam-like" compounds from bovine urine.
On the structures of crambescins B and C1.
Flavonone and chalcone derivatives from Cryptocarya kurzii.
Potent inhibitors of histamine release, two novel triterpenoids from the Okinawan marine sponge Penares incrustans.
Antineoplastic agents, 103. The isolation and structure of hypoestestatins 1 and 2 from the East African Hypoestes verticillaris.
Phytochemical and biological screening of Saudi medicinal plants, Part 6. Isolation of 2 alpha-hydroxyalantolactone the antileukemic principle of Francoeuria crispa.
New verticillin and glisoprenin analogues from gliocladium catenulatum, a mycoparasite of aspergillus flavus sclerotia
A cyclitol derivative as a replication inhibitor from the marine sponge Petrosia sp.
Cardiovascular effects of aspidofractinine-type alkaloids from Kopsia.
Squamotacin: an annonaceous acetogenin with cytotoxic selectivity for the human prostate tumor cell line (PC-3).
Synthesis and evaluation of 1-(arylsulfonyl)-2-[(methoxycarbonyl)sulfenyl]-1-methylhydrazines++ + as antineoplastic agents.
O-carbamoylsalicylates: agents for modification of hemoglobins.
Quantitative structure-activity relationships for the inhibition of Escherichia coli dihydrofolate reductase by 5-(substituted benzyl)-2,4-diaminopyrimidines.
Inactivation of gamma-aminobutyric acid aminotransferase by (S,E)-4-amino-5-fluoropent-2-enoic acid and effect on the enzyme of (E)-3-(1-aminocyclopropyl)-2-propenoic acid.
Synthesis and biochemical properties of 8-amino-6-fluoro-9-beta-D-ribofuranosyl-9H-purine.
Structure-activity relationships in 1,4-benzodioxan-related compounds. Investigation on the role of the dehydrodioxane ring on alpha 1-adrenoreceptor blocking activity.
Synthesis of 11H-pyridocarbazoles and derivatives. Comparison of their DNA binding and antitumor activity with those of 6H- and 7H-pyridocarbazoles.
Synthesis and biological activities of arginine-vasopressin analogues with 4-hydroxyproline in position 7.
Acetylenic nucleosides. 4. 1-beta-D-arabinofuranosyl-5-ethynylcytosine. Improved synthesis and evaluation of biochemical and antiviral properties.
New alpha-methylene gamma-lactone derivatives of substituted nucleic acid bases as potential anticancer agents.
Conformation and activity of tetrahydrofuran lignans and analogues as specific platelet activating factor antagonists.
Structure-activity relationships among analogues of pemedolac, cis-1-ethyl-1,3,4,9-tetrahydro-4-(phenylmethyl)pyrano[3,4-b]indo le-1-a cetic acid, a potent analgesic agent.
Structural studies on bioactive compounds. 4. A structure-antitumor activity study on analogues of N-methylformamide.
Aromatase inhibition by 5-substituted pyrimidines and dihydropyrimidines.
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 5. 3',5'-Dimethoxy-4'-substituted-benzyl analogues of trimethoprim.
5-[(Aminoalkyl)amino]-substituted anthra[1,9-cd]pyrazol-6(2H)-ones as novel anticancer agents. Synthesis and biological evaluation.
Nonsteroidal antiinflammatory agents. 14. Synthesis and pharmacological profile of 6-chloro-5-(cyclopentylmethyl)indan-1-carboxylic acid.
Dibenz[b,e]oxepinalkanoic acids as nonsteroidal antiinflammatory agents. 4. Synthesis and evaluation of 4-(4,10-dihydro-10-oxothieno[3,2-c] [1]benzoxepin-8-yl)butanol and -butyric acid and related derivatives.
Dependence of beta-lactamase stability on substructures within beta-lactam antibiotics.
2,3-dihydro-3-(1-pyrryl)spiro[benzofuran-2,4'-piperidine]s and 2,3-dihydro-3-(1-pyrryl)spiro[benzofuran-2,3'-pyrrolidine]s: novel antihypertensive agents.
N-(Phosphonoacetyl)amino phosphonates. Phosphonate analogues of N-(phosphonoacetyl)-L-aspartic acid (PALA).
6,7-Dihydro-5-[[(cis-2-hydroxy-trans-3-phenoxycyclopentyl)amino] methyl]-2-methylbenzo[b]thiophen-4(5H)-one: a novel alpha 1-adrenergic receptor antagonist and renal vasodilator.
Inhibition of dihydrofolate reductase: structure-activity correlations of quinazolines based upon molecular shape analysis.
Synthesis of a novel class of heteroaromatic amino acids and their use in the preparation of analogues of luteinizing hormone-releasing hormone.
Radioiodine-labeled N,N-dimethyl-N'-(2-hydroxy-3-alkyl-5-iodobenzyl)-1,3-propanediamines for brain perfusion imaging.
Synthesis and anthelmintic activity of 5(6)-(benzimidazol-2-ylcarbamoyl) and (4-substituted piperazin-1-yl)benzimidazoles.
3-Alkyl-2-aryl-3H-naphth[1,2-d]imidazoles, a novel class of nonacidic antiinflammatory agents.
Synthesis and central dopaminergic effects of N-(4,6-dimethyl-2-pyridinyl)benzamides.
Synthesis and antileishmanial activity of 6-methoxy-4-methyl-N-[6-(substituted-1-piperazinyl)hexyl]-8-quinolinamines and related compounds.
Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo.
Cyclic peptides from an endophytic fungus obtained from a mangrove leaf (Kandelia candel).
Studies on terpenoids produced by actinomycetes: oxaloterpins A, B, C, D, and E, diterpenes from Streptomyces sp. KO-3988.
Discorhabdins revisited: cytotoxic alkaloids from southern australian marine sponges of the genera Higginsia and Spongosorites.
Citrinin dimers from the halotolerant fungus Penicillium citrinum B-57.
Nitrogen-containing verticillene diterpenoids from the Taiwanese soft coral Cespitularia taeniata.
Synthesis of valiolamine and some precursors for bioactive carbaglycosylamines from (-)-vibo-quercitol produced by biogenesis of myo-inositol.
Derrubone, an inhibitor of the Hsp90 protein folding machinery.
Macrolactins O-R, glycosylated 24-membered lactones from Bacillus sp. AH159-1.
Ten-membered lactones from the marine-derived fungus Curvularia sp.
Kempopeptins A and B, serine protease inhibitors with different selectivity profiles from a marine cyanobacterium, Lyngbya sp.
5-alkylresorcinols from Merulius incarnatus.
Steroids and sesquiterpenoids from the soft corals Dendronephthya gigantea and Lemnalia cervicorni.
A new secosterol from the Indonesian octocoral Pachyclavularia violacea.
Hirsutellide A, a new antimycobacterial cyclohexadepsipeptide from the entomopathogenic fungus Hirsutella kobayasii.
A common protein fold topology shared by flavonoid biosynthetic enzymes and therapeutic targets.
Antifungal flavonoids from Hildegardia barteri.
New decalin derivatives, eujavanoic acids A and B, from Eupenicillium javanicum.
A dihydroflavonol glucoside from Commiphora africana that mediates DNA strand scission.
Antitumor agents, 71. Nudaphantin, a new cytotoxic germacranolide, and elephantopin from Elephantopus nudatus.
Stellettin A, a new triterpenoid pigment from the marine sponge Stelletta tenuis.
Antihypertensive activity of 6-O-galloyl-D-glucose, a phenolic glycoside from Sapium sebiferum.
Toxicants from mangrove plants, V. Isolation of the piscicide, 2-hydroxy-5-methoxy-3-undecyl-1,4 benzoquinone (5-O-methylembelin) from Aegiceras corniculatum.
New cycloartanol sulfates from the alga Tydemania expeditionis: inhibitors of the protein tyrosine kinase pp60v-src.
Plant anticancer agents, XXXIV. Cucurbitacins from Elaeocarpus dolichostylus.
Cytotoxic diterpenoids from Isodon megathyrsus.
Nepheliosyne A, new C47 acetylenic acid from the Okinawan marine sponge Xestospongia sp.
Anti-AIDS agents, 10. Acacetin-7-O-beta-D-galactopyranoside, an anti-HIV principle from Chrysanthemum morifolium and a structure-activity correlation with some related flavonoids.
New diterpenes from the gorgonian Solenopodium excavatum.
Isolation and structure of harzianum A: a new trichothecene from Trichoderma harzianum.
Secondary metabolites by chemical screening, 26.1 7-O-beta-D-galactosyl-brefeldin A via transglycosylation with Penicillium brefeldianum.
A monogalactosyl diacylglycerol from a cultured marine dinoflagellate, Scrippsiella trochoidea.
The crystal structure and cytotoxicity of goniodiol-7-monoacetate from Goniothalamus amuyon.
New mycalolides from the marine sponge Mycale magellanica and their interconversion.
Plasmid-mediated resistance to cephalosporins in Salmonella enterica serovar Typhi.
10-Oximeguanacone, the first nitrogenated acetogenin derivative found to be a potent inhibitor of mitochondrial complex I.
Isolation and characterization of an antiviral flavonoid from Waldsteinia fragarioides.
Cystodytins D-I, new cytotoxic tetracyclic aromatic alkaloids from the Okinawan marine tunicate Cystodytes dellechiajei.
A flavone with antiinflammatory activity from the roots of Rhus undulata.
Plant metabolites. New compounds and anti-inflammatory activity of Uncaria tomentosa.
Correlation of the anticholinesterase and molluscicidal activity of the latex of Euphorbia royleana on the snail Lymnaea acuminata.
The isolation of loliolide from an Indian Ocean opisthobranch mollusc.
2,2-Difluoro-5-hexyne-1,4-diamine: a potent enzyme-activated inhibitor of ornithine decarboxylase.
Synthesis and biological activity of analogues of beta-chlornaltrexamine and beta-funaltrexamine at opioid receptors.
Studies on hindered phenols and analogues. 1. Hypolipidemic and hypoglycemic agents with ability to inhibit lipid peroxidation.
Development of phosphonate derivatives of gadolinium chelates for NMR imaging of calcified soft tissues.
Synthesis and biological activity of the four stereoisomers of 6-[4-[3-[[2-hydroxy-3-[4-[2- (cyclopropylmethoxy)ethyl]phenoxy]propyl]amino]-propionamido] phenyl]-5-methyl-4,5-dihydro-3(2H)-pyridazinone, a combined vasodilator and beta-adrenoceptor antagonist.
Comparison of (-)-eseroline with (+)-eseroline and dihydroseco analogues in antinociceptive assays: confirmation of rubreserine structure by X-ray analysis.
Isozyme-specific enzyme inhibitors. 12. C- and N-methylmethionines as substrates and inhibitors of methionine adenosyltransferases of normal and hepatoma rat tissues.
Leukotriene receptor antagonists. 4. Synthesis and leukotriene D4/E4 receptor antagonist activity of 4-(alkyl)acetophenone derivatives.
Facile synthesis of 2-[(3-aminopropyl)thio]adenosine 5'-diphosphate: a key intermediate for the synthesis of molecular probes of adenosine 5'-diphosphate function.
Unsaturated heterocyclic amines as potent time-dependent inhibitors of dopamine beta-hydroxylase.
Imidazo[2,1-b]benzothiazoles. 2. New immunosuppressive agents.
Chemical aspects of metoprolol metabolism. Asymmetric synthesis and absolute configuration of the 3-[4-(1-hydroxy-2-methoxyethyl)phenoxy]-1-(isopropylamino)-2-propanols , the diastereomeric benzylic hydroxylation metabolites.
Bis(4-hydroxyphenyl)[2-(phenoxysulfonyl)phenyl]methane: isolation and structure elucidation of a novel estrogen from commercial preparations of phenol red (phenolsulfonphthalein)
Synthesis and dopamine autoreceptor activity of a 5-(methylmercapto)methyl-substituted derivative of (+/-)-3-PPP (3-(3-hydroxyphenyl)-1-n-propylpiperidine).
Antiulcer agents. 1. Gastric antisecretory and cytoprotective properties of substituted imidazo[1,2-a]pyridines.
3-Alkyl-3-hydroxyglutaric acids: a new class of hypocholesterolemic HMG CoA reductase inhibitors. 1.
Sulfur analogues of psychotomimetic agents. Monothio analogues of mescaline and isomescaline.
Sulfur analogues of psychotomimetic agents. 3. Ethyl homologues of mescaline and their monothio analogues.
(Acylaryloxy)acetic acid diuretics. 5. [(2-Alkyl- and 2,2-disubstituted-1,3-dioxo-5-indanyl)oxy]acetic acids.
Cytonic acids A and B: novel tridepside inhibitors of hCMV protease from the endophytic fungus Cytonaema species.
Gamma-lactone carbazoles from Clausena anisata.
Inhibition of renin by angiotensinogen peptide fragments containing the hydroxy amino acid residue 5-amino-3-hydroxy-7-methyloctanoic acid.
Tetrahdroxysqualene from Rhus taitensis shows antimycobacterial activity against Mycobacterium tuberculosis.
Cembrane diterpenoids from the taiwanese soft coral Sarcophyton stolidotum.
Synthesis and antineoplastic activity of a novel series of phosphoramide mustard analogues of pyrimidine deoxyribonucleosides.
Antiviral constituents against respiratory viruses from Mikania micrantha.
Synthesis and antiallergy activity of 4-oxopyrano[3,2-b]indoles.
Chemistry, pharmacology, and structure-activity relationships with a new type of imidazolines exerting a specific bradycardic action at a cardiac site.
synthesis and antihypertensive activity of 2-sulfonamido- and 2-sulfamido-1,3,4,6,7,11b alpha-hexahydro-2H-benzo[a]quinolizines.
Allylprodine analogues as receptor probes. Evidence that phenolic and nonphenolic ligands interact with different subsites on identical opioid receptors.
Antineoplastic agents. 534. isolation and structure of sansevistatins 1 and 2 from the African Sansevieria ehrenbergii.
Cimipronidine, a cyclic guanidine alkaloid from Cimicifuga racemosa.
Lanostane triterpenoids and triterpene glycosides from the fruit body of Fomitopsis pinicola and their inhibitory activity against COX-1 and COX-2.
Isolation and characterization of five new tetrasaccharide glycosides from the roots of Ipomoea stans and their cytotoxic activity.
Glaciapyrroles A, B, and C, pyrrolosesquiterpenes from a Streptomyces sp. isolated from an Alaskan marine sediment.
Cespihypotins Q-V, verticillene diterpenoids from Cespitularia hypotentaculata.
Cytotoxic prenylflavonoids from Artocarpus elasticus.
A new cytotoxic calyculinamide derivative, geometricin A, from the Australian sponge Luffariella geometrica.
Sesquiterpenoids from Artemisia gilvescens and an anti-MRSA compound.
Ipomoeassins A-E, cytotoxic macrocyclic glycoresins from the leaves of Ipomoea squamosa from the Suriname rainforest.
Structure and absolute configuration of nyasol and hinokiresinol via synthesis and vibrational circular dichroism spectroscopy.
27-norlanostane glycosides from the bulbs of Muscari paradoxum.
Chemical constituents from the Colombian medicinal plant Maytenus laevis.
Chromenes from the brown alga Sargassum siliquastrum.
Acylphloroglucinol derivatives from Mahurea palustris.
The transgenic Arabidopsis plant system, pER8-GFP, as a powerful tool in searching for natural product estrogen-agonists/antagonists.
Pentasaccharide glycosides from the roots of Ipomoea murucoides.
KPC-producing extreme drug-resistant Klebsiella pneumoniae isolate from a patient with diabetes mellitus and chronic renal failure on hemodialysis in South Korea.
Alkoxyalkyl esters of 9-(s)-(3-hydroxy-2-phosphonomethoxypropyl) adenine are potent and selective inhibitors of hepatitis B virus (HBV) replication in vitro and in HBV transgenic mice in vivo.
Effects of ceftobiprole and oxacillin on mecA expression in methicillin-resistant Staphylococcus aureus clinical isolates.
Cytotoxic and antimalarial alkaloids from the bulbs of Crinum amabile.
Comparative pharmacokinetics of ceftaroline in rats, rabbits, and monkeys following a single intravenous or intramuscular injection.
Developments in marine natural products. Receptor-specific bioactive compounds.
In vitro activity of fidaxomicin (OPT-80) tested against contemporary clinical isolates of Staphylococcus spp. and Enterococcus spp.
Isolation of picropolygamain from the resin of Bursera simaruba.
Synergistic effect of flavones and flavonols against herpes simplex virus type 1 in cell culture. Comparison with the antiviral activity of propolis.
5-Epi-isospongiaquinone, a new sesquiterpene/quinone antibiotic from an Australian marine sponge, Spongia hispida.
Chemical investigation and anti-inflammatory activity of Vitex negundo seeds.
Fasting increases tobramycin oral absorption in mice.
Marine alkaloids, 15. Two alkaloids, flustramine E and debromoflustramine B, from the marine bryozoan Flustra foliacea.
Specificity of induction of the vanA and vanB operons in vancomycin-resistant enterococci by telavancin.
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
In vitro activities of telavancin and six comparator agents against anaerobic bacterial isolates.
3-aminopyridazine derivatives with atypical antidepressant, serotonergic, and dopaminergic activities.
Imidazo[1,2-a]pyrimidines and imidazo[1,2-a]pyrazines: the role of nitrogen position in inotropic activity.
Lysosomotropic agents. 7. Broad-spectrum antifungal activity of lysosomotropic detergents.
Mitomycin C analogues with a substituted hydrazine at position 7. Synthesis, spectral properties, and biological activity.
Potential tumor- or organ-imaging agents. 27. Polyiodinated 1,3-disubstituted and 1,2,3-trisubstituted triacylglycerols.
Dopamine agonists related to 3-allyl-6-chloro-2,3,4,5-tetrahydro-1-(4-hydroxyphenyl)-1H-3-benzaz epi ne-7, 8-diol. 6-Position modifications.
Radioiodinated benzodiazepines: agents for mapping glial tumors.
Synthesis and inhibition of human acrosin and trypsin and acute toxicity of aryl 4-guanidinobenzoates.
New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1.
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
Synthesis and dopamine agonist and antagonist effects of (R)-(-)- and (S)-(+)-11-hydroxy-N-n-propylnoraporphine.
Quantitative structure-activity relationships of the bitter thresholds of amino acids, peptides, and their derivatives.
Cardiotonic agents. 1-Methyl-7-(4-pyridyl)-5,6,7,8-tetrahydro-3 (2H)-isoquinolinones and related compounds. Synthesis and activity.
Improved delivery through biological membranes. 13. Brain-specific delivery of dopamine with a dihydropyridine in equilibrium with pyridinium salt type redox delivery system.
Bicyclic lactones derived from kainic acid as novel selective antagonists of neuroexcitatory amino acids.
Synthesis and anticholinergic properties of the enantiomers of 4-(isopropylamino)-2-(2-pyridyl)-2-phenylbutyramide, the mono-N-dealkylated metabolite of disopyramide.
2-Arylpyrazolo[4,3-c]quinolin-3-ones: novel agonist, partial agonist, and antagonist of benzodiazepines.
Synthesis and pharmacological evaluation of conformationally restricted phenothiazine analogues.
Synthesis and hypoglycemic activity of phenylalkyloxiranecarboxylic acid derivatives.
A new stable prostacyclin mimic, 7-oxoprostaglandin I2.
Aminocaprophenone- and pyrrolidine-type alkaloids from the leaves of Ficus septica.
Synthesis and biochemical screening of phenylselenium-substituted steroid hormones.
Prostaglandins and congeners. 25. Inhibition of gastric acid secretion. Replacement of the carboxylate moiety of a prostaglandin with a hydroxymethylketo functional group.
2,4-Diamino-5-benzylpyrimidines and analogues as antibacterial agents. 2. C-Alkylation of pyrimidines with Mannich bases and application to the synthesis of trimethoprim and analogues.
[1-beta-Mercapto-beta,beta-cyclopentamethylenepropionic acid),2-(O-methyl)tyrosine ]argine-vasopressin and [1-beta-mercapto-beta,beta-cyclopentamethylenepropionic acid)]argine-vasopressine, two highly potent antagonists of the vasopressor response to arginine-vasopressin.
Hemolytic polar steroidal constituents of the starfish Aphelasterias japonica.
Computer graphics in drug design: molecular modeling of thyroid hormone-prealbumin interactions.
N2-1H-benzimidazol-2-yl-N4-phenyl-2,4-pyrimidinediamines and N2-1H-benzimidazol-2-yl-5,6,7,8-tetrahydro-N4-phenyl-2,4-quinazolinediamines as potential antifilarial agents.
Synthesis and antiarrhythmic and parasympatholytic properties of substituted phenols. 1. Heteroarylamine derivatives.
Halogenated boldine derivatives with enhanced monoamine receptor selectivity.
Gastric antisecretory agents. 1. Antisecretory and antiulcer activity of 5H-[1]benzopyrano[2,3-b]pyridin-5-ylureas and 5H-[1]benzothiopyrano[2,3-b]pyridin-5-ylureas.
Avrainvilloside, a 6-deoxy-6-aminoglucoglycerolipid from the green alga Avrainvillea nigricans.
Neuroprotective and antioxidant activity of compounds from the aerial parts of Dioscorea opposita.
Dihydrochalcones from the leaves of Pieris japonica.
Oxygenated terpenoids from a formosan soft coral Sinularia gibberosa.
Cytotoxic benzo[j]fluoranthene metabolites from Hypoxylon truncatum IFB-18, an endophyte of Artemisia annua.
Tenellones A and B from a Diaporthe sp.: two highly substituted benzophenone inhibitors of parasite cGMP-dependent protein kinase activity.
Thiobutacin, a novel antifungal and antioomycete antibiotic from Lechevalieria aerocolonigenes.
Montacin and cis-montacin, two new cytotoxic monotetrahydrofuran annonaceous acetogenins from Annona montana.
Hypoxia-selective antitumor agents: norsesterterpene peroxides from the marine sponge Diacarnus levii preferentially suppress the growth of tumor cells under hypoxic conditions.
C35 terpenoids from the bark of Calocedrus macrolepis var. formosana with activity against human cancer cell lines.
Monoterpene lactones from the seeds of Nephelium lappaceum.
Ophiocerins A-D and ophioceric acid: tetrahydropyran derivatives and an africane sesquiterpenoid from the freshwater aquatic fungus Ophioceras venezuelense.
Diterpenoids from Tetraclinis articulata that inhibit various human leukocyte functions.
Kalanchosine dimalate, an anti-inflammatory salt from Kalanchoe brasiliensis.
Terpenoid tetrahydroisoquinoline alkaloids emetine, klugine, and isocephaeline inhibit the activation of hypoxia-inducible factor-1 in breast tumor cells.
Insect antifeedants from Croton jatrophoides: structures of zumketol, zumsenin, and zumsenol.
Lignans and their degraded derivatives from Sarcostemma acidum.
Antiinflammatory activity of coumarins from Santolina oblongifolia.
New phenylpropanoid esters of sucrose from Polygonum lapathifolium.
New metabolites from the sponge Spongia agaricina.
Ophirapstanol trisulfate, a new biologically active steroid sulfate from the deep water marine sponge Topsentia ophiraphidites.
Cell-based screen for identification of inhibitors of tubulin polymerization.
Cytotoxic geranyl stilbenes from Macaranga schweinfurthii.
Ryanodyl 3-(pyridine-3-carboxylate): a novel ryanoid from Ryania insecticide.
Determination of cardenolides in hairy root cultures of Digitalis lanata by enzyme-linked immunosorbent assay.
Taxinine M, a new tetracyclic taxane from Taxus brevifolia.
Occurrence of gerrardine in Cassipourea guianensis.
Antitumor agents, 65. Brusatol and cleomiscosin-A, antileukemic principles from Brucea javanica.
Structure-activity relations of polyfunctional diterpenes of the daphnane type. I. Revised structure for resiniferatoxin and structure-activity relations of resiniferonol and some of its esters.
Biologically active metabolites from Xenorhabdus spp., Part 1. Dithiolopyrrolone derivatives with antibiotic activity.
The isolation and structure of modified bioactive nucleosides from Jaspis johnstoni.
Cyclic polyketide peroxides and acyclic diol analogues from the sponge Plakortis lita.
Plant anticancer agents. XXII. Isolation of a phorbol diester and its delta 5,6-7 beta-hydroperoxide derivative from Ostodes paniculata.
New jaspamide derivatives from the marine sponge Jaspis splendans collected in Vanuatu.
2-O-alpha-D-galactopyranosyl glycerol hexaacetate from Ruellia brittoniana.
Catharanthus alkaloids, XXXVIII. Confirming structural evidence and antineoplastic activity of the bisindole alkaloids leurosine-N'b-oxide (pleurosine), roseadine and vindolicine from Catharanthus roseus.
Sideroxylonal C, a new inhibitor of human plasminogen activator inhibitor type-1, from the flowers of Eucalyptus albens.
Excitatory amino acid neurotransmission.
Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
3-[(2-ethoxyphenoxy)methyl]piperidine derivatives. Synthesis and antidepressant activity.
Modification of the hydroxy lactone ring of camptothecin: inhibition of mammalian topoisomerase I and biological activity.
Synthesis and pharmacological evaluation of some 6-substituted 7-methyl-1,4-dioxa-7-azaspiro[4.5]decanes as potential dopamine agonists.
Heterocyclic quinones with potential antitumor activity. 2. Synthesis and antitumor activity of some benzimidazole-4,7-dione derivatives.
Evaluation of the side arm of (naphthylvinyl)pyridinium inhibitors of choline acetyltransferase.
Rational design of enzyme inhibitors: multisubstrate analogue inhibitors.
Syntheses of 5,6,7- and 5,7,8-trioxygenated 3',4'-dihydroxyflavones having alkoxy groups and their inhibitory activities against arachidonate 5-lipoxygenase.
Functional cholesteryl binding agents: synthesis, characterization, and evaluation of antibody binding to modified phospholipid vesicles.
Molecular design toward biologically significant compounds based on platelet activating factor: a highly selective agonist as a potential antihypertensive agent.
Chiral DNA gyrase inhibitors. 2. Asymmetric synthesis and biological activity of the enantiomers of 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H- pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid (ofloxacin).
Analgetic and antiinflammatory 7-aroylbenzofuran-5-ylacetic acids and 7-aroylbenzothiophene-5-ylacetic acids.
Dimeric 1,4-dihydropyridines as calcium channel antagonists.
[125I]-1-(2,5-dimethoxy-4-iodophenyl)-2-amino-propane: an iodinated radioligand that specifically labels the agonist high-affinity state of 5-HT2 serotonin receptors.
Acrylamide derivatives as antiallergic agents. 2. Synthesis and structure-activity relationships of N-[4-[4-(diphenylmethyl)-1-piperazinyl]butyl]-3-(3-pyridyl)acryl amides.
Conformationally restricted congeners of hypotensive and platelet aggregation inhibitors: 6-aryl-5-methyl-4,5-dihydro-3(2H)-pyridazinones derived from 5H-indeno[1,2-c]pyridazine.
Diuretic agents related to indapamide. 1. Synthesis and activity of 1-substituted 2-(4-chloro-3-sulfamoylbenzamido)isoindolines.
N2-(gamma-D-Glutamyl)-meso-2(L),2'(D)-diaminopimelic acid as the minimal prerequisite structure of FK-156: its acyl derivatives with potent immunostimulating activity.
Beta 1-selective adrenoceptor antagonists: examples of the 2-[4-[3-(substituted-amino)-2-hydroxypropoxy]phenyl]imidazole class.
Oxidation of uric acid. 4. Synthesis, structure, and diabetogenic action of 5-imino-2,4,6(1H,3H,5H)-pyrimidinetrione salts and their alloxan-like covalent adducts.
Anticoccidial activity of crown polyethers.
Synthesis and antiarrhythmic activity of new [(dialkylamino)alkyl]pyridylacetamides.
Synthesis and antitumor activity of 2-beta-D-ribofuranosylselenazole-4- carboxamide and related derivatives.
Ferric ion sequestering agents. 11. Synthesis and kinetics of iron removal from transferrin of catechoyl derivatives of desferrioxamine B.
Synthesis and antiherpetic activity of some 4-[(aryloxy)alkyl]pyrazoles.
Synthesis and antiinflammatory activity of 2,2'-diaminobiphenyl derivatives.
Bioactivation of the antitumor drugs 9-hydroxyellipticine and derivatives by a peroxidase-hydrogen peroxide system.
Computer-assisted structure-activity studies of chemical carcinogens. Aromatic amines.
Synthesis and antitumor activity of simple vinyl and alpha-methylene-gamma-butyrolactone sulfonate esters and silyl enol ethers.
Synthesis and antischistosomal activity of certain pyrazolo[1,5-a]pyrimidines.
Pyridoquinoxaline N-oxides. 2. Synthesis and antibacterial activity of tricyclic lactams.
Prostaglandin isosteres. 2. Chain-modified thiazolidinone prostaglandin analogues as renal vasodilators.
Substituted imidazo[2,3-alpha]pyridine-2-carbamate anthelmintics.
A new cembranolide from the soft coral Sinularia capillosa.
Aminomethyl-1,2,4-benzothiadiazines as potential analogues of gamma-aminobutyric acid. Unexpected discovery of a taurine antagonist.
Lorneamides A and B: two new aromatic amides from a southern Australian marine actinomycete.
New oleanene triterpenoid saponins from Madhuca longifolia.
Cerylimycins [corrected] A and B: antibacterial triterpenes from the new species Tricholoma sp. AU1.
Isolation of gelsedine-type indole alkaloids from Gelsemium elegans and evaluation of the cytotoxic activity of gelsemium alkaloids for A431 epidermoid carcinoma cells.
Rautandiols A and B, pterocarpans and cytotoxic constituents from Neorautanenia mitis.
Cytotoxic flavonol glycosides from Triplaris cumingiana.
Cyclic peptides of the nocardamine class from a marine-derived bacterium of the genus Streptomyces.
Homoflavonoids from Ophioglossum petiolatum.
Indoleamine 2,3-dioxygenase inhibitors from the Northeastern Pacific Marine Hydroid Garveia annulata.
Schisandrene, a dibenzocyclooctadiene lignan from Schisandra chinensis: structure-antioxidant activity relationships of dibenzocyclooctadiene lignans.
Communesins G and H, new alkaloids from the psychrotolerant fungus Penicillium rivulum.
Bisnortriterpenes from Salacia madagascariensis.
3-Nitropropionic acid (3-NPA), a potent antimycobacterial agent from endophytic fungi: is 3-NPA in some plants produced by endophytes?
An apigenin-derived xanthine oxidase inhibitor from Palhinhaea cernua.
A cyclopeptide from the Insect pathogenic fungus Cordyceps sp. BCC 1788.
Hispidin derivatives from the mushroom Inonotus xeranticus and their antioxidant activity.
Callysponginol sulfate A, an MT1-MMP inhibitor isolated from the marine sponge Callyspongia truncata.
Interference by naturally occurring fatty acids in a noncellular enzyme-based aromatase bioassay.
DNA polymerase beta inhibitors from Sandoricum koetjape.
Anticandidal activity of eupolauridine and onychine, alkaloids from Cleistopholis patens.
Cytotoxic and antimicrobial alkaloids from the Fijian sponge Xestospongia caycedoi.
Cylindol A, a novel biphenyl ether with 5-lipoxygenase inhibitory activity, and a related compound from Imperata Cylindrica.
Antiplatelet aggregation principles of Dendrobium loddigesii.
Four new dimeric peptide alkaloids, anchinopeptolides B-D, and cycloanchinopeptolide C, congeners of anchinopeptolide A, from the Mediterranean marine sponge Anchinoe tenacior.
Auranticins A and B: two new depsidones from a mangrove isolate of the fungus Preussia aurantiaca.
Marine soft corals of the genus Pseudopterogorgia: a resource for novel anti-inflammatory diterpenoids.
Studies on inhibitors of skin-tumor promotion, I. Inhibitory effects of triterpenes from Euptelea polyandra on Epstein-Barr virus activation.
5'-Hydroxyisoavrainvilleol, a new diphenylmethane derivative from the tropical green alga Avrainvillea nigricans.
UV-mediated genotoxicity of furanoquinoline and of certain tryptophan-derived alkaloids.
1'-(2-Phenyl-ethylene)-ditryptophenaline, a new dimeric diketopiperazine from Aspergillus flavus.
Cylindrene, a novel sesquiterpenoid from Imperata cylindrica with inhibitory activity on contractions of vascular smooth muscle.
Studies on iridoids of tissue cultures of Penstemon serrulatus: isolation and their antiproliferative properties.
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
BEL-2, an extended-spectrum beta-lactamase with increased activity toward expanded-spectrum cephalosporins in Pseudomonas aeruginosa.
Jaspisamides A-C, new cytotoxic macrolides from the Okinawan sponge Jaspis sp.
Sesquiterpenes from clove (Eugenia caryophyllata) as potential anticarcinogenic agents.
4-acetylaplykurodin B and aplykurodinone B, two ichthyotoxic degraded sterols from the Mediterranean mollusk Aplysia fasciata.
Murine model of a disseminated infection by the novel fungus Fonsecaea monophora and successful treatment with posaconazole.
Plant anticancer agents, XLIII. (E,E)-7, 12-dioxo-octadeca-8, 10-dien-1-oic acid (ostopanic acid), a cytotoxic fatty acid from Ostodes Paniculata.
Studies on the acetogenins of Formosan annonaceous plants. II. Cytotoxic acetogenins from Annona reticulata.
Antibacterial activity of N-pentylpantothenamide is due to inhibition of coenzyme a synthesis.
Cardiotonic agents. 2. (Imidazolyl)aroylimidazolones, highly potent and selective positive inotropic agents.
Synthesis and renal vasodilator activity of some dopamine agonist 1-aryl-2,3,4,5-tetrahydro-1H-3-benzazepine-7,8-diols: halogen and methyl analogues of fenoldopam.
3-(1-Indolinyl)benzylamines: a new class of analgesic agents.
Indazoles as indole bioisosteres: synthesis and evaluation of the tropanyl ester and amide of indazole-3-carboxylate as antagonists at the serotonin 5HT3 receptor.
Studies on prodrugs. 7. Synthesis and antimicrobial activity of 3-formylquinolone derivatives.
Isoprenoid (phosphinylmethyl)phosphonates as inhibitors of squalene synthetase.
Tranexamic acid derivatives with enhanced absorption.
Artificial siderophores. 1. Synthesis and microbial iron transport capabilities.
Selective thromboxane synthetase inhibitors and antihypertensive agents. New derivatives of 4-hydrazino-5H-pyridazino[4,5-b]indole, 4-hydrazinopyridazino[4,5-a]indole, and related compounds.
Design and synthesis of sodium (beta R*, gamma S*)-4-[[3-(4-acetyl-3-hydroxy-2-propylphenoxy)propyl] thio]-gamma-hydroxy-beta-methylbenzenebutanoate: a novel, selective, and orally active receptor antagonist of leukotriene D4.
(8 beta)-Ergoline-8-carboxylic acid cycloalkyl esters as serotonin antagonists: structure-activity study.
Structure-activity studies of trichothecenes: cytotoxicity of analogues and reaction products derived from T-2 toxin and neosolaniol.
Synthesis, pharmacological action, and receptor binding affinity of the enantiomeric 1-(1-phenyl-3-methylcyclohexyl)piperidines.
Potent angiotensin II antagonists with non-beta-branched amino acids in position 5.
Sustained brain-specific delivery of estradiol causes long-term suppression of luteinizing hormone secretion.
Ring-hydroxylated analogues of lucanthone as antitumor agents.
Isoxicam and related 4-hydroxy-N-isoxazolyl-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides. Potent nonsteroidal antiinflammatory agents.
Preliminary studies of mesoionic 3-(substituted-aryl)-psi-oxatriazoles as potential antihypertensive agents.
Synthesis and evaluation of the male antifertility properties of a series of N-unsubstituted sulfamates.
Junceellolides E-G, new briarane diterpenes from the West Pacific Ocean gorgonian Junceella fragilis.
Synthesis and cardiovascular activity of a new series of cyclohexylaralkylamine derivatives related to perhexiline.
Synthesis, in vitro opiate activity, and intramolecular tyrosine--tryptophan distances of [4-tryptophan]enkephalin analogues. A reassessment of conformational models of enkephalin in solution.
Antioxidant Lignans from the Fruits of Broussonetia papyrifera.
8-Hydroxy-2-(di-n-propylamino)tetralin, a new centrally acting 5-hydroxytryptamine receptor agonist.
CR377, a new pentaketide antifungal agent isolated from an endophytic fungus.
Synthesis and DNA binding of [3-[2'-(2-acetamidoethyl)-2,4'-bithiazole-4-carboxamido]propyl[dimethylsulfonium chloride, a fragment of bleomycin A2.
Octanol-physiological buffer distribution coefficients of lipophilic amines by reversed-phase high-performance liquid chromatography and their correlation with biological activity.
Prodrugs of L-cysteine as liver-protective agents. 2(RS)-Methylthiazolidine-4(R)-carboxylic acid, a latent cysteine.
Effects of certain hallucinogenic amphetamine analogues on the release of [3H]serotonin from rat brain synaptosomes.
Preparation of 2-amino-4(3H)-oxopyrimido[5,4-b] [1,4]thiazines (5-thiapterins) and their evaluation as cofactors for phenylalanine hydroxylase.
Aminotetralins as narcotic antagonists. 2. Synthesis and opiate-related activity of 1-phenyl-3-aminotetralins.
Beta-adrenoceptor stimulant properties of amidoalkylamino-substituted 1-aryl-2-ethanols and 1-(aryloxy)-2-propanols.
Hachijodines A-G: seven new cytotoxic 3-alkylpyridine alkaloids from two marine sponges of the genera Xestospongia and amphimedon.
cis-parthenolid-9-one from Anvillea garcinii.
Hyperjovinols A and B: Two new phloroglucinol derivatives from Hypericum jovis with antioxidant activity in cell cultures.
New biologically active triterpenoid saponins from Scabiosa tschiliensis.
Tupuseleiamides and basiliskamides, new acyldipeptides and antifungal polyketides produced in culture by a Bacillus laterosporus isolate obtained from a tropical marine habitat.
The sapogenin atroviolacegenin and its diglycoside atroviolaceoside from Allium atroviolaceum.
Chaetoglobosins Q, R, and T, three further new metabolites from Chaetomium globosum.
Phaeofurans and sorbicillin analogues from a fungicolous Phaeoacremonium species (NRRL 32148).
Cytotoxic diterpenoids from the soft coral Sarcophyton crassocaule.
Tricin from a malagasy connaraceous plant with potent antihistaminic activity.
Lowdenic acid: a new antifungal polyketide-derived metabolite from a new fungicolous Verticillium sp.
5,6:8,9-diepoxy and other cytotoxic sterols from the marine sponge Homaxinella sp.
Indole alkaloids from Cephalanceropsis gracilis.
Anti-babesial and anti-plasmodial compounds from Phyllanthus niruri.
Cinnamylphenols from Phyllodium pulchellum.
2-substituted furans from the roots of Polyalthia evecta.
Parasitenone, a new epoxycyclohexenone related to gabosine from the marine-derived fungus Aspergillus parasiticus.
Isolation and absolute configuration of ent-Halimane diterpenoids from Hymenaea courbaril from the Suriname rain forest.
Penasulfate A, a new alpha-glucosidase inhibitor from a marine sponge Penares sp.
Antitumor agents, 74. Bruceanol-A and -B, two new antileukemic quassinoids from Brucea antidysenterica.
Antineoplastic agents, 178. Isolation and structure of lychnostatins 1 and 2 from the South American Lychnophora antillana.
Coriadienin, the first annonaceous acetogenin with two double bonds isolated from Annona coriaceae.
Effect of Polygonum hydropiper sulfated flavonoids on lens aldose reductase and related enzymes.
Antitubercular natural products: berberine from the roots of commercial Hydrastis canadensis powder. Isolation of inactive 8-oxotetrahydrothalifendine, canadine, beta-hydrastine, and two new quinic acid esters, hycandinic acid esters-1 and -2.
New iridoids from the medicinal plant Barleria prionitis with potent activity against respiratory syncytial virus.
Isolation of 2-(3'-bromo-4'-hydroxyphenol)ethanamine from the New Zealand ascidian Cnemidocarpa bicornuta.
Novel cytotoxic cembranoids from the soft coral Sinularia flexibilis.
Globostellatic acids A-D, new cytotoxic isomalabaricane triterpenes from the marine sponge Stelletta globostellata.
Multidrug-resistance modulators from Stephania japonica.
Dendroamides, new cyclic hexapeptides from a blue-green alga. Multidrug-resistance reversing activity of dendroamide A.
Tetrin C, a new glycosylated polyene macrolide antibiotic produced by Streptomyces sp. GK9244.
Characterization of 6-epi-3-anhydroophiobolin B from Cochliobolus heterostrophus.
From a phagostimulant natural product to semisynthetic antifeedants against Spodoptera littoralis larvae: chemical transformations of the neoclerodane diterpenoid scutegalin B.
Sesquiterpenoids of the drimane class from a sponge of the genus Dysidea.
Schizanrins [corrected] B, C, D, and E, four new lignans from Kadsura matsudai and their antihepatitis activities.
Isolation of guaianoid pigments from the gorgonian Calicogorgia granulosa.
Activities of plant-derived phenols in a fibroblast cell culture model
Tsugicoline E, a new polyoxygenated protoilludane sesquiterpene from the fungus laurilia tsugicola1
Two fungal lanostane derivatives as phospholipase A2 inhibitors.
Studies on 1,2,3-triazoles. 13. (Piperazinylalkoxy) [1]benzopyrano[2,3-d]-1,2,3-triazol-9(1H)-ones with combined H1-antihistamine and mast cell stabilizing properties.
Conformationally defined adrenergic agents. 3. Modifications to the carbocyclic ring of 5,6-dihydroxy-1-(2-imidazolinyl)tetralin: improved separation of alpha 1 and alpha 2 adrenergic activities.
Structure-activity relationships in prazosin-related compounds. Effect of replacing a piperazine ring with an alkanediamine moiety on alpha 1-adrenoreceptor blocking activity.
Synthesis and anticholinesterase activity of (-)-N1-norphysostigmine, (-)-eseramine, and other N(1)-substituted analogues of (-)-physostigmine.
Synthesis and antitumor activities of unsymmetrically substituted 1,4-bis[(aminoalkyl)amino]anthracene-9,10-diones and related systems.
Synthesis and evaluation of a series of 2'-O-acyl derivatives of 9-beta-D-arabinofuranosyladenine as antiherpes agents.
Synthesis and evaluation of potential radioligands for the progesterone receptor.
Streptazones A, B(1), B(2), C, and D: new piperidine alkaloids from streptomycetes.
Modifications of primaquine as antimalarials. 3. 5-Phenoxy derivatives of primaquine.
Synthesis of some quaternary ammonium alkylating agents and their effects on soman-inhibited acetylcholinesterase.
Synthesis of [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors.
Pyrazolo[3,4-d]pyrimidine ribonucleosides as anticoccidials. 2. Synthesis and activity of some nucleosides of 4-(alkylamino)-1H-pyrazolo[3, 4-d]pyrimidines.
Analogues and derivatives of tenoxicam. 1. Synthesis and antiinflammatory activity of analogues with different residues on the ring nitrogen and the amide nitrogen.
An extension of the f-fragment method for the calculation of hydrophobic constants (log P) of conformationally defined systems.
Synthesis of analogues of the carboxyl protease inhibitor pepstatin. Effect of structure in subsite P3 on inhibition of pepsin.
Novel orally active inhibitors of passive cutaneous anaphylaxis in rats: N-[2-(4-pyridinyl)-4-pyrimidinyl]ureas and dialkyl [[[2-(4-pyridinyl)-4-pyrimidinyl]amino]methylene]malonates.
Synthesis, evaluation of chemical reactivity, and murine antineoplastic activity of 2-hydroxy-5-(3,4-dichlorophenyl)-6,7-bis(hydroxymethyl)-2,3-dihydro-1H- pyrrolizine bis(2-propylcarbamate) and 2-acyloxy derivatives as potential water-soluble prodrugs.
Potential anticonvulsants. 1. 5-Benzylhydantoins.
A quantitative structure-activity relationship study of the inhibitory action of a series of enkephalin-like peptides in the guinea pig ileum and mouse vas deferens bioassays.
Nostocyclyne A, a novel antimicrobial cyclophane from the cyanobacterium Nostoc sp.
2-(Aminomethyl)phenols, a new class of saluretic agents. 3. Effects of functional group reorientation and modification.
Pyrazolopyrimidine nucleosides. 12. Synthesis and biological activity of certain pyrazolo[3,4-d]pyrimidine nucleosides related to adenosine.
Comparison of quantitative structure-activity relationships of the inhibition of leukemia cells in culture with the inhibition of dihydrofolate reductase from leukemia cells and other cell types.
New skeletal sesquiterpenoids, caprariolides A-D, from Capraria biflora and their insecticidal activity.
Two new biologically active triterpene saponins from Acanthophyllum squarrosum.
Isoxazolidine-3,5-diones as lens aldose reductase inhibitors.
Alkaline phosphatase inhibition by a series of pyrido[2,1-b]quinazolines: A possible relationship with cromolyn-like antiallergy activity.
Theory and application of molecular potential energy fields in molecular shape analysis: a quantitative structure--activity relationship study of 2,4-diamino-5-benzylpyrimidines as dihydrofolate reductase inhibitors.
Ancistrolikokines A-C: new 5,8'-coupled naphthylisoquinoline alkaloids from Ancistrocladus likoko.
Constituents from the leaves of Phellodendron amurense var. wilsonii and their bioactivity.
Triterpenoid constituents isolated from the bark of Abies sachalinensis.
A new biologically active malyngamide from a New Zealand collection of the sea hare Bursatella leachii.
Haploscleridamine, a novel tryptamine-derived alkaloid from a sponge of the order haplosclerida: an inhibitor of cathepsin K.
Derrisin, a new rotenoid from Derris malaccensis plain and anti-Helicobacter pylori activity of its related constituents.
Bioactivity profiling using HPLC/microtiter-plate analysis: application to a New Zealand marine alga-derived fungus, Gliocladium sp.
Structures of new friedelane-type triterpenes and eudesmane-type sesquiterpene and aldose reductase inhibitors from Salacia chinensis.
Purealidin S and purpuramine J, bromotyrosine alkaloids from the Fijian marine sponge Druinella sp.
Gaboroquinones A and B and 4'-O-demethylknipholone-4'-O-beta-D-glucopyranoside, phenylanthraquinones from the roots of Bulbine frutescens.
A new sesquiterpenoid quinone and other related compounds from the Okinawan marine sponge Dactylospongia elegans.
Saponins from Polygala japonica and their effects on a forced swimming test in mice.
Purification, structure determination, and antimicrobial activity of neutramycins B-G.
Antifungal agents from the roots of Cudrania cochinchinensis against Candida, Cryptococcus, and Aspergillus species.
Agastinol and agastenol, novel lignans from Agastache rugosa and their evaluation in an apoptosis inhibition assay.
Isolation and characterization of miscellaneous secondary metabolites of Deprea subtriflora.
Eudesmane derivatives and other sesquiterpenes from Laggera alata.
New sesquiterpene derivatives from the red alga Laurencia scoparia. Isolation, structure determination, and anthelmintic activity.
New steroid glycosides from the deep-water starfish Mediaster murrayi.
Plant anticancer agents. XXIII. 6 alpha-senecioyloxychaparrin, a new antileukemic quassinoid from Simaba multiflora.
A new bromopyrrole alkaloid and the optical resolution of the racemate from the marine sponge homaxinella sp
Two new natural azafluorene alkaloids and a cytotoxic aporphine alkaloid from Polyalthia longifolia.
CAF-603: a new antifungal carotane sesquiterpene. Isolation and structure elucidation.
Malayenolides A-D, novel diterpenes from the indonesian sea pen veretillum malayense
Carotenoids of tunicates. III. The structural elucidation of two new marine carotenoids, amarouciaxanthin A and B.
Cytotoxic principles from the sap of Kalmia latifolia.
Quanolirones I and II, two new human cytomegalovirus protease inhibitors produced by Streptomyces sp. WC76535.
Guttiferone F, the first prenylated benzophenone from Allanblackia stuhlmannii.
Antioxidant metabolites from the tunicate Amaroucium multiplicatum.
The effect of ginsenoside-Rb2 on nitrogen balance.
Constituents of Erysimum inconspicuum. Two sulfur-containing lactone compounds.
Constituents of Nealchornea yapurenis (Euophorbiaceae).
A concise conversion of (-)-sclareol into (+)-coronarin E and (-)-7-epi-coronarin A
12-epi-teuscordonin and other neoclerodanes from Teucrium bicolor.
Antineoplastic agents. 398. Isolation and structure elucidation of cephalostatins 18 and 19.
Potential inhibitors of platelet aggregation from plant sources, V. Anthraquinones from seeds of Cassia obtusifolia and related compounds.
Justicidin B, a cytotoxic principle from Justicia pectoralis.
Production of anti-tumor-promoting iridoid glucosides in Genipa americana and its cell cultures.
Antitumor agents. 39. Bruceantinoside-A and -B, novel antileukemic quassinoid glucosides from Brucea antidysenterica.
Antitumor agents, 85. Cicutoxin, an antileukemic principle from Cicuta maculata, and the cytotoxicity of the related derivatives.
A novel synthesis of colchicide and analogues from thiocolchicine and congeners: reevaluation of colchicide as a potential antitumor agent.
Synthesis and antiviral activity of various 3'-azido, 3'-amino, 2',3'-unsaturated, and 2',3'-dideoxy analogues of pyrimidine deoxyribonucleosides against retroviruses.
N2-(4-Substituted-2,6-dichlorophenyl)-N1,N1-dimethylformamidines as antihypertensive and diuretic agents.
Synthesis, structure, and antitumor activity of N-salicyloyl-N'-(2-furylthiocarbonyl)hydrazine and its copper(II) complex.
Synthesis and pharmacological evaluation of a new class of 2-(2-aminothiazol-4-yl)-2-hydrazonoacetamido cephalosporins.
Synthesis and antimetastatic properties of stereoisomeric tricyclic bis(dioxopiperazines) in the Lewis lung carcinoma model.
Synthesis and biological activity of new peptide segments of gastrin exhibiting gastrin antagonist property.
Synthesis and antifungal activity of (E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphtha lenemethanamine (SF 86-327) and related allylamine derivatives with enhanced oral activity.
5-(Alkylsulfonyl)salicylanilides as potential dental antiplaque agents.
Antitumor agents. 78. Inhibition of human DNA topoisomerase II by podophyllotoxin and alpha-peltatin analogues.
Esters of N,N-disubstituted 2-hydroxyacetamides as a novel highly biolabile prodrug type for carboxylic acid agents.
Inhibition of cathepsin D by substrate analogues containing statine and by analogues of pepstatin.
Psychotropic agents: synthesis and antipsychotic activity of substituted beta-carbolines.
Thonningianins A and B, new antioxidants from the African medicinal herb Thonningia sanguinea.
Synthesis of 3-hydroxycyclophosphamide and studies related to its possible role in the metabolism of cyclophosphamide.
Inhibitors of gastric acid secretion: 3,4-diamino-1,2,5-thiadiazole 1-oxides and 1,1-dioxides as urea equivalents in a series of histamine H2-receptor antagonists.
Inhibition of inosinic acid dehydrogenase by 8-substituted purine nucleotides.
Oleanane-type isomeric triterpenoids from Barringtonia racemosa.
Chemical modification of aminoglycosides. 3. Synthesis of 2"-deoxykanamycins from neamine.
Novel cytotoxic diterpenes from Casearia arborea.
Synthesis and evaluation of 1,2,3,4-tetrahydro[1]benzothieno[2,3-h]isoquinolines as dopamine antagonists.
Potential histamine H2-receptor blockers. 3- and 2-indole derivatives as immobile analogues of tautomeric forms of cimetidine.
Synthesis and pharmacological activity of 6-aryl-2-azabicyclo[4.2.1]nonanes.
Synthesis and antiinflammatory activity of hexahydrothiopyrano[4,3-c]pyrazoles and related analogues.
Mitomycin C and porfiromycin analogues with substituted ethylamines at position 7.
Synthesis and antiallergy activity of 5-oxo-5H-thiazolo[2,3-b]quinazolinecarboxylic acids.
A new insecticidal pyranocyclohexenedione from kunzea ericifolia
New antibacterial metabolites from the cyanobacterium Nostoc commune(EAWAG 122b).
beta-adrenergic blocking agents. 24. Heterocyclic substituted 1-(aryloxy)-3-[[(amido)alkyl]amino]propan-2-ols.
Structure-activity relationships of some technetium-99m labeled [(thioethyl)amino] carboxylates.
Resolution and absolute configuration of an ergoline-related dopamine agonist, trans-4,4a,5,6,7,8,8a,9-Octahydro-5-propyl-1H(or 2H)-pyrazolo[3,4-g]quinoline.
Anticoccidial derivatives of 6-azauracil. 5. Potentiation by benzophenone side chains.
Synthesis of 11,12-epoxydrim-8,12-en-11-ol, 11,12-diacetoxydrimane, and warburganal from (-)-sclareol.
Two new minor polybrominated dibenzo-p-dioxins from the marine sponge Dysidea dendyi.
Cytotoxic monotetrahydrofuran acetogenins from Disepalum plagioneurum.
Isolation and structures of avicins D and G: in vitro tumor-inhibitory saponins derived from Acacia victoriae.
Total synthesis and biological evaluation of (5Z,9Z)-5,9-hexadecadienoic acid, an inhibitor of human topoisomerase I.
Antiproliferative triterpene saponins from Entada africana.
ent-Trachylobane diterpenoids from Xylopia langsdorffiana.
An antiinflammatory galactolipid from rose hip (Rosa canina) that inhibits chemotaxis of human peripheral blood neutrophils in vitro.
New onoceranoid triterpene constituents from Lansium domesticum.
Heliotropamide, a novel oxopyrrolidine-3-carboxamide from Heliotropium ovalifolium.
Synthesis of salvinorin A analogues as opioid receptor probes.
New anthracene derivatives from Coussarea macrophylla.
PSII inhibitory activity of resorcinolic lipids from Sorghum bicolor.
Sodium 1-(12-hydroxy)octadecanyl sulfate, an MMP2 inhibitor, isolated from a tunicate of the family Polyclinidae.
Engineering of the spinosyn PKS: directing starter unit incorporation.
New seco-prezizaane-type sesquiterpenes, jiadifenin with neurotrophic activity and 1,2-dehydroneomajucin from Illicium jiadifengpi.
In vivo assessment of the antimicrobial activity of a calcium-deficient apatite vancomycin drug delivery system in a methicillin-resistant Staphylococcus aureus rabbit osteomyelitis experimental model.
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
In vitro activity of a new isothiazoloquinolone, ACH-702, against Mycobacterium tuberculosis and other mycobacteria.
Inhibition of angiotensin-I-converting enzyme by tetrahydroxyxanthones isolated from Tripterospermum lanceolatum.
Two new tryptophan-derived alkaloids from the Okinawan marine sponge Aplysina sp.
In vitro properties of BAL30072, a novel siderophore sulfactam with activity against multiresistant gram-negative bacilli.
Biologic activities of the TolC-like protein of Neisseria meningitidis as assessed by functional complementation in Escherichia coli.
Ethnobotanical drug discovery based on medicine men's trials in the African savanna: screening of east African plants for antimicrobial activity II.
Three new cytotoxic metabolites from the marine sponge Plakortis halichondrioides.
Pantherinine, a cytotoxic aromatic alkaloid, and 7-deazainosine from the ascidian Aplidium pantherinum.
Trailing or paradoxical growth of Candida albicans when exposed to caspofungin is not associated with microsatellite genotypes.
Full Resistance and decreased susceptibility to carbapenems in IMP-13-producing Pseudomonas aeruginosa isolates from an outbreak.
Bisamides from Aglaia species: structure analysis and potential to reverse drug resistance with cultured cells.
Interaction of ceftobiprole with the low-affinity PBP 5 of Enterococcus faecium.
Further bioactive cembranolide diterpenes from the gorgonian Eunicea succinea.
Comparison of the anti-herpes simplex virus activities of propolis and 3-methyl-but-2-enyl caffeate.
Synthesis and structure-activity relationships of cytotoxic 7-hydroxy sterols.
Inhibition of chicken liver dihydrofolate reductase by 5-(substituted benzyl)-2,4-diaminopyrimidines. A quantitative structure-activity relationship and graphics analysis.
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
Hybromet: a ligand for purifying opioid receptors.
Leukotriene receptor antagonists. 1. Synthesis and structure-activity relationships of alkoxyacetophenone derivatives.
N-benzylpiperazino derivatives of 3-nitro-4-hydroxycoumarin with H1 antihistamine and mast cell stabilizing properties.
Synthesis and evaluation of 2-substituted 1-methyl-1-(4-tolylsulfonyl)hydrazines as antineoplastic agents.
A novel class of cardiotonics. Synthesis and pharmacological properties of [4-(substituted-amino)phenyl]pyridazinones and related derivatives.
Design of alternate substrate inhibitors of serine proteases. Synergistic use of alkyl substitution to impede enzyme-catalyzed deacylation.
Radioiodinated p-iodoclonidine: a high-affinity probe for the alpha 2-adrenergic receptor.
Inhibitors of cyclic AMP phosphodiesterase. 1. Analogues of cilostamide and anagrelide.
Synthesis and quantitative structure-activity relationships of antiallergic 2-hydroxy-N-1H-tetrazol-5-ylbenzamides and N-(2-hydroxyphenyl)-1H-tetrazole-5-carboxamides.
Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors.
Leukotriene receptor antagonists. 2. The [[(tetrazol-5-ylaryl)oxy]methyl]acetophenone derivatives.
Potential antitumor agents. 46. Structure-activity relationships for acridine monosubstituted derivatives of the antitumor agent N-[2-(dimethylamino)ethyl]-9-aminoacridine-4-carboxamide.
Irreversible enzyme inhibitors. 202. Candidate active-site-directed irreversible inhibitors of 5-fluoro-2'-deoxyuridine phosphorylase from Walker 256 rat tumor derived from 1-benzyl-5-(3-ethoxybenzyl)uracil.
Halichonadin E, a dimeric sesquiterpenoid from the sponge Halichondria sp.
Acanthosulfate, a sulfated hydroxyhydroquinone sesterterpenoid from the sponge Acanthodendrilla sp.
Cytotoxic ent-kauranoids from the medicinal plant Isodon xerophilus.
Cytotoxic clerodane diterpenoids and their hydrolysis products from Casearia nigrescens from the rainforest of Madagascar.
Sesquiterpene lactones from the root tubers of Lindera aggregata.
Bipinnatins K-Q, minor cembrane-type diterpenes from the West Indian Gorgonian Pseudopterogorgia kallos: isolation, structure assignment, and evaluation of biological activities.
Synthesis and antileukemic activity of 1-methyl-2,5-diphenyl-3,4-bis(hydroxymethyl)-, 1,2,3-triphenyl-4,5-bis(hydroxymethyl)-, and 1-methyl-2,3-diphenyl-4,5-bis(hydroxymethyl)pyrrole bis(N-methylcarbamate).
Structural characterization of daptomycin analogues A21978C1-3(d-Asn11) produced by a recombinant Streptomyces roseosporus strain.
Alboatisins A-C, ent-atisene diterpenoids from Isodon albopilosus.
Quantitative structure-activity relationships by distance geometry: thyroxine binding site.
Mollamides B and C, Cyclic hexapeptides from the indonesian tunicate Didemnum molle.
Potential prophylactic antitumor activity of retinylidene 1,3-diketones.
N,N'-Dialkylbis(dichlorophenyl)ethylenediamines and -imidazolidines: relationship between structure and estradiol receptor affinity.
Aromatic cyclic peroxides and related keto-compounds from the Plakortis sp. component of a sponge consortium.
Mammalian alkaloids. 8. Synthesis and biological effects of tetrahydropapaveroline related 1-benzyltetrahydroisoquinolines.
4a,9b-trans-8-Fluoro-5-(4-fluorophenyl)-2-[4-(4-fluorophenyl)-4-hydroxybutyl]-2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole hydrochloride, a new potent neuroleptic.
Two unusual acetogenins from the roots of Annona salzmanii.
Antimalarial dihydroisocoumarins produced by Geotrichum sp., an endophytic fungus of Crassocephalum crepidioides.
Isolation and in vitro antiplasmodial activities of alkaloids from Teclea trichocarpa: in vivo antimalarial activity and X-ray crystal structure of normelicopicine.
Novel diterpene lactones from Suregada multiflora.
Schizopeptin 791, a new anabeanopeptin-like cyclic peptide from the cyanobacterium Schizothrix sp.
Pimarane diterpene and cytochalasin derivatives from the endophytic fungus Eutypella scoparia PSU-D44.
Cycloleonuripeptides E and F, cyclic nonapeptides from Leonurus heterophyllus.
Brominated polyacetylenes from the Philippines sponge Diplastrella sp.
Anti-inflammatory constituents and new pterocarpanoid of Crotalaria pallida.
Novel cytotoxic oxygenated C29 sterols from the Colombian marine sponge Polymastia tenax.
(+)-N-Deoxymilitarinone A, a neuritogenic pyridone alkaloid from the insect pathogenic fungus Paecilomyces farinosus.
New cytotoxic bis 5-alkylresorcinol derivatives from the leaves of Oncostemon bojerianum from the Madagascar rainforest.
New acylated triterpene saponins from Silene fortunei that modulate lymphocyte proliferation.
Lipoxygenase inhibitory constituents from Periploca aphylla.
Biotransformation of imperatorin by Aspergillus flavus.
New myrsinol-related polyfunctional pentacyclic diterpene esters from roots of Euphorbia prolifera.
In vitro evaluation of antifungal properties of 8.O.4'-neolignans.
A new glycoside antimicrobial agent from Persoonia linearis x pinifolia.
Novel anti-HIV lancilactone C and related triterpenes from Kadsura lancilimba.
Synthesis of (+/-)-cassumunins A and B, new curcuminoid antioxidants having protective activity of the living cell against oxidative damage.
Munchiwarin, a prenylated chalcone from crotalaria trifoliastrum
Studies on zoapatle, II. Leucanthanolide, a novel sesquiterpene lactone from Montanoa leucantha ssp. leucantha.
3'-prenyl-4'-methoxy-isoflavone-7-O-beta-D-(2''-O-p-coumaroyl) glucopyranoside, a novel phytoestrogen from Sopubia delphinifolia.
Patellamide F, A new cytotoxic cyclic peptide from the colonial ascidian Lissoclinum patella.
Ability of different flavonoids to inhibit the procoagulant activity of adherent human monocytes.
Epolones: novel sesquiterpene-tropolones from fungus OS-F69284 that induce erythropoietin in human cells.
(Hydroxymethyl)acylfulvene: an illudin derivative with superior antitumor properties.
Specific inhibition of human immunodeficiency virus type 1 reverse transcriptase mediated by soulattrolide, a coumarin isolated from the latex of calophyllum teysmannii.
Dihydrolicoisoflavone, a new isoflavanone from Swartzia polyphylla.
Cytotoxic acylated Spermidine from a soft coral, Sinularia sp.
Certain norditerpenoid alkaloids and their cardiovascular action.
Spongiacidins A-D, new bromopyrrole alkaloids from hymeniacidon sponge
Antioxidant flavonoid glycosides from Daphniphyllum calycinum.
Barceloneic acid A, a new farnesyl-protein transferase inhibitor from a Phoma species.
Sinugibberol, a new cytotoxic cembranoid diterpene from the soft coral Sinularia gibberosa.
Two new nitrogenous sesquiterpenes from the sponge Axinyssa aplysinoides.
Makaluvamine N: a new pyrroloiminoquinone from Zyzzya fuliginosa.
Okaramines H and I, new okaramine congeners, from aspergillus aculeatus
Vinylogous amino acid esters: a new class of inactivators for thiol proteases.
1-Ethyl-7-[3-[(ethylamino)methyl]-1-pyrrolidinyl]-6,8-difluoro-1,4- dihydro-4-oxo-3-quinoline-carboxylic acid. New quinolone antibacterial with potent gram-positive activity.
Potent antagonists of vasopressin antidiuretic activity that lack the beta,beta-cyclopentamethylene-beta-mercaptopropionic acid substitution at position 1.
Chemically stable homocinnamyl analogues of the leukotrienes: synthesis and preliminary biological evaluation.
Conformationally restrained fentanyl analogues. 2. Synthesis and analgetic evaluation of perhydro-1,6-naphthyridin-2-ones.
Angiotensin-converting enzyme inhibitors: synthesis and biological activity of acyl tripeptide analogues of enalapril.
Nucleosides. 136. Synthesis and antiviral effects of several 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl)-5-alkyluracils. Some structure-activity relationships.
Preparation and biological evaluation of a potential photoaffinity label for the prostaglandin H2/thromboxane A2 receptor.
Receptor binding sites of hypoglycemic sulfonylureas and related [(acylamino)alkyl]benzoic acids.
Comparative pharmacology in the rat of ketamine and its two principal metabolites, norketamine and (Z)-6-hydroxynorketamine.
Cardiac glycosides. 6. Gitoxigenin C16 acetates, formates, methoxycarbonates, and digitoxosides. Synthesis and Na+,K+-ATPase inhibitory activities.
Antineoplastic activity of 3'-(chloroethyl)nitrosourea analogues of 2'-deoxyuridine and 2'-deoxy-5-fluorouridine.
Conformationally defined adrenergic agents. 5. Resolution, absolute configuration, and pharmacological characterization of the enantiomers of 2-(5,6-dihydroxy-1,2,3,4-tetrahydro-1-naphthyl)imidazoline: a potent agonist at alpha-adrenoceptors.
Synthesis and evaluation of radioiodinated (E)-18-iodo-17-octadecenoic acid as a model iodoalkenyl fatty acid for myocardial imaging.
(E)-2-(3,4-dimethoxyphenyl)-3-fluoroallylamine: a selective, enzyme-activated inhibitor of type B monoamine oxidase.
Structure-taste correlation of L-aspartyl dipeptides using SIMCA method.
Noval antitumor nitrosoureas and related compounds and their reactions with DNA.
DNA intercalating compounds as potential antitumor agents. 1. Preparation and properties of 7H-pyridocarbazoles.
Synthesis of 8-aryltetrahydroisoquinolines as dopamine antagonists and evaluation for potential neuroleptic activity.
Acylphloroglucinol, biyouyanagiol, biyouyanagin B, and related spiro-lactones from Hypericum chinense.
Hyaluronidase inhibitors from "Cimicifugae Rhizoma" (a mixture of the rhizomes of Cimicifuga dahurica and C. heracleifolia).
Inhibitors of polyamine biosynthesis. 8. Irreversible inhibition of mammalian S-adenosyl-L-methionine decarboxylase by substrate analogues.
Naamidines H and I, cytotoxic imidazole alkaloids from the Indonesian marine sponge Leucetta chagosensis.
Ecdysteroids from the Antarctic tunicate Synoicum adareanum.
Synthesis and anticancer activity of nitrosourea derivatives of phensuximide.
Metabolism of 6-substituted benzo[a]pyrene derivatives: O-dealkylation and regiospecificity in aromatic hydroxylation.
Prostaglandins and congeners. 22. Synthesis of 11-substituted derivatives of 11-deoxyprostaglandins E1 and E2. Potential bronchodilators.
Congeners of the alpha conformer of dopamine derived from octahydrobenz[h]isoquinoline.
Indole derivatives from a marine sponge-derived yeast as DPPH radical scavengers.
Mechanism of decomposition of N-hydroxyacetaminophen, a postulated toxic metabolite of acetaminophen.
2,4-Diamino-5-benzylpyrimidines as antibacterial agents. 4. 6-Substituted trimethoprim derivatives from phenolic Mannich intermediates. Application to the synthesis of trimethoprim and 3,5-dialkylbenzyl analogues.
Synthesis and pharmacology of 8-amino-3-(cyclopropylmethyl)-1,2,3,4,5,6-hexahydro-cis-6,11-dimethyl-2,6-methano-3-benzazocine and related compounds.
Some spiro analogues of the potent analgesic ketobemidone.
An antimicrobial guanidine-bearing sesterterpene from the cultured cyanobacterium Scytonema sp.
Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives.
Novel acylated triterpene glycosides from Muraltia heisteria.
Chemical constituents of Millettia taiwaniana: structure elucidation of five new isoflavonoids and their cancer chemopreventive activity.
A new bioactive sesterterpene and antiplasmodial alkaloids from the marine sponge hyrtios cf. erecta.
Two novel anti-emetic principles of Alpinia katsumadai.
New sesterterpenes from the Antarctic sponge Suberites sp.
New chromanone acids with antibacterial activity from Calophyllum brasiliense.
Bioactive constituents from Asparagus cochinchinensis.
Antineoplastic agents. 488. Isolation and structure of yukonin from a yukon territory fungus.
Globulixanthones A and B, two new cytotoxic xanthones with isoprenoid groups from the root bark of Symphonia globulifera.
New eremophilenolides from Ligulariopsis shichuana.
New nitrogenous Germacranes from a Thai marine sponge, Axinyssa n. sp.
Agonodepsides a and B: two new depsides from a filamentous fungus F7524.
Pachastrissamine, a cytotoxic anhydrophytosphingosine from a marine sponge, Pachastrissa sp.
Antifungal stilbenoids from Stemona collinsae.
New dimeric naphthopyrones from Aspergillus niger.
Cationic reduction of bastadin-4 to bastadin-5. Preparation of 5-[2h]-bastadin-5 by site-specific isotopic labeling.
Aureoverticillactam, a novel 22-atom macrocyclic lactam from the marine actinomycete Streptomyces aureoverticillatus.
Isolation and structure determination of an antimicrobial ester from a marine sediment-derived bacterium.
Antimicrobial agents from higher plants. Dragon's blood resin.
Triterpenes and saponins from Rudgea viburnioides.
Isolation of flavonoids and a chalcone from Helichrysum odoratissimum and synthesis of helichrysetin.
Antitumor agents, 112. Emarginatine B, a novel potent cytotoxic sesquiterpene pyridine alkaloid from Maytenus emarginata.
Isolation and structure determination of novel phosphatidylinositol kinase inhibitors, echiguanines A and B, from Streptomyces sp.
Synthesis of naphthoquinoles as potential antitumor agents related to jacaranone.
10'-Hydroxyusambarensine, a new antimalarial bisindole alkaloid from the roots of Strychnos usambarensis.
A pentacyclic triterpene with anti-inflammatory and analgesic activity from the roots of Commiphora merkeri.
Enhancement of biofilm formation by subinhibitory concentrations of macrolides in icaADBC-positive and -negative clinical isolates of Staphylococcus epidermidis.
Plant anticancer agents, XLII. Cytotoxic constituents from Wikstroemia elliptica.
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
Constitutents of Magnolia Grandiflora. III. Toxic principle of the wood.
Antitumor agents 50. 1 Morindaparvin-A, a new antileukemic anthraquinone, and alizarin-1-methyl ether from Morinda parvifolia, and the antileukemic activity of the related derivatives.
A new spermatostatic glycoside from the soft coral Sinularia crispa.
Anti-inflammatory compounds from Sideritis javalambrensis n-hexane extract.
Studies on inhibitors of skin-tumor promotion. Inhibitory effects of triterpenes from Cochlospermum tinctorium on Epstein-Barr virus activation.
Plant metabolites. Structure and in vitro antiviral activity of quinovic acid glycosides from Uncaria tomentosa and Guettarda platypoda.
Antiplatelet effects and vasorelaxing action of some constituents of Formosan plants.
Catharanthus alkaloids. XXXVI. Isolation of vincaleukoblastine (VLB) and periformyline from Catharanthus trichophyllus and pericyclivine from Catharanthus roseus.
Identification of an activator of the retinoid X receptor.
Two new macrolide sesquiterpene pyridine alkaloids from Maytenus emarginata: emarginatine G and the cytotoxic emarginatine F.
Pulcherralpin, a new diterpene ester from Caesalpinia pulcherrima.
Substituted 1-benzylimidazole-2-thiols as potent and orally active inhibitors of dopamine beta-hydroxylase.
Drug design via pharmacophore identification. Dopaminergic activity of 3H-benz[e]indol-8-amines and their mode of interaction with the dopamine receptor.
Synthesis, absolute configuration, and antibacterial activity of 6,7-dihydro-5,8-dimethyl-9-fluoro-1-oxo-1H,5H- benzo[ij]quinolizine-2-carboxylic acid.
Structure-activity relationship in PAF-acether. 3. Hydrophobic contribution to agonistic activity.
Dichloro[1,2-bis(4-hydroxyphenyl)ethylenediamine]platinum(II) complexes: an approach to develop compounds with a specific effect on the hormone-dependent mammary carcinoma.
Bicyclic lactam inhibitors of angiotensin converting enzyme.
Synthesis and hypolipidemic activities of 5-thienyl-4-oxazoleacetic acid derivatives.
Potential antiatherosclerotic agents. 5. An acyl-CoA:cholesterol O-acyltransferase inhibitor with hypocholesterolemic activity.
Substituted benzamides with conformationally restricted side chains. 1. Quinolizidine derivatives as selective gastric prokinetic agents.
Synthesis and pharmacological evaluation of cis-2,3,3a,4,5,6,7,7a-octahydro-3-oxoisoxazolo[5,4-c]pyridine: a structural analogue of the GABA agonist THIP.
Synthesis, biological evaluation, and quantitative structure-activity relationship analysis of 2-hydroxy-1H-isoindolediones as new cytostatic agents.
Inhibition of renin by substrate analogue inhibitors containing the olefinic amino acid 5(S)-amino-7-methyl-3(E)-octenoic acid.
9-(2-Fluorobenzyl)-6-(methylamino)-9H-purine hydrochloride. Synthesis and anticonvulsant activity.
Studies on Ca2+ channel antagonists. 5-[(3,4-Dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyphenyl)-2- isopropylpentyl isothiocyanate, a chemoaffinity ligand derived from verapamil.
Plant antitumor agents. 22. Isolation of 11-hydroxycamptothecin from Camptotheca acuminata Decne: total synthesis and biological activity.
(beta-Chloro-alpha-aminoethyl)phosphonic acids as inhibitors of alanine racemase and D-alanine:D-alanine ligase.
Pilocarpic acid esters as novel sequentially labile pilocarpine prodrugs for improved ocular delivery.
Synthesis and antineoplastic evaluations of 5,8-bis[(aminoalkyl)amino]-1-azaanthracene-9,10-diones.
Importance of the aromatic ring in adrenergic amines. 5. Nonaromatic analogues of phenylethanolamine as inhibitors of phenylethanolamine N-methyltransferase: role of hydrophobic and steric interactions.
Tetrahydro-2-benzoxepins: a novel family of hypotensives.
Eupha-7,9(11),24-trien-3beta-ol ("antiquol C") and other triterpenes from Euphorbia antiquorum latex and their inhibitory effects on Epstein-Barr virus activation.
Antimalarials. 12. Preparation of carbon isosteres of selected 4-pyridinemethanols as suppressive antimalarials.
Two new cytotoxic carbonimidic dichlorides from the nudibranch Reticulidia fungia.
Aristolactams and dioxoaporphines from Fissistigma balansae and Fissistigma oldhamii.
Rolloamides A and B, cytotoxic cyclic heptapeptides isolated from the Caribbean marine sponge Eurypon laughlini.
Sesquiterpene lactones from Scorzonera austriaca.
Synthesis of some 5-phenylhexahydroazepino[4,5-b]indoles as potential neuroleptic agents.
(+/-)-trans-2-(Aminomethyl)cyclobutanecarboxylic acid hydrochloride: a rigid analogue of gamma-aminobutyric acid.
Diaryl amidine derivatives as oncornaviral DNA polymerase inhibitors.
Laetirobin from the parasitic growth of Laetiporus sulphureus on Robinia pseudoacacia.
Moluccensins H-J, 30-ketophragmalin limonoids from Xylocarpus moluccensis.
2-(Aminomethyl)phenols, a new class of saluretic agents. 2. Synthesis and pharmacological properties of the 5-aza isostere of 2-(aminomethyl)-4-(1,1-dimethylethyl)-6-iodophenol.
Asterolaurins A-F, xenicane diterpenoids from the Taiwanese soft coral Asterospicularia laurae.
Effect of changing the COOH-terminal amide group present in the hydrophilic cluster of oxytocin to dimethylamide.
Synthetic modulators of the complement system. 1. Synthesis and biological activity of 5,5',5''-[1,3,6-naphthalenetriyltris(sulfonylimino)]-tris[1,3-benzenedisulfonic acid] hexasodium salt.
Third Smissman Award address: reminiscences and musings of a classical medicinal chemist.
Tyrosinase-inhibitory constituents from the twigs of Cinnamomum cassia.
Isolation and structural elucidation of euryjanicins B-D, proline-containing cycloheptapeptides from the Caribbean marine sponge Prosuberites laughlini.
Symplostatin 3, a new dolastatin 10 analogue from the marine cyanobacterium Symploca sp. VP452.
Santolindiacetylene, a polyacetylene derivative isolated from the essential oil of Santolina canescens.
Konbamidin, a new indole alkaloid from the Okinawan marine sponge Ircinia sp.
Antiinflammatory constituents of Celastrus orbiculatus inhibit the NF-kappaB activation and NO production.
Polyoxygenated dysidea sterols that inhibit the binding of [I125] IL-8 to the human recombinant IL-8 receptor type A.
Quinoline alkaloids and other constituents of Melicope semecarpifolia with antiplatelet aggregation activity.
Isolation and characterization of polybrominated diphenyl ethers as inhibitors of microtubule assembly from the marine sponge Phyllospongia dendyi collected at Palau.
Theopederins K and L. Highly potent cytotoxic metabolites from a marine sponge Discodermia species.
Anti-AIDS agents. 48.(1) Anti-HIV activity of moronic acid derivatives and the new melliferone-related triterpenoid isolated from Brazilian propolis.
Ma'iliohydrin, a cytotoxic chamigrene dibromohydrin from a Philippine Laurencia species.
Discorhabdins I and L, cytotoxic alkaloids from the sponge Latrunculia brevis.
Kawaguchipeptin B, an antibacterial cyclic undecapeptide from the cyanobacterium Microcystis aeruginosa.
Brasilidine A, a new cytotoxic isonitrile-containing indole alkaloid from the actinomycete Nocardia brasiliensis.
Phomadecalins A-D and phomapentenone A: new bioactive metabolites from Phoma sp. NRRL 25697, a fungal colonist of Hypoxylon stromata.
Synthesis, conformational analysis, and cytotoxicity of new analogues of the natural cyclodepsipeptide jaspamide.
Cyclopentabenzofuran lignan protein synthesis inhibitors from Aglaia odorata.
Hortein, a new natural product from the fungus Hortaea werneckii associated with the sponge Aplysina aerophoba.
Serrulatane diterpenes with antimycobacterial activity isolated from the West Indian sea whip Pseudopterogorgia elisabethae.
New cytotoxic cembranes from the sea pen Gyrophyllum sibogae.
(8a alpha,12a alpha,13a alpha)-5,8,8a,9,10,11,12,12a,13,13a-decahydro- 3-methoxy-12-(methylsulfonyl)-6H-isoquino[2,1-g][1,6]naphthyridi ne, a potent and highly selective alpha 2-adrenoceptor antagonist.
Synthesis and biological evaluation of cyclopropyl analogues of 2-amino-5-phosphonopentanoic acid.
4-[(Carboxymethyl)oxy]- and 4-[(carboxymethyl)amino]-5,7-dichloroquinoline-2-carboxylic acid: new antagonists of the strychnine-insensitive glycine binding site on the N-methyl-D-aspartate receptor complex.
Synthesis and dopamine receptor affinity of (R)-(-)-2-fluoro-N-n-propylnorapomorphine: a highly potent and selective dopamine D2 agonist.
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 8. Side chain ether analogues of lovastatin.
Quantitative structure-activity relationships of antitumor guanidinothiazolecarboxamides with survival enhancement for therapy in the 3LL Lewis lung carcinoma model.
N-azamonobactams. 2. Synthesis of some N-iminoacetic acid and N-glycyl analogues.
Benzofurans as mechanism-based inhibitors of dopamine beta-hydroxylase.
Synthesis, DNA-binding properties, and antitumor activity of novel distamycin derivatives.
2-(Fluoromethyl)-3-phytyl-1,4-naphthoquinone and its 2,3-epoxide. Inhibition of vitamin K epoxide reductase.
Synthesis of a series of nitrothiophenes with basic or electrophilic substituents and evaluation as radiosensitizers and as bioreductively activated cytotoxins.
Development of a novel series of (2-quinolinylmethoxy)phenyl-containing compounds as high-affinity leukotriene D4 receptor antagonists. 2. Effects of an additional phenyl ring on receptor affinity.
Synthetic approaches to the guanosine and xanthosine analogues 5-amino-3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazin-7-one and 3-beta-D-ribofuranosylpyrazolo[3,4-e][1,3]oxazine-5,7-dione and studies of their antitumor potential.
Potent inhibitory effect of a series of modified cyclodextrin sulfates (mCDS) on the replication of HIV-1 in vitro.
Characterization of tamulamides A and B, polyethers isolated from the marine dinoflagellate Karenia brevis.
Alpha 2-adrenergic agonists/antagonists: the synthesis and structure-activity relationships of a series of indolin-2-yl and tetrahydroquinolin-2-yl imidazolines.
Resolution, absolute configuration, and cholinergic enantioselectivity of (+)- and (-)-cis-2-methyl-5-[(dimethylamino)methyl]-1,3-oxathiolane methiodide.
Pepstatin-derived inhibitors of aspartic proteinases. A close look at an apparent transition-state analogue inhibitor.
Synthesis of a tricyclic aphidicolin analogue that inhibits DNA synthesis in vitro.
Synthesis of a new chemically and metabolically stable prostacyclin analogue with high and long-lasting oral activity.
Bis(bioreductive) alkylating agents: synthesis and biological activity in a nude mouse human carcinoma model.
Octahydropyrazino[2',3':3,4]pyrido[1,2-a]indoles. A new class of potent antihypertensive agents.
Sulfur-interrupted 8-amino side chain analogues of 4-methyl-5-[m-(trifluoromethyl)phenoxy]primaquine as potential antimalarial agents.
[3H]Batrachotoxinin A 20 alpha-benzoate binding to voltage-sensitive sodium channels: a rapid and quantitative assay for local anesthetic activity in a variety of drugs.
Fluorine-containing amino acids and their derivatives. 4. Synthesis and antibacterial activity of threo and erythro 1-fluorodehydroxylated chloramphenicol analogues.
5-(Halomethyl)-2-pyranones as irreversible inhibitors of alpha-chymotrypsin.
Synthetic analogues of tetrahydrobiopterin with cofactor activity for aromatic amino acid hydroxylases.
A quantitative structure-activity relationship and molecular graphics analysis of hydrophobic effects in the interactions of inhibitors with alcohol dehydrogenase.
Synthesis and biological properties of 9-(trans-4-hydroxy-2-buten-1-yl)adenine and guanine: open-chain analogues of neplanocin A.
22-Hydroxycholesterol derivatives as HMG CoA reductase suppressors and serum cholesterol lowering agents.
4-Aroyl-1,3-dihydro-2H-imidazol-2-ones: a new class of cardiotonic agents. 2. Effect of 4-pyridoyl substituents and related compounds.
3-Hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors. 5. 6-(Fluoren-9-yl)- and 6-(fluoren-9-ylidenyl)-3,5-dihydroxyhexanoic acids and their lactone derivatives.
Synthesis and biological evaluation of novel dimiracetam derivatives useful for the treatment of neuropathic pain.
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
A new synthesis of the ORL-1 antagonist 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidinyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397) and activity in a calcium mobilization assay.
Orally active 1,2,4-trioxepanes: synthesis and antimalarial activity of a series of 7-arylvinyl-1,2,4-trioxepanes against multidrug-resistant Plasmodium yoelii in Swiss mice.
Synthesis, cytostatic, and antiviral activity of novel 6-[2-(dialkylamino)ethyl]-, 6-(2-alkoxyethyl)-, 6-[2-(alkylsulfanyl)ethyl]-, and 6-[2-(dialkylamino)vinyl]purine nucleosides.
Synthesis and cytotoxic activity of pyrazino[1,2-b]-isoquinolines, 1-(3-isoquinolyl)isoquinolines, and 6,15-iminoisoquino[3,2-b]-3-benzazocines.
Non-ATP competitive glycogen synthase kinase 3beta (GSK-3beta) inhibitors: study of structural requirements for thiadiazolidinone derivatives.
Design of new potent and selective secretory phospholipase A2 inhibitors. Part 5: synthesis and biological activity of 1-alkyl-4-[4,5-dihydro-1,2,4-[4H]-oxadiazol-5-one-3-ylmethylbenz-4'-yl(oyl)] piperazines.
beta-Keto sulfones as inhibitors of 11beta-hydroxysteroid dehydrogenase type I and the mechanism of action.
Synthesis, cytotoxic evaluation, and DNA binding of novel thiazolo[5,4-b]quinoline derivatives.
Synthesis, determination of the absolute configuration of tonkinelin, and inhibitory action with bovine heart mitochondrial complex I.
Direct diazo-transfer reaction on beta-lactam: synthesis and preliminary biological activities of 6-triazolylpenicillanic acids.
Design, synthesis and cardioprotective effect of a new class of dual-acting agents: phenolic tetrahydro-beta-carboline RGD peptidomimetic conjugates.
3-(3,4,5-Trimethoxyphenyl)-1-oxo-2-propene: a novel pharmacophore displaying potent multidrug resistance reversal and selective cytotoxicity.
Synthesis of carbamate derivatives of iejimalides. Retention of normal antiproliferative activity and localization of binding in cancer cells.
Synthesis of O-prenylated and O-geranylated derivatives of 5-benzylidene2,4-thiazolidinediones and evaluation of their free radical scavenging activity as well as effect on some phase II antioxidant/detoxifying enzymes.
Synthesis, structural revision, and antioxidant activities of antimutagenic homoisoflavonoids from Hoffmanosseggia intricata.
Discovery and design of benzimidazolone based inhibitors of p38 MAP kinase.
Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands.
Tubulin polymerization inhibitors with a fluorinated phthalimide skeleton derived from thalidomide.
New spiro-piperidines as 5-HT2B receptor antagonists.
Novel 2-oxoimidazolidine-4-carboxylic acid derivatives as hepatitis C virus NS3-4A serine protease inhibitors: synthesis, activity, and X-ray crystal structure of an enzyme inhibitor complex.
Nonpeptide alpha V beta 3 antagonists. Part 9: Improved pharmacokinetic profile through the use of an aliphatic, des-amide backbone.
Discovery of novel 1-phenyl-cycloalkane carbamides as potent and selective influenza fusion inhibitors.
Synthesis and in vitro binding studies of piperazine-alkyl-naphthamides: impact of homology and sulphonamide/carboxamide bioisosteric replacement on the affinity for 5-HT1A, alpha2A, D4.2, D3 and D2L receptors.
Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC).
Arylsulfonamides: a study of the relationship between activity and conformational preferences for a series of factor Xa inhibitors.
Synthesis and monoamine transporter affinity of front bridged tricyclic 3beta-(4'-halo or 4'-methyl)phenyltropanes bearing methylene or carbomethoxymethylene on the bridge to the 2beta-position.
Anti-cancer activities of diospyrin, its derivatives and analogues.
Imidazoles: SAR and development of a potent class of cyclin-dependent kinase inhibitors.
Synthesis and biological evaluation of a focused library of beauveriolides.
Pyrrolidinyl pyridone and pyrazinone analogues as potent inhibitors of prolyl oligopeptidase (POP).
Intravenous voriconazole after toxic oral administration.
Expanded-spectrum beta-lactamase PER-1 in an environmental Aeromonas media isolate from Switzerland.
AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.
Capsular type and antibiotic resistance in Streptococcus agalactiae isolates from patients, ranging from newborns to the elderly, with invasive infections.
Improved murine model of malaria using Plasmodium falciparum competent strains and non-myelodepleted NOD-scid IL2Rgammanull mice engrafted with human erythrocytes.
oqxAB encoding a multidrug efflux pump in human clinical isolates of Enterobacteriaceae.
Inactivation of the glycoside hydrolase NagZ attenuates antipseudomonal beta-lactam resistance in Pseudomonas aeruginosa.
The diarylquinoline R207910 is bactericidal against Mycobacterium leprae in mice at low dose and administered intermittently.
Tetracycline resistance gene tet(W) in the pathogenic bacterium Clostridium difficile.
Stereoselective phosphorylation of cyclopropavir by pUL97 and competitive inhibition by maribavir.
KPC-2-producing Enterobacter cloacae and pseudomonas putida coinfection in a liver transplant recipient.
Comparative efficacies of telavancin and vancomycin in preventing device-associated colonization and infection by Staphylococcus aureus in rabbits.
Characterization of pABVA01, a plasmid encoding the OXA-24 carbapenemase from Italian isolates of Acinetobacter baumannii.
Antifungal activities of natural and synthetic iron chelators alone and in combination with azole and polyene antibiotics against Aspergillus fumigatus.
In vivo selection of reduced susceptibility to carbapenems in Acinetobacter baumannii related to ISAba1-mediated overexpression of the natural bla(OXA-66) oxacillinase gene.
Identification of novel allosteric nonpeptidergic inhibitors of the human cytomegalovirus-encoded chemokine receptor US28.
2,3-diarylxanthones as strong scavengers of reactive oxygen and nitrogen species: a structure-activity relationship study.
Synthesis of branched 9-[2-(2-phosphonoethoxy)ethyl]purines as a new class of acyclic nucleoside phosphonates which inhibit Plasmodium falciparum hypoxanthine-guanine-xanthine phosphoribosyltransferase.
Novel aminopeptidase N inhibitors derived from antineoplaston AS2-5 (Part I).
Synthesis and optimization of thiadiazole derivatives as a novel class of substrate competitive c-Jun N-terminal kinase inhibitors.
Design and synthesis of 3-phenyltetrahydronaphthalenic derivatives as new selective MT2 melatoninergic ligands. Part II.
Potent DNA-directed alkylating agents: Synthesis and biological activity of phenyl N-mustard-quinoline conjugates having a urea or hydrazinecarboxamide linker.
Proteasome inhibition in human breast cancer cells with high catechol-O-methyltransferase activity by green tea polyphenol EGCG analogs.
Synthesis and antiviral evaluation of thieno[3,4-d]pyrimidine C-nucleoside analogues of 2',3'-dideoxy- and 2',3'-dideoxy-2',3'-didehydro-adenosine and -inosine.
Design and synthesis of selective inhibitors of placental alkaline phosphatase.
Synthesis of 2- and 17-substituted estrone analogs and their antiproliferative structure-activity relationships compared to 2-methoxyestradiol.
Prenylated pterocarpans as bacterial neuraminidase inhibitors.
The biological activity and metabolic stability of peptidic bifunctional compounds that are opioid receptor agonists and neurokinin-1 receptor antagonists with a cystine moiety.
Cytosporones, coumarins, and an alkaloid from the endophytic fungus Pestalotiopsis sp. isolated from the Chinese mangrove plant Rhizophoramucronata.
Preparation and antitubercular activities of alkylated amino alcohols and their glycosylated derivatives.
Selective angiotensin II AT(2) receptor agonists devoid of the imidazole ring system.
Synthesis, DNA binding, and cytotoxicity studies of pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates.
Synthesis of novel antitumoural analogues of dysidiolide from ent-halimic acid.
Synthesis and in vitro PDT activity of miscellaneous porphyrins with amino acid and uracil.
Synthesis of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives as inhibitors of human liver glycogen phosphorylase a.
Sulfadiazine/hydroxypropyl-beta-cyclodextrin host-guest system: Characterization, phase-solubility and molecular modeling.
The design and synthesis of N-1-alkylated-5-aminoarylalkylsubstituted-6-methyluracils as potential non-nucleoside HIV-1 RT inhibitors.
Synthesis of analogues of a flexible thiopyrylium photosensitizer for purging blood-borne pathogens and binding mode and affinity studies of their complexes with DNA.
Novel acyclic enediynes inhibit Cyclin A and Cdc25C expression and induce apoptosis phenomenon to show potent antitumor proliferation.
Structure-activity relationships and CoMFA of N-3 substituted phenoxypropyl piperidine benzimidazol-2-one analogues as NOP receptor agonists with analgesic properties.
Synthesis, antifungal and antimycobacterial activities of new bis-imidazole derivatives, and prediction of their binding to P450(14DM) by molecular docking and MM/PBSA method.
Synthesis and structure-activity relationship of 7-(substituted)-aminomethyl-4-quinolone-3-carboxylic acid derivatives.
Synthesis and evaluation of antifungal properties of a series of the novel 2-amino-5-oxo-4-phenyl-5,6,7,8-tetrahydroquinoline-3-carbonitrile and its analogues.
2-Alkenylthieno[2,3-b]pyridine-5-carbonitriles: Potent and selective inhibitors of PKCtheta.
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.
Synthesis and PKCtheta inhibitory activity of a series of 4-(indol-5-ylamino)thieno[2,3-b]pyridine-5-carbonitriles.
Inhibition of Src kinase activity by 7-[(2,4-dichloro-5-methoxyphenyl)amino]-2-heteroaryl-thieno[3,2-b]pyridine-6-carbonitriles.
Camptothecin binds to a synthetic peptide identified by a T7 phage display screen.
New fluorinated pyrrolidine and azetidine amides as dipeptidyl peptidase IV inhibitors.
A three-residue, continuous binding epitope peptidomimetic of ShK toxin as a Kv1.3 inhibitor.
Action of a novel pyrrolo[1,2-c][1.3]benzodiazepine on the viability of Jurkat and neuronal/glial cells.
A simple in vitro assay for assessing the reactivity of nitrile containing compounds.
Discovery and SAR of para-alkylthiophenoxyacetic acids as potent and selective PPARdelta agonists.
Synthesis of 4-substituted pyrido[2,3-d]pyrimidin-4(1H)-one as analgesic and anti-inflammatory agents.
Beyond the MEK-pocket: can current MEK kinase inhibitors be utilized to synthesize novel type III NCKIs? Does the MEK-pocket exist in kinases other than MEK?
Synthesis and cyclooxygenase inhibitory activities of some N-acylhydrazone derivatives of isoxazolo[4,5-d]pyridazin-4(5H)-ones.
Hepatitis C NS5B polymerase inhibitors: 4,4-Dialkyl-1-hydroxy-3-oxo-3,4-dihydronaphthalene-3-yl benzothiadiazine derivatives.
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Synthesis and biological evaluation of azobicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes.
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP(1) receptor antagonist for the treatment of inflammatory pain.
Derivatives of (2R,3R,4S)-2-aminomethylpyrrolidine-3,4-diol are selective alpha-mannosidase inhibitors.
Selective, orally active MMP inhibitors with an aryl backbone.
Structural modification of 3-arylisoquinolines to isoindolo[2,1-b]isoquinolinones for the development of novel topoisomerase 1 inhibitors with molecular docking study.
Emergence of quinolone-resistant Bordetella pertussis in Japan.
Resistance selection studies comparing the activity of razupenem (PTZ601) to vancomycin and linezolid against eight methicillin-resistant and two methicillin-susceptible Staphylococcus aureus strains.
Development, validation, and routine application of a high-performance liquid chromatography method coupled with a single mass detector for quantification of itraconazole, voriconazole, and posaconazole in human plasma.
Nationwide investigation of extended-spectrum beta-lactamases, metallo-beta-lactamases, and extended-spectrum oxacillinases produced by ceftazidime-resistant Pseudomonas aeruginosa strains in France.
Efficacy of single-dose liposomal amphotericin B or micafungin prophylaxis in a neutropenic murine model of invasive pulmonary aspergillosis.
Molecular and biochemical characterization of SHV-56, a novel inhibitor-resistant beta-lactamase from Klebsiella pneumoniae.
In vitro activity of TR-700, the antibacterial moiety of the prodrug TR-701, against linezolid-resistant strains.
Characterization of an ABCG-like transporter from the protozoan parasite Leishmania with a role in drug resistance and transbilayer lipid movement.
Lysine-enriched cecropin-mellitin antimicrobial peptides with enhanced selectivity.
In vitro activities of panduratin A against clinical Staphylococcus strains.
Effect of a single dose of ritonavir on the pharmacokinetic behavior of elvucitabine, a nucleoside reverse transcriptase inhibitor, administered in healthy volunteers.
The phenolic diterpene totarol inhibits multidrug efflux pump activity in Staphylococcus aureus.
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
Posaconazole mono- or combination therapy for treatment of murine zygomycosis.
Antimicrobial studies with the Pseudomonas aeruginosa two-allele library require caution.
Antischistosomal activity of hexadecyloxypropyl cyclic 9-(S)-[3-hydroxy-2-(phosphonomethoxy)propyl]adenine and other alkoxyalkyl esters of acyclic nucleoside phosphonates assessed by schistosome worm killing in vitro.
Synthesis, antimalarial activity, and cellular toxicity of new arylpyrrolylaminoquinolines.
Statistical molecular design of a focused salicylidene acylhydrazide library and multivariate QSAR of inhibition of type III secretion in the Gram-negative bacterium Yersinia.
Synthesis, biological evaluation and molecular docking studies of amide-coupled benzoic nitrogen mustard derivatives as potential antitumor agents.
The bisnaphthalimides as new active lead compounds against Plasmodium falciparum.
Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads.
Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.
Beta-ketophosphonates as beta-lactamase inhibitors: Intramolecular cooperativity between the hydrophobic subsites of a class D beta-lactamase.
Facile synthesis of diazido-functionalized biaryl compounds as radioisotope-free photoaffinity probes by Suzuki-Miyaura coupling.
Interaction between ghrelin and the ghrelin receptor (GHS-R1a), a NMR study using living cells.
Aminopyridinecarboxamide-based inhibitors: Structure-activity relationship.
1,2,3-Selenadiazole thioacetanilides: synthesis and anti-HIV activity evaluation.
Synthesis of a second generation chroman/catechol hybrids and evaluation of their activity in protecting neuronal cells from oxidative stress-induced cell death.
Design and synthesis of piperidine farnesyltransferase inhibitors with reduced glucuronidation potential.
First synthesis of 7alpha- and 7beta-amino-DHEA, dehydroepiandrosterone (DHEA) analogues and preliminary evaluation of their cytotoxicity on Leydig cells and TM4 Sertoli cells.
Synthesis and antidiabetic activity of 2,5-disubstituted-3-imidazol-2-yl-pyrrolo[2,3-b]pyridines and thieno[2,3-b]pyridines.
Anti-AIDS agents 66: syntheses and anti-HIV activity of phenolic and aza 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) derivatives.
Mono- and disalicylic acid derivatives: PTP1B inhibitors as potential anti-obesity drugs.
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 6: Opioid receptor binding properties of cyclic variants of 8-carboxamidocyclazocine.
Synthesis, checkpoint kinase 1 inhibitory properties and in vitro antiproliferative activities of new pyrrolocarbazoles.
A novel series of parenteral cephalosporins exhibiting potent activities against Pseudomonas aeruginosa and other Gram-negative pathogens: synthesis and structure-activity relationships.
Evaluation of novel hyphodermin derivatives as glycogen phosphorylase a inhibitors.
Synthetic homoserine lactone-derived sulfonylureas as inhibitors of Vibrio fischeri quorum sensing regulator.
Gamma-carboline derivatives with anti-bovine viral diarrhea virus (BVDV) activity.
Synthesis and pharmacological evaluation of peptide-mimetic protease-activated receptor-1 antagonists containing novel heterocyclic scaffolds.
Novel thyroid hormone receptor antagonists with an N-alkylated diphenylamine skeleton.
Synthesis and preliminary pharmacological evaluation of the four stereoisomers of (2S)-2-(2'-phosphono-3'-phenylcyclopropyl)glycine, the first class of 3'-substituted trans C1'-2'-2-(2'-phosphonocyclopropyl)glycines.
New triterpenoid saponins with strong alpha-glucosidase inhibitory activity from the roots of Gypsophila oldhamiana.
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
Synthesis and antifungal activity of 1H-pyrrolo[3,2-g]quinoline-4,9-diones and 4,9-dioxo-4,9-dihydro-1H-benzo[f]indoles.
Solid-phase parallel synthesis of azarene pyrrolidinones as factor Xa inhibitors.
BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline.
Synthesis and structure-activity relationship of N-(3-azabicyclo[3.1.0]hex-6-ylmethyl)-5-(2-pyridinyl)-1,3-thiazol-2-amines derivatives as NPY Y5 antagonists.
Chemo-enzymatic synthesis of the Galili epitope Gal(alpha)(1-->3)Galbeta(1-->4)GlcNAc on a homogeneously soluble PEG polymer by a multi-enzyme system.
Phenoxypyrimidine inhibitors of p38alpha kinase: synthesis and statistical evaluation of the p38 inhibitory potencies of a series of 1-(piperidin-4-yl)-4-(4-fluorophenyl)-5-(2-phenoxypyrimidin-4-yl) imidazoles.
Antimycobacterial activity of ionic fullerene derivatives.
Resolution of a CPzI precursor, synthesis and biological evaluation of (+) and (-)-N-Boc-CPzI: a further validation of the relationship between chemical solvolytic stability and cytotoxicity.
Synthesis and biological evaluation of helicid analogues as mushroom tyrosinase inhibitors.
New hydroxypyrimidinone-containing sulfonamides as carbonic anhydrase inhibitors also acting as MMP inhibitors.
Carbamoyloximes as novel non-competitive mGlu5 receptor antagonists.
Syntheses and structure-activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel alpha7 neuronal nicotinic receptor (NNR) ligands.
16Beta-hydroxy-5alpha-cholestane-3,6-dione, a novel cytotoxic oxysterol from the red alga Jania rubens.
Synthesis and evaluation of 4-deacetoxyagosterol A as an MDR-modulator.
Biaryl ethers as potent allosteric inhibitors of reverse transcriptase and its key mutant viruses: aryl substituted pyrazole as a surrogate for the pyrazolopyridine motif.
Synthesis and structure-activity relationships of sinenxan A derivatives as multidrug resistance reversal agents.
S-benzylisothiourea derivatives as small-molecule inhibitors of indoleamine-2,3-dioxygenase.
In vitro susceptibility of field isolates of Leishmania donovani to Miltefosine and amphotericin B: correlation with sodium antimony gluconate susceptibility and implications for treatment in areas of endemicity.
Truncated tni module adjacent to the complex integron of salmonella genomic island 1 in Salmonella enterica serovar Virchow.
Low penetration of oseltamivir and its carboxylate into cerebrospinal fluid in healthy Japanese and Caucasian volunteers.
Design and synthesis of benzofuranic derivatives as new ligands at the melatonin-binding site MT3.
Identification of a novel trimethoprim resistance gene, dfrK, in a methicillin-resistant Staphylococcus aureus ST398 strain and its physical linkage to the tetracycline resistance gene tet(L).
Complete nucleotide sequences of plasmids pEK204, pEK499, and pEK516, encoding CTX-M enzymes in three major Escherichia coli lineages from the United Kingdom, all belonging to the international O25:H4-ST131 clone.
TEM-168, a heretofore laboratory-derived TEM beta-lactamase variant found in an Escherichia coli clinical isolate.
Role of plasma proteins in pharmacokinetics of micafungin, an antifungal antibiotic, in analbuminemic rats.
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
In vitro phenotypic susceptibility of human immunodeficiency virus type 2 clinical isolates to protease inhibitors.
OXA-143, a novel carbapenem-hydrolyzing class D beta-lactamase in Acinetobacter baumannii.
Detection of the novel extended-spectrum beta-lactamase OXA-161 from a plasmid-located integron in Pseudomonas aeruginosa clinical isolates from Spain.
First organisms with acquired metallo-beta-lactamases (IMP-13, IMP-22, and VIM-2) reported in Austria.
Activity of Tigecycline against Coryneform Bacteria of Clinical Interest and Listeria monocytogenes.
Novel antioxidant agents deriving from molecular combination of Vitamin C and NO-donor moieties.
Synthesis of 2-(5-((5-(4-chlorophenyl)furan-2-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)acetic acid derivatives and evaluation of their cytotoxicity and induction of apoptosis in human leukemia cells.
Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin.
Novel acyl coenzyme A (CoA): diacylglycerol acyltransferase-1 inhibitors: synthesis and biological activities of diacylethylenediamine derivatives.
Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists.
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 1: discovery and exploration of the carboxyamide side chain.
Synthesis of 5-deoxy-beta-D-galactofuranosides as tools for the characterization of beta-D-galactofuranosidases.
Synthesis, and biological evaluation of 2-(4-aminophenyl)benzothiazole derivatives as photosensitizing agents.
Thienylhalomethylketones: Irreversible glycogen synthase kinase 3 inhibitors as useful pharmacological tools.
Synthesis, vasorelaxant activity and antihypertensive effect of benzo[d]imidazole derivatives.
Virtual fragment screening for novel inhibitors of 6-phosphogluconate dehydrogenase.
Carboxylated calixarenes bind strongly to CD69 and protect CD69(+) killer cells from suicidal cell death induced by tumor cell surface ligands.
Identification of novel quinazolin-4(3H)-ones as inhibitors of thermolysin, the prototype of the M4 family of proteinases.
Second generation of alpha-tocopherol analogs-nitric oxide donors: Synthesis, physicochemical, and biological characterization.
Synthesis, biological evaluation and SAR study of novel pyrazole analogues as inhibitors of Mycobacterium tuberculosis.
Imidazolidines as new anti-Trypanosoma cruzi agents: biological evaluation and structure-activity relationships.
Enantiospecific synthesis and cytotoxicity of 7-(4-methoxyphenyl)-6-phenyl-2,3,8,8a-tetrahydroindolizin-5(1H)-one enantiomers.
1,5-Disubstituted 1,2,3-triazoles as cis-restricted analogues of combretastatin A-4: Synthesis, molecular modeling and evaluation as cytotoxic agents and inhibitors of tubulin.
Norcantharimides, synthesis and anticancer activity: Synthesis of new norcantharidin analogues and their anticancer evaluation.
Synthesis and antimicrobial activity of some new thiazolyl thiazolidine-2,4-dione derivatives.
Pyrimidinone-peptoid hybrid molecules with distinct effects on molecular chaperone function and cell proliferation.
Affinity purification and characterization of a key enzyme responsible for circadian rhythmic control of nyctinasty in Lespedeza cuneata L.
Synthesis of penaresidin derivatives and its biological activity.
Synthesis of neutral and cationic tripyridylporphyrin-D-galactose conjugates and the photoinactivation of HSV-1.
Phosphonate-linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates: synthesis, DNA-binding affinity and cytotoxicity.
The role of lipophilicity in determining binding affinity and functional activity for 5-HT2A receptor ligands.
1-(2-Carboxyindol-5-yloxy)propan-2-ones as inhibitors of human cytosolic phospholipase A2alpha: synthesis, biological activity, metabolic stability, and solubility.
Design and synthesis of trans 2-(furan-2-yl)vinyl heteroaromatic iodides with antitumour activity.
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Application of a novel in silico high-throughput screen to identify selective inhibitors for protein-protein interactions.
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
One-pot multicomponent synthesis and anti-microbial evaluation of 2'-(indol-3-yl)-2-oxospiro(indoline-3,4'-pyran) derivatives.
Subtype-selectivity of metal-dependent methionine aminopeptidase inhibitors.
3-Aryl-5-phenoxymethyl-1,3-oxazolidin-2-ones as positive allosteric modulators of mGluR2 for the treatment of schizophrenia: Hit-to-lead efforts.
Modifications of C-2 on the pyrroloquinoline template aimed at the development of potent herpesvirus antivirals with improved aqueous solubility.
Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.
Identification of benzimidazole-based inhibitors of the mitogen activated kinase-5 signaling pathway.
Synthesis and biological evaluation of oxoindolin-3-ylidene ethyl benzothiohydrazides as non-peptide TPO mimics.
N-tetrahydrothiochromenoisoxazole-1-carboxamides as selective antagonists of cloned human 5-HT2B.
Antitumor agents 278. 4-Amino-2H-benzo[h]chromen-2-one (ABO) analogs as potent in vitro anti-cancer agents.
The development and SAR of pyrrolidine carboxamide 11beta-HSD1 inhibitors.
Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.
Monastrol analogs: a synthesis of pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged azolopyrimidine derivatives and their biological screening.
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase.
Probing the cannabinoid CB1/CB2 receptor subtype selectivity limits of 1,2-diarylimidazole-4-carboxamides by fine-tuning their 5-substitution pattern.
In vitro activity of ceftaroline against Streptococcus pneumoniae isolates exhibiting resistance to penicillin, amoxicillin, and cefotaxime.
In vitro activities of tigecycline and 10 other antimicrobials against nonpigmented rapidly growing mycobacteria.
Effects of zidovudine and stavudine on mitochondrial DNA of differentiating 3T3-F442a cells are not associated with imbalanced deoxynucleotide pools.
In vitro activities at pH 5.0 and pH 7.0 and in vivo efficacy of flucytosine against Aspergillus fumigatus.
Study of the in vitro activities of rifaximin and comparator agents against 536 anaerobic intestinal bacteria from the perspective of potential utility in pathology involving bowel flora.
CS-8958, a prodrug of the new neuraminidase inhibitor R-125489, shows long-acting anti-influenza virus activity.
Surveillance of community-based reservoirs reveals the presence of CTX-M, imported AmpC, and OXA-30 beta-lactamases in urine isolates of Klebsiella pneumoniae and Escherichia coli in a U.S. community.
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
Clinical isolates of Aspergillus species remain fully susceptible to voriconazole in the post-voriconazole era.
Two new dfr genes in trimethoprim-resistant integron-negative Escherichia coli isolates.
Combined real-time PCR and pyrosequencing strategy for objective, sensitive, specific, and high-throughput identification of reduced susceptibility to penicillins in Neisseria meningitidis.
Fitness of Streptococcus pneumoniae fluoroquinolone-resistant strains with topoisomerase IV recombinant genes.
Edelfosine induces an apoptotic process in Leishmania infantum that is regulated by the ectopic expression of Bcl-XL and Hrk.
The KQ element, a complex genetic region conferring transferable resistance to carbapenems, aminoglycosides, and fluoroquinolones in Klebsiella pneumoniae.
Vancomycin MICs for methicillin-resistant Staphylococcus aureus isolates differ based upon the susceptibility test method used.
Plasmid-mediated 16S rRNA methylases among extended-spectrum beta-lactamase-producing Enterobacteriaceae isolates.
Comparison of disk diffusion and agar dilution methods for erythromycin, ciprofloxacin, and tetracycline susceptibility testing of Campylobacter coli and for tetracycline susceptibility testing of Campylobacter jejuni subsp. jejuni.
Hepatoprotective amide constituents from the fruit of Piper chaba: Structural requirements, mode of action, and new amides.
Evaluation of 3,4-dihydroquinazoline-2(1H)-thiones as inhibitors of alpha-MSH-induced melanin production in melanoma B16 cells.
Synthesis and biological evaluation of 14-(aminoalkyl-aminomethyl)aromathecins as topoisomerase I inhibitors: investigating the hypothesis of shared structure-activity relationships.
Anti-AIDS agents 82: synthesis of seco-(3'R,4'R)-3',4'-di-O-(S)-camphanoyl-(+)-cis-khellactone (DCK) derivatives as novel anti-HIV agents.
Utilization of the 1,2,3,5-thiatriazolidin-3-one 1,1-dioxide scaffold in the design of potential inhibitors of human neutrophil proteinase 3.
New chloro,fluorobenzylindole derivatives as integrase strand-transfer inhibitors (INSTIs) and their mode of action.
Design, synthesis, and biological evaluation of novel estradiol-bisphosphonate conjugates as bone-specific estrogens.
Synthesis and evaluation of novel phenoxypropanolamine derivatives containing acetanilides as potent and selective beta3-adrenergic receptor agonists.
ATP competitive inhibitors of D-alanine-D-alanine ligase based on protein kinase inhibitor scaffolds.
Syntheses and biological activities of fluorescent-labeled analogs of acylpolyamine toxin NPTX-594 isolated from the venom of Madagascar Joro spider.
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
Carbonic anhydrase inhibitors. The nematode alpha-carbonic anhydrase of Caenorhabditis elegans CAH-4b is highly inhibited by 2-(hydrazinocarbonyl)-3-substituted-phenyl-1H-indole-5-sulfonamides.
E-Combretastatin and E-resveratrol structural modifications: antimicrobial and cancer cell growth inhibitory beta-E-nitrostyrenes.
Antifungal activity of synthetic di(hetero)arylamines based on the benzo[b]thiophene moiety.
The synthesis and the in vitro cytotoxicity studies of bisnaphthalimidopropyl polyamine derivatives against colon cancer cells and parasite Leishmania infantum.
1-Aminocyclopentane-1,2,4-tricarboxylic acids screening on glutamatergic and serotonergic systems.
Synthesis of 1,3-diphenyl-2-propen-1-one derivatives and evaluation of their biological activities.
A novel series of parenteral cephalosporins exhibiting potent activities against both Pseudomonas aeruginosa and other gram-negative pathogens. Part 2: Synthesis and structure-activity relationships.
Facile preparation of new 4-phenylamino-3-quinolinecarbonitrile Src kinase inhibitors via 7-fluoro intermediates: identification of potent 7-amino analogs.
Design, synthesis and structure-activity study of shorter hexa peptide analogues as HIV-1 protease inhibitors.
Parallel solid synthesis of inhibitors of the essential cell division FtsZ enzyme as a new potential class of antibacterials.
HSP90-like artificial chaperone activity based on indole beta-cyclodextrin.
Substrate specificity analysis and inhibitor design of homoisocitrate dehydrogenase.
One pot synthesis of pyrimidine and bispyrimidine derivatives and their evaluation for anti-inflammatory and analgesic activities.
Synthesis of diverse analogues of Oenostacin and their antibacterial activities.
The influence of esters and carboxylic acids as the N-substituent of opioids. Part 1: Benzomorphans.
Synthesis and evaluation of a series of C5'-substituted duocarmycin SA analogs.
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350.
A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection.
1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides as potent factor Xa inhibitors. Part 2: A survey of P4 motifs.
Novel quinazoline-quinoline alkaloids with cytotoxic and DNA topoisomerase II inhibitory activities.
Synthesis and antibacterial activity of 3-keto-6-O-carbamoyl-11,12-cyclic thiocarbamate erythromycin A derivatives.
Factor VIIa inhibitors: improved pharmacokinetic parameters.
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators.
Synthesis of symmetrical C- and pseudo-symmetrical O-linked disaccharide analogs for arabinosyltransferase inhibitory activity in Mycobacterium tuberculosis.
Tritium radiolabelling of PB28, a potent sigma-2 receptor ligand: pharmacokinetic and pharmacodynamic characterization.
Antiproliferative activity of 4-chloro-5,6-dihydro-2H-pyrans. Part 2: Enhancement of drug cytotoxicity.
Ethacrynic acid analogues lacking the alpha,beta-unsaturated carbonyl unit--potential anti-metastatic drugs.
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.
Himbacine analogs as muscarinic receptor antagonists--effects of tether and heterocyclic variations.
Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics.
Approaches towards the stabilization of hemiaminal function at ornithine unit of mulundocandin.
Alpha-methylation at benzylic fragment of N-aryl-N'-benzyl ureas provides TRPV1 antagonists with better pharmacokinetic properties and higher efficacy in inflammatory pain model.
The mechanism of action of beta-D-2'-deoxy-2'-fluoro-2'-C-methylcytidine involves a second metabolic pathway leading to beta-D-2'-deoxy-2'-fluoro-2'-C-methyluridine 5'-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase.
First report of plasmid-mediated qnrA1 in a ciprofloxacin-resistant Escherichia coli strain in Latin America.
Increases in SLT2 expression and chitin content are associated with incomplete killing of Candida glabrata by caspofungin.
Activities of daptomycin and comparative antimicrobials, singly and in combination, against extracellular and intracellular Staphylococcus aureus and its stable small-colony variant in human monocyte-derived macrophages and in broth.
Carbapenem resistance among Pseudomonas aeruginosa strains from India: evidence for nationwide endemicity of multiple metallo-beta-lactamase clones (VIM-2, -5, -6, and -11 and the newly characterized VIM-18).
BK Virus replication in vitro: limited effect of drugs interfering with viral uptake and intracellular transport.
Antimicrobial resistance genes associated with Salmonella enterica serovar newport isolates from food animals.
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
Effect of 14-membered-ring macrolides on production of interleukin-8 mediated by protease-activated receptor 2 in human keratinocytes.
Characterization of a naturally occurring class D beta-lactamase from Achromobacter xylosoxidans.
Effect of antimicrobial compounds on Balamuthia mandrillaris encystment and human brain microvascular endothelial cell cytopathogenicity.
Prevalence of the erm(T) gene in clinical isolates of erythromycin-resistant group D Streptococcus and Enterococcus.
Contribution of the autolysin AtlA to the bactericidal activity of amoxicillin against Enterococcus faecalis JH2-2.
A peptide with a ProGln C terminus in the human saliva peptidome exerts bactericidal activity against Propionibacterium acnes.
KHM-1, a novel plasmid-mediated metallo-beta-lactamase from a Citrobacter freundii clinical isolate.
Carbapenem-resistant Acinetobacter baumannii isolates expressing the blaOXA-23 gene associated with ISAba4 in Belgium.
Outbreak of Acinetobacter baumannii with chromosomally encoded VIM-1 undetectable by imipenem-EDTA synergy tests.
Emergence of plasmid-mediated quinolone resistance among non-Typhi Salmonella enterica isolates from humans in the United States.
Plasmid-mediated qepA gene among Escherichia coli clinical isolates from Japan.
Chromane derivatives of small aromatic molecules: Chemoenzymatic synthesis and growth inhibitory activity on human tumor cell line LoVo WT.
Synthesis, tautomerism, and antimicrobial, anti-HCV, anti-SSPE, antioxidant, and antitumor activities of arylazobenzosuberones.
Synthesis and antiproliferative evaluation of pyrazolo[1,5-a]-1,3,5-triazine myoseverin derivatives.
Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists.
Inhibitory activity of Brazilian green propolis components and their derivatives on the release of cys-leukotrienes.
Bioorganic synthesis of a recombinant HIV-1 fusion inhibitor, SC35EK, with an N-terminal pyroglutamate capping group.
Synthesis and biological evaluation of the metabolites of 2-(1-{3-[(6-chloronaphthalen-2-yl)sulfonyl]propanoyl}piperidin-4-yl)-5-methyl-1,2-dihydro-3H-imidazo[1,5-c]imidazol-3-one.
Botulinum neurotoxin serotype A inhibitors: small-molecule mercaptoacetamide analogs.
Synthesis and antitumor activity of novel amsacrine analogs: the critical role of the acridine moiety in determining their biological activity.
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
The alkyl-connected 2-amino-6-vinylpurine (AVP) crosslinking agent for improved selectivity to the cytosine base in RNA.
Structural-activity relationship study of highly-functionalized imidazolines as potent inhibitors of nuclear transcription factor-kappaB mediated IL-6 production.
Discovery of potent cholecystokinin-2 receptor antagonists: elucidation of key pharmacophore elements by X-ray crystallographic and NMR conformational analysis.
Design and synthesis of new potent anticancer pyrazoles with high FLT3 kinase inhibitory selectivity.
Design, synthesis, and preliminary in vitro and in silico antiviral activity of [4,7]phenantrolines and 1-oxo-1,4-dihydro-[4,7]phenantrolines against single-stranded positive-sense RNA genome viruses.
Conformationally locked thiosugars as potent alpha-mannosidase inhibitors: synthesis, biochemical and docking studies.
Cytotoxic dibromotyrosine-derived metabolites from the sponge Aplysina gerardogreeni.
Design, synthesis, and in vivo evaluation of oxamniquine methacrylate and acrylamide prodrugs.
Synthesis and biological activity of new melatonin dimeric derivatives.
The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists.
Analgesic agents without gastric damage: design and synthesis of structurally simple benzenesulfonanilide-type cyclooxygenase-1-selective inhibitors.
Substitution at the 8-position of 3''-deoxy-cyclic ADP-carbocyclic-ribose, a highly potent Ca2+-mobilizing agent, provides partial agonists.
Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists.
Asymmetric synthesis and stereochemical structure-activity relationship of (R)- and (S)-8-[1-(2,4-dichlorophenyl)-2-imidazol-1-yl-ethoxy] octanoic acid heptyl ester, a potent inhibitor of allene oxide synthase.
Cyathane diterpenes from Sarcodon cyrneus and evaluation of their activities of neuritegenesis and nerve growth factor production.
Studies toward the structural optimization of new brazilizone-related trypanocidal 1,3,4-thiadiazole-2-arylhydrazone derivatives.
Activation and inhibition of DNA methyltransferases by S-adenosyl-L-homocysteine analogues.
Structure-activity studies on 1,3-dioxane-2-carboxylic acid derivatives, a novel class of subtype-selective peroxisome proliferator-activated receptor alpha (PPARalpha) agonists.
Towards the second generation of Boceprevir: Dithianes as an alternative P2 substituent for 2,2-dimethyl cycloproyl proline in HCV NS3 protease inhibitors.
Discovery of a novel series of potent S1P1 agonists.
Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations.
Substituted tetrahydrocarbazoles with potent activity against human papillomaviruses.
Exploration of novel thiobarbituric acid-, rhodanine- and thiohydantoin-based HIV-1 integrase inhibitors.
Discovery and structure-guided drug design of inhibitors of 11beta-hydroxysteroid-dehydrogenase type I based on a spiro-carboxamide scaffold.
Discovery of potent non-urea inhibitors of soluble epoxide hydrolase.
Design and synthesis of isoform-selective phospholipase D (PLD) inhibitors. Part II. Identification of the 1,3,8-triazaspiro[4,5]decan-4-one privileged structure that engenders PLD2 selectivity.
Serratezomines D and E, new Lycopodium alkaloids from Lycopodium serratum var. serratum.
Cytotoxic bromotyrosine derivatives from a two-sponge association of Jaspis sp. and Poecillastra sp.
Rational design of novel glycomimetics: inhibitors of concanavalin A.
Novel 2-imidazoles as potent, selective and CNS penetrant alpha1A adrenoceptor partial agonists.
Designing rapid onset selective serotonin re-uptake inhibitors. Part 3: Site-directed metabolism as a strategy to avoid active circulating metabolites: structure-activity relationships of (thioalkyl)phenoxy benzylamines.
N-((8-hydroxy-5-substituted-quinolin-7-yl)(phenyl)methyl)-2-phenyloxy/amino-acetamide inhibitors of ADAMTS-5 (Aggrecanase-2).
Identifying structural features on 1,1-diphenyl-hexahydro-oxazolo[3,4-a]pyrazin-3-ones critical for Neuropeptide S antagonist activity.
Synthesis and cytotoxic activity of heterocyclic ring-substituted betulinic acid derivatives.
Safety and activity of the immune modulator HE2000 on the incidence of tuberculosis and other opportunistic infections in AIDS patients.
Two clinical strains of Klebsiella pneumoniae carrying plasmid-borne blaIMP-4, blaSHV-12, and armA isolated at a Pediatric Center in Shanghai, China.
Occurrence of efflux mechanism and cephalosporinase variant in a population of Enterobacter aerogenes and Klebsiella pneumoniae isolates producing extended-spectrum beta-lactamases.
In vitro susceptibility of various genotypic strains of Toxoplasma gondii to pyrimethamine, sulfadiazine, and atovaquone.
Emergence of the quinolone resistance-mediating gene aac(6')-Ib-cr in extended-spectrum-beta-lactamase-producing Klebsiella isolates collected in Slovenia between 2000 and 2005.
SC29EK, a peptide fusion inhibitor with enhanced alpha-helicity, inhibits replication of human immunodeficiency virus type 1 mutants resistant to enfuvirtide.
Simvastatin treatment shows no effect on the incidence of cerebral malaria or parasitemia during experimental malaria.
Prevalence and risk factors for selection of quinolone-resistant Escherichia coli strains in fecal flora of patients receiving quinolone therapy.
Potential basis for amphotericin B resistance in Aspergillus terreus.
Comparative in vitro activities of caspofungin and micafungin, determined using the method of the European Committee on Antimicrobial Susceptibility Testing, against yeast isolates obtained in France in 2005-2006.
Antianaerobic activity of sulopenem compared to six other agents.
Impact of mycophenolic acid on the functionality of human polymorphonuclear neutrophils and dendritic cells during interaction with Aspergillus fumigatus.
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
Synthesis, antioxidant properties and radioprotective effects of new benzothiazoles and thiadiazoles.
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase.
Repairing faulty genes by aminoglycosides: development of new derivatives of geneticin (G418) with enhanced suppression of diseases-causing nonsense mutations.
Discovery of trans-N-[1-(2-fluorophenyl)-3-pyrazolyl]-3-oxospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4'-carboxamide, a potent and orally active neuropeptide Y Y5 receptor antagonist.
Design of new potent and selective secretory phospholipase A(2) inhibitors. 6-Synthesis, structure-activity relationships and molecular modelling of 1-substituted-4-[4,5-dihydro-1,2,4-(4H)-oxadiazol-5-one-3-yl(methyl)]-functionalized aryl piperazin/one/dione derivatives.
Discovery of potent and orally active 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as novel allosteric glucokinase activators.
New pyridazine derivatives: synthesis, chemistry and biological activity.
Design, synthesis and antibacterial activity of novel andrographolide derivatives.
Pyrazolone-fused combretastatins and their precursors: synthesis, cytotoxicity, antitubulin activity and molecular modeling studies.
Synthesis and biological evaluation of 4-(hydroxyimino)arylmethyl diarylpyrimidine analogues as potential non-nucleoside reverse transcriptase inhibitors against HIV.
Amide-containing diketoacids as HIV-1 integrase inhibitors: synthesis, structure-activity relationship analysis, and biological activity.
Synthesis of puromycin derivatives with backbone-elongated substrates and associated translation inhibitory activities.
Study of chemical stability of antivirally active 5-azacytosine acyclic nucleoside phosphonates using NMR spectroscopy.
Isolation, structure and biological activities of platencin A(2)-A(4) from Streptomyces platensis.
QSAR studies and pharmacophore identification for arylsubstituted cycloalkenecarboxylic acid methyl esters with affinity for the human dopamine transporter.
Aminoglycoside antibiotic derivatives: preparation and evaluation of toxicity on cochlea and vestibular tissues and antimicrobial activity.
Synthesis, antiviral and antitumor activity of 2-substituted-5-amidino-benzimidazoles.
Biflavonoids isolated from Selaginella tamariscina regulate the expression of matrix metalloproteinase in human skin fibroblasts.
Substituted 6-amino-4H-[1,2]dithiolo[4,3-b]pyrrol-5-ones: synthesis, structure-activity relationships, and cytotoxic activity on selected human cancer cell lines.
Synthesis, DNA binding, and cytotoxicity of 1,4-bis(2-amino-ethylamino)anthraquinone-amino acid conjugates.
Parallel synthesis of a series of potentially brain penetrant aminoalkyl benzoimidazoles.
Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents.
Synthesis and evaluation of amino-threoses in D- and L-series: are five membered ring amino-sugars more potent glycosidase inhibitors than the six membered ones?
7-Substituted-melatonin and 7-substituted-1-methylmelatonin analogues: effect of substituents on potency and binding affinity.
Structure-activity relationships in the inhibition of monoamine oxidase B by 1-methyl-3-phenylpyrroles.
1,4-Bis(alkylamino)benzo[g]phthalazines able to form dinuclear complexes of Cu(II) which as free ligands behave as SOD inhibitors and show efficient in vitro activity against Trypanosoma cruzi.
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
Synthesis and SAR of azolopyrimidines as potent and selective dipeptidyl peptidase-4 (DPP4) inhibitors for type 2 diabetes.
Aryl boronic acid inhibition of synthetic melanin polymerization.
Synthesis and anti-HIV activity evaluation of 1-[(alkenyl or alkynyl or alkyloxy)methyl]-5-alkyl-6-(1-naphthoyl)-2,4-pyrimidinediones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.
Aryl O- and S-galactosides and lactosides as specific inhibitors of human galectins-1 and -3: role of electrostatic potential at O-3.
Synthesis and screening of bicyclic carbohydrate-based compounds: a novel type of antivirals.
Structure-activity relationship studies on niphimycin, a guanidylpolyol macrolide antibiotic. Part 1: The role of the N-methyl-N''-alkylguanidinium moiety.
Synthesis and biological evaluation of dialkylsubstituted maleic anhydrides as novel inhibitors of Cdc25 dual specificity phosphatases.
Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity.
Development of a selective and potent radioactive ligand for histamine H(3) receptors: A compound potentially useful for receptor occupancy studies.
Synthesis and base-pairing properties of C-nucleotides having 1-substituted 1H-1,2,3-triazoles.
Semi-synthetic analogs of pinitol as potential inhibitors of TNF-alpha cytokine expression in human neutrophils.
Synthesis and antitumor activity of substituted triazolo[4,3-a]pyrimidin-6-sulfonamide with an incorporated thiazolidinone moiety.
Design, synthesis, and anti-HCV activity of thiourea compounds.
Discovery of pentacyclic compounds as potent inhibitors of hepatitis C virus NS5B RNA polymerase.
Carbamate derivatives of betulinic acid and betulin with selective cytotoxic activity.
Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands.
Linezolid resistance in Staphylococcus aureus: gene dosage effect, stability, fitness costs, and cross-resistances.
Apricitabine does not select additional drug resistance mutations in tissue culture in human immunodeficiency virus type 1 variants containing K65R, M184V, or M184V plus thymidine analogue mutations.
Postantibiotic effect of tigecycline against 14 gram-positive organisms.
In Vitro activity of the new azole isavuconazole (BAL4815) compared with six other antifungal agents against 162 Cryptococcus neoformans isolates from Cuba.
Betulinic acid derivatives that target gp120 and inhibit multiple genetic subtypes of human immunodeficiency virus type 1.
In vitro activities of various antifungal drugs against Aspergillus terreus: Global assessment using the methodology of the European committee on antimicrobial susceptibility testing.
Identification of 16S rRNA methylase-producing Acinetobacter baumannii clinical strains in North America.
Effects of serum on in vitro susceptibility testing of echinocandins.
In vitro activity of Iclaprim against respiratory and bacteremic isolates of Streptococcus pneumoniae.
Tigecycline Efflux as a Mechanism for Nonsusceptibility in Acinetobacter baumannii.
SCO-1, a novel plasmid-mediated class A beta-lactamase with carbenicillinase characteristics from Escherichia coli.
Tetracycline resistance in group a streptococci: emergence on a global scale and influence on multiple-drug resistance.
The P-113 fragment of histatin 5 requires a specific peptide sequence for intracellular translocation in Candida albicans, which is independent of cell wall binding.
Activity of the Diaminopyrimidine AR-709 against recently collected multidrug-resistant isolates of invasive Streptococcus pneumoniae from North America.
Antimicrobial activity of omiganan pentahydrochloride against contemporary fungal pathogens responsible for catheter-associated infections.
2-Deoxy-2,3-didehydro-N-acetylneuraminic acid analogs structurally modified by thiocarbamoylalkyl groups at the C-4 position: Synthesis and biological evaluation as inhibitors of human parainfluenza virus type 1.
A simple synthesis of four stereoisomers of roseoside and their inhibitory activity on leukotriene release from mice bone marrow-derived cultured mast cells.
Hetero-Diels-Alder reaction of 1,3-bis(trimethylsilyloxy)-1,3-butadienes with arylsulfonylcyanides. Synthesis and antimicrobial activity of 4-hydroxy-2-(arylsulfonyl)pyridines.
Identification of 4-[1-[3-chloro-4-[N'-(5-fluoro-2-methylphenyl)ureido]phenylacetyl]-(4S)-fluoro-(2S)-pyrrolidinylmethoxy]benzoic acid as a potent, orally active VLA-4 antagonist.
Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor.
Synthesis, biological evaluation and molecular modelling of N-heterocyclic dipeptide aldehydes as selective calpain inhibitors.
Synthesis and in vitro toxicity of 4-MTA, its characteristic clandestine synthesis byproducts and related sulfur substituted alpha-alkylthioamphetamines.
Synthesis and evaluation of unsymmetrical polyamine derivatives as antitumor agents.
Interaction of drug based binuclear mixed-ligand complexes with DNA.
Molecular modifications on carboxylic acid derivatives as potent histone deacetylase inhibitors: Activity and docking studies.
Novel DNA intercalators without basic side chains as efficient antitumor agents: design, synthesis and evaluation of benzo-[c,d]-indol-malononitrile derivatives.
Bioconjugates of curcumin display improved protection against glutathione depletion mediated oxidative stress in a dopaminergic neuronal cell line: Implications for Parkinson's disease.
Antitumour polyether macrolides: four new halichondrins from the New Zealand deep-water marine sponge Lissodendoryx sp.
A new antiangiogenic C24 oxylipin from the soft coral Sinularia numerosa.
Synthesis and structure-immunosuppressive activity relationships of bakuchiol and its derivatives.
2(S)-(Cycloalk-1-enecarbonyl)-1-(4-phenyl-butanoyl)pyrrolidines and 2(S)-(aroyl)-1-(4-phenylbutanoyl)pyrrolidines as prolyl oligopeptidase inhibitors.
4-amino-5-aryl-6-arylethynylpyrimidines: structure-activity relationships of non-nucleoside adenosine kinase inhibitors.
Comparative rates of sialylation by recombinant trans-sialidase and inhibitor properties of synthetic oligosaccharides from Trypanosoma cruzi mucins-containing galactofuranose and galactopyranose.
Synthesis and evaluation of isosteres of N-methyl indolo[3,2-b]-quinoline (cryptolepine) as new antiinfective agents.
C6-(N,N-butyl-methyl-heptanamide) derivatives of estrone and estradiol as inhibitors of type 1 17beta-hydroxysteroid dehydrogenase: Chemical synthesis and biological evaluation.
A new modification of anti-tubercular active molecules.
Design, synthesis, and evaluation of non-steroidal farnesoid X receptor (FXR) antagonist.
Synthesis and biological activities of analogs of D-glucosyl-l-tyrosine, a humoral factor that stimulates transcription of the acyl-CoA binding protein in the pheromone gland of the Silkmoth, Bombyx mori.
The synthesis of alpha,beta-unsaturated carbonyl derivatives with the ability to inhibit both glutathione S-transferase P1-1 activity and the proliferation of leukemia cells.
Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
Design, synthesis, and evaluation of 2-aryl-3-heteroaryl-1,3-thiazolidin-4-ones as anti-HIV agents.
Synthesis and c-Src inhibitory activity of imidazo[1,5-a]pyrazine derivatives as an agent for treatment of acute ischemic stroke.
Cyclic monophosphate prodrugs of base-modified 2'-C-methyl ribonucleosides as potent inhibitors of hepatitis C virus RNA replication.
Identification of a novel boron-containing antibacterial agent (AN0128) with anti-inflammatory activity, for the potential treatment of cutaneous diseases.
Identification of 2-arylbenzimidazoles as potent human histamine H4 receptor ligands.
Carbonic anhydrase inhibitors. Inhibition of the cytosolic human isozymes I and II, and the transmembrane, tumor-associated isozymes IX and XII with substituted aromatic sulfonamides activatable in hypoxic tumors.
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-dysiherbaine.
Synthesis and antibacterial activity of 3-O-acyl-6-O-carbamoyl erythromycin A derivatives.
2,3,7-Trisubstituted pyrazolo[1,5-d][1,2,4]triazines: functionally selective GABAA alpha3-subtype agonists.
Expedited SAR study of high-affinity ligands to the alpha(2)delta subunit of voltage-gated calcium channels: Generation of a focused library using a solution-phase Sn2Ar coupling methodology.
The synthesis and biological evaluation of dopamine transporter inhibiting activity of substituted diphenylmethoxypiperidines.
(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
Investigation of glycine alpha-ketoamide HCV NS3 protease inhibitors: effect of carboxylic acid isosteres.
Design and optimization of potent, selective antagonists of Oxytocin.
In vitro SAR of pyrrolidine-containing histamine H3 receptor antagonists: trends across multiple chemical series.
Development of potent, allosteric dual Akt1 and Akt2 inhibitors with improved physical properties and cell activity.
Design and evaluation of analogues of the bacterial cell-wall peptidoglycan motif L-Lys-D-Ala-D-Ala for use in a vancomycin biosensor.
4-arylcyclohexylalanine analogs as potent, selective, and orally active inhibitors of dipeptidyl peptidase IV.
Isothiazolidinone inhibitors of PTP1B containing imidazoles and imidazolines.
Assessment of serum (1->3)-beta-D-glucan concentration as a measure of disease burden in a murine model of invasive pulmonary aspergillosis.
Posaconazole therapeutic drug monitoring: a reference laboratory experience.
Characterization of macrolide efflux pump mef subclasses detected in clinical isolates of Streptococcus pyogenes isolated between 1999 and 2005.
E240V substitution increases catalytic efficiency toward ceftazidime in a new natural TEM-type extended-spectrum beta-lactamase, TEM-149, from Enterobacter aerogenes and Serratia marcescens clinical isolates.
Urine bactericidal activity against Escherichia coli isolates exhibiting different resistance phenotypes/genotypes in an in vitro pharmacodynamic model simulating urine concentrations obtained after oral administration of a 400-milligram single dose of cefditoren-pivoxil.
Pyrrolidine dithiocarbamate and diethyldithiocarbamate are active against growing and nongrowing persister Mycobacterium tuberculosis.
Pharmacodynamics of doxycycline in a murine malaria model.
Plasmid-mediated carbapenem-hydrolyzing beta-lactamase KPC-2 in Klebsiella pneumoniae isolate from Greece.
Statins alone are ineffective in cerebral malaria but potentiate artesunate.
Quinolone resistance in Neisseria gonorrhoeae: rapid genotyping of quinolone resistance-determining regions in gyrA and parC genes by melting curve analysis predicts susceptibility.
Oral and parenteral therapeutic options for outpatient urinary infections caused by enterobacteriaceae producing CTX-M extended-spectrum beta-lactamases.
Daptomycin produces an enhanced bactericidal activity compared to ceftriaxone, measured by [3H]choline release in the cerebrospinal fluid, in experimental meningitis due to a penicillin-resistant pneumococcal strain without lysing its cell wall.
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
In vitro activity of tigecycline against multidrug-resistant Acinetobacter baumannii and selection of tigecycline-amikacin synergy.
In vitro activities of miltefosine and two novel antifungal biscationic salts against a panel of 77 dermatophytes.
IMP-15-producing Pseudomonas aeruginosa strain isolated in a U.S. medical center: a recent arrival from Mexico.
First occurrence of an IMP metallo-beta-lactamase in Aeromonas caviae: IMP-19 in an isolate from France.
Characterization of the carbapenem-hydrolyzing oxacillinase oxa-58 in an Acinetobacter genospecies 3 clinical isolate.
Discovery of novel thieno[2,3-d]pyrimidin-4-yl hydrazone-based inhibitors of cyclin D1-CDK4: synthesis, biological evaluation and structure-activity relationships. Part 2.
Investigating the anti-proliferative activity of styrylazanaphthalenes and azanaphthalenediones.
Structure-activity relationship study on polyglutamine binding peptide QBP1.
Cytotoxic and anti-inflammatory cembranoids from the Dongsha Atoll soft coral Sarcophyton crassocaule.
Isolation, structure and antibacterial activity of pleosporone from a pleosporalean ascomycete discovered by using antisense strategy.
New potent imidazoisoquinolinone derivatives as anti-Trypanosoma cruzi agents: biological evaluation and structure-activity relationships.
Colony stimulating factor-1 receptor as a target for small molecule inhibitors.
6-Bicycloaryl substituted (S)- and (R)-5,6-dihydro-2H-pyran-2-ones: asymmetric synthesis, and anti-proliferative properties.
Antimalarial activity enhancement in hydroxymethylcarbonyl (HMC) isostere-based dipeptidomimetics targeting malarial aspartic protease plasmepsin.
Studies on novel 2-imidazolidinones and tetrahydropyrimidin-2(1H)-ones as potential TACE inhibitors: design, synthesis, molecular modeling, and preliminary biological evaluation.
Synthesis and structure-activity relationships of 2-acylamino-4,6-diphenylpyridine derivatives as novel antagonists of GPR54.
Design and synthesis of membrane fusion inhibitors against the feline immunodeficiency virus.
Solution-phase parallel synthesis of substituted chalcones and their antiparasitary activity against Giardia lamblia.
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder.
Antinociceptive and antiinflammatory activities and QSAR studies on 2-substituted-4,5-diphenyl-1H-imidazoles.
Design of endoperoxides with anti-Candida activity.
Synthesis and evaluation of antitumor activity of novel N-acyllavendamycin analogues and quinoline-5,8-diones.
Syntheses and anti-cancer activities of 2-[1-(indol-3-yl-/pyrimidin-5-yl-/pyridine-2-yl-/quinolin-2-yl)-but-3-enylamino]-2-phenyl-ethanols.
Antitumor studies. Part 1: design, synthesis, antitumor activity, and AutoDock study of 2-deoxo-2-phenyl-5-deazaflavins and 2-deoxo-2-phenylflavin-5-oxides as a new class of antitumor agents.
Design, synthesis, and antitumor activity of new bis-aminomethylnaphthalenes.
Stress-driven discovery of metabolites from the phytopathogenic fungus Leptosphaeria maculans: structure and activity of leptomaculins A-E.
Synthesis and antitumor activity of C-9 epimers of the tetrahydrofuran containing acetogenin 4-deoxyannoreticuin.
Construction of polyamine-modified uridine and adenosine derivatives--evaluation of DNA binding capacity and cytotoxicity in vitro.
Introduction of the 4-(4-bromophenyl)benzenesulfonyl group to hydrazide analogs of Ilomastat leads to potent gelatinase B (MMP-9) inhibitors with improved selectivity.
Antimicrobial and cytotoxic arylazoenamines. Part III: antiviral activity of selected classes of arylazoenamines.
Structure-activity relationship of flavonoids as influenza virus neuraminidase inhibitors and their in vitro anti-viral activities.
Synthesis and in vivo evaluation of 11-substituted estradiol derivatives as anti-implantation agents.
Development of novel 2-[4-(aminoalkoxy)phenyl]-4(3H)-quinazolinone derivatives as potent and selective histamine H3 receptor inverse agonists.
Studies of the metabolic stability in cells of 5-(trifluoroacetyl)thiophene-2-carboxamides and identification of more stable class II histone deacetylase (HDAC) inhibitors.
N-pyridin-3-yl- and N-quinolin-3-yl-benzamides: modulators of human vanilloid receptor 1 (TRPV1).
1-Benzylbenzimidazoles: the discovery of a novel series of bradykinin B(1) receptor antagonists.
Synthesis and structure-activity relationships of (R)-1-alkyl-3-[2-(2-amino)phenethyl]-5-(2-fluorophenyl)-6-methyluracils as human GnRH receptor antagonists.
Epoxygenase eicosanoids: synthesis of tetrahydrofuran-diol metabolites and their vasoactivity.
Design, docking, and synthesis of novel indeno[1,2-c]isoquinolines for the development of antitumor agents as topoisomerase I inhibitors.
Synthesis and biological activities of novel indole derivatives as potent and selective PPARgamma modulators.
The discovery and unique pharmacological profile of RO4938581 and RO4882224 as potent and selective GABAA alpha5 inverse agonists for the treatment of cognitive dysfunction.
Boron-containing phenoxyacetanilide derivatives as hypoxia-inducible factor (HIF)-1alpha inhibitors.
Dienyl diketones as anticancer agents: synthesis and biological evaluation of some aromatic derivatives.
Synthesis and biological evaluation of substituted 4-(OBz)phenylalanine derivatives as novel N-type calcium channel blockers.
Pyrrolo[3,2,1-ij]quinoline derivatives, a 5-HT2c receptor agonist with selectivity over the 5-HT2a receptor: potential therapeutic applications for epilepsy and obesity.
Design and optimisation of selective serotonin re-uptake inhibitors with high synthetic accessibility: part 2.
Novel derivatives of ISO-1 as potent inhibitors of MIF biological function.
Part 1: Structure-Activity Relationship (SAR) investigations of fused pyrazoles as potent, selective and orally available inhibitors of p38alpha mitogen-activated protein kinase.
Synthesis and evaluation of 2,7-diamino-thiazolo[4,5-d] pyrimidine analogues as anti-tumor epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors.
Differential effects of quinoline antimalarials on endocytosis in Plasmodium falciparum.
Rifaximin does not induce toxin production or phage-mediated lysis of Shiga toxin-producing Escherichia coli.
Influence of inoculum size on the selection of resistant mutants of Escherichia coli in relation to mutant prevention concentrations of marbofloxacin.
In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.
bla(IMP-4) in different genetic contexts in Enterobacteriaceae isolates from Australia.
Potency of SMP-601, a novel carbapenem, in hematogenous murine bronchopneumonia caused by methicillin-resistant and vancomycin-intermediate Staphylococcus aureus.
In vivo efficacy of ceftaroline (PPI-0903), a new broad-spectrum cephalosporin, compared with linezolid and vancomycin against methicillin-resistant and vancomycin-intermediate Staphylococcus aureus in a rabbit endocarditis model.
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
The Anti-Trypanosoma cruzi activity of posaconazole in a murine model of acute Chagas' disease is less dependent on gamma interferon than that of benznidazole.
In vitro evaluation of the activities of telavancin, cefazolin, and vancomycin against methicillin-susceptible and methicillin-resistant Staphylococcus aureus in peritoneal dialysate.
Aspirin antagonism in isoniazid treatment of tuberculosis in mice.
Evaluation of Etest method for determining isavuconazole MICs against Cryptococcus gattii and Cryptococcus neoformans.
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
blaVIM-2-harboring integrons isolated in India, Russia, and the United States arise from an ancestral class 1 integron predating the formation of the 3' conserved sequence.
Derivatives of schisandrin with increased inhibitory potential on prostaglandin E(2) and leukotriene B(4) formation in vitro.
Tetrahydroisoquinolines as dopaminergic ligands: 1-Butyl-7-chloro-6-hydroxy-tetrahydroisoquinoline, a new compound with antidepressant-like activity in mice.
Design, synthesis and dopamine D4 receptor binding activities of new N-heteroaromatic 5/6-ring Mannich bases.
Synthesis and cytotoxic activity of 5,6-heteroaromatically annulated pyridine-2,4-diamines.
Synthesis of a new cytotoxic cephalostatin/ritterazine analogue from hecogenin and 22-epi-hippuristanol.
Multivalent catanionic GalCer analogs derived from first generation dendrimeric phosphonic acids.
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.
Structure-activity relationships of 3,5-disubstituted benzamides as glucokinase activators with potent in vivo efficacy.
Synthesis, molecular docking and biological evaluation of metronidazole derivatives as potent Helicobacter pylori urease inhibitors.
Synthesis and pharmacological evaluation of novel 1- and 8-substituted-3-furfuryl xanthines as adenosine receptor antagonists.
Push-pull benzothiazole derivatives as probes for detecting beta-amyloid plaques in Alzheimer's brains.
Synthesis and bradykinin inhibitory activity of novel non-peptide compounds, and evaluation of in vivo analgesic activity.
Synthesis and in vitro antiprotozoal evaluation of substituted phenalenone analogues.
Synthesis and pharmacological evaluation of 1,2,3,4-tetrahydropyrazino[1,2-a]indole and 2-[(phenylmethylamino)methyl]-1H-indole analogues as novel melatoninergic ligands.
Piperidine variations in search for non-imidazole histamine H(3) receptor ligands.
Design and SAR of new substituted purines bearing aryl groups at N9 position as HIV-1 Tat-TAR interaction inhibitors.
Discovery and stereoselective synthesis of the novel isochroman neurokinin-1 receptor antagonist 'CJ-17,493'.
In vitro inhibition of salicylic acid derivatives on human cytosolic carbonic anhydrase isozymes I and II.
Nootropic alpha7 nicotinic receptor allosteric modulator derived from GABAA receptor modulators.
Design of helical, oligomeric HIV-1 fusion inhibitor peptides with potent activity against enfuvirtide-resistant virus.
From the Cover: Antipsychotic drug-induced weight gain mediated by histamine H1 receptor-linked activation of hypothalamic AMP-kinase.
Designer enediynes generate DNA breaks, interstrand cross-links, or both, with concomitant changes in the regulation of DNA damage responses.
Hemopressin is an inverse agonist of CB1 cannabinoid receptors.
Food web-specific biomagnification of persistent organic pollutants.
Structural basis for the high all-trans-retinaldehyde reductase activity of the tumor marker AKR1B10.
Novel and potent inhibitors of stearoyl-CoA desaturase-1. Part I: Discovery of 3-(2-hydroxyethoxy)-4-methoxy-N-[5-(3-trifluoromethylbenzyl)thiazol-2-yl]benzamide.
Smart conferring of nuclease resistance to DNA by 3'-end protection using 2',4'-bridged nucleoside-5'-triphosphates.
6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective alpha1A adrenoceptor partial agonists.
Carbonic anhydrase inhibitors. Synthesis of 2,4,6-trimethylpyridinium derivatives of 2-(hydrazinocarbonyl)-3-aryl-1H-indole-5-sulfonamides acting as potent inhibitors of the tumor-associated isoform IX and XII.
Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications.
[(11)C]PR04.MZ, a promising DAT ligand for low concentration imaging: Synthesis, efficient (11)C-O-methylation and initial small animal PET studies.
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Design, structure-activity relationship, and pharmacokinetic profile of pyrazole-based indoline factor Xa inhibitors.
Design, synthesis and antiproliferative properties of oligomers with chromophore units linked by amide backbones.
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
O-Spiro C-aryl glucosides as novel sodium-dependent glucose co-transporter 2 (SGLT2) inhibitors.
Synthesis and antimicrobial studies on novel chloro-fluorine containing hydroxy pyrazolines.
Discovery of the first known small-molecule inhibitors of heme-regulated eukaryotic initiation factor 2alpha (HRI) kinase.
Regioselective synthesis of methylated epigallocatechin gallate via nitrobenzenesulfonyl (Ns) protecting group.
(4-Piperidinyl)-piperazine: a new platform for acetyl-CoA carboxylase inhibitors.
In vitro activities of CG400549, a novel FabI inhibitor, against recently isolated clinical staphylococcal strains in Korea.
Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
A Candida albicans petite mutant strain with uncoupled oxidative phosphorylation overexpresses MDR1 and has diminished susceptibility to fluconazole and voriconazole.
Presence of plasmid-mediated quinolone resistance in Klebsiella pneumoniae isolates possessing blaKPC in the United States.
Sequencing and comparative genomic analysis of pK29, a 269-kilobase conjugative plasmid encoding CMY-8 and CTX-M-3 beta-lactamases in Klebsiella pneumoniae.
Novel complex class 1 integron bearing an ISCR1 element in an Escherichia coli isolate carrying the blaCTX-M-14 gene.
Paradoxical effect of Echinocandins across Candida species in vitro: evidence for echinocandin-specific and candida species-related differences.
Atorvastatin is 10-fold more active in vitro than other statins against Plasmodium falciparum.
Prospective randomized trial of empiric therapy with trimethoprim-sulfamethoxazole or doxycycline for outpatient skin and soft tissue infections in an area of high prevalence of methicillin-resistant Staphylococcus aureus.
Comparison of antimicrobial resistance profiles among extended-spectrum-beta-lactamase-producing and acquired AmpC beta-lactamase-producing Escherichia coli isolates from Canadian intensive care units.
Binding of ceftobiprole and comparators to the penicillin-binding proteins of Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, and Streptococcus pneumoniae.
The Lys234Arg substitution in the enzyme SHV-72 is a determinant for resistance to clavulanic acid inhibition.
In vitro susceptibilities of 217 clinical isolates of zygomycetes to conventional and new antifungal agents.
Clonal spread of mef-positive macrolide-resistant Streptococcus pneumoniae isolates causing invasive disease in adults in Germany.
Postantibiotic effects and bactericidal activities of levofloxacin and gatifloxacin at concentrations simulating those of topical ophthalmic administration against fluoroquinolone-resistant and fluoroquinolone-sensitive methicillin-resistant Staphylococcus aureus strains.
Emergence of the plasmid-mediated quinolone resistance gene qnrS1 in Escherichia coli isolates in Greece.
Relationship of blood level and susceptibility in voriconazole treatment of histoplasmosis.
Effects of piperaquine, chloroquine, and amodiaquine on drug uptake and of these in combination with dihydroartemisinin against drug-sensitive and -resistant Plasmodium falciparum strains.
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism.
Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine.
Stereochemical studies on the novel monoamine oxidase B substrates (1R,6S)- and (1S,6R)-3-methyl-6-phenyl-3-aza-bicyclo[4.1.0]heptane.
Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines.
Design and synthesis of new 1,3-benzthiazinan-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
Synthesis and preliminary antibacterial evaluation of simplified thiomarinol analogs.
Synthesis and screening of a cyclic peptide library: discovery of small-molecule ligands against human prolactin receptor.
Arabinose 5-phosphate analogues as mechanistic probes for Neisseria meningitidis 3-deoxy-D-manno-octulosonate 8-phosphate synthase.
Synthesis and in vitro anti-hepatitis B virus activity of 6H-[1]benzothiopyrano[4,3-b]quinolin-9-ols.
Isolation, structure, and antibacterial activity of thiazomycin A, a potent thiazolyl peptide antibiotic from Amycolatopsis fastidiosa.
Tetrahydropyridine-4-carboxamides as novel, potent transient receptor potential vanilloid 1 (TRPV1) antagonists.
Enaminones 8: CoMFA and CoMSIA studies on some anticonvulsant enaminones.
Enhanced affinity of ketotifen toward tamarind seed polysaccharide in comparison with hydroxyethylcellulose and hyaluronic acid: a nuclear magnetic resonance investigation.
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Modulation of gene expression via disruption of NF-kappaB signaling by a bacterial small molecule.
Metabolism and pharmacokinetics of a novel Src kinase inhibitor TG100435 ([7-(2,6-dichloro-phenyl)-5-methyl-benzo[1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine) and its active N-oxide metabolite TG100855 ([7-(2,6-dichloro-phenyl)-5-methylbenzo[1,2,4]triazin-3-yl]-{4-[2-(1-oxy-pyrrolidin-1-yl)-ethoxy]-phenyl}-amine).
Crystal structures of Saccharomyces cerevisiae N-myristoyltransferase with bound myristoyl-CoA and inhibitors reveal the functional roles of the N-terminal region.
Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species.
S-adenosylmethionine-dependent protein methylation in mammalian cytosol via tyrphostin modification by catechol-O-methyltransferase.
Hepatitis C virus NS5A is a direct substrate of casein kinase I-alpha, a cellular kinase identified by inhibitor affinity chromatography using specific NS5A hyperphosphorylation inhibitors.
Survival in the presence of antifungals: genome-wide expression profiling of Aspergillus niger in response to sublethal concentrations of caspofungin and fenpropimorph.
Interaction between HIV-1 Rev and integrase proteins: a basis for the development of anti-HIV peptides.
Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate.
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.
Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).
Synthesis of selenophene derivatives as novel CHK1 inhibitors.
Discovery of piperidin-4-yl-aminopyrimidines as HIV-1 reverse transcriptase inhibitors. N-benzyl derivatives with broad potency against resistant mutant viruses.
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents.
Synthesis and PGE(2) production inhibition of 1H-furan-2,5-dione and 1H-pyrrole-2,5-dione derivatives.
Synthesis and SAR of 4-substituted-2-aminopyrimidines as novel c-Jun N-terminal kinase (JNK) inhibitors.
Relationships between the structures of flavanone derivatives and their effects in enhancing early growth response-1 gene expression.
A new class of 5-HT2B antagonists possesses favorable potency, selectivity, and rat pharmacokinetic properties.
Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy.
Beta-C-glycosiduronic acids and beta-C-glycosyl compounds: new PTP1B inhibitors.
Exploring a pocket for polycycloaliphatic groups in the CXCR3 receptor with the aid of a modular synthetic strategy.
New functionalized 1,2,4-trioxepanes: synthesis and antimalarial activity against multi-drug resistant P. yoelii in mice.
Novel BK channel openers containing dehydroabietic acid skeleton: structure-activity relationship for peripheral substituents on ring C.
Synthesis and biological activity of anticoccidial agents: 5,6-diarylimidazo[2,1-b][1,3]thiazoles.
In vitro activity of the oxazolidinone RWJ-416457 against linezolid-resistant and -susceptible staphylococci and enterococci.
Diversity of penicillin binding proteins among clinical Streptococcus pneumoniae strains from Portugal.
gyrA and parC Mutations and associated quinolone resistance in Vibrio anguillarum serotype O2b strains isolated from farmed Atlantic cod (Gadus morhua) in Norway.
Isobolographic analysis of pharmacodynamic interactions between antifungal agents and ciprofloxacin against Candida albicans and Aspergillus fumigatus.
Safety and pharmacokinetics of Bevirimat (PA-457), a novel inhibitor of human immunodeficiency virus maturation, in healthy volunteers.
In vitro study of Candida tropicalis isolates exhibiting paradoxical growth in the presence of high concentrations of caspofungin.
Detection of the erythromycin rRNA methylase gene erm(A) in Enterococcus faecalis.
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
In Vitro activities of isepamicin, other aminoglycosides, and capreomycin against clinical isolates of rapidly growing mycobacteria in Taiwan.
Synergy of human immunodeficiency virus protease inhibitors with chloroquine against Plasmodium falciparum in vitro and Plasmodium chabaudi in vivo.
Antimicrobial susceptibilities of Peptostreptococcus anaerobius and the newly described Peptostreptococcus stomatis isolated from various human sources.
Natural polymorphisms in the human immunodeficiency virus type 2 protease can accelerate time to development of resistance to protease inhibitors.
Comparison of the efficacies of oral beta-lactams in selection of Haemophilus influenzae transformants with mutated ftsI genes.
Multiclonal outbreak of Klebsiella pneumoniae producing extended-spectrum beta-lactamase CTX-M-2 and novel variant CTX-M-59 in a neonatal intensive care unit in Brazil.
Synthesis of (nor)tropeine (di)esters and allosteric modulation of glycine receptor binding.
Synthesis and cytotoxicity evaluation of 22,23-oxygenated stigmastane derivatives.
Modulating paclitaxel bioavailability for targeting prostate cancer.
Synthesis and structure-activity relationships study of novel anti-tumor carbamate anhydrovinblastine analogues.
Synthesis, structure-activity relationships and molecular modeling studies of new indole inhibitors of monoamine oxidases A and B.
Myricetin inhibits Escherichia coli DnaB helicase but not primase.
A new opioid designed multiple ligand derived from the micro opioid agonist endomorphin-2 and the delta opioid antagonist pharmacophore Dmt-Tic.
Isolation and syntheses of polymethoxyflavones and hydroxylated polymethoxyflavones as inhibitors of HL-60 cell lines.
Thiahomoisocitrate: a highly potent inhibitor of homoisocitrate dehydrogenase involved in the alpha-aminoadipate pathway.
Efficient synthesis of the first betulonic acid-acetylene hybrids and their hepatoprotective and anti-inflammatory activity.
Combinatorial chemistry in the agrosciences.
Petrosamine, a potent anticholinesterase pyridoacridine alkaloid from a Thai marine sponge Petrosia n. sp.
Solution- and solid-phase synthesis and anti-HIV activity of maslinic acid derivatives containing amino acids and peptides.
Inhibition of human dimethylarginine dimethylaminohydrolase-1 by S-nitroso-L-homocysteine and hydrogen peroxide. Analysis, quantification, and implications for hyperhomocysteinemia.
HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitro.
Structure and regulation of the human Nek2 centrosomal kinase.
Expression cloning of a Na+-independent aromatic amino acid transporter with structural similarity to H+/monocarboxylate transporters.
The sister of P-glycoprotein represents the canalicular bile salt export pump of mammalian liver.
Synthesis and SAR of heterocyclic carboxylic acid isosteres based on 2-biarylethylimidazole as bombesin receptor subtype-3 (BRS-3) agonists for the treatment of obesity.
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.
Fragment-based discovery and optimization of BACE1 inhibitors.
Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.
Structure-activity relationship study of novel tissue transglutaminase inhibitors.
Antimalarial activity of 2,4,6-trisubstituted pyrimidines.
Fluorescent metal ion indicators based on benzoannelated crown systems: a green fluorescent indicator for intracellular sodium ions.
Identification of a sulfonamide series of CCR2 antagonists.
Imidazopyridine derivatives as potent and selective Polo-like kinase (PLK) inhibitors.
N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors.
Development of dual-acting prodrugs for circumventing multidrug resistance.
Aryl sulphonyl amides as potent agonists of the growth hormone secretagogue (ghrelin) receptor.
Peri-substituted hexahydro-indolones as novel, potent and selective human EP3 receptor antagonists.
Activation and inhibition of leukotriene A4 hydrolase aminopeptidase activity by diphenyl ether and derivatives.
Synthesis and bioevaluation of hybrid 4-aminoquinoline triazines as a new class of antimalarial agents.
Structure-activity relationship study of a novel necroptosis inhibitor, necrostatin-7.
Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assay.
Inhibition of NF-kB and metalloproteinase-9 expression and secretion by parthenolide derivatives.
Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.
Carbonic anhydrase inhibitors: crystallographic and solution binding studies for the interaction of a boron-containing aromatic sulfamide with mammalian isoforms I-XV.
1,4-Dihydroindeno[1,2-c]pyrazoles as potent checkpoint kinase 1 inhibitors: extended exploration on phenyl ring substitutions and preliminary ADME/PK studies.
Himbacine derived thrombin receptor antagonists: discovery of a new tricyclic core.
Phenylpiperidine-benzoxazinones as urotensin-II receptor antagonists: synthesis, SAR, and in vivo assessment.
Dammarane-type saponins from the flower buds of Panax ginseng and their effects on human leukemia cells.
Selective kappa-opioid antagonists related to naltrindole. Effect of side-chain spacer in the 5'-amidinoalkyl series.
Carbohydrate-modulated DNA photocleavage: design, synthesis, and evaluation of novel glycosyl anthraquinones.
In vitro susceptibilities of Mycoplasma putrefaciens field isolates.
Histatin-derived monomeric and dimeric synthetic peptides show strong bactericidal activity towards multidrug-resistant Staphylococcus aureus in vivo.
Antiviral and anti-inflammatory effects of rosmarinic acid in an experimental murine model of Japanese encephalitis.
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
Global challenge of multidrug-resistant Acinetobacter baumannii.
Maintenance of therapeutic concentrations of caspofungin after temporary treatment interruption (48 hours) in a child with invasive aspergillosis.
Pyrazinoic acid and its n-propyl ester inhibit fatty acid synthase type I in replicating tubercle bacilli.
A novel insertion sequence, ISPA26, in oprD of Pseudomonas aeruginosa is associated with carbapenem resistance.
Identification and structural characterization of I84C and I84A mutations that are associated with high-level resistance to human immunodeficiency virus protease inhibitors and impair viral replication.
Measurement of voriconazole activity against Candida albicans, C. glabrata, and C. parapsilosis isolates using time-kill methods validated by high-performance liquid chromatography.
Altered pharmacokinetics of voriconazole in a patient with liver cirrhosis.
Design and synthesis of novel oxazole containing 1,3-dioxane-2-carboxylic acid derivatives as PPAR alpha/gamma dual agonists.
Cross-resistance to medical and agricultural azole drugs in yeasts from the oropharynx of human immunodeficiency virus patients and from environmental Bavarian vine grapes.
N-Aroyl-3,5-bis(benzylidene)-4-piperidones: a novel class of antimycobacterial agents.
In vitro activities of amphotericin B, caspofungin, itraconazole, posaconazole, and voriconazole against 45 clinical isolates of zygomycetes: comparison of CLSI M38-A, Sensititre YeastOne, and the Etest.
Identification and characterization of a new metallo-beta-lactamase, IND-5, from a clinical isolate of Chryseobacterium indologenes.
Synergistic interactions of the antiretroviral protease inhibitors saquinavir and ritonavir with chloroquine and mefloquine against Plasmodium falciparum in vitro.
Treatment and outcomes of infections by methicillin-resistant Staphylococcus aureus at an ambulatory clinic.
3D QSAR of novel estrogen-RGD peptide conjugates: getting insight into structural dependence of anti-osteoporosis activity and side effect of estrogen in ERT.
Synthesis and antitumor activity evaluations of albumin-binding prodrugs of CC-1065 analog.
Inhibition of aldose reductase from cataracted eye lenses by finger millet (Eleusine coracana) polyphenols.
Synthesis and structure-activity relationship of a novel series of heterocyclic sulfonamide gamma-secretase inhibitors.
Glucose-based spiro-heterocycles as potent inhibitors of glycogen phosphorylase.
Synthesis and in vitro biological activity of retinyl retinoate, a novel hybrid retinoid derivative.
Novel azabicyclo[3.2.2]nonane derivatives and their activities against Plasmodium falciparum K1 and Trypanosoma brucei rhodesiense.
Structure and estrogenic activity of new lignans from Iryanthera lancifolia.
Discovery and structure-activity relationship of N-phenyl-1H-pyrazolo[3,4-b]quinolin-4-amines as a new series of potent apoptosis inducers.
Synthesis and biological activities of quinazoline derivatives with ortho-phenol-quaternary ammonium salt groups.
Enhancement of oral drug absorption-effect of lipid conjugation on the enzymatic stability and intestinal permeability of l-Glu-l-Trp-NH(2).
Benzhydrylquinazolinediones: novel cytosolic phospholipase A2alpha inhibitors with improved physicochemical properties.
The synthesis of ursolic acid derivatives with cytotoxic activity and the investigation of their preliminary mechanism of action.
Synthesis and inhibitory activity against COX-2 catalyzed prostaglandin production of chrysin derivatives.
Synthesis, structure analysis, and antibacterial activity of some novel 10-substituted 2-(4-piperidyl/phenyl)-5,5-dioxo[1,2,4]triazolo[1,5-b][1,2,4]benzothiadiazine derivatives.
Toward novel HIV-1 integrase binding inhibitors: molecular modeling, synthesis, and biological studies.
Potent, nonsteroidal selective androgen receptor modulators (SARMs) based on 8H-[1,4]oxazino[2,3-f]quinolin-8-ones.
Synthesis and inhibitory activity against human monoamine oxidase of N1-thiocarbamoyl-3,5-di(hetero)aryl-4,5-dihydro-(1H)-pyrazole derivatives.
Rational design, synthesis, and structure-activity relationship of benzoxazolones: new potent mglu5 receptor antagonists based on the fenobam structure.
Synthesis and biological activity of alpha-glucosyl C24:0 and C20:2 ceramides.
Anti-tubercular agents. Part IV: Synthesis and antimycobacterial evaluation of nitroheterocyclic-based 1,2,4-benzothiadiazines.
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.
Molecular iodine promoted synthesis of new pyrazolo[3,4-d]pyrimidine derivatives as potential antibacterial agents.
Cyclonatsudamine A, a new vasodilator cyclic peptide from Citrus natsudaidai.
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors.
ABC synthesis and antitumor activity of a series of Annonaceous acetogenin analogs with a threo, trans, threo, trans, threo-bis-tetrahydrofuran core unit.
Selection of inhibitory peptides for Aurora-A kinase from a phage-displayed library of helix-loop-helix peptides.
Three-component, one-pot synthesis of novel 2,4-substituted 5-azolylthiopyrimidine library for screening against anti-influenza virus A.
Synthesis and antimicrobial activity of novel C-linked imidazole glycoconjugates.
Solid-phase synthesis and biological evaluation of a uridinyl branched peptide urea library.
Synthesis and antibacterial activity of C11, C12-cyclic urea analogues of ketolides.
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
A new class of bradykinin B1 receptor antagonists with high oral bioavailability and minimal PXR activity.
Facile formation of hydrophilic derivatives of 5H-8,9-dimethoxy-5-[2-(N,N-dimethylamino)ethyl]-2,3-methylenedioxydibenzo[c,h] [1,6]naphthyridin-6-one (ARC-111) and its 12-aza analog via quaternary ammonium intermediates.
Synthesis and SAR of novel imidazoles as potent and selective cannabinoid CB2 receptor antagonists with high binding efficiencies.
Discovery of carmegliptin: a potent and long-acting dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Synthesis of pyrrolo[2,3-d]pyrimidine derivatives and their antiproliferative activity against melanoma cell line.
Soluble polyphenols: synthesis and bioavailability of 3,4',5-tri(alpha-D-glucose-3-O-succinyl) resveratrol.
Synthesis of novel pyrazole carboxamide derivatives and discovery of modulators for apoptosis or autophagy in A549 lung cancer cells.
Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI).
Studies on aromatic compounds: inhibition of calpain I by biphenyl derivatives and peptide-biphenyl hybrids.
2,5-Diaminopyrimidines and 3,5-disubstituted azapurines as inhibitors of glycogen synthase kinase-3 (GSK-3).
S-(2-(acylamino)phenyl) 2,2-dimethylpropanethioates as CETP inhibitors.
1,3-disubstituted 4-aminopiperidines as useful tools in the optimization of the 2-aminobenzo[a]quinolizine dipeptidyl peptidase IV inhibitors.
Discovery of novel and potent benzhydryl-tropane trypanocides highly selective for Trypanosoma cruzi.
Design, synthesis, and antitumor activity of bile acid-polyamine-nucleoside conjugates.
Mining biologically-active molecules for inhibitors of fatty acid amide hydrolase (FAAH): identification of phenmedipham and amperozide as FAAH inhibitors.
Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
Location of persisting mycobacteria in a Guinea pig model of tuberculosis revealed by r207910.
Combination of amphotericin B with flucytosine is active in vitro against flucytosine-resistant isolates of Cryptococcus neoformans.
Bioactive alkenylphenols from Piper obliquum.
Effects of imipenem-cilastatin, ertapenem, piperacillin-tazobactam, and ceftriaxone treatments on persistence of intestinal colonization by extended-spectrum-beta-lactamase-producing Klebsiella pneumoniae strains in mice.
Calcineurin inhibition or mutation enhances cell wall inhibitors against Aspergillus fumigatus.
RCAI-17, 22, 24-26, 29, 31, 34-36, 38-40, and 88, the analogs of KRN7000 with a sulfonamide linkage: their synthesis and bioactivity for mouse natural killer T cells to produce Th2-biased cytokines.
The Ssk1p response regulator and Chk1p histidine kinase mutants of Candida albicans are hypersensitive to fluconazole and voriconazole.
In vitro activities of different inhibitors of bacterial transcription against Staphylococcus epidermidis biofilm.
Determination of the primary target of a quinolone drug and the effect of quinolone resistance-conferring mutations by measuring quinolone sensitivity based on its mode of action.
Molecular epidemiology of imipenem-resistant Acinetobacter haemolyticus and Acinetobacter baumannii isolates carrying plasmid-mediated OXA-40 from a Portuguese hospital.
Antimicrobial susceptibility and synergy studies of Burkholderia cepacia complex isolated from patients with cystic fibrosis.
Structure-toxicity relationship of aminoglycosides: correlation of 2'-amine basicity with acute toxicity in pseudo-disaccharide scaffolds.
Galanin message-associated peptide suppresses growth and the budded-to-hyphal-form transition of Candida albicans.
Salicylanilides: selective inhibitors of interleukin-12p40 production.
In vitro antifungal activity of polyfunctionalized 2-(hetero)arylquinolines prepared through imino Diels-Alder reactions.
Function-oriented synthesis applied to the anti-botulinum natural product toosendanin.
New and selective ryanodine receptor activators for insect control.
Selective small molecule inhibitors of the potential breast cancer marker, human arylamine N-acetyltransferase 1, and its murine homologue, mouse arylamine N-acetyltransferase 2.
NO-glibenclamide derivatives: prototypes of a new class of nitric oxide-releasing anti-diabetic drugs.
Discovery of N-[(1R,2S,5S)-2-{[(5-chloroindol-2-yl)carbonyl]amino}-5-(dimethylcarbamoyl)cyclohexyl]-5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamide hydrochloride: a novel, potent and orally active direct inhibitor of factor Xa.
Steroidal bivalent ligands for the estrogen receptor: design, synthesis, characterization and binding affinities.
Cooperative alkylation of double-strand human telomere repeat sequences by PI polyamides with 11-base-pair recognition based on a heterotrimeric design.
Synthesis and pharmacological evaluation of new arylpiperazines N-[4-[4-(aryl) piperazine-1-yl]-phenyl]-amine derivatives: putative role of 5-HT1A receptors.
Synthesis and structure-activity relationships of N-(4-amino-2,6-diisopropylphenyl)-N'-(1,4-diarylpiperidine-4-yl)methylureas as anti-hyperlipidemic agents.
Inhibitors of tubulin polymerization: synthesis and biological evaluation of hybrids of vindoline, anhydrovinblastine and vinorelbine with thiocolchicine, podophyllotoxin and baccatin III.
Design and synthesis of a novel tyrosine kinase inhibitor template.
Conformation-opioid activity relationships of bicyclic guanidines from 3D similarity analysis.
Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors.
Xanthones from Cudrania tricuspidata displaying potent alpha-glucosidase inhibition.
Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors.
Ergoline derivatives as highly potent and selective antagonists at the somatostatin sst 1 receptor.
Dipeptidyl alpha-fluorovinyl Michael acceptors: synthesis and activity against cysteine proteases.
Hybrid angiogenesis inhibitors: synthesis and biological evaluation of bifunctional compounds based on 1-deoxynojirimycin and aryl-1,2,3-triazoles.
Protein subtype-targeting through ligand epimerization: talose-selectivity of galectin-4 and galectin-8.
New 1,8-naphthyridine and quinoline derivatives as CB2 selective agonists.
Synthesis and structure-activity relationships of thieno[2,3-b]pyrroles as antagonists of the GnRH receptor.
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 4: functionalization of the benzopyran A-ring.
[(S)-gamma-(4-Aryl-1-piperazinyl)-l-prolyl]thiazolidines as a novel series of highly potent and long-lasting DPP-IV inhibitors.
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors.
3-Amino-2-hydroxyamides and related compounds as inhibitors of methionine aminopeptidase-2.
Discovery of 2-amino-6-carboxamidobenzothiazoles as potent Lck inhibitors.
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: highly potent against human enzyme within a cellular environment.
Synthesis and cytotoxicity of desmethoxycallipeltin B: lack of a quinone methide for the cytotoxicity of callipeltin B.
Synthesis of fluorescent and photoaffinity-labeled derivatives of bisphenol A and their inhibitory activity toward hypoxic expression of erythropoietin.
OSW-1 analogues: modification of the carbohydrate moiety.
Synthesis and antiproliferative activity of unnatural enantiomers of 7-epi-goniofufurone and crassalactone C.
Design and synthesis of a series of meta aniline-based LFA-1 ICAM inhibitors.
A serine protease inhibitor from hemolymph of green mussel, Perna viridis.
Semi-synthesis and biological activity of gamma-lactones analogs of camptothecin.
Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor.
4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors.
Design of high-affinity peptide conjugates with optimized fluorescence quantum yield as markers for small peptide transporter PEPT1 (SLC15A1).
Synthesis of 4'-modified noraristeromycins to clarify the effect of the 4'-hydroxyl groups for inhibitory activity against S-adenosyl-L-homocysteine hydrolase.
Synthesis of small molecule inhibitors of the orphan nuclear receptor steroidogenic factor-1 (NR5A1) based on isoquinolinone scaffolds.
Discovery of a potent and selective c-Kit inhibitor for the treatment of inflammatory diseases.
Novel 3-alkoxy-1H-pyrazolo[3,4-d]pyrimidines as EGFR and erbB2 receptor tyrosine kinase inhibitors.
The design, synthesis and structure-activity relationships of 1-aryl-4-aminoalkylisoquinolines: a novel series of CRF-1 receptor antagonists.
Enhanced anti-influenza A virus activity of (-)-epigallocatechin-3-O-gallate fatty acid monoester derivatives: effect of alkyl chain length.
Investigation of Beckett-Casy model 1: synthesis of novel 16,17-seco-naltrexone derivatives and their pharmacology.
A single step purification for autolytic zinc proteinases.
Structure-based design, synthesis and biological evaluation of new N-carboxyphenylpyrrole derivatives as HIV fusion inhibitors targeting gp41.
Novel non-peptidic vinylsulfones targeting the S2 and S3 subsites of parasite cysteine proteases.
Synthesis and biochemical evaluation of a range of sulfonated derivatives of 4-hydroxybenzyl imidazole as highly potent inhibitors of rat testicular 17alpha-hydroxylase/17,20-lyase (P-450(17alpha)).
Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity.
2-Phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors: a study on the importance of modifications at the side chain on the activity.
Fosamprenavir plus ritonavir increases plasma ketoconazole and ritonavir exposure, while amprenavir exposure remains unchanged.
First occurrence of an Escherichia coli clinical isolate producing the VIM-1/VIM-2 hybrid metallo-beta-lactamase VIM-12.
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
Susceptibility of acinetobacter strains isolated from deployed U.S. military personnel.
Synthesis of 6-substituted 1-phenylbenzazepines and their dopamine D(1) receptor activities.
Quinupristin-dalfopristin nonsusceptibility in pneumococci from sickle cell disease patients.
Axial chirality and affinity at the GABA(A) receptor of pyrimido[1,2-a][1,4]benzodiazepines and related compounds.
The efficacy and selectivity of tumor cell killing by Akt inhibitors are substantially increased by chloroquine.
Synthesis, structure and antibacterial activity of novel 1-(5-substituted-3-substituted-4,5-dihydropyrazol-1-yl)ethanone oxime ester derivatives.
Building skeletally diverse architectures on the Indoline Scaffold: the discovery of a chemical probe of focal adhesion kinase signaling networks.
Synthesis, resolution, stereochemistry, and molecular modeling of (R)- and (S)-2-acetyl-1-(4'-chlorophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline AMPAR antagonists.
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
Peptidyl epoxides extended in the P' direction as cysteine protease inhibitors: effect on affinity and mechanism of inhibition.
Synthesis and biological evaluation of novel 6-substituted 5-alkyl-2-(arylcarbonylmethylthio)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
Influence of 6- or 8-substitution on the antiviral activity of 3-arylalkylthiomethylimidazo[1,2-a]pyridine against human cytomegalovirus (CMV) and varicella-zoster virus (VZV): part II.
Effect of carbapenem administration on establishment of intestinal colonization by vancomycin-resistant enterococci and Klebsiella pneumoniae in mice.
Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR.
Identification of a bioactive compound isolated from Brazilian propolis type 6.
New N-substituted 9-azabicyclo[3.3.1]nonan-3alpha-yl phenylcarbamate analogs as sigma2 receptor ligands: synthesis, in vitro characterization, and evaluation as PET imaging and chemosensitization agents.
p-Guanidinoethyl calixarene and parent phenol derivatives exhibiting antibacterial activities. Synthesis and biological evaluation.
Studies on anti-HIV quinolones: new insights on the C-6 position.
E,E-2-Benzylidene-6-(nitrobenzylidene)cyclohexanones: syntheses, cytotoxicity and an examination of some of their electronic, steric, and hydrophobic properties.
Non-vanillyl resiniferatoxin analogues as potent and metabolically stable transient receptor potential vanilloid 1 agonists.
Synthesis and antiviral activity evaluation of acyclic 2'-azanucleosides bearing a phosphonomethoxy function in the side chain.
A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone.
Antimicrobial natural products as beta-ketoacyl-acyl carrier protein synthase III inhibitors.
Expanding the repertoire of small molecule transcriptional activation domains.
Syntheses and biological evaluations of carbosilane dendrimers uniformly functionalized with sialyl alpha(2-->3) lactose moieties as inhibitors for human influenza viruses.
Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides.
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
N-Benzyl-1-heteroaryl-3-(trifluoromethyl)-1H-pyrazole-5-carboxamides as inhibitors of co-activator associated arginine methyltransferase 1 (CARM1).
A series of bisaryl imidazolidin-2-ones has shown to be selective and orally active 5-HT2C receptor antagonists.
Inhibitory activity of cyclohexenyl chalcone derivatives and flavonoids of fingerroot, Boesenbergia rotunda (L.), towards dengue-2 virus NS3 protease.
A rapid synthesis of lavendustin-mimetic small molecules by click fragment assembly.
The effect of the pyridyl nitrogen position in pyridylpiperazine sigma ligands.
Synthesis and molluscicidal activity of some new thiophene, thiadiazole and pyrazole derivatives.
Optimization of alpha-ketoamide based p38 inhibitors through modifications to the region that binds to the allosteric site.
Racemic and chiral sulfoxides as potential prodrugs of the COX-2 inhibitors Vioxx and Arcoxia.
The discovery and initial optimisation of pyrrole-2-carboxamides as inhibitors of p38alpha MAP kinase.
Design and synthesis of disubstituted (4-piperidinyl)-piperazine derivatives as potent acetyl-CoA carboxylase inhibitors.
Phenanthrenes from Dendrobium nobile and their inhibition of the LPS-induced production of nitric oxide in macrophage RAW 264.7 cells.
Synthesis and evaluation of novel 1-(2-acylhydrazinocarbonyl)-cycloalkyl carboxamides as interleukin-1beta converting enzyme (ICE) inhibitors.
Carbonic anhydrase activators: L-Adrenaline plugs the active site entrance of isozyme II, activating better isoforms I, IV, VA, VII, and XIV.
Non-basic ligands for aminergic GPCRs: the discovery and development diaryl sulfones as selective, orally bioavailable 5-HT2A receptor antagonists for the treatment of sleep disorders.
Phenylcyclohexene and phenylcyclohexadiene substituted compounds having retinoid antagonist activity.
Novel pyridine derivatives as potent and selective CB2 cannabinoid receptor agonists.
Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
Synthesis and optimization of 2-pyridin-3-yl-benzo[d][1,3]oxazin-4-one based inhibitors of human neutrophil elastase.
Synthesis and SAR studies of 1,4-diazabicyclo[3.2.2]nonane phenyl carbamates--subtype selective, high affinity alpha7 nicotinic acetylcholine receptor agonists.
A novel class of H3 antagonists derived from the natural product guided synthesis of unnatural analogs of the marine bromopyrrole alkaloid dispyrin.
1-[4-(N-Benzylamino)phenyl]-3-phenylurea derivatives as a new class of hypoxia-inducible factor-1alpha inhibitors.
Synthesis and evaluation of arylalkoxy- and biarylalkoxy-phenylamide and phenylimidazoles as potent and selective sphingosine-1-phosphate receptor subtype-1 agonists.
New quinoline NK3 receptor antagonists with CNS activity.
Quinazolines as potent and highly selective PDE5 inhibitors as potential therapeutics for male erectile dysfunction.
Discovery of novel sphingosine kinase-1 inhibitors. Part 2.
Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.
Synthesis and evaluation of beta-carboline derivatives as inhibitors of human immunodeficiency virus.
Discovery of highly selective inhibitors of human fatty acid binding protein 4 (FABP4) by virtual screening.
Identification of potent and selective VEGFR receptor tyrosine kinase inhibitors having new amide isostere headgroups.
Remote functionalization of SCH 39166: discovery of potent and selective benzazepine dopamine D1 receptor antagonists.
Leukotriene B4 photoaffinity probes: design, synthesis and evaluation of new arylazide-1,3-disubstituted cyclohexanes.
(E) -6-(1-alkyloxyiminoalkyl)-5,8-dimethoxy-1,4-naphthoquinones: synthesis, cytotoxic activity and antitumor activity.
Synthesis, DNA-binding ability and evaluation of antitumour activity of triazolo[1,2,4]benzothiadiazine linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates.
Microwave-assisted solid phase synthesis, PEGylation, and biological activity studies of glucagon-like peptide-1(7-36) amide.
Aph(3')-IIc, an aminoglycoside resistance determinant from Stenotrophomonas maltophilia.
Semi-synthetic analogues of thiostrepton delimit the critical nature of tail region modifications in the control of protein biosynthesis and antibacterial activity.
Nanomolar affinity, iminosugar-based chemical probes for specific labeling of lysosomal glucocerebrosidase.
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
New N-(phenoxydecyl)phthalimide derivatives displaying potent inhibition activity towards alpha-glucosidase.
Inhibition of monoamine oxidase B by N-methyl-2-phenylmaleimides.
Synthesis and biological evaluation of asymmetric gramicidin S analogues containing modified D-phenylalanine residues.
Synthesis and biological evaluation of flavan-3-ol derivatives as positive modulators of GABAA receptors.
Apoptotic activities in closely related styryllactone stereoisomers toward human tumor cell lines: Investigation of synergism of styryllactone-induced apoptosis with TRAIL.
Stereoselective synthesis of beta-1-C-substituted 1,4-dideoxy-1,4-imino-D-galactitols and evaluation as UDP-galactopyranose mutase inhibitors.
Investigations on the 2-thiazolylhydrazyne scaffold: synthesis and molecular modeling of selective human monoamine oxidase inhibitors.
Structure-based virtual screening approach to the discovery of novel inhibitors of factor-inhibiting HIF-1: identification of new chelating groups for the active-site ferrous ion.
Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor.
Active core structure of terfestatin A, a new specific inhibitor of auxin signaling.
Syntheses and biological evaluation of topoisomerase I-targeting agents related to 11-[2-(N,N-dimethylamino)ethyl]-2,3-dimethoxy-8,9-methylenedioxy-11H-isoquino[4,3-c]cinnolin-12-one (ARC-31).
Design, synthesis, and biological evaluation of novel quinoline derivatives as HIV-1 Tat-TAR interaction inhibitors.
Synthesis of triazole-linked beta-C-glycosyl dimers as inhibitors of PTP1B.
Optimizing the enzymatic synthesis of beta-D-galactopyranosyl-D-xyloses for their use in the evaluation of lactase activity in vivo.
Thiocarbamates as non-nucleoside HIV-1 reverse transcriptase inhibitors. Part 2: Parallel synthesis, molecular modelling and structure-activity relationship studies on analogues of O-(2-phenylethyl)-N-phenylthiocarbamate.
RCAI-8, 9, 18, 19, and 49-52, conformationally restricted analogues of KRN7000 with an azetidine or a pyrrolidine ring: Their synthesis and bioactivity for mouse natural killer T cells to produce cytokines.
Monoquaternary pyridinium salts with modified side chain-synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase.
Studies on quinones. Part 43: Synthesis and cytotoxic evaluation of polyoxyethylene-containing 1,4-naphthoquinones.
Structure-activity relationship of uniconazole, a potent inhibitor of ABA 8'-hydroxylase, with a focus on hydrophilic functional groups and conformation.
Synthesis and structure-activity relationship studies of theophylline analogs on population responses in the rat hippocampus in vitro.
Design, synthesis, and biological evaluation of Mannich bases of heterocyclic chalcone analogs as cytotoxic agents.
Design and synthesis of a siderophore conjugate as a potent PSMA inhibitor and potential diagnostic agent for prostate cancer.
New estrogenic compounds isolated from Broussonetia kazinoki.
Design, synthesis, and biological activity of bicyclic radester analogues as Hsp90 inhibitors.
Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: discovery of highly potent and selective analogs with improved human microsomal stability.
Morroniside cinnamic acid conjugate as an anti-inflammatory agent.
Design, synthesis, and structure-activity relationship study of conformationally constrained analogs of indole-3-carboxamides as novel CB1 cannabinoid receptor agonists.
2' biaryl amides as novel and subtype selective M1 agonists. Part I: Identification, synthesis, and initial SAR.
Discovery of aminopyridines substituted with benzoxazole as orally active c-Met kinase inhibitors.
Sulfonamido, azidosulfonyl and N-acetylsulfonamido analogues of rofecoxib: 4-[4-(N-acetylsulfonamido)phenyl]-3-(4-methanesulfonylphenyl)-2(5H)furanone is a potent and selective cyclooxygenase-2 inhibitor.
Synthesis of new thiophene and benzo[b]thiophene hydrazide derivatives as human NPY Y(5) antagonists.
Water-soluble PDE4 inhibitors for the treatment of dry eye.
Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds.
Synthesis and evaluation of pyrazolidine derivatives as dipeptidyl peptidase IV (DP-IV) inhibitors.
QSAR studies on 1,2-dithiole-3-thiones: modeling of lipophilicity, quinone reductase specific activity, and production of growth hormone.
1,4-Diazepane-2,5-diones as novel inhibitors of LFA-1.
Synthesis and structure-activity relationships of isoxazole carboxamides as growth hormone secretagogue receptor antagonists.
Synthesis and biological evaluation of fenobam analogs as mGlu5 receptor antagonists.
Fluorescence resonance energy transfer in a novel cyclodextrin-peptide conjugate for detecting steroid molecules.
Synthesis of N-aryl-3-(indol-3-yl)propanamides and their immunosuppressive activities.
Cyclin-dependent kinase 4 inhibitors as a treatment for cancer. Part 1: identification and optimisation of substituted 4,6-bis anilino pyrimidines.
Synthesis and evaluation of methyl ether derivatives of the vancomycin, teicoplanin, and ristocetin aglycon methyl esters.
Contribution of BlaA and BlaB beta-lactamases to antibiotic susceptibility of Yersinia enterocolitica biovar 1B.
In vitro antiviral activity of V-073 against polioviruses.
Comparison of tigecycline and vancomycin for treatment of experimental foreign-body infection due to methicillin-resistant Staphylococcus aureus.
Efficacy of iclaprim against wild-type and thymidine kinase-deficient methicillin-resistant Staphylococcus aureus isolates in an in vitro fibrin clot model.
Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients.
Mitochondrial DNA depletion in rat liver induced by fosalvudine tidoxil, a novel nucleoside reverse transcriptase inhibitor prodrug.
Inhaled voriconazole for prevention of invasive pulmonary aspergillosis.
Complete nucleotide sequence of Klebsiella pneumoniae multidrug resistance plasmid pKP048, carrying blaKPC-2, blaDHA-1, qnrB4, and armA.
Antimicrobial susceptibility and mutations involved in clarithromycin resistance in Helicobacter pylori isolates from patients in the western central region of Colombia.
Molecular mechanisms of macrolide resistance in clinical isolates of Mycoplasma pneumoniae from China.
Novel variants of the qnrB gene, qnrB22 and qnrB23, in Citrobacter werkmanii and Citrobacter freundii.
First report of KPC-2-producing Klebsiella pneumoniae strains in Brazil.
Safety and outcomes of open-label deferasirox iron chelation therapy for mucormycosis.
Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
Identification of triazinoindol-benzimidazolones as nanomolar inhibitors of the Mycobacterium tuberculosis enzyme TDP-6-deoxy-d-xylo-4-hexopyranosid-4-ulose 3,5-epimerase (RmlC).
Synthesis of tetraglucosyl- and tetrapolyamine-tetrabenzoporphyrin conjugates for an application in PDT.
Benzyl 1,2,3,5,11,11a-hexahydro-3,3-dimethyl-1-oxo-6H-imidazo[3',4':1,2]pyridin[3,4-b]indole-2-substituted acetates: One-pot-preparation, anti-tumor activity, docking toward DNA and 3D QSAR analysis.
Phosphate ester derivatives of homocamptothecin: synthesis, solution stabilities and antitumor activities.
Alpneumines A-H, new anti-melanogenic indole alkaloids from Alstonia pneumatophora.
Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase.
Improved P2 phenylglycine-based hepatitis C virus NS3 protease inhibitors with alkenylic prime-side substituents.
Synthesis and CYP24A1 inhibitory activity of N-(2-(1H-imidazol-1-yl)-2-phenylethyl)arylamides.
Synthesis, molecular modeling, and biological evaluation of cinnamic acid metronidazole ester derivatives as novel anticancer agents.
Antineoplastic agents 582. Part 1: Isolation and structure of a cyclobutane-type sesquiterpene cancer cell growth inhibitor from Coprinus cinereus (Coprinaceae).
Novel semisynthetic derivatives of betulin and betulinic acid with cytotoxic activity.
Inhibitory effect of novel tetrahydropyrimidine-2(1H)-thiones on melanogenesis.
Synthesis and biological properties of iron chelators based on a bis-2-(2-hydroxy-phenyl)-thiazole-4-carboxamide or -thiocarboxamide (BHPTC) scaffold.
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Structure-activity relationship studies on quorum sensing ComX(RO-E-2) pheromone.
Antiviral activity of berberine and related compounds against human cytomegalovirus.
Microwave-assisted [6+4]-cycloaddition of fulvenes and alpha-pyrones to azulene-indoles: facile syntheses of novel antineoplastic agents.
Human beta3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides.
alpha-Ketocarboxylic acid-based inhibitors of protein tyrosine phosphatases.
Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz.
Selectivity of inhibition of matrix metalloproteases MMP-3 and MMP-2 by succinyl hydroxamates and their carboxylic acid analogues is dependent on P3' group chirality.
Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells.
A series of quinoline analogues as potent inhibitors of C. albicans prolyl tRNA synthetase.
Discovery and SAR of 2-amino-5-[(thiomethyl)aryl]thiazoles as potent and selective Itk inhibitors.
Design and synthesis of 2,3,4,9-tetrahydro-1H-carbazole and 1,2,3,4-tetrahydro-cyclopenta[b]indole derivatives as non-nucleoside inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase.
Designing rapid onset selective serotonin re-uptake inhibitors. Part 1: Structure-activity relationships of substituted (1S,4S)-4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydro-1-naphthaleneamine.
Synthesis and evaluation of 3D templates based on a taxane skeleton to circumvent P-glycoprotein-associated multidrug resistance of cancer.
Uric acid may inhibit glucose-induced insulin secretion via binding to an essential arginine residue in rat pancreatic beta-cells.
2,3-Diarylthiophenes as selective EP1 receptor antagonists.
Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.
Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
Isoindolinone ureas: a novel class of KDR kinase inhibitors.
7-Methoxybenzofuran-4-carboxamides as PDE 4 inhibitors: a potential treatment for asthma.
N-hydroxyformamide peptidomimetics as TACE/matrix metalloprotease inhibitors: oral activity via P1' isobutyl substitution.
5-HT(3)R binding of lerisetron: an interdisciplinary approach to drug-Receptor interactions.
Antitumor agents. Part 212. Bucidarasins A-C, three new cytotoxic clerodane diterpenes from Bucida buceras.
Discovery of zoniporide: a potent and selective sodium-hydrogen exchanger type 1 (NHE-1) inhibitor with high aqueous solubility.
Synthesis of phenylglycine derivatives as potent and selective antagonists of group III metabotropic glutamate receptors.
Synthesis and antiproliferative evaluation of 7-aminosubstituted pyrroloiminoquinone derivatives.
Biologically active oligodeoxyribonucleotides. Part 12: N2-methylation of 2'-deoxyguanosines enhances stability of parallel G-quadruplex and anti-HIV-1 activity.
Preparation, characterization, molecular modeling and in vitro activity of paclitaxel-cyclodextrin complexes.
Increase of the adenallene anti-HIV activity in cell culture using its bis(tBuSATE) phosphotriester derivative.
Asymmetric synthesis and antitumor activity of cycloalkanin.
Combined NK1 and NK2 tachykinin receptor antagonists: synthesis and structure-activity relationships of novel oxazolidine analogues.
Design and synthesis of bio-isosteres of thymidine triphosphate.
Diastereoselective synthesis of octahydro-14H-benzo[g]quinolino-[2,3-a]quinolidines. Improved cytotoxic activity against human brain tumor cell lines as a result of the increased rigidity of the molecular backbone.
New acetylene based histamine H3 receptor antagonists derived from the marine natural product verongamine.
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994.
Importance of the C28-C38 hydrophobic domain of okadaic acid for potent inhibition of protein serine-threonine phosphatases 1 and 2A.
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.
Substituted quinolines induce inhibition of proliferation of HTLV-1 infected cells.
Bis(acridinylthiourea)platinum(II) complexes: synthesis, DNA affinity, and biological activity in glioblastoma cells.
Cell permeation of a Trypanosoma brucei aldolase inhibitor: evaluation of different enzyme-labile phosphate protecting groups.
Inhibitors of VEGF receptors-1 and -2 based on the 2-((pyridin-4-yl)ethyl)pyridine template.
Modification of the clozapine structure by parallel synthesis.
N-Tetrahydroquinolinyl, N-quinolinyl and N-isoquinolinyl biaryl carboxamides as antagonists of TRPV1.
PTP-1B inhibitors: cyclopenta[d][1,2]-oxazine derivatives.
Synthesis of constrained ceramide analogs and their potent antileukemic activities.
Semisynthesis of C-ring modified triptolide analogues and their cytotoxic activities.
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Design and synthesis of substituted phenylpropanoic acid derivatives as human peroxisome proliferator-activated receptor alpha/delta dual agonists.
Synthesis and anthelmintic properties of arylquinolines with activity against drug-resistant nematodes.
Synthesis of 2-[3-(7-Chloro-quinolin-4-ylamino)-alkyl]-1-(substituted phenyl)-2,3,4,9-tetrahydro-1H-beta-carbolines as a new class of antimalarial agents.
Characterization of the two major CYP450 metabolites of ozonide (1,2,4-trioxolane) OZ277.
Separate synthesis and evaluation of glucitol bis-phosphate and mannitol bis-phosphate, as competitive inhibitors of fructose bis-phosphate aldolases.
Synthesis and antioxidant activities of 3,5-dialkoxy-4-hydroxycinnamamides.
Design and characterization of mechanism-based inhibitors for the tyrosine aminomutase SgTAM.
Synthesis and structure-activity relationship of 4-(2-aryl-cyclopropylamino)-quinoline-3-carbonitriles as EGFR tyrosine kinase inhibitors.
Convenient synthesis of indeno[1,2-c]isoquinolines as constrained forms of 3-arylisoquinolines and docking study of a topoisomerase I inhibitor into DNA-topoisomerase I complex.
Synthesis of hybrid acetogenins, alpha,beta-unsaturated-gamma-lactone-free nitrogen-containing heterocyclic analogues, and their cytotoxicity against human cancer cell lines.
Structure-based design of a new class of highly selective aminoimidazo[1,2-a]pyridine-based inhibitors of cyclin dependent kinases.
Synthesis of 4-(5-[18F]fluoromethyl-3-phenylisoxazol-4-yl)benzenesulfonamide, a new [18F]fluorinated analogue of valdecoxib, as a potential radiotracer for imaging cyclooxygenase-2 with positron emission tomography.
4-(2-Pyridyl)piperazine-1-benzimidazoles as potent TRPV1 antagonists.
3-(1,2,3-Triazol-1-yl)-1-thio-galactosides as small, efficient, and hydrolytically stable inhibitors of galectin-3.
6-Aryl-4-methylsulfanyl-2H-pyran-2-one-3-carbonitriles as PPAR-gamma activators.
Examining the correlations between GSK-3 inhibitory properties and anti-convulsant efficacy of valproate and valproate-related compounds.
A short, stereoselective, and common approach for the synthesis of 4,5-disubstituted delta-lactones simplactone B and its C-5 analogue.
A general carbometalation, three component coupling strategy for the synthesis of alpha,beta-unsaturated gamma-sultines including thio-rofecoxib, a selective COX-2 inhibitor.
HCV NS5B polymerase-bound conformation of a soluble sulfonamide inhibitor by 2D transferred NOESY.
Design, synthesis, and evaluation of estradiol-linked genotoxicants as anti-cancer agents.
Synthesis and biological evaluation of 3-benzyl-1-methyl- and 1-methyl-3-phenyl-isothioureas as potential inhibitors of iNOS.
Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.
Novel design principle validated: glucopyranosylidene-spiro-oxathiazole as new nanomolar inhibitor of glycogen phosphorylase, potential antidiabetic agent.
Tricyclic azepine derivatives as selective brain penetrant 5-HT6 receptor antagonists.
SAR development of polycyclic guanine derivatives targeted to the discovery of a selective PDE5 inhibitor for treatment of erectile dysfunction.
Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives.
Gastric cytoprotective activity of ilicic aldehyde: structure-activity relationships.
New potential antibacterials: a synthetic route to N-aryloxazolidinone/3-aryltetrahydroisoquinoline hybrids.
Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Reversal of anticancer drug resistance by COTC based on intracellular glutathione and glyoxalase I.
Tryptamine-based human beta3-adrenergic receptor agonists. Part 3: improved oral bioavailability via modification of the sulfonamide moiety.
Substituted benzylamino-6-(trifluoromethyl)pyrimidin-4(1H)-ones: a novel class of selective human A-FABP inhibitors.
Two new irreversible inhibitors of dihydrodipicolinate synthase: diethyl (E,E)-4-oxo-2,5-heptadienedioate and diethyl (E)-4-oxo-2-heptenedioate.
Synthesis and pharmacological evaluation of piperidinoalkanoyl-1,2,3,4-tetrahydroisoquinoline derivatives as novel specific bradycardic agents.
Identification and optimization of novel partial agonists of neuromedin B receptor using parallel synthesis.
Discovering selective agonists of endothelial target for acetylcholine (ETA) via diversity-guided pharmacophore simplification and simulation.
(+/-)-cis-(6-Ethyl-tetrahydropyran-2-yl)-formic acid: a novel substance with antinociceptive properties.
Fluorescence-labeled sphingosines as substrates of sphingosine kinases 1 and 2.
Design and synthesis of novel Cdc25A-inhibitors having phosphate group as a hydrophilic residue.
Identification of a potent and stable antiproliferative agent by the prodrug formation of a thiolate histone deacetylase inhibitor.
Inhibition of the mitochondrial F1F0-ATPase by ligands of the peripheral benzodiazepine receptor.
Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors.
The stability of pseudopeptides bearing sulfoximines as chiral backbone modifying element towards proteinase K.
Design of quinolinedione-based geldanamycin analogues.
Synthesis and SAR evaluation of oxadiazolopyrazines as selective Haemophilus influenzae antibacterial agents.
Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor.
Targeting thrombin and factor VIIa: design, synthesis, and inhibitory activity of functionally relevant indolizidinones.
Novel bicyclic oxazolone derivatives as anti-angiogenic agents.
4-Aryl/cycloalkyl-5-phenyloxazole derivatives as selective COX-2 inhibitors.
The design and synthesis of a novel series of indole derived selective ET(A) antagonists.
Synthesis and structure-activity relationships of aminoalkylazetidines as ORL1 receptor ligands.
Synthesis and structure--activity relationship of novel aminotetralin derivatives with high micro selective opioid affinity.
Synthesis and biological activity of n-butylphthalide derivatives.
Novel lopinavir analogues incorporating non-Aromatic P-1 side chains--synthesis and structure--activity relationships.
Synthesis and evaluation of 5-HT(2A) and 5-HT(2C) receptor binding affinities of novel pyrimidine derivatives.
Antifungal Sordarins. Part 4: synthesis and structure--activity relationships of 3',4'-fused alkyl-tetrahydrofuran derivatives.
Focused library approach for identification of new N-acylphenylalanines as VCAM/VLA-4 antagonists.
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 1: P(4) and side-chain modifications for improved in vitro potency.
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P(1) structure-activity relationships of the substituted 1-(2-Naphthyl)-1H-pyrazole-5-carboxylamides.
QSAR study of heparanase inhibitors activity using artificial neural networks and Levenberg-Marquardt algorithm.
Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.
Synthesis and antibacterial activity of novel 7-(3-substituted-3 or 4-trifluoromethyl-1-pyrrolidinyl)-8-methoxyfluoroquinolones.
Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.
The synthesis and evaluation of benzannelated-azatoxins: the benzazatoxins.
Synthesis and biochemical evaluation of guanidino-alkyl-ribitol derivatives as nucleoside hydrolase inhibitors.
Synthesis and biological evaluation of 4-alkylamino-6-(2-hydroxyethyl)-2-methylthiopyrimidines as new rubella virus inhibitors.
3,4-Dihydroquinazoline derivatives as novel selective T-type Ca2+ channel blockers.
Novel thrombin inhibitors incorporating weakly basic heterobicyclic P1-arginine mimetics: optimization via modification of P1 and P3 moieties.
Phosphonic acid analogs of GABA through reductive dealkylation of phosphonic diesters with lithium trialkylborohydrides.
Antitubercular agents. Part 2: new thiolactomycin analogues active against Mycobacterium tuberculosis.
Enzyme cleavable and biotinylated photoaffinity ligand with diazirine.
Synthesis and histone deacetylase inhibitory activity of cyclic tetrapeptides containing a retrohydroxamate as zinc ligand.
Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.
Synthesis and evaluation of 4-triazolylflavans as new aromatase inhibitors.
Synthesis and biological activity of novel antibacterial quinazolines.
1,2-Benzothiazine 1,1-dioxide alpha-ketoamide analogues as potent calpain I inhibitors.
Cytochrome P450/NADPH-dependent formation of trans epoxides from trans-arachidonic acids.
Design, synthesis, and SAR of anthranilamide-based factor Xa inhibitors with improved functional activity.
Synthesis and in vitro activity of novel isoxazolyl tetrahydropyridinyl oxazolidinone antibacterial agents.
Synthesis and antioxidant efficiency of a new amphiphilic spin-trap derived from PBN and lipoic acid.
Hypocholesterolemic activity of hesperetin derivatives.
Total synthesis of (R,R,R)- and (S,S,S)-schweinfurthin F: differences of bioactivity in the enantiomeric series.
Synthesis and activity of Combretastatin A-4 analogues: 1,2,3-thiadiazoles as potent antitumor agents.
Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.
Newer tetracycline derivatives: synthesis, anti-HIV, antimycobacterial activities and inhibition of HIV-1 integrase.
Synthesis and antimalarial evaluation of a series of piperazinyl flavones.
Studies towards the conception of new selective PPARbeta/delta ligands.
13C bis-labeled pyrroles: a tool for the identification of the rat metabolism of 3-methyl pyrrole-2,4-dicarboxylic acid 2-propyl ester 4-(1,2,2-trimethyl-propyl) ester.
Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.
Benzyl ether structure-activity relationships in a series of ketopiperazine-based renin inhibitors.
Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP.
1-Amino-1,2,3,4-tetrahydronaphthalene-2-carboxylic acid as a Tic mimetic: application in the synthesis of potent human melanocortin-4 receptor selective agonists.
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.
(2R)-2-methylchromane-2-carboxylic acids: discovery of selective PPARalpha agonists as hypolipidemic agents.
Semi-synthesis and biological evaluation of analogues of UK-2A, a novel antifungal antibiotic from Streptomyces sp. 517-02.
Synthesis of Pseudomonas quorum-sensing autoinducer analogs and structural entities required for induction of apoptosis in macrophages.
Analysis of anti-PDE3 activity of 2-morpholinochromone derivatives reveals multiple mechanisms of anti-platelet activity.
Design and synthesis of 4-phenyl piperidine compounds targeting the mu receptor.
Sialyl Lewis(x) analogs based on a quinic acid scaffold as the fucose mimic.
Synthesis and evaluation of novel pseudomycin side-chain analogues. Part 3.
An unhydrolyzable analogue of N-(4-hydroxyphenyl)retinamide. synthesis and preliminary biological studies.
Conformationally restricted homotryptamines. Part 4: Heterocyclic and naphthyl analogs of a potent selective serotonin reuptake inhibitor.
Discovery of (-)-6-[2-[4-(3-fluorophenyl)-4-hydroxy-1-piperidinyl]-1-hydroxyethyl]-3,4-dihydro-2(1H)-quinolinone--a potent NR2B-selective N-methyl D-aspartate (NMDA) antagonist for the treatment of pain.
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.
3-(Arylsulfonyl)-1-(azacyclyl)-1H-indoles are 5-HT(6) receptor modulators.
Synthesis and pharmacological characterization of constrained analogues of Vestipitant as in vitro potent and orally active NK(1) receptor antagonists.
Identification of a novel 3,5-disubstituted pyridine as a potent, selective, and orally active inhibitor of Akt1 kinase.
Antibacterial activity of (-)-deoxypseudophrynaminol versus its racemate and derivatives.
Synthesis of fluorescent derivatives of wortmannin and demethoxyviridin as probes for phosphatidylinositol 3-kinase.
Synthesis and antibacterial activities of chiral 1,3-oxazinan-2-one derivatives.
Isolation, synthesis, and anti-tumor activities of a novel class of podocarpic diterpenes.
Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists.
Synthesis and evaluation of 2-anilino-3-phenylsulfonyl-6-methylpyridines as corticotropin-releasing factor1 receptor ligands.
Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE).
Inhibitors of the serotonin transporter protein (SERT): the design and synthesis of biotinylated derivatives of 3-(1,2,3,6-tetrahydro-pyridin-4-yl)-1H-indoles. High-affinity serotonergic ligands for conjugation with quantum dots.
Synthesis, structure-activity relationships, and anxiolytic activity of 7-aryl-6,7-dihydroimidazoimidazole corticotropin-releasing factor 1 receptor antagonists.
Functionalized head-to-head hairpin polyamides: synthesis, double-stranded DNA-binding activity and affinity.
1-((S)-gamma-substituted prolyl)-(S)-2-cyanopyrrolidine as a novel series of highly potent DPP-IV inhibitors.
Antimitotic activity and reversal of breast cancer resistance protein-mediated drug resistance by stilbenoids from Bletilla striata.
Synthesis of new N-(2-(trifluoromethyl)pyridin-4-yl)anthranilic acid derivatives and their evaluation as anticancer agents.
One-pot synthesis of 5-phenylimino, 5-thieno or 5-oxo-1,2,3-dithiazoles and evaluation of their antimicrobial and antitumor activity.
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
New highly selective inhibitors of class II fructose-1,6-bisphosphate aldolases.
Potent transglutaminase inhibitors, aryl beta-aminoethyl ketones.
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.
Synthesis and anticancer activity of novel 3,4-diarylthiazol-2(3H)-ones (imines).
Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Pyrrole[2,3-d]azepino compounds as agonists of the farnesoid X receptor (FXR).
Design, synthesis and evaluation of aspirin analogues having an additional carboxylate substituent for antithrombotic activity.
Synthesis, antitumor evaluation and DNA photocleaving activity of novel methylthiazonaphthalimides with aminoalkyl side chains.
Synthesis and structure-activity relationship of 3-phenyl-3H-quinazolin-4-one derivatives as CXCR3 chemokine receptor antagonists.
Synthesis, in vivo and in vitro biological activity of novel azaline B analogs.
Aglycon specificity profiling of alpha-glucosidases using synthetic probes.
N-(4-Fluorobenzyl)-3-hydroxy-9,9-dimethyl-4-oxo-6,7,8,9-tetrahydro-4H-pyrazino[1,2-a]pyrimidine-2-carboxamides a novel class of potent HIV-1 integrase inhibitors.
Synthesis and evaluation of cis-3,4-disubstituted piperidines as potent CC chemokine receptor 2 (CCR2) antagonists.
First synthesis of alpha-aminoalkyl-(N-substituted)thiocarbamoyl-phosphinates: inhibitors of aminopeptidase N (APN/CD13) with the new zinc-binding group.
Fungicidal activity of truncated analogues of dihydrosphingosine.
Synthesis of barbiturate-based methionine aminopeptidase-1 inhibitors.
Lead identification of 2-iminobenzimidazole antagonists of the chemokine receptor CXCR3.
Chemical resolution of +/- -calanolide A, +/- -cordatolide A and their 11-demethyl analogues.
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 1. Design, synthesis, and lead identification.
beta-N-Biaryl ether sulfonamide hydroxamates as potent gelatinase inhibitors: part 2. Optimization of alpha-amino substituents.
Synthesis and SAR of alpha-sulfonylcarboxylic acids as potent matrix metalloproteinase inhibitors.
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Synthesis of benz[d]indeno[1,2-b]pyran-5,11-diones: versatile intermediates for the design and synthesis of topoisomerase I inhibitors.
Beta-diketo acids with purine nucleobase scaffolds: novel, selective inhibitors of the strand transfer step of HIV integrase.
Development of mitochondria-targeted derivatives of resveratrol.
Itk kinase inhibitors: initial efforts to improve the metabolical stability and the cell activity of the benzimidazole lead.
Red light-activated phosphorothioate oligodeoxyribonucleotides.
Derivatives of (3S)-N-(biphenyl-2-ylmethyl)pyrrolidin-3-amine as selective noradrenaline reuptake inhibitors: Reducing P-gp mediated efflux by modulation of H-bond acceptor capacity.
Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold.
Synthesis and pharmacological evaluation of Tic-hydantoin derivatives as selective sigma1 ligands. Part 1.
In vitro and in vivo evaluation of O-alkyl derivatives of tramadol.
Synthesis and antitumor activity of cyclodepsipeptide zygosporamide and its analogues.
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 2.
Click chemistry based rapid one-pot synthesis and evaluation for protease inhibition of new tetracyclic triazole fused benzodiazepine derivatives.
N-[(3S)-Pyrrolidin-3-yl]benzamides as novel dual serotonin and noradrenaline reuptake inhibitors: impact of small structural modifications on P-gp recognition and CNS penetration.
Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists.
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
Design, synthesis and cytotoxicity of 7-deoxy aryl discodermolide analogues.
N,N-Diethyl-4-[(3-hydroxyphenyl)(piperidin-4-yl)amino] benzamide derivatives: the development of diaryl amino piperidines as potent delta opioid receptor agonists with in vivo anti-nociceptive activity in rodent models.
N1-Alkyl pyrimidinediones as non-nucleoside inhibitors of HIV-1 reverse transcriptase.
Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation.
Design, synthesis and evaluation of carbamate-modified (-)-N(1)-phenethylnorphysostigmine derivatives as selective butyrylcholinesterase inhibitors.
Benzo[d]imidazole inhibitors of Coactivator Associated Arginine Methyltransferase 1 (CARM1)--Hit to Lead studies.
In vitro and in vivo anti-Leishmania activity of polysubstituted synthetic chalcones.
Synthesis and evaluation of 2-amino-dihydrotetrabenzine derivatives as probes for imaging vesicular monoamine transporter-2.
Cellular localization and allele-selective inhibition of mutant huntingtin protein by peptide nucleic acid oligomers containing the fluorescent nucleobase [bis-o-(aminoethoxy)phenyl]pyrrolocytosine.
Synthesis and binding affinity of potential atypical antipsychotics with the tetrahydroquinazolinone motif.
Design and synthesis of novel nitrogen-containing polyhydroxylated aromatics as HIV-1 integrase inhibitors from caffeic acid phenethyl ester.
Identification of a novel 1'-[5-((3,5-dichlorobenzoyl)methylamino)-3-(3,4-dichlorophenyl)-4-(methoxyimino)pentyl]-2-oxo-(1,4'-bipiperidine) as a dual NK(1)/NK(2) antagonist.
Synthesis and evaluation of the sunflower derived trypsin inhibitor as a potent inhibitor of the type II transmembrane serine protease, matriptase.
Tight binding ligand approach to oligosaccharide-grafted protein.
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.
Synthesis of novel fluorescent probes for the molecular chaperone Hsp90.
Synthesis and DNA-binding affinity of A-C8/C-C2 alkoxyamido-linked pyrrolo[2,1-c][1,4]benzodiazepine dimers.
Synthesis and evaluation of aminophosphinic acid derivatives as inhibitors of renal dipeptidase.
Synthesis and biological evaluation of novel, selective, nonsteroidal glucocorticoid receptor antagonists.
Discovery of orally active prostaglandin D2 receptor antagonists.
3,4-Dihydronaphthalen-1(2H)-ones: novel ligands for the benzodiazepine site of alpha5-containing GABAA receptors.
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists.
De novo synthesis of two new cytotoxic tiazofurin analogues with modified sugar moieties.
Discovery of a potent, selective and orally active canine COX-2 inhibitor, 2-(3-difluoromethyl-5-phenyl-pyrazol-1-yl)-5-methanesulfonyl-pyridine.
Butyl 2-(4-[1.1'-biphenyl]-4-yl-1H-imidazol-2-yl)ethylcarbamate, a potent sodium channel blocker for the treatment of neuropathic pain.
3-Methoxycarbonyl-5-nitrophenyl boronic acid: high affinity diol recognition at neutral pH.
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors.
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.
The discovery of small molecule carbamates as potent dual alpha(4)beta(1)/alpha(4)beta(7) integrin antagonists.
Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors.
Structure-activity relationship study of 9-aminoacridine compounds in scrapie-infected neuroblastoma cells.
Synthesis of 2-amino-4-(7-azaindol-3-yl)pyrimidines as cyclin dependent kinase 1 (CDK1) inhibitors.
Critical modifications of the ISO-1 scaffold improve its potent inhibition of macrophage migration inhibitory factor (MIF) tautomerase activity.
A highly selective kappa-opioid receptor agonist with low addictive potential and dependence liability.
Design, synthesis and biological evaluations of novel oxindoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. Part I.
Synthesis and SAR of heteroaryl-phenyl-substituted pyrazole derivatives as highly selective and potent canine COX-2 inhibitors.
N-thiolated 2-oxazolidinones: a new family of antibacterial agents for methicillin-resistant Staphylococcus aureus and Bacillus anthracis.
Pyridoxine as a template for the design of antiplatelet agents.
Identification of a potent and rapidly reversible inhibitor of the 20S-proteasome.
Synthesis and biological activity of new 5-O-sugar modified ketolide and 2-fluoro-ketolide antibiotics.
Synthesis and anticonvulsant activity of new 2-substituted-5- [2-(2-fluorophenoxy)phenyl]-1,3,4-oxadiazoles and 1,2,4-triazoles.
Synthesis of aromatic compounds containing a 1,1-dialkyl-2-trifluoromethyl group, a bioisostere of the tert-alkyl moiety.
Pyrrolidines as potent functional agonists of the human melanocortin-4 receptor.
1-(2-Phenoxyphenyl)methanamines: SAR for dual serotonin/noradrenaline reuptake inhibition, metabolic stability and hERG affinity.
Application of multicomponent reactions to antimalarial drug discovery. Part 3: discovery of aminoxazole 4-aminoquinolines with potent antiplasmodial activity in vitro.
Design, synthesis, and biological evaluation of tricyclic heterocycle-tetraamine conjugates as potent NMDA channel blockers.
Substituted 2-pyrrolinone inhibitors of HIV-1 integrase.
Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists.
Synthesis and biological evaluation of 3-aminopyrrolidine derivatives as CC chemokine receptor 2 antagonists.
Benzopyrans as selective estrogen receptor beta agonists (SERBAs). Part 3: synthesis of cyclopentanone and cyclohexanone intermediates for C-ring modification.
7-Phenylplatensimycin and 11-methyl-7-phenylplatensimycin: more potent analogs of platensimycin.
Inhibitors of hepatitis C virus NS3.4A protease. Effect of P4 capping groups on inhibitory potency and pharmacokinetics.
A cell-based assay that targets methionine aminopeptidase in a physiologically relevant environment.
Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs.
Discovery of cyclicsulfonamide derivatives as 11 beta-hydroxysteroid dehydrogenase 1 inhibitors.
Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.
Synthesis of a novel peptidic photoaffinity probe for the PTP-1B enzyme.
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.
Triterpene based compounds with potent anti-maturation activity against HIV-1.
Epimerisation of lutein to 3'-epilutein in processed foods.
A highly toxic morphine-3-glucuronide derivative.
Synthesis and affinity of a possible byproduct of electrophilic radiolabeling of [123I]IBZM.
11,12-epoxyeicosatrienoic acid (11,12-EET): structural determinants for inhibition of TNF-alpha-induced VCAM-1 expression.
Application of the Suzuki-Miyaura cross-coupling to increase antimicrobial potency generates promising novel antibacterials.
Synthesis and biological study of 2-amino-4-aryl-5-chloropyrimidine analogues as inhibitors of VEGFR-2 and cyclin dependent kinase 1 (CDK1).
New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems.
Dipeptidyl-alpha,beta-epoxyesters as potent irreversible inhibitors of the cysteine proteases cruzain and rhodesain.
Synthesis of new benzimidazole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates with efficient DNA-binding affinity and potent cytotoxicity.
New chemotypes for cathepsin K inhibitors.
Enantioselective synthesis and vanilloid activity evaluation of 1-beta-(p-methoxycinnamoyl)polygodial, an antinociceptive compound from Drymis winteri barks.
Bioisosteric replacement of dihydropyrazole of 4S-(-)-3-(4-chlorophenyl)-N-methyl-N'-[(4-chlorophenyl)-sulfonyl]-4-phenyl-4,5-dihydro-1H-pyrazole-1-caboxamidine (SLV-319) a potent CB1 receptor antagonist by imidazole and oxazole.
Design and synthesis of (E)-1,1,2-triarylethenes: novel inhibitors of the cyclooxygenase-2 (COX-2) isozyme.
Novel bis-arylsulfonamides and aryl sulfonimides as inactivators of plasminogen activator inhibitor-1 (PAI-1).
Generation of potent coagulation protease inhibitors utilizing zinc-mediated chelation.
Total synthesis and biological evaluation of ustiloxin natural products and two analogs.
Addressing species specific metabolism and solubility issues in a quinoline series of oral PDE4 inhibitors.
Synthesis and molecular docking studies of 1-phenyl-4-glycosyl-dihydropyridines as potent antileishmanial agents.
NMR analysis of tautomerisms of active pinacidil-type potassium channel openers and a less active one.
Probing the structural and topological requirements for CCR2 antagonism: holographic QSAR for indolopiperidine derivatives.
Cryptolepine analogues containing basic aminoalkyl side-chains at C-11: synthesis, antiplasmodial activity, and cytotoxicity.
Discovery of indenopyrazoles as EGFR and VEGFR-2 tyrosine kinase inhibitors by in silico high-throughput screening.
DNA gyrase inhibitory activity of ellagic acid derivatives.
5-Aminomethylquinoxaline-2,3-diones. Part II: N-aryl derivatives as novel NMDA/glycine and AMPA antagonists.
Design and synthesis of 7-hydroxy-1H-benzoimidazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Ferulic acid and benzothiazole dimer derivatives with high binding affinity to beta-amyloid fibrils.
Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids.
Discovery of potent and selective bicyclic A(2B) adenosine receptor antagonists via bioisosteric amide replacement.
Synthesis and in vitro evaluation of (18)F-labelled S-fluoroalkyl diarylguanidines: Novel high-affinity NMDA receptor antagonists for imaging with PET.
Discovery of halo-nitrobenzamides with potential application against human African trypanosomiasis.
Novel 5-aryl-1,3-dihydro-indole-2-thiones. potent, orally active progesterone receptor agonists.
Synthesis and biological evaluation of novel 2-(1H-imidazol-4-yl)cyclopropane carboxylic acids: key intermediates for H3 histamine receptor ligands.
Pyrimido[5,4-e][1,2,4]triazine-5,7(1H,6H)-dione derivatives: their cytoprotection effect from rotenone toxicity and preliminary DMPK properties.
Vacuolar-type H(+)-ATPase inhibitory activity of synthetic analogues of the concanamycins: is the hydrogen bond network involving the lactone carbonyl, the hemiacetal hydroxy group, and the C-19 hydroxy group essential for the biological activity of the concanamycins?
Novel potent antagonists of human neuropeptide Y Y5 receptors. Part 2: substituted benzo[a]cycloheptene derivatives.
Novel antineoplastic agents with efficacy against multidrug resistant tumor cells.
General synthesis of 3-substituted alkenyl GABA as potential anticonvulsants.
5-Arylamino-2-methyl-4,7-dioxobenzothiazoles as inhibitors of cyclin-dependent kinase 4 and cytotoxic agents.
Comparison of different heterocyclic scaffolds as substrate analog PDE5 inhibitors.
Discovery of novel conformationally constrained tropane-based biaryl and arylacetylene ligands as potent and selective norepinephrine transporter inhibitors and potential antidepressants.
N-[(3S)-1-benzylpyrrolidin-3-yl]-(2-thienyl)benzamides: human dopamine D4 ligands with high affinity for the 5-HT2A receptor.
Inhibition of Tpl2 kinase and TNF-alpha production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships.
Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1.
Equipotent activity in both enantiomers of a series of ketopiperazine-based renin inhibitors.
Bicyclic nucleoside inhibitors of Varicella-Zoster virus: the effect of branching in the p-alkylphenyl side chain.
Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): The side chain benzylic methylene.
Pyrazolo[1,5-a]pyrimidines as estrogen receptor ligands: defining the orientation of a novel heterocyclic core.
3D-QSAR and QSSR studies of 3,8-diazabicyclo[4.2.0]octane derivatives as neuronal nicotinic acetylcholine receptors by comparative molecular field analysis (CoMFA).
Discovery of 2,3,5-trisubstituted pyridine derivatives as potent Akt1 and Akt2 dual inhibitors.
Discovery of small molecule agonists for the bombesin receptor subtype 3 (BRS-3) based on an omeprazole lead.
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor.
Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents.
Novel factor Xa inhibitors based on a 2-carboxyindole scaffold: SAR of P4 substituents in combination with a neutral P1 ligand.
Synthesis and QSAR studies of pyrimido[4,5-d]pyrimidine-2,5-dione derivatives as potential antimicrobial agents.
New pyrimido[5,4-b]indoles and [1]benzothieno[3,2-d]pyrimidines: high affinity ligands for the alpha(1)-adrenoceptor subtypes.
Synthesis and evaluation of duocarmycin SA analogs incorporating the methyl 1,2,8,8a-tetrahydrocyclopropa[c]oxazolo[2,3-e]indol-4-one-6-carboxylate (COI) alkylation subunit.
Piperazinyl pyrimidine derivatives as potent gamma-secretase modulators.
From arylureas to biarylamides to aminoquinazolines: discovery of a novel, potent TRPV1 antagonist.
Synthesis and biological evaluation of substituted 2-phenyl-2H-indazole-7-carboxamides as potent poly(ADP-ribose) polymerase (PARP) inhibitors.
Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors.
Design and synthesis of new stabilized combi-triazenes for targeting solid tumors expressing the epidermal growth factor receptor (EGFR) or its closest homologue HER2.
Design and synthesis of dipeptidyl nitriles as potent, selective, and reversible inhibitors of cathepsin C.
Structural characteristics of flavanones and flavones from Cudrania tricuspidata for neuraminidase inhibition.
Structure-activity relationship of etomidate derivatives at the GABA(A) receptor: Comparison with binding to 11beta-hydroxylase.
Optimization of piperidin-4-yl-urea-containing melanin-concentrating hormone receptor 1 (MCH-R1) antagonists: Reducing hERG-associated liabilities.
2-Arylimino-5,6-dihydro-4H-1,3-thiazines as a new class of cannabinoid receptor agonists. Part 1: discovery of CB2 receptor selective compounds.
Hit-to-Lead studies: the discovery of potent, orally bioavailable thiazolopyrimidine CXCR2 receptor antagonists.
Phenolic P2/P3 core motif as thrombin inhibitors--design, synthesis, and X-ray co-crystal structure.
Benzimidazol-2-yl or benzimidazol-2-ylthiomethyl benzoylguanidines as novel Na+/H+ exchanger inhibitors, synthesis and protection against ischemic-reperfusion injury.
N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.
Design and synthesis of N-methylmaleimide indolocarbazole bearing modified 2-acetamino acid moieties as Topoisomerase I inhibitors.
Synthesis of novel di- and tricationic carbapenems with potent anti-MRSA activity.
Semisynthesis and antiproliferative evaluation of a series of 3'-aminoflavones.
Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.
2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.
Synthesis and antimycobacterial activity of ferrocenyl ethambutol analogues and ferrocenyl diamines.
Silanediol peptidomimetics. Evaluation of four diastereomeric ACE inhibitors.
Synthesis and biological evaluation of alkoxycoumarins as novel nematicidal constituents.
A regiospecific synthesis of a series of 1-sulfonyl azepinoindoles as potent 5-HT6 ligands.
Synthesis of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-acridone/acridine hybrids as potential DNA-binding agents.
Parallel synthesis and structure-activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors.
Synthesis and antioxidant properties of substituted 3-benzylidene-7-alkoxychroman-4-ones.
Synthesis and characterization of 8-ethynyl-1,3-dihydro-benzo[b][1,4]diazepin-2-one derivatives: new potent non-competitive metabotropic glutamate receptor 2/3 antagonists. Part 1.
Synthesis and antifungal activity of 6-hydroxycinnolines.
Arylphthalazines: identification of a new phthalazine chemotype as inhibitors of VEGFR kinase.
Optimization of CRF1R binding affinity of 2-(2,4,6-trichlorophenyl)-4-trifluoromethyl-5-aminomethylthiazoles through rapid and selective parallel synthesis.
Design and evaluation of novel nonsteroidal dissociating glucocorticoid receptor ligands.
Pyrrolo[1,2-a][1,4]benzodiazepine: a novel class of non-azole anti-dermatophyte anti-fungal agents.
Structure-driven HtL: design and synthesis of novel aminoindazole inhibitors of c-Jun N-terminal kinase activity.
Quinazolinone fungal efflux pump inhibitors. Part 2: In vitro structure-activity relationships of (N-methyl-piperazinyl)-containing derivatives.
Design, synthesis, and biological evaluation of novel T-Type calcium channel antagonists.
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors.
Synthesis and structure-activity relationships of uracil derived human GnRH receptor antagonists: (R)-3-[2-(2-amino)phenethyl]-1-(2,6-difluorobenzyl)-6-methyluracils containing a substituted thiophene or thiazole at C-5.
Novel p38 inhibitors with potent oral efficacy in several models of rheumatoid arthritis.
Synthesis and inhibition of Src kinase activity by 7-ethenyl and 7-ethynyl-4-anilino-3-quinolinecarbonitriles.
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides.
Synthesis and biological activities of novel 4"-alkylidene avermectin derivatives.
Heterocyclic ketones as inhibitors of histone deacetylase.
Methyl 2-(2-(4-formylphenoxy)acetamido)-2-substituted acetate derivatives: a new class of acetylcholinesterase inhibitors.
N-[1-(2-Phenylethyl)pyrrolidin-3-yl]-1-adamantanecarboxamides as novel 5-HT2 receptor antagonists.
3alpha-(4-Substituted phenyl)nortropane-2beta-carboxylic acid methyl esters show selective binding at the norepinephrine transporter.
3D-QSAR studies on unsaturated 4-azasteroids as human 5alpha-reductase inhibitors: a self organizing molecular field analysis approach.
Thrombin receptor (PAR-1) antagonists. Heterocycle-based peptidomimetics of the SFLLR agonist motif.
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.
Synthesis of a high-mannose-type glycopeptide analog containing a glucose-asparagine linkage.
Microsomal triglyceride transfer protein inhibitors: discovery and synthesis of alkyl phosphonates as potent MTP inhibitors and cholesterol lowering agents.
Inhibition of telomerase by BIBR 1532 and related analogues.
Replacing the pyrophosphate group of HMB-PP by a diphosphonate function abrogates Its potential to activate human gammadelta T cells but does not lead to competitive antagonism.
Discovery of a novel series of DHODH inhibitors by a docking procedure and QSAR refinement.
Terephthalamide derivatives as mimetics of the helical region of Bak peptide target Bcl-xL protein.
A series of spirocyclic analogues as potent inhibitors of bacterial phenylalanyl-tRNA synthetases.
Thiourea inhibitors of herpesviruses. Part 3: Inhibitors of varicella zoster virus.
Potent and selective inhibitors of platelet-derived growth factor receptor phosphorylation. Part 4: structure-activity relationships for substituents on the quinazoline moiety of 4-[4-(N-substituted(thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives.
trans-3,4-dimethyl-4-(3-carboxamidophenyl)piperidines: a novel class of micro-selective opioid antagonists.
Discovery of selective phosphonamide-based inhibitors of tumor necrosis factor-alpha converting enzyme (TACE).
Identification of a dual histamine H1/H3 receptor ligand based on the H1 antagonist chlorpheniramine.
Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 2: 8-formamidocyclazocine analogues.
Optimization of alpha-acylaminoketone ecdysone agonists for control of gene expression.
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. III: synthesis, antiviral and pharmacokinetic profiles of symmetrical heteroaryl carboxamides.
Structure activity relationship studies of carboxamido-biaryl ethers as opioid receptor antagonists (OpRAs). Part 2.
Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor.
Pyrrolidine-carboxamides and oxadiazoles as potent hNK1 antagonists.
Synthesis and biological evaluation of L-cysteine derivatives as mitotic kinesin Eg5 inhibitors.
Design and synthesis of a new, conformationally constrained, macrocyclic small-molecule inhibitor of STAT3 via 'click chemistry'.
Design, synthesis and characterization of N9/N7-substituted 6-aminopurines as VEGF-R and EGF-R inhibitors.
Design and synthesis of mimics of S-adenosyl-L-homocysteine as potential inhibitors of erythromycin methyltransferases.
Structure-based design and synthesis of a novel class of Src SH2 inhibitors.
8-acenaphthen-1-yl-1-phenyl-1,3,8-triaza-spiro[4.5]decan-4-one derivatives as orphanin FQ receptor agonists.
New cyclic peptide proteasome inhibitors.
Biochemical basis for differences in metabolism-dependent genotoxicity by two diazinylpiperazine-based 5-HT2C receptor agonists.
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Synthesis and CB1 cannabinoid receptor affinity of 4-alkoxycarbonyl-1,5-diaryl-1,2,3-triazoles.
Discovery of thiophene inhibitors of polo-like kinase.
The design, synthesis and biological evaluation of 7-alkoxy-4-heteroarylamino-3-cyanoquinolines as dual inhibitors of c-Src and iNOS.
Imidazo[5,1-f][1,2,4]triazin-2-amines as novel inhibitors of polo-like kinase 1.
Synthesis and calpain inhibitory activity of peptidomimetic compounds with constrained amino acids at the P2 position.
Design and synthesis of novel diphenacoum-derived, conformation-restricted vitamin K 2,3-epoxide reductase inhibitors.
Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.
Potent achiral agonists of the growth hormone secretagogue (ghrelin) receptor. Part 2: Lead optimisation.
Potent antagonists of the CCR2b receptor. Part 3: SAR of the (R)-3-aminopyrrolidine series.
Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Anti-Pneumocystis carinii and antiplasmodial activities of primaquine-derived imidazolidin-4-ones.
Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates.
Synthesis and evaluation of naphthyridine compounds as antimalarial agents.
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
A novel class of sodium/calcium exchanger inhibitors: design, synthesis, and structure-activity relationships of 4-phenyl-3-(piperidin-4-yl)-3,4-dihydro-2(1H)-quinazolinone derivatives.
A new series of pyridinyl-alkynes as antagonists of the metabotropic glutamate receptor 5 (mGluR5).
Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849.
Replacing the cyclohexene-linker of FR181157 leading to novel IP receptor agonists: orally active prostacyclin mimetics. Part 6.
Dipeptidyl nitriles as human dipeptidyl peptidase I inhibitors.
Fish venom (Pterios volitans) peptide reduces tumor burden and ameliorates oxidative stress in Ehrlich's ascites carcinoma xenografted mice.
Discovery of novel isothiazole inhibitors of the TrkA kinase: structure-activity relationship, computer modeling, optimization, and identification of highly potent antagonists.
Development of N-2,4-pyrimidine-N-phenyl-N'-phenyl ureas as inhibitors of tumor necrosis factor alpha (TNF-alpha) synthesis. Part 1.
Propionylpiperazines as human melanocortin-4 receptor ligands.
Factor VIIa inhibitors: a prodrug strategy to improve oral bioavailability.
Piperazinyl oxime ethers as NK-1 receptor antagonists.
Pentacyclic triterpenes. Part 1: the first examples of naturally occurring pentacyclic triterpenes as a new class of inhibitors of glycogen phosphorylases.
Piperazinyl-glutamate-pyridines as potent orally bioavailable P2Y12 antagonists for inhibition of platelet aggregation.
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Interaction of chiral MS-245 analogs at h5-HT6 receptors.
Discovery of a novel and potent series of dianilinopyrimidineurea and urea isostere inhibitors of VEGFR2 tyrosine kinase.
Synthesis, biological activity and tubulin binding poses of 1-deoxy-9-(R)-dihydrotaxane analogs.
Dipeptidyl peptidase IV inhibitors derived from beta-aminoacylpiperidines bearing a fused thiazole, oxazole, isoxazole, or pyrazole.
Synthesis, SAR and antibacterial studies on novel chalcone oxazolidinone hybrids.
Synthesis and biological evaluation of 9-substituted tetracycline derivatives.
Synthesis and biological evaluation of 1-benzyl-5-(3-biphenyl-2-yl-propyl)-1H-imidazole as novel farnesyltransferase inhibitor.
Synthesis and evaluation of substrate-mimicking cytosolic phospholipase A2 inhibitors--reducing the lipophilicity of the arachidonyl chain isostere.
The identification and optimization of a N-hydroxy urea series of flap endonuclease 1 inhibitors.
Discovery of a novel, potent and selective human beta3-adrenergic receptor agonist.
Synthesis of ether analogues derived from HUN-7293 and evaluation as inhibitors of VCAM-1 expression.
Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles.
Synthesis and anti-inflammatory effects of novel pimarane diterpenoid analogs.
Design and synthesis of o-trifluoromethylbiphenyl substituted 2-amino-nicotinonitriles as inhibitors of farnesyltransferase.
Synthesis and biological results of the technetium-99m-labeled 4-nitroimidazole for imaging tumor hypoxia.
3-(2-pyrrolidin-1-ylethyl)-5-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives as high affinity human 5-HT(1B/1D) ligands.
Diamine-based human histamine H3 receptor antagonists: (4-aminobutyn-1-yl)benzylamines.
Regioselective synthesis and antimicrobial screening of novel ketocarbazolodispiropyrrolidine derivatives.
Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
Synthesis and testing of peptides for anti-prion activity.
A diaryl sulfide, sulfoxide, and sulfone bearing structural similarities to combretastatin A-4.
Effects of 2-(substituted-sulfanyl)-3,5-dihydro-imidazole-4-one and 2-(substituted-sulfanyl)-1H-imidazole-4,5-dione derivatives on serum HDL-cholesterol.
Synthesis and evaluation of antiplatelet activity of trihydroxychalcone derivatives.
Synthesis, SAR and intramolecular hydrogen bonding pattern of 1,3,5-trisubstituted 4,5-dihydropyrazoles as potent cannabinoid CB(1) receptor antagonists.
Evaluation of a 3-amino-8-azabicyclo[3.2.1]octane replacement in the CCR5 antagonist maraviroc.
Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives.
Puupehanol, a sesquiterpene-dihydroquinone derivative from the marine sponge Hyrtios sp.
A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1,n-alkane-di-N-butylcarbamates.
Novel use of chemical shift in NMR as molecular descriptor: a first report on modeling carbonic anhydrase inhibitory activity and related parameters.
1-Aryl-4,6-diamino-1,2-dihydrotriazine as antimalarial agent: a new synthetic route.
6'-Methylpyrido[3,4-b]norhomotropane: synthesis and outstanding potency in relation to the alpha4beta2 nicotinic receptor pharmacophore model.
Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Dimethoxybenzo[i]phenanthridine-12-carboxylic acid derivatives and 6H-dibenzo[c,h][2,6]naphthyridin-5-ones with potent topoisomerase I-targeting activity and cytotoxicity.
Nocathiacin I analogues: synthesis, in vitro and in vivo biological activity of novel semi-synthetic thiazolyl peptide antibiotics.
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.
Benzodiazepine inhibitors of the MMPs and TACE. Part 2.
Duloxetine (Cymbalta), a dual inhibitor of serotonin and norepinephrine reuptake.
Synthesis and activity of substituted carbamates as potentiators of the alpha4beta2 nicotinic acetylcholine receptor.
N-ferrocenylmethyl, N'-methyl-2-substituted benzimidazolium iodide salts with in vitro activity against the Leishmania infantum parasite strain L1.
Synthesis and evaluation of 2-pyridyl pyrimidines with in vitro antiplasmodial and antileishmanial activity.
Synthesis and structure-activity relationships of 2-phenyl-1-[(pyridinyl- and piperidinylmethyl)amino]-3-(1H-1,2,4-triazol-1-yl)propan-2-ols as antifungal agents.
Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.
Synthesis, biological activity, and X-ray crystal structural analysis of diaryl ether inhibitors of malarial enoyl acyl carrier protein reductase. Part 1: 4'-substituted triclosan derivatives.
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
Discovery and optimisation of a potent and selective tertiary sulfonamide oxytocin antagonist.
Metal-free artificial nucleases based on simple oxime and hydroxylamine scaffolds.
Allosteric inhibitors of Akt1 and Akt2: a naphthyridinone with efficacy in an A2780 tumor xenograft model.
Identification and optimization of a novel series of [2.2.1]-oxabicyclo imide-based androgen receptor antagonists.
Design, synthesis, and thrombin-inhibitory activity of pyridin-2-ones as P2/P3 core motifs.
Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Novel heterocycle-substituted pyrimidines as inhibitors of NF-kappaB transcription regulation related to TNF-alpha cytokine release.
Neutral 5-substituted 4-anilinoquinazolines as potent, orally active inhibitors of erbB2 receptor tyrosine kinase.
2-Substituted 4-, 5-, and 6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones and 2-substituted 4,5-bis[(1E)-3-oxo-3-phenylprop-1-en-1-yl]pyridazin-3(2H)-ones as potent platelet aggregation inhibitors: design, synthesis, and SAR studies.
Synthesis and inhibitory activity of 4-alkynyl and 4-alkenylquinazolines: identification of new scaffolds for potent EGFR tyrosine kinase inhibitors.
Synthesis and biological evaluation of 5-(pyridin-2-yl)thiazoles as transforming growth factor-beta type1 receptor kinase inhibitors.
Studies on the reactivity of CDDO, a promising new chemopreventive and chemotherapeutic agent: implications for a molecular mechanism of action.
Design of selective phenylglycine amide tissue factor/factor VIIa inhibitors.
Benzimidazole derivatives as novel nonpeptide luteinizing hormone-releasing hormone (LHRH) antagonists. Part 2: Benzimidazole-5-sulfonamides.
Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-indoles as novel 5-HT6 receptor ligands.
Simultaneous identification of multiple receptors of natural product using an optimized cDNA phage display cloning.
Structure-activity relationships of a novel series of melanin-concentrating hormone (MCH) receptor antagonists.
Tris-azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Lead discovery of quinoxalinediones as an inhibitor of dipeptidyl peptidase-IV (DPP-IV) by high-throughput screening.
5-Aryl-imidazolin-2-ones as a scaffold for potent antioxidant and memory-improving activity.
Synthesis of a new class of camptothecin derivatives, the long-chain fatty acid esters of 10-hydroxycamptothecin, as a potent prodrug candidate, and their in vitro metabolic conversion by carboxylesterases.
Novel constrained CCK-B dipeptoid antagonists derived from pipecolic acid.
Synthesis and anticholinesterase activity of huperzine A analogues containing phenol and catechol replacements for the pyridone ring.
Synthesis and in vitro cytotoxicity of 9-anilinoacridines bearing N-mustard residue on both anilino and acridine rings.
[(11)C]Dimebon, radiosynthesis and lipophilicity of a new potential PET agent for imaging of Alzheimer's disease and Huntington's disease.
Synthesis and biological evaluation of new heterocyclic quinolinones as anti-parasite and anti-HIV drug candidates.
Pyrazolone based TGFbetaR1 kinase inhibitors.
Synthesis and anticonvulsant activity of some novel 3-aryl amino/amino-4-aryl-5-imino-Delta2-1,2,4-thiadiazoline.
Synthesis and antibacterial evaluation of 1beta-methyl-2-[5-(1-methoxyimino-2-substituted sulfonamide ethyl)pyrrolidin-3-ylthio]carbapenems and their related compounds.
Evaluation of myorelaxant activity of 7-substituted hexahydroquinoline derivatives in isolated rabbit gastric fundus.
Synthesis and antihypertensive effects of new methylthiomorpholinphenol derivatives.
Antimalarial activity and synthesis of new trisubstituted pyrimidines.
3-Arylidene-1-(4-nitrophenylmethylene)-3,4-dihydro-1H-naphthalen-2-ones and related compounds displaying selective toxicity and reversal of multidrug resistance in neoplastic cells.
Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2).
Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents.
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
The development of new bicyclic pyrazole-based cytokine synthesis inhibitors.
Pyrrolo[2,1-c][1,4]benzodiazepine-anthraquinone conjugates. Synthesis, DNA binding and cytotoxicity.
3,4-disubstituted azetidinones as selective inhibitors of the cysteine protease cathepsin K. Exploring P3 elements for potency and selectivity.
Synthesis of some new 4(3H)-quinazolinone-2-carboxaldehyde thiosemicarbazones and their metal complexes and a study on their anticonvulsant, analgesic, cytotoxic and antimicrobial activities - part-1.
Synthesis and preliminary biological evaluation of new derivatives of the marine alkaloid leucettamine B as kinase inhibitors.
Synthesis, characterization, antimicrobial and antitumor screening of some diorganotin(IV) complexes of 2-[(9H-Purin-6-ylimino)]-phenol.
Preparation of spermine conjugates with acidic retinoids with potent ribonuclease P inhibitory activity.
Synthesis of amidine and amide derivatives and their evaluation for anti-inflammatory and analgesic activities.
Inhibition of topoisomerase I by naphthoquinone derivatives.
Quinolone-based IMPDH inhibitors: introduction of basic residues on ring D and SAR of the corresponding mono, di and benzofused analogues.
Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.
Synthesis and biological evaluation of a novel series of 1,5-benzothiazepine derivatives as potential antimicrobial agents.
To determine the cytotoxicity of chlorambucil and one of its nitro-derivatives, conjugated to prasterone and pregnenolone, towards eight human cancer cell-lines.
Convenient one-pot synthesis of novel 2-substituted benzimidazoles, tetrahydrobenzimidazoles and imidazoles and evaluation of their in vitro antibacterial and antifungal activities.
Synthesis of 2-sulfanyl-6-methyl-1,4-dihydropyrimidines as a new class of antifilarial agents.
Synthesis and biological property of carba and 20-deoxo analogues of arenastatin A.
Nonsteroidal progesterone receptor antagonists based on 6-thiophenehydroquinolines.
Novel oximes having 5-benzyl-2,4-thiazolidinedione as antihyperglycemic agents: synthesis and structure-activity relationship.
Novel tetrahydrochinoline derived CETP inhibitors.
Coumarins as novel 17beta-hydroxysteroid dehydrogenase type 3 inhibitors for potential treatment of prostate cancer.
Synthesis and evaluation of 3'-azido-2',3'-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus.
Towards development of selective and reversible pyrazoline based MAO-inhibitors: Synthesis, biological evaluation and docking studies.
Functional and biochemical analysis of a key series of ramoplanin analogues.
Optimising metabolic stability in lipophilic chemical space: the identification of a metabolically stable pyrazolopyrimidine CRF-1 receptor antagonist.
Spiroadamantyl 1,2,4-trioxolane, 1,2,4-trioxane, and 1,2,4-trioxepane pairs: relationship between peroxide bond iron(II) reactivity, heme alkylation efficiency, and antimalarial activity.
Interaction of kendomycin and semi-synthetic analogues with the anti-apoptotic protein Bcl-xl.
A diaminocyclohexyl analog of SNS-032 with improved permeability and bioavailability properties.
Synthesis and biological evaluation of C-12' substituted vinflunine derivatives.
3-(4-(6-Fluoroalkoxy-3,4-dihydroisoquinoline-2(1H)-yl)cyclohexyl)-1H-indole-5-carbonitriles for SERT imaging: chemical synthesis, evaluation in vitro and radiofluorination.
Parallel synthesis and antileishmanial activity of ether-linked phospholipids.
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda(6)-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 3: Further optimization of the 2-, 6-, and 7'-substituents and initial pharmacokinetic assessments.
Synthesis and neuropharmacological evaluation of esters of R(-)-N-alkyl-11-hydroxy-2-methoxynoraporphines.
Identification of novel inhibitors of extracellular signal-regulated kinase 2 based on the structure-based virtual screening.
6-heteroaryl-pyrazolo[3,4-b]pyridines: potent and selective inhibitors of glycogen synthase kinase-3 (GSK-3).
Liquid-phase synthesis of a pegylated adenosine-oligoarginine conjugate, cell-permeable inhibitor of cAMP-dependent protein kinase.
Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.
Synthesis of three enantiomeric pairs of scyllo-inositol phosphate and molecular interactions between all possible regioisomers of scyllo-inositol phosphate and inositol 1,4,5-trisphosphate 3-kinase.
Discovery and preliminary evaluation of 5-(4-phenylbenzyl)oxazole-4-carboxamides as prostacyclin receptor antagonists.
Identification of a series of highly potent activators of the Nurr1 signaling pathway.
Arylsulfonamides as a new class of cannabinoid CB1 receptor ligands: identification of a lead and initial SAR studies.
Design and effective synthesis of novel templates, 3,7-diphenyl-4-amino-thieno and furo-[3,2-c]pyridines as protein kinase inhibitors and in vitro evaluation targeting angiogenetic kinases.
Natural inhibitors targeting osteoclast-mediated bone resorption.
Kinase-mediated trapping of bi-functional conjugates of paclitaxel or vinblastine with thymidine in cancer cells.
Adenosine phosphonate inhibitors of lipid II: alanyl tRNA ligase MurM from Streptococcus pneumoniae.
Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X7 antagonists.
Synthesis of some new bioactive 3-amino-2-mercapto-5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4(3H)-one derivatives.
Synthesis and antiviral activity of C-fluoro-branched cyclopropyl nucleosides.
Chemotherapy of leishmaniasis Part VI: synthesis and bioevaluation of some novel terpenyl S,N- and N,N-acetals.
Structural and theoretical studies of [6-bromo-1-(4-fluorophenylmethyl)-4(1H)-quinolinon-3-yl)]-4-hydroxy-2-oxo-3-butenoic acid as HIV-1 integrase inhibitor.
Structure-activity relationship analysis of substituted 4-quinolinamines, antagonists of immunostimulatory CpG-oligodeoxynucleotides.
Landomycin A inhibits DNA synthesis and G1/S cell cycle progression.
Synthesis and biological activity of 2-methyl-20-epi analogues of 1 alpha,25-dihydroxyvitamin D3.
Probing the importance of spacial and conformational domains in captopril analogs for angiotensin converting enzyme activity.
Synthesis and 5 alpha-reductase inhibitory activity of 8-substituted benzo[f]quinolinones derived from palladium mediated coupling reactions.
Naphthalenebis[alpha,alpha-difluoromethylenephosphonates] as potent inhibitors of protein tyrosine phosphatases.
Rational design of boropeptide thrombin inhibitors: beta, beta-dialkyl-phenethylglycine P2 analogs of DuP 714 with greater selectivity over complement factor I and an improved safety profile.
Design, synthesis and antimicrobial activities of some new quinoline derivatives carrying 1,2,3-triazole moiety.
Novel potent antimitotic heterocyclic ketones: synthesis, antiproliferative activity, and structure-activity relationships.
Design, synthesis and in vitro/in vivo evaluation of orally bioavailable prodrugs of a catechol-O-methyltransferase inhibitor.
2,5-Disubstituted pyridines as potent GPR119 agonists.
Synthesis and free radical scavenging activity of a novel metabolite from the fungus Colletotrichum gloeosporioides.
Solvent free synthesis of 1,5-disubstituted tetrazoles derived from Baylis Hillman acetates as potential TNF-alpha inhibitors.
Novel keto-enamine Schiffs bases from 7-hydroxy-4-methyl-2-oxo-2H-benzo[h] chromene-8,10-dicarbaldehyde as potential antidyslipidemic and antioxidant agents.
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists. Part 2.
Synthesis and in vitro antibacterial activities of novel oxazolidinones.
Antibacterial activity of a novel series of 3-bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione derivatives--an extended structure-activity relationship study.
3,4,5-Trisubstituted isoxazoles as novel PPARdelta agonists: Part 1.
Synthesis and antimicrobial activity of 1-(4-aryl-2-thiazolyl)-3-(2-thienyl)-5-aryl-2-pyrazoline derivatives.
Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as alpha2/alpha3 subtype selective GABA A agonists for the treatment of anxiety.
Synthesis and anticancer activity of a novel class of flavonoids: 2,4-diarylchromane[4,3-d]-delta(1,9b)-1,2,3-thiadiazolines.
1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors.
Hydroxylated N-alkyl-4-piperidinyl-2,3-diarylpyrrole derivatives as potent broad-spectrum anticoccidial agents.
Nitrone derivatives of trolox as neuroprotective agents.
Beta-lactam compounds as apparently uncompetitive inhibitors of HIV-1 protease.
Synthesis and biological evaluation of novel steroidal pyrazoles as substrates for bile acid transporters.
Anti-coxsackievirus B3 activity of 2-amino-3-nitropyrazolo[1,5-a]pyrimidines and their analogs.
Triamino derivatives of triazolotriazine and triazolopyrimidine as adenosine A2a receptor antagonists.
Synthesis of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-benzimidazole conjugates with remarkable DNA-binding affinity.
Synthesis of novel phytosphingosine derivatives and their preliminary biological evaluation for enhancing radiation therapy.
Synthesis and antituberculosis activity of some N-pyridyl-N'-thiazolylhydrazine derivatives.
Antimitotic activity of lobaric acid and a new benzofuran, sakisacaulon A from Stereocaulon sasakii.
Discovery of novel phosphonate derivatives as hepatitis C virus NS3 protease inhibitors.
Design, synthesis and structure-activity relationships of (1H-pyridin-4-ylidene)amines as potential antimalarials.
Small, non-peptide C5a receptor antagonists: part 1.
Organocatalytic synthesis and sterol 14alpha-demethylase binding interactions of enantioriched 3-(1H-1,2,4-triazol-1-yl)butyl benzoates.
Design and synthesis of new potent, silent 5-HT1A antagonists by covalent coupling of aminopropanol derivatives with selective serotonin reuptake inhibitors.
Imidazo-pyrazine derivatives as potent CXCR3 antagonists.
Synthesis and antibacterial activity of 3-O-carbamoyl derivatives of 6,11-di-O-methylerythromycin A: a novel class of acylides.
Cytotoxicity against cholangiocarcinoma cell lines of zerumbone derivatives.
Constraining the amide bond in N-sulfonylated dipeptide VLA-4 antagonists.
Novel HCV NS5B polymerase inhibitors derived from 4-(1',1'-dioxo-1',4'-dihydro-1'lambda6-benzo[1',2',4']thiadiazin-3'-yl)-5-hydroxy-2H-pyridazin-3-ones. Part 1: exploration of 7'-substitution of benzothiadiazine.
New ultra-short acting hypnotic: synthesis, biological evaluation, and metabolic profile of ethyl 8-oxo-5,6,7,8-tetrahydro-thiazolo[3,2-a][1,3]diazepin-3-carboxylate (HIE-124).
7-Azaindole derivatives as potential partial nicotinic agonists.
Discovery and structure-activity relationships of new steroidal compounds bearing a carboxy-terminal side chain as androgen receptor pure antagonists.
Cytotoxicity of the novel spin trapping compound 5-ethoxycarbonyl-3,5-dimethyl-pyrroline N-oxide (3,5-EDPO) and its derivatives.
The 5-HT3 antagonist tropisetron (ICS 205-930) is a potent and selective alpha7 nicotinic receptor partial agonist.
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
Antiproliferative effects of dibenzocyclooctadiene lignans isolated from Schisandra chinensis in human cancer cells.
Scaffold hopping in the rational design of novel HIV-1 non-nucleoside reverse transcriptase inhibitors.
Dipeptidyl aspartyl fluoromethylketones as potent caspase inhibitors: peptidomimetic replacement of the P(2) amino acid by 2-aminoaryl acids and other non-natural amino acids.
Discovery of novel indazole-linked triazoles as antifungal agents.
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
Synthesis and SAR of novel conformationally-restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 1: Substituted pyrazoles.
Discovery of a novel class of benzazepinone Na(v)1.7 blockers: potential treatments for neuropathic pain.
Design, synthesis, and molecular modeling studies of 5'-deoxy-5'-ureidoadenosine: 5'-ureido group as multiple hydrogen bonding donor in the active site of S-adenosylhomocysteine hydrolase.
4-Substituted-7-azaindoles bearing a ureidobenzofuranone moiety as potent and selective, ATP-competitive inhibitors of the mammalian target of rapamycin (mTOR).
Synthesis and biological evaluation of novel allophenylnorstatine-based HIV-1 protease inhibitors incorporating high affinity P2-ligands.
Syntheses and antibacterial activity of phendioxy substituted cyclic enediynes.
Studies on the novel alpha-glucosidase inhibitory activity and structure-activity relationships for andrographolide analogues.
Arylanthranilodinitriles: a new biaryl class of antileishmanial agents.
Synthesis and antiproliferative activity of two new tiazofurin analogues with 2'-amido functionalities.
Synthesis and in vitro evaluation of novel derivatives of diphenylsulfide as serotonin transporter ligands.
Anti-malarial activity of Baylis-Hillman adducts from substituted 2-chloronicotinaldehydes.
Novel pyridopyrimidine derivatives as inhibitors of stable toxin a (STa) induced cGMP synthesis.
Synthesis and biological evaluation of arylhydrazinocyanoacrylates and N-aryl pyrazolecarboxylates.
A pyrimidine-pyrazolone nucleoside chimera with potent in vitro anti-orthopoxvirus activity.
A bulge binding agent with novel wedge-shape topology for stimulation of DNA triplet repeat strand slippage synthesis.
2-Alkylamino- and alkoxy-substituted 2-amino-1,3,4-oxadiazoles-O-Alkyl benzohydroxamate esters replacements retain the desired inhibition and selectivity against MEK (MAP ERK kinase).
Design at the atomic level: design of biaryloxazolidinones as potent orally active antibiotics.
Carbonic anhydrase inhibitors: inhibition of the beta-class enzymes from the fungal pathogens Candida albicans and Cryptococcus neoformans with simple anions.
Functionalized 3-amino-imidazo[1,2-a]pyridines: a novel class of drug-like Mycobacterium tuberculosis glutamine synthetase inhibitors.
Identification of new Hsp90 inhibitors by structure-based virtual screening.
Bis-anthracenyl isoxazolyl amides have enhanced anticancer activity.
Tricyclic thienopyridine-pyrimidones/thienopyrimidine-pyrimidones as orally efficacious mGluR1 antagonists for neuropathic pain.
Novel HDAC6 isoform selective chiral small molecule histone deacetylase inhibitors.
Synthesis and sulfatase inhibitory activities of (E)- and (Z)-4-hydroxytamoxifen sulfamates.
Synthesis, molecular modeling and preliminary biological evaluation of 1-amino-3-phosphono-3-cyclopentene-1-carboxylic acid and 1-amino-3-phosphono-2-cyclopentene-1-carboxylic acid, two novel agonists of metabotropic glutamate receptors of group III.
Antitumour activity of sphingoid base adducts of phenethyl isothiocyanate.
Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.
Thiazole-derived potent, highly bioavailable short duration growth hormone secretagogues.
Identification and characterization of m4 selective muscarinic antagonists.
New generation dopaminergic agents. 2. Discovery of 3-OH-phenoxyethylamine and 3-OH-N1-phenylpiperazine dopaminergic templates.
Synthesis and biological evaluation of the suberoylanilide hydroxamic acid (SAHA) beta-glucuronide and beta-galactoside for application in selective prodrug chemotherapy.
Three dimensional pharmacophore modelling for c-Kit receptor tyrosine kinase inhibitors.
Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation.
5-Nitro-2-furyl derivative actives against Trypanosoma cruzi: preliminary in vivo studies.
Synthesis and structure-activity relationship of novel indene N-oxide derivatives as potent peroxisome proliferator activated receptor gamma (PPARgamma) agonists.
Design, synthesis and hypolipidemic activity of novel 2-(m-tolyloxy) isobutyric acid derivatives.
Synthesis, molecular modeling studies and selective inhibitory activity against MAO of N1-propanoyl-3,5-diphenyl-4,5-dihydro-(1H)-pyrazole derivatives.
Adenosine-anchored triphosphate subsite probing: distinguishing between HER-2 and HER-4 tyrosine protein kinases.
A novel and efficient one step synthesis of 2-amino-5-cyano-6-hydroxy-4-aryl pyrimidines and their anti-bacterial activity.
Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.
Pyridone derivatives as potent, orally bioavailable VLA-4 integrin antagonists.
Discovery of orally active butyrolactam 11beta-HSD1 inhibitors.
Structure-activity relationships of N-substituted piperazine amine reuptake inhibitors.
Synthesis, molecular modeling studies, and selective inhibitory activity against monoamine oxidase of N,N'-bis[2-oxo-2H-benzopyran]-3-carboxamides.
Synthesis and evaluation of 4-substituted benzylamine derivatives as beta-tryptase inhibitors.
Synthesis and HIV-integrase strand transfer inhibition activity of 7-hydroxy[1,3]thiazolo[5,4-b]pyridin-5(4H)-ones.
Pharmacophore-guided lead optimization: the rational design of a non-zinc coordinating, sub-micromolar inhibitor of the botulinum neurotoxin serotype a metalloprotease.
Discovery of potent and orally active MTP inhibitors as potential anti-obesity agents.
4-Aminophenoxyacetic acids as a novel class of reversible cathepsin K inhibitors.
Crystal structure of human ERK2 complexed with a pyrazolo[3,4-c]pyridazine derivative.
Rapid hit to lead evaluation of pyrazolo[3,4-d]pyrimidin-4-one as selective and orally bioavailable mGluR1 antagonists.
Chemotherapy of leishmaniasis. Part V: Synthesis and in vitro bioevaluation of novel pyridinone derivatives.
Acid-catalyzed synthesis of oxathiolone fused chalcones. Comparison of their activity toward various microorganisms and human cancer cells line.
Phosphonoxins: rational design and discovery of a potent nucleotide anti-Giardia agent.
Novel neofusapyrones isolated from Verticillium dahliae as potent antifungal substances.
The comparative antimalarial properties of weak base and neutral synthetic ozonides.
Carbonic anhydrase inhibitors; fluorinated phenyl sulfamates show strong inhibitory activity and selectivity for the inhibition of the tumor-associated isozymes IX and XII over the cytosolic ones I and II.
Multiple strategies for the preparation of a sulfur-35 labeled NPC1L1 radioligand.
Synthesis, configurational stability and stereochemical biological evaluations of (S)- and (R)-5-hydroxythalidomides.
Theoretical models of pentamidine analogs activity based on their DNA minor groove complexes.
Design, synthesis and biological evaluation of new ionone derivatives as potential neuroprotective agents in cerebral ischemia.
Synthesis of 4-oxo-4,7-dihydrofuro[2,3-b]pyridine-5-carboxamides with broad-spectrum human herpesvirus polymerase inhibition.
Development of a fluorescence polarization based assay for histone deacetylase ligand discovery.
New tetrazole-based selective anandamide uptake inhibitors.
Discovery of trypanocidal thiosemicarbazone inhibitors of rhodesain and TbcatB.
1H-Pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoid receptor antagonists with high functional activity.
Structure-based design, synthesis, and study of pyrazolo[1,5-a][1,3,5]triazine derivatives as potent inhibitors of protein kinase CK2.
Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.
Synthesis and biological evaluation of N-acetyl-beta-aryl-1,2-didehydroethylamines as new HIV-1 RT inhibitors in vitro.
Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.
Design of potent inhibitors of human beta-secretase. Part 2.
Structure-activity relationships of the ultrapotent vanilloid resiniferatoxin (RTX): the homovanillyl moiety.
N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists.
Structurally diverse 5-substituted pyrimidine nucleosides as inhibitors of Leishmania donovani promastigotes in vitro.
Identification of potent agonists of photoreceptor-specific nuclear receptor (NR2E3) and preparation of a radioligand.
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Opioid receptor binding and antinociceptive activity of the analogues of endomorphin-2 and morphiceptin with phenylalanine mimics in the position 3 or 4.
Molecular modeling studies to predict the possible binding modes of endomorphin analogs in mu opioid receptor.
From natural products to achiral drug prototypes: potent thrombin inhibitors based on P2/P3 dihydropyrid-2-one core motifs.
First experimental identification of Ras-inhibitor binding interface using a water-soluble Ras ligand.
Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1).
Addressing the malaria drug resistance challenge using flow cytometry to discover new antimalarials.
Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.
Discovery of non-peptidergic MrgX1 and MrgX2 receptor agonists and exploration of an initial SAR using solid-phase synthesis.
Structure-activity relationship studies on a series of cyclohexylpiperazines bearing a phanylacetamide as ligands of the human melanocortin-4 receptor.
A small library of trisubstituted pyrimidines as antimalarial and antitubercular agents.
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands--part II.
Design and synthesis of a novel class of dual PPARgamma/delta agonists.
1,3-Disubstituted-imidazo[1,5-a]pyrazines as insulin-like growth-factor-I receptor (IGF-IR) inhibitors.
Synthesis of OSW saponin analogs with modified sugar residues and their antiproliferative activities.
Aminopyridine carboxamides as c-Jun N-terminal kinase inhibitors: targeting the gatekeeper residue and beyond.
Benzimidazole-2-carboxamides as novel NR2B selective NMDA receptor antagonists.
Estrogen receptor ligands. Part 16: 2-Aryl indoles as highly subtype selective ligands for ERalpha.
Optimization and SAR for dual ErbB-1/ErbB-2 tyrosine kinase inhibition in the 6-furanylquinazoline series.
Synthesis of substituted aryloxy alkyl and aryloxy aryl alkyl imidazoles as antileishmanial agents.
Synthesis and structure-activity relationships of 3-phenyl-2-propenamides as inhibitors of glycogen phosphorylase a.
Dithiocarbamic acid esters as anticancer agent. Part 1: 4-substituted-piperazine-1-carbodithioic acid 3-cyano-3,3-diphenyl-propyl esters.
Synthesis and biological evaluation of biphenylsulfonamide carboxylate aggrecanase-1 inhibitors.
Diarylacetylene piperidinyl amides as novel anxiolytics.
1-Aryl-3,4-dihydro-1H-quinolin-2-one derivatives, novel and selective norepinephrine reuptake inhibitors.
Synthesis of (1,4)-naphthoquinono-[3,2-c]-1H-pyrazoles and their (1,4)-naphthohydroquinone derivatives as antifungal, antibacterial, and anticancer agents.
Terpenoids. III: Synthesis and biological evaluation of 23-hydroxybetulinic acid derivatives as novel inhibitors of glycogen phosphorylase.
Further studies on ethenyl and ethynyl-4-phenylamino-3-quinolinecarbonitriles: identification of a subnanomolar Src kinase inhibitor.
Semisynthesis and pharmacological activities of Tetrac analogs: angiogenesis modulators.
Amide analogs of antifungal dioxane-triazole derivatives: synthesis and in vitro activities.
Benzothiophene and naphthalene derived constrained SERMs.
Synthesis and in vitro DMPK profiling of a 1,2-dioxolane-based library with activity against Plasmodium falciparum.
Discovery and biological profile of isoindolinone derivatives as novel metabotropic glutamate receptor 1 antagonists: a potential treatment for psychotic disorders.
Improving potency and selectivity of a new class of non-Zn-chelating MMP-13 inhibitors.
cis-6-oxo-hexahydro-2-oxa-1,4-diazapentalene and cis-6-oxo-hexahydropyrrolo[3,2-c]pyrazole based scaffolds: design rationale, synthesis and cysteinyl proteinase inhibition.
Discovery and investigation of a novel class of thiophene-derived antagonists of the human glucagon receptor.
Modulators of the human CCR5 receptor. Part 1: Discovery and initial SAR of 1-(3,3-diphenylpropyl)-piperidinyl amides and ureas.
The synthesis and evaluation of [2.2.1]-bicycloazahydantoins as androgen receptor antagonists.
Development of subtype-selective ligands as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Synthesis of analogues of a potent antitumor saponin OSW-1.
Synthesis and antitumour activity of pyrene-linked pyrrolo [2,1-c]benzodiazepine hybrids.
Syntheses and radical scavenging activities of resveratrol derivatives.
Effects of fluorine substitution of cytosine analogues on the binding affinity to HIV-1 reverse transcriptase.
Design and synthesis of novel cyanoguanidine ATP-sensitive potassium channel openers for the treatment of overactive bladder.
In vitro and in vivo profile of 5-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-1H-indole-2-carboxylic acid benzylmethyl carbamoylamide (dirlotapide), a novel potent MTP inhibitor for obesity.
Modifications of the GSK3beta substrate sequence to produce substrate-mimetic inhibitors of Akt as potential anti-cancer therapeutics.
A catch-and-release strategy for the combinatorial synthesis of 4-acylamino-1,3-thiazoles as potential CDK5 inhibitors.
Pyrimido[1,2-b]-1,2,4,5-tetrazin-6-ones as HCMV protease inhibitors: a new class of heterocycles with flavin-like redox properties.
Synthesis and insulin-sensitizing activity of a novel kind of benzopyran derivative.
Synthesis and biological evaluation of unprecedented classes of spiro-beta-lactams and azido-beta-lactams as acyl-CoA:cholesterol acyltransferase inhibitors.
Pyrazolo[1,5-a]pyrimidine-based inhibitors of HCV polymerase.
Optimization of azepanone calcitonin gene-related peptide (CGRP) receptor antagonists: development of novel spiropiperidines.
Design, synthesis and analgesic properties of novel conformationally-restricted N-acylhydrazones (NAH).
Effect of linker substitution on the binding of butorphan univalent and bivalent ligands to opioid receptors.
N-substituted bis-C-alkyloxadiazolones as dual effectors: efficient intermediates to amidoximes or amidines and prodrug candidates of potent antimalarials.
Optimization of piperidyl-ureas as inhibitors of soluble epoxide hydrolase.
Structure-activity relationship studies of small-molecule inhibitors of Wnt response.
Structure-based design and parallel synthesis of N-benzyl isatin oximes as JNK3 MAP kinase inhibitors.
Synthesis and characterization of a BODIPY-labeled derivative of Soraphen A that binds to acetyl-CoA carboxylase.
Discovery of novel selective HER-2 sheddase inhibitors through optimization of P1 moiety.
Polyketide synthase thioesterases catalyze rapid hydrolysis of peptidyl thioesters.
N-Hydroxy-1,2-disubstituted-1H-benzimidazol-5-yl acrylamides as novel histone deacetylase inhibitors: design, synthesis, SAR studies, and in vivo antitumor activity.
Synthesis and PKCtheta inhibitory activity of a series of 4-indolylamino-5-phenyl-3-pyridinecarbonitriles.
3D-QSAR studies of triazafluorenone inhibitors of metabotropic glutamate receptor subtype 1.
Synthesis and preliminary bioactivity assays of 3,4-dichloro-5-(omega-hydroxyalkylamino)-2(5H)-furanones.
Synthesis and antimicrobial activity of cholic acid hydrazone analogues.
Asymmetric synthesis and anti-HIV activity of L-carbocyclic 2',3'-didehydro-2',3'-dideoxyadenosine.
Novel 1,3-disubstituted-5,10-dihydro-5,10-dioxo-1H-benzo[g] isochromene-3 carboxamides as potent antitumor agents.
Evaluation of phosphorus-containing inhibitors of gamma-glutamyl hydrolase.
Discovery of novel 1-arylmethyl pyrrolidin-2-yl ethanol amines as calcium-sensing receptor antagonists.
Synthesis and preliminary biological evaluation of (2S,1'R,2'S)- and (2S,1'S,2'R)-2-(2'-phosphonocyclopropyl)glycines, two novel conformationally constrained l-AP4 analogues.
Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis.
C-5 Substituted heteroaryl 3-pyridinecarbonitriles as PKCtheta inhibitors: Part I.
Substituted benzothiadizine inhibitors of Hepatitis C virus polymerase.
Design, synthesis, and biological evaluation of novel human 5'-deoxy-5'-methylthioadenosine phosphorylase (MTAP) substrates.
New analogues of agmatine with higher affinity to imidazoline receptors.
Submicromolar phosphinic inhibitors of Escherichia coli aspartate transcarbamoylase.
Cathepsin B inhibitory activities of three new phthalate derivatives isolated from seahorse, Hippocampus Kuda Bleeler.
Bradykinin B1 receptor antagonists: an alpha-hydroxy amide with an improved metabolism profile.
Flavylium salts as in vitro precursors of potent ligands to brain GABA-A receptors.
Synthesis of a natural product-inspired eight-membered ring lactam library via ring-closing metathesis.
Pleuromutilin derivatives having a purine ring. Part 1: new compounds with promising antibacterial activity against resistant Gram-positive pathogens.
Fluorination of triptolide and its analogues and their cytotoxicity.
Development of an efficient and selective radioligand for bradykinin B1 receptor occupancy studies.
Tocopherol long chain fatty alcohols decrease the production of TNF-alpha and NO radicals by activated microglial cells.
From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
3,5-Disubstituted quinolines as novel c-Jun N-terminal kinase inhibitors.
Potent 2'-aminoanilide inhibitors of cFMS as potential anti-inflammatory agents.
Synthesis and antibacterial activity of O-substituted nocathiacin I derivatives.
Oxyguanidines. Part 2: Discovery of a novel orally active thrombin inhibitor through structure-based drug design and parallel synthesis.
(2S,1'S,2'R,3'R)-2(2'-Carboxy-3'-hydroxymethylcyclopropyl)glycine-[3H], a potent and selective radioligand for labeling group 2 and 3 metabotropic glutamate receptors.
Synthesis and structure-activity relationships of 4-oxo-1-phenyl-3,4,6,7-tetrahydro-[1,4]diazepino[6,7,1-hi]indoles: novel PDE4 inhibitors.
6-Acylamino-2-[(alkylsulfonyl)oxy]-1H-isoindole-1,3-dione mechanism-based inhibitors of human leukocyte elastase.
Organoiodine(III) mediated synthesis of 3,9-diaryl- and 3,9-difuryl-bis-1,2,4-triazolo[4,3-a][4,3-c]pyrimidines as antibacterial agents.
4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists.
Synthesis of spermidine and norspermidine dimers as high affinity polyamine transport inhibitors.
Pyrrolylquinoxalinediones carrying a piperazine residue represent highly potent and selective ligands to the homomeric kainate receptor GluR5.
Benzamide-based thiolcarbamates: a new class of HIV-1 NCp7 inhibitors.
Ganglioside GM1 mimics: lipophilic substituents improve affinity for cholera toxin.
Synthesis and biological evaluation of 4-[(3-methyl-3H-imidazol-4-yl)-(2-phenylethynyl-benzyloxy)-methyl]-benzonitrile as novel farnesyltransferase inhibitor.
A novel class of apical sodium co-dependent bile acid transporter inhibitors: the 1,2-benzothiazepines.
Evaluation of fluorescently labeled xylopyranosides as probes for proteoglycan biosynthesis.
Structure-activity relationship in the 3-iodo-4-phenoxypyridinone (IOPY) series: The nature of the C-3 substituent on anti-HIV activity.
Regioselective synthesis and cytotoxicities of camptothecin derivatives modified at the 7-, 10- and 20-positions.
The synthesis and SAR of 2-amino-pyrrolo[2,3-d]pyrimidines: a new class of Aurora-A kinase inhibitors.
A novel oxazine ring closure reaction affording (Z)-((E)-2-styrylbenzo[b]furo[3,2-d][1,3]oxazin-4-ylideno)acetaldehydes and their anti-osteoclastic bone resorption activity.
Design and synthesis of substituted pyridine derivatives as HIF-1alpha prolyl hydroxylase inhibitors.
An orally active corticotropin releasing factor 1 receptor antagonist from 8-aryl-1,3a,7,8-tetraaza-cyclopenta[a]indenes.
7-(aryl/heteroaryl-2-ylethynyl)-4-phenylamino-3-quinolinecarbonitriles as new Src kinase inhibitors: addition of water solubilizing groups.
New competitive inhibitors of cytosolic (NADH-dependent) rabbit muscle glycerophosphate dehydrogenase.
Development of a novel therapeutic suppressor of brain proinflammatory cytokine up-regulation that attenuates synaptic dysfunction and behavioral deficits.
5-Heteroatom-substituted pyrazoles as canine COX-2 inhibitors: Part 2. Structure-activity relationship studies of 5-alkylethers and 5-thioethers.
Amino substituted analogs of 1-phenyl-3-phenylimino-2-indolones with potent galanin Gal3 receptor binding affinity and improved solubility.
The design, synthesis, and evaluation of two universal doxorubicin-linkers: preparation of conjugates that retain topoisomerase II activity.
Identification and characterization of amino-piperidinequinolones and quinazolinones as MCHr1 antagonists.
Asymmetric synthesis of the L-fuco-nojirimycin, a nanomolar alpha-L-fucosidase inhibitor.
Biological evaluation of 1-alkyl-3-phenylthioureas as orally active HDL-elevating agents.
Nitrogen-bridged substituted 8-arylquinolines as potent PDE IV inhibitors.
HCV NS5B polymerase inhibitors 1: Synthesis and in vitro activity of 2-(1,1-dioxo-2H-[1,2,4]benzothiadiazin-3-yl)-1-hydroxynaphthalene derivatives.
Discovery of 5-substituted 2-amino-4-chloro-8-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7,8-dihydropteridin-6(5H)-ones as potent and selective Hsp90 inhibitors.
Synthesis of analogs of forodesine HCl, a human purine nucleoside phosphorylase inhibitor-Part II.
Aryloxypyrazines as highly selective antagonists of Oxytocin.
Long chain amines and long chain ammonium salts as novel inhibitors of dynamin GTPase activity.
Isoxazole-3-hydroxamic acid derivatives as peptide deformylase inhibitors and potential antibacterial agents.
Synthesis of methylphenidate analogues and their binding affinities at dopamine and serotonin transport sites.
Carbonic anhydrase inhibitors. Interaction of 2-(hydrazinocarbonyl)-3-phenyl-1H-indole-5-sulfonamide with 12 mammalian isoforms: kinetic and X-ray crystallographic studies.
5'-halogenated analogs of oxymorphindole.
Optimization of a pyrazoloquinolinone class of Chk1 kinase inhibitors.
On-resin cyclization of peptide ligands of the Vascular Endothelial Growth Factor Receptor 1 by copper(I)-catalyzed 1,3-dipolar azide-alkyne cycloaddition.
Synthesis of 2,3-diaryl-1,3-thiazolidine-4-one derivatives as selective cyclooxygenase (COX-2) inhibitors.
5(Z)-benzylidene-1,2-dihydro-9-hydroxy-10-methoxy-2,2,4-trimethyl-5H-1-aza-6-oxa-chrysenes as non-steroidal glucocorticoid receptor modulators.
Primary amides as selective inhibitors of cathepsin K.
Synthesis and antitumour activity of new tiazofurin analogues bearing a 2,3-anhydro functionality in the furanose ring.
Parasiticidal 2-alkoxy- and 2-aryloxyiminoalkyl trifluoromethanesulfonanilides.
2-(2-(2-Ethoxybenzoylamino)-4-chlorophenoxy)-N-(2-ethoxybenzoyl)benzamine inhibits EAT cell induced angiogenesis by down regulation of VEGF secretion.
DNA cleavage promoted by 2,9-dimethyl-4,7-diazadecane-2,9-dithiol (DDD) derivatives.
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A.
Synthesis and biological properties of new 1 beta-methylcarbapenems.
Novel modified tripeptide inhibitors of alpha 4 beta 7 mediated lymphoid cell adhesion to MAdCAM-1.
Proposed structural basis of interaction of piperine and related compounds with monoamine oxidases.
Structure-based design of diaminopyranosides as a novel inhibitor core unit of HIV proteases.
Scaffold-based design and synthesis of potent N-type calcium channel blockers.
Stereoselective total synthesis of a potent natural antifungal compound (6S)-5,6,dihydro-6-[(2R)-2-hydroxy-6-phenyl hexyl]-2H-pyran-2-one.
Anthranilic sulfonamide CCK1/CCK2 dual receptor antagonists I: discovery of CCKR1 selectivity in a previously CCKR2-selective lead series.
Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors.
Evaluation of synthetic sphingolipid analogs as ligands for peroxisome proliferator-activated receptors.
Allosteric inhibitors of Akt1 and Akt2: discovery of [1,2,4]triazolo[3,4-f][1,6]naphthyridines with potent and balanced activity.
HY251, a novel cell cycle inhibitor isolated from Aralia continentalis, induces G1 phase arrest via p53-dependent pathway in HeLa cells.
Immucillins in custom catalytic-site cavities.
Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption.
Isolation, characterization and antiplasmodial activity of steroidal alkaloids from Funtumia elastica (Preuss) Stapf.
Synthesis and antibacterial activity of hydrolytically stable (-)-epicatechin gallate analogues for the modulation of beta-lactam resistance in Staphylococcus aureus.
A new multi-gram synthetic route to labeling precursors for the D(2/3) PET agent 18F-fallypride.
Opioids and efflux transporters. Part 3: P-glycoprotein substrate activity of 3-hydroxyl addition to meperidine analogs.
Synthesis and structure-activity relationships of new disubstituted phenyl-containing 3,4-diamino-3-cyclobutene-1,2-diones as CXCR2 receptor antagonists.
Synthesis of all stereoisomers of 3-hydroxypipecolic acid and 3-hydroxy-4,5-dehydropipecolic acid and their evaluation as glycosidase inhibitors.
Synthesis and antimycobacterial evaluation of new trans-cinnamic acid hydrazide derivatives.
Synthesis and SAR of potent and orally bioavailable tert-butylpyrrolidine archetype derived melanocortin subtype-4 receptor modulators.
Conformationally restricted macrocyclic analogues of combretastatins.
Discovery of azetidinone acids as conformationally-constrained dual PPARalpha/gamma agonists.
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor alpha agonists.
Optimization of biaryl Selective HDAC1&2 Inhibitors (SHI-1:2).
Solid-phase synthesis of Stat3 inhibitors incorporating O-carbamoylserine and O-carbamoylthreonine as glutamine mimics.
Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors.
A new non-azole inhibitor of ABA 8'-hydroxylase: effect of the hydroxyl group substituted for geminal methyl groups in the six-membered ring.
Discovery of potent CRTh2 (DP2) receptor antagonists.
Inhibition of P-glycoprotein-mediated multidrug efflux by aminomethylene and ketomethylene analogs of reversins.
Synthesis and evaluation of two 18F-labeled imidazo[1,2-a]pyridine analogues as potential agents for imaging beta-amyloid in Alzheimer's disease.
Tricyclic azepine derivatives: pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors.
Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists.
Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
Development of photoaffinity probes for gamma-secretase equipped with a nitrobenzenesulfonamide-type cleavable linker.
Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
4-hydroxyisoleucine an unusual amino acid as antidyslipidemic and antihyperglycemic agent.
DNA binding specificity and cytotoxicity of novel antitumor agent Ge132 derivatives.
Structure-activity relationship studies on tetralin carboxamide growth hormone secretagogue receptor antagonists.
N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.
A novel series of potent gamma-secretase inhibitors based on a benzobicyclo[4.2.1]nonane core.
Synthesis and antiviral activity against Coxsackie virus B3 of some novel benzimidazole derivatives.
4-Acylamino-and 4-ureidobenzamides as melanin-concentrating hormone (MCH) receptor 1 antagonists.
Novel beta-(imidazol-4-yl)-beta-amino acids: solid-phase synthesis and study of their inhibitory activity against geranylgeranyl protein transferase type I.
1-(1-Naphthyl)piperazine as a novel template for 5-HT6 serotonin receptor ligands.
[3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.
Synthesis and antibacterial activity of some aryloxy/thioaryloxy oxazolidinone derivatives.
High-throughput identification of fucosyltransferase inhibitors using carbohydrate microarrays.
Design and synthesis of beta-amino-alpha-hydroxy amide derivatives as inhibitors of MetAP2 and HUVEC growth.
A new 2-carbamoyl pteridine that inhibits mycobacterial FtsZ.
Discovery of a novel potent Na+/Ca2+ exchanger inhibitor: design, synthesis and structure-activity relationships of 3,4-dihydro-2(1H)-quinazolinone derivatives.
Small molecule biaryl FSH receptor agonists. Part 1: Lead discovery via encoded combinatorial synthesis.
Complestatin synthetic studies; the effect of the amino acid configuration on peptide backbone conformation in the common western BCD macrocycle.
Design and synthesis of novel chrysene-linked pyrrolo[2,1-c][1,4]-benzodiazepine hybrids as potential DNA-binding agents.
Adenine derived inhibitors of the molecular chaperone HSP90-SAR explained through multiple X-ray structures.
4,5-Disubstituted-1,3-oxazolidin-2-imine derivatives: a new class of orally bioavailable nitric oxide synthase inhibitor.
Rational design and synthesis of novel nucleotide anti-Giardia agents.
Synthesis of novel diaryl ethers and their evaluation as antimitotic agents.
5H-8,9-dimethoxy-5-(2-N,N-dimethylaminoethyl)dibenzo[c,h][1,6]naphthyridin-6-ones and related compounds as TOP1-targeting agents: influence of structure on the ternary cleavable complex formation.
Stereoselective synthesis of phosphoramidate alpha(2-6)sialyltransferase transition-state analogue inhibitors.
5-Piperazinyl pyridine carboxamide bradykinin B1 antagonists.
2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists.
Carbonic anhydrase activators: activation of isozyme XIII with amino acids and amines.
Discovery of 3-hydroxy-4-carboxyalkylamidino-5-arylamino-isothiazoles as potent MEK1 inhibitors.
Aziridine-2,3-dicarboxylate inhibitors targeting the major cysteine protease of Trypanosoma brucei as lead trypanocidal agents.
2,4-Diamino-quinazolines as inhibitors of beta-catenin/Tcf-4 pathway: Potential treatment for colorectal cancer.
Analysis of HIF-1 inhibition by manassantin A and analogues with modified tetrahydrofuran configurations.
Expedient solid-phase synthesis of both symmetric and asymmetric diol libraries targeting aspartic proteases.
Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists.
The inhibitory effects of squalene-derived triterpenes on protein phosphatase PP2A.
Amino propynyl benzoic acid building block in rigid spacers of divalent ligands binding to the Syk SH2 domains with equally high affinity as the natural ligand.
Synthesis and in vitro antiprotozoal activity of 5-nitrothiophene-2-carboxaldehyde thiosemicarbazone derivatives.
Design, synthesis, and neuraminidase inhibitory activity of GS-4071 analogues that utilize a novel hydrophobic paradigm.
Synthesis and calpain inhibitory activity of alpha-ketoamides with 2,3-methanoleucine stereoisomers at the P2 position.
Synthesis and biological activity of a bivalent nucleotide inhibitor of ribonucleotide reductase.
Phosphonamidate and phosphothioate dipeptides as potential inhibitors of VanX.
Synthesis of glycolipid analogues that disrupt binding of HIV-1 gp120 to galactosylceramide.
Design, synthesis and antimuscarinic activity of some imidazolium derivatives.
The synthesis and anti-MRSA activity of amidinium-substituted 2-dibenzofuranylcarbapenems.
Interaction of tyrosyl aryl dipeptides with S. aureus tyrosyl tRNA synthetase: inhibition and crystal structure of a complex.
Studies towards the identification of putative bioactive conformation of potent vasodilator arylidene N-acylhydrazone derivatives.
10-omega-phenylalkyl-9(10H)-anthracenones as inhibitors of keratinocyte growth with reduced membrane damaging properties.
Resveratrol as a new type of DNA-cleaving agent.
Design and synthesis of SH3 domain binding ligands: modifications of the consensus sequence XPpXP.
Anti-AIDS agents. 31. Synthesis and anti-HIV activity of 4-substituted 3',4'-di-O-(-)-camphanoyl-(+)-cis-khellactone (DCK) thiolactone analogs.
A highly sensitive fluorogenic probe for cytochrome P450 activity in live cells.
Azaflavones compared to flavones as ligands to the benzodiazepine binding site of brain GABA(A) receptors.
4-Amino-2-cyanopyrimidines: novel scaffold for nonpeptidic cathepsin S inhibitors.
Synthesis and positive inotropic activity of N-(4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-7-yl)-2-(piperazin-1-yl)acetamide derivatives.
Tetrahydro anthranilic acid as a surrogate for anthranilic acid: application to the discovery of potent niacin receptor agonists.
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.
Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy.
Synthesis and free radical scavenging activity of some new spiropyranocoumarins.
Fluorescent 7-diethylaminocoumarin pyrrolobenzodiazepine conjugates: synthesis, DNA interaction, cytotoxicity and differential cellular localization.
Synthesis and biological evaluation of novel 1-O- and 14-O-derivatives of oridonin as potential anticancer drug candidates.
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.
P2Y1 receptor antagonists as novel antithrombotic agents.
Synthesis and QSAR studies on hypotensive 1-[3-(4-substituted phenylthio) propyl]-4-(substituted phenyl) piperazines.
Imidazo[1,2-a]pyridines: a potent and selective class of cyclin-dependent kinase inhibitors identified through structure-based hybridisation.
Synthesis and in vitro biological evaluation of aryl boronic acids as potential inhibitors of factor XIa.
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
5-((1H-pyrazol-4-yl)methylene)-2-thioxothiazolidin-4-one inhibitors of ADAMTS-5.
Synthesis and evaluation of N-acyl sulfonamides as potential prodrugs of cyclin-dependent kinase inhibitor JNJ-7706621.
(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.
Inhibition of alpha-chymotrypsin with thiol-bearing substrate analogues in the presence of zinc ion.
Synthesis and evaluation of novel bacterial rRNA-binding benzimidazoles by mass spectrometry.
Peptidyl aldehydes as slow-binding inhibitors of dual-specificity phosphatases.
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 3: 5-Substituted 3-phenyl-1,2,4-oxadiazoles as potent antagonists.
Synthesis and anticancer activity of side chain analogs of the crambescidin alkaloids.
Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity.
The total synthesis of an aurone isolated from Uvaria hamiltonii: aurones and flavones as anticancer agents.
A general synthesis of 1-aryl carbamoyl-2-alkyl-4-aryl substituted semicarbazides as nonbasic factor Xa inhibitors.
Novel thiol-based TACE inhibitors: rational design, synthesis, and SAR of thiol-containing aryl sulfonamides.
7-Hydroxynaphthalen-1-yl-urea and -amide antagonists of human vanilloid receptor 1.
Discovery of [7-(2,6-dichlorophenyl)-5-methylbenzo [1,2,4]triazin-3-yl]-[4-(2-pyrrolidin-1-ylethoxy)phenyl]amine--a potent, orally active Src kinase inhibitor with anti-tumor activity in preclinical assays.
An efficient synthesis of quinoxaline derivatives from 4-chloro-4-deoxy-alpha-D-galactose and their cytotoxic activities.
Design and synthesis of beta-methoxyacrylate analogues via click chemistry and biological evaluations.
Epibatidine isomers and analogues: structure-activity relationships.
N-hydroxyurea--a versatile zinc binding function in the design of metalloenzyme inhibitors.
Bicyclo[3.1.0]hexyl urea melanin concentrating hormone (MCH) receptor-1 antagonists: impacting hERG liability via aryl modifications.
Thiosialoside clusters using carbosilane dendrimer core scaffolds as a new class of influenza neuraminidase inhibitors.
Discovery and initial SAR of inhibitors of interleukin-1 receptor-associated kinase-4.
Depeptidization efforts on P3-P2' alpha-ketoamide inhibitors of HCV NS3-4A serine protease: effect on HCV replicon activity.
Design of novel, potent, and selective human beta-tryptase inhibitors based on alpha-keto-[1,2,4]-oxadiazoles.
Simple mono-derivatisation of the aryl moiety of D4A and DDA-based phosphoramidate prodrugs significantly enhances their anti-HIV potency in cell culture.
Synthesis and SAR of thioester and thiol inhibitors of IMP-1 metallo-beta-lactamase.
Design and synthesis of novel pyrrolobenzodiazepine (PBD) prodrugs for ADEPT and GDEPT.
Synthesis and monoamine transporter affinity of 3-aryl substituted trop-2-enes.
Solid-phase synthesis and anti-infective activity of a combinatorial library based on the natural product anisomycin.
Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
New HIV-1 replication inhibitors of the styryquinoline class bearing aroyl/acyl groups at the C-7 position: synthesis and biological activity.
Design, synthesis, and evaluation of novelly substituted benzimidazole compounds as angiotensin II receptor antagonists.
Synthesis and evaluation of piperazine and homopiperazine analogues of JS-K, an anti-cancer lead compound.
Protein tyrosine phosphatase 1B inhibitory effects of depsidone and pseudodepsidone metabolites from the Antarctic lichen Stereocaulon alpinum.
Selective urokinase-type plasminogen activator (uPA) inhibitors. Part 3: 1-isoquinolinylguanidines.
Benzimidazoles as new potent and selective DP antagonists for the treatment of allergic rhinitis.
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Synthesis and evaluation of indenopyrazoles as cyclin-dependent kinase inhibitors. Part 4: Heterocycles at C3.
Novel nonpeptidic inhibitors of HIV-1 protease obtained via a new multicomponent chemistry strategy.
Chloroquine-astemizole hybrids with potent in vitro and in vivo antiplasmodial activity.
Glucose-lowering in a db/db mouse model by dihydropyridine diacid glycogen phosphorylase inhibitors.
Synthesis of 1-methyl-3-phenylpyrazolo[4,3-b]pyridines via a methylation of 4-phthalimino-3-phenylpyrazoles and optimization toward highly potent corticotropin-releasing factor type-1 antagonists.
Pyrazolo[1,5-a]pyrimidin-7-yl phenyl amides as novel antiproliferative agents: exploration of core and headpiece structure-activity relationships.
Synthesis of caged peptides using caged lysine: application to the synthesis of caged AIP, a highly specific inhibitor of calmodulin-dependent protein kinase II.
Nitroglycosylated meso-arylporphyrins as photoinhibitors of gram positive bacteria.
Synthesis and biological evaluation of new tetrahydronaphthalene derivatives as thromboxane receptor antagonists.
Synthesis and antibacterial activity of O-methyl derivatives of azalide antibiotics: II. 6-OME derivatives via clarithromycin.
A novel synthesis of 7-aryl-8-fluoro-pyrrolo[1,2-a]pyrimid-4-ones as potent, stable GnRH receptor antagonists.
The design, synthesis and evaluation of novel HIV-1 protease inhibitors with high potency against PI-resistant viral strains.
Design and synthesis of 6-substituted amino-4-oxa-1-azabicyclo[3,2,0]heptan-7-one derivatives as cysteine proteases inhibitors.
Effect of structural modification on the inhibitory selectivity of rutaecarpine derivatives on human CYP1A1, CYP1A2, and CYP1B1.
Inhibition of ADP-triggered blood platelet aggregation by diadenosine polyphosphate analogues.
Structure determination and comparison of BM567, a sulfonylurea, with terbogrel, two compounds with dual action, thromboxane receptor antagonism and thromboxane synthase inhibition.
Design and synthesis of novel antibacterial agents with inhibitory activity against DNA polymerase III.
Synthesis and biological activity of the new 5-fluorocytosine derivatives, 5'-deoxy-N-alkyloxycarbonyl-5-fluorocytosine-5'-carboxylic acid.
1-Oxacephem-based human chymase inhibitors: discovery of stable inhibitors in human plasma.
Synthesis and antitumor activity of novel paclitaxel-chlorambucil hybrids.
Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1.
The design and synthesis of novel NK1/NK2 dual antagonists.
Beta-carbonyl substituted glutathione conjugates as inhibitors Of O. volvulus GST2.
2-Arylindole-3-acetamides: FPP-competitive inhibitors of farnesyl protein transferase.
1,8-Naphthyridines VIII. Novel 5-aminoimidazo[1,2-a] [1,8]naphthyridine-6-carboxamide and 5-amino[1,2,4]triazolo[4,3-a] [1,8]naphthyridine-6-carboxamide derivatives showing potent analgesic or anti-inflammatory activity, respectively, and completely devoid of acute gastrolesivity.
Arachidonic acid amide inhibitors of gap junction cell-cell communication.
Use of the Suzuki reaction for the synthesis of aryl-substituted heterocycles as corticotropin-releasing hormone (CRH) antagonists.
Synthesis and antibacterial activity of novel oxazolidinones with methylene oxygen- and methylene sulfur-linked substituents at C5-position.
New type of anti-diabetic compounds from the processed leaves of Hydrangea macrophylla var. thunbergii (Hydrangeae Dulcis Folium).
alpha,alpha-Cyclic aminoacids as useful scaffolds for the preparation of hNK(2) receptor antagonists.
RXR-LXR heterodimer modulators for the potential treatment of dyslipidemia.
Benzopyran sulfonamides as KV1.5 potassium channel blockers.
Bioisostere of valtrate, anti-HIV principle by inhibition for nuclear export of Rev.
Heteroaryl beta-tetralin ureas as novel antagonists of human TRPV1.
A novel series of potent cytotoxic agents targeting G2/M phase of the cell cycle and demonstrating cell killing by apoptosis in human breast cancer cells.
Design, synthesis, and structure-activity relationship studies of new phenolic DNA gyrase inhibitors.
Synthesis and cytotoxic activity of trisubstituted-1,3,5-triazines.
Novel small molecule bradykinin B1 receptor antagonists. Part 3: hydroxyurea derivatives.
Synthesis and structure-activity relationships of novel pyrimido[1,2-b]indazoles as potential anticancer agents against A-549 cell lines.
Use of 5-hydroxy-4H-benzo[1,4]oxazin-3-ones as beta2-adrenoceptor agonists.
Stereochemistry-activity relationship of orally active tetralin S1P agonist prodrugs.
Toll-like receptor 2 antagonists. Part 1: preliminary SAR investigation of novel synthetic phospholipids.
Azadideoxyadenosine: synthesis, enzymology, and anti-HIV activity.
Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1beta converting enzyme inhibitors.
Novel peptide derivatives of bleomycin A5: synthesis, antitumor activity and interaction with DNA.
Design and syntheses of melanocortin subtype-4 receptor agonists. Part 2: discovery of the dihydropyridazinone motif.
Novel 4-N-substituted aryl pent-2-ene-1,4-dione derivatives of piperazinyloxazolidinones as antibacterials.
Arylphthalazines. Part 2: 1-(Isoquinolin-5-yl)-4-arylamino phthalazines as potent inhibitors of VEGF receptors I and II.
New orally active spiro 1,2,4-trioxanes with high antimalarial potency.
In pursuit of alpha4beta2 nicotinic receptor partial agonists for smoking cessation: carbon analogs of (-)-cytisine.
Exploiting a basic chemosensitizing pharmacophore hypothesis. Part 1: synthesis and biological evaluation of novel arylbromide and bicyclic chemosensitizers against drug-resistant malaria parasites.
Identification of a 5-HT4 receptor antagonist clinical candidate through side-chain modification.
Synthesis and structure-activity relationship of N-alkyl Gly-boro-Pro inhibitors of DPP4, FAP, and DPP7.
Identification of 4-piperazin-1-yl-quinazoline template based aryl and benzyl thioureas as potent, selective, and orally bioavailable inhibitors of platelet-derived growth factor (PDGF) receptor.
Synthesis of S-alkyl L-homocysteine analogues of glutathione and their kinetic studies with gamma-glutamyl transpeptidase.
Highly diastereoselective inverse electron demand (IED) Diels-Alder reaction mediated by chiral salen-AlCl complex: the first, target-oriented synthesis of pyranoquinolines as potential antibacterial agents.
N-[18F]fluoroethylpiperidin-4-ylmethyl butyrate: a novel radiotracer for quantifying brain butyrylcholinesterase activity by positron emission tomography.
The design and synthesis of novel inhibitors of NADH:ubiquinone oxidoreductase.
N-Acridin-9-yl-butane-1,4-diamine derivatives: high-affinity ligands of the alpha2delta subunit of voltage gated calcium channels.
Novel chromene derivatives as TNF-alpha inhibitors.
Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists--Increasing selectivity over hERG.
Pharmacophore identification of KSP inhibitors.
N-Phenyl-N'-(2-chloroethyl)urea analogues of combretastatin A-4: Is the N-phenyl-N'-(2-chloroethyl)urea pharmacophore mimicking the trimethoxy phenyl moiety?
Synthesis and structure-activity relationships of thieno[2,3-d]pyrimidine-2,4-dione derivatives as potent GnRH receptor antagonists.
Structure-activity relationship (SAR) studies of quinoxalines as novel HCV NS5B RNA-dependent RNA polymerase inhibitors.
4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists.
Ureas with histamine H3-antagonist receptor activity--a new scaffold discovered by lead-hopping from cinnamic acid amides.
Kynurenic acid amides as novel NR2B selective NMDA receptor antagonists.
Synthesis, enzymatic inhibition, and cancer cell growth inhibition of novel delta-lactam-based histone deacetylase (HDAC) inhibitors.
Design and parallel synthesis of piperidine libraries targeting the nociceptin (N/OFQ) receptor.
Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: synthesis and structure-activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors.
Synthesis and structure-activity studies of novel benzocycloheptanone oxazolidinone antibacterial agents.
Novel C-3 N-urea, amide, and carbamate dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole analogs as potent TIE-2 and VEGF-R2 dual inhibitors.
Parallel strategies for the preparation and selection of liver-targeted glucocorticoid receptor antagonists.
Suitably functionalised pyrimidines as potential antimycotic agents.
Highly potent growth hormone secretagogues: hybrids of NN703 and ipamorelin.
Discovery of potent and selective succinyl hydroxamate inhibitors of matrix metalloprotease-3 (stromelysin-1).
Design and synthesis of 3-substituted benzamide derivatives as Bcr-Abl kinase inhibitors.
Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists.
Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer.
3-(5-Chloro-2,4-dihydroxyphenyl)-pyrazole-4-carboxamides as inhibitors of the Hsp90 molecular chaperone.
Structural basis for the GSK-3beta binding affinity and selectivity against CDK-2 of 1-(4-aminofurazan-3yl)-5-dialkylaminomethyl-1H-[1,2,3] triazole-4-carboxylic acid derivatives.
First small molecular inhibitors of T. brucei dolicholphosphate mannose synthase (DPMS), a validated drug target in African sleeping sickness.
Synthesis and cytotoxic activities of 6-chloro-7-arylamino-5,8-isoquinolinediones.
Macrolide biosynthesis: a single cytochrome P450, PicK, is responsible for the hydroxylations that generate methymycin, neomethymycin, and picromycin in Streptomyces venezuelae.
Purin-8-ones as corticotropin-releasing hormone (CRH-R1) receptor antagonists.
Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity.
Biological activity of fragments and analogues of the potent dimeric opioid peptide, biphalin.
High affinity, selective neurokinin 2 and neurokinin 3 receptor antagonists from a common structural template.
Sulfonamide derivatives of benzylamine block cholesterol biosynthesis in HepG2 cells: a new type of potent squalene epoxidase inhibitors.
QSAR of 1,1'-(1,2-ethylenebisbenzyl)bis(4-substitutedpyridinium) dibromides as choline kinase inhibitors: a different approach for antiproliferative drug design.
The synthesis of a new type of anthracene DNA intercalator.
Excellent acceleration of the Diels-Alder reaction by microwave irradiation for the synthesis of new fluorine-substituted ligands of NMDA receptor.
Synthesis of benzanilide derivatives as dual acting agents with alpha 1-adrenoceptor antagonistic action and steroid 5-alpha reductase inhibitory activity.
Conformationally constrained NO synthase inhibitors: rigid analogs of L-N-iminoethylornithine.
Malonyl alpha-mercaptoketones and alpha-mercaptoalcohols, a new class of matrix metalloproteinase inhibitors.
Synthesis and properties of 11-(3,5-di-tert-butyl-2-hydroxyphenylcarbamoyl)undecanoic acid, a new amphiphilic antioxidant.
Novel alpha-amino-acid phenolic ester derivatives with intravenous anaesthetic activity.
alpha(1)-Adrenoceptor agonists: the identification of novel alpha(1A )subtype selective 2'-heteroaryl-2-(phenoxymethyl)imidazolines.
Design, synthesis and biological activity of novel C2-C3' N-Linked macrocyclic taxoids.
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective alpha(V)beta(3) antagonists.
Novel 4-piperidinopyridine inhibitors of oxidosqualene cyclase-lanosterol synthase derived by consideration of inhibitor pK(a).
Discovery of (R)-1-[2-hydroxy-3-(4-hydroxy-phenyl)-propyl]-4-(4-methyl-benzyl)-piperidin-4-ol: a novel NR1/2B subtype selective NMDA receptor antagonist.
7-Pyrrolidinyl- and 7-piperidinyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
7-Alkyl- and 7-cycloalkyl-5-aryl-pyrrolo[2,3-d]pyrimidines--potent inhibitors of the tyrosine kinase c-Src.
Discovery of 1-(4-phenoxypiperidin-1-yl)-2-arylaminoethanone stearoyl-CoA desaturase 1 inhibitors.
Gypsophin: a novel alpha-glucosidase inhibitory cyclic peptide from the roots of Gypsophila oldhamiana.
Rynaxypyr: a new insecticidal anthranilic diamide that acts as a potent and selective ryanodine receptor activator.
Synthesis and structure-activity relationship of a novel, non-hydroxamate series of TNF-alpha converting enzyme inhibitors.
Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template.
Arene cis-dihydrodiols: useful precursors for the preparation of analogues of the anti-tumour agent, 2-crotonyloxymethyl-(4R,5R,6R)-4,5,6-trihydroxycyclohex-2-enone (COTC).
Imidazopiperidine amides as dipeptidyl peptidase IV inhibitors for the treatment of diabetes.
1-Alkyl-2-aryl-4-(1-naphthoyl)pyrroles: new high affinity ligands for the cannabinoid CB1 and CB2 receptors.
High dopamine transporter selectivity can be displayed by remarkably simple non-nitrogen containing inhibitors.
Binding of methoxy-substituted N1-benzenesulfonylindole analogs at human 5-HT6 serotonin receptors.
Preparation of 1-(4-methoxyphenyl)-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-ones as potent, selective and bioavailable inhibitors of coagulation factor Xa.
Discovery of novel hydroxy pyrazole based factor IXa inhibitor.
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.
Discovery of 3,3-disubstituted piperidine-derived trisubstituted ureas as highly potent soluble epoxide hydrolase inhibitors.
Synthesis of novel [1,2]-diamines with antituberculosis activity.
Application of combinatorial biocatalysis for a unique ring expansion of dihydroxymethylzearalenone.
Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.
Total synthesis and antihypertensive activity of (+/-)7,8-dihydroxy-3-methyl-isochromanone-4.
Synthesis and biological evaluation on novel analogs of 9-methylstreptimidone, an inhibitor of NF-kappaB.
Synthesis of C-8 methanesulphonate substituted pyrrolobenzodiazepines as potential antitumour agents.
Bis-azaaromatic quaternary ammonium salts as ligands for the blood-brain barrier choline transporter.
Heteroaryl-linked 5-(1H-benzimidazol-1-yl)-2-thiophenecarboxamides: potent inhibitors of polo-like kinase 1 (PLK1) with improved drug-like properties.
N-Benzylsalicylthioamides as novel compounds with promising antimycotic activity.
Novel histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine scaffold.
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors.
Tetrahydrobenzothiophene inhibitors of hepatitis C virus NS5B polymerase.
Design, synthesis, and biological evaluation of the N-diarylalkenyl-piperidinecarboxylic acid derivatives as GABA uptake inhibitors (I).
Prostaglandin phospholipid conjugates with unusual biophysical and cytotoxic properties.
Modulation of 11beta-hydroxysteroid dehydrogenase type 1 activity by 1,5-substituted 1H-tetrazoles.
Synthesis and pharmacological evaluation of 1,1,3-substituted urea derivatives as potent TNF-alpha production inhibitors.
Discovery, SAR, and X-ray structure of novel biaryl-based dipeptidyl peptidase IV inhibitors.
Isolation, structure elucidation, preparation, and biological properties of neolambertellin.
Antiviral 6-amino-quinolones: molecular basis for potency and selectivity.
Ceratinadins A-C, new bromotyrosine alkaloids from an Okinawan marine sponge Pseudoceratina sp.
Synthesis and antimicrobial activity of novel fluorine containing 4-(substituted-2-hydroxybenzoyl)-1H-pyrazoles and pyrazolyl benzo[d]oxazoles.
Design, synthesis and SAR of phenylamino-substituted 5,11-dihydro-dibenzo[a,d]cyclohepten-10-ones and 11H-dibenzo[b,f]oxepin-10-ones as p38 MAP kinase inhibitors.
Azinomycin inspired bisepoxides: influence of linker structure on in vitro cytotoxicity and DNA interstrand cross-linking.
Non-competitive inhibitors of metabotropic glutamate receptor 5 (mGluR5).
Bridgehead modification of trihalocycloheptabenzopyridine leads to a potent farnesyl protein transferase inhibitor with improved oral metabolic stability.
Synthesis and biological evaluation of gemcitabine-lipid conjugate (NEO6002).
Synthesis and neurotrophic activity of nonimmunosuppressant cyclosporin A derivatives.
Syntheses and anti-MRSA activities of the C3 analogs of mansonone F, a potent anti-bacterial sesquiterpenoid: insights into its structural requirements for anti-MRSA activity.
Human ACAT-1 and -2 inhibitory activities of saucerneol B, manassantin A and B isolated from Saururus chinensis.
Tyrokeradines A and B, new bromotyrosine alkaloids with an imidazolyl-quinolinone moiety from a verongid sponge.
Pi-delocalized beta-carbolinium cations as potential antimalarials.
Tricyclic pyridones as functionally selective human GABAA alpha 2/3 receptor-ion channel ligands.
The synthesis and structure-activity relationships of 3-amino-4-benzylquinolin-2-ones; discovery of novel KCNQ2 channel openers.
Synthesis of a novel nitroimidazole-spermidine derivative as a tumor-targeted hypoxia-selective cytotoxin.
Novel targeting strategy based on multimeric ligands for drug delivery and molecular imaging: homooligomers of alpha-MSH.
HIV-1 protease inhibitors with picomolar potency against PI-resistant HIV-1 by modification of the P1' substituent.
Evaluation of series of isobenzofuranone dimers as PKCalpha ligands: implication for the distance between the two ligand binding sites.
A novel approach to the synthesis of cytotoxic C2-C3 unsaturated pyrrolo[2,1-c]benzodiazepines (PBDs) with conjugated acrylyl C2-substituents.
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
Farnesoid X-activated receptor antagonists from a marine sponge Spongia sp.
1-Arylpiperazinyl-4-cyclohexylamine derived isoindole-1,3-diones as potent and selective alpha-1a/1d adrenergic receptor ligands.
A new class of anti-MRSA and anti-VRE agents: preparation and antibacterial activities of indole-containing compounds.
Chemically programmed antibodies: endothelin receptor targeting CovX-Bodies.
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta3 adrenergic receptor agonists.
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
Quinonic derivatives active against a virulent strain of Toxoplasma gondii. Synthesis of 2-methylfuro[2,3-g]- and [3,2-g]isoquinolinetriones.
Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists.
A convenient extension of the Wessely-Moser rearrangement for the synthesis of substituted alkylaminoflavones as neuroprotective agents in vitro.
4-Thiazolidinones: novel inhibitors of the bacterial enzyme MurB.
Synthesis and antiviral activities of N-9-oxypurine 1,3-dioxolane and 1,3-oxathiolane nucleosides.
Structure-activity relationships of biphenyl tetrazoles as metallo-beta-lactamase inhibitors.
Identification and initial structure-activity relationships of a novel non-peptide quinolone GnRH receptor antagonist.
PDE4 inhibitors: new xanthine analogues.
First synthesis of alternating SATE-phosphotriester/phosphodiester prooligonucleotides on solid support.
In vitro inhibitory effects of DNA topoisomerase II by fernane-type triterpenoids isolated from a Euphorbia genus.
Discovery of a novel series of selective MMP inhibitors: identification of the gamma-sulfone-thiols.
1,2-disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors.
Beta-analogs of PLG (L-prolyl-L-leucyl-glycinamide): ex-chiral pool syntheses and dopamine D2 receptor modulating effects.
2-Aryl-3,6-dialkyl-5-dialkylaminopyrimidin-4-ones as novel crf-1 receptor antagonists.
The antimicrobial natural product chuangxinmycin and some synthetic analogues are potent and selective inhibitors of bacterial tryptophanyl tRNA synthetase.
The synthesis and structure-activity relationships of 4-aryl-3-aminoquinolin-2-ones: a new class of calcium-dependent, large conductance, potassium (maxi-K) channel openers targeted for post-stroke neuroprotection.
Design of non-peptide CCK2 and NK1 peptidomimetics using 1-(2-nitrophenyl)thiosemicarbazide as a novel common scaffold.
Structure-activity relationships for analogues of the phenazine-based dual topoisomerase I/II inhibitor XR11576.
Initial structure-activity relationship studies of a novel series of pyrrolo[1,2-a]pyrimid-7-ones as GnRH receptor antagonists.
Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model.
Synthesis of some newer analogues of substituted dibenzoyl phenol as potent anti-inflammatory agents.
Structure-based virtual screening approach to identify novel classes of Cdc25B phosphatase inhibitors.
Studies on 1-O-acetylbritannilactone and its derivative, (2-O-butyloxime-3-phenyl)-propionyl-1-O-acetylbritannilactone ester.
Design and synthesis of bridged gamma-lactams as analogues of beta-lactam antibiotics.
Statin-derived 1,3-oxazinan-2-ones as submicromolar inhibitors of LFA-1/ICAM-1 interaction: stabilization of the metabolically labile vanillyl side chain.
SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.
MexAB-OprM specific efflux pump inhibitors in Pseudomonas aeruginosa. Part 2: achieving activity in vivo through the use of alternative scaffolds.
Synthesis and biological activity of N-Acylated ornithine analogues of daptomycin.
New anti-malarial peroxides with in vivo potency derived from spongean metabolites.
Novel, potent phenethylamide inhibitors of the hepatitis C virus (HCV) NS3 protease: probing the role of P2 aryloxyprolines with hybrid structures.
Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.
Diastereoselective synthesis of glycosylated prolines as alpha-glucosidase inhibitors and organocatalyst in asymmetric aldol reaction.
Quinazoline and benzimidazole MCH-1R antagonists.
Structure-activity relationship of benzo[b]thiophene-2-sulfonamide derivatives as novel human chymase inhibitors.
Polyoxometalates--a new class of potent ecto-nucleoside triphosphate diphosphohydrolase (NTPDase) inhibitors.
Pyrimidinone antibiotics--heterocyclic analogues with improved antibacterial spectrum.
Monocyclic thiophenes as protein tyrosine phosphatase 1B inhibitors: capturing interactions with Asp48.
ERbeta ligands. Part 5: synthesis and structure-activity relationships of a series of 4'-hydroxyphenyl-aryl-carbaldehyde oxime derivatives.
Novel 7-phenylsulfanyl-1,2,3,4,10,10a-hexahydro-pyrazino[1,2-a]indoles as dual serotonin 5-HT2C and 5-HT6 receptor ligands.
Design, synthesis and evaluation of potential inhibitors of HIV gp120-CD4 interactions.
Multidrug resistance reversal activity of permethyl ningalin B amide derivatives.
Simple aromatic compounds containing propenone moiety show considerable dual COX/5-LOX inhibitory activities.
Synthesis and antiviral activities of novel N-alkoxy-arylsulfonamide-based HIV protease inhibitors.
Synthesis and evaluation of potential inhibitors of eIF4E cap binding to 7-methyl GTP.
A proof of the specificity of kanamycin-ribosomal RNA interaction with designed synthetic analogs and the antibacterial activity.
Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Quinazolinethiones and quinazolinediones, novel inhibitors of inosine monophosphate dehydrogenase: synthesis and initial structure-activity relationships.
A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.
2-(2-[3-(pyridin-3-yloxy)phenyl]-2H-tetrazol-5-yl) pyridine: a highly potent, orally active, metabotropic glutamate subtype 5 (mGlu5) receptor antagonist.
Synthesis and cytotoxicity of water soluble quaternary salt derivatives of camptothecin.
Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status.
Synthesis and antibacterial activity of 2,4,6-tri substituted s-triazines.
Tetrahydroisoquinoline derivatives as melatonin MT2 receptor antagonists.
Synthesis and biological studies of 1-amino beta-carbolines.
New pyrazolo[3,4-d]pyrimidines endowed with A431 antiproliferative activity and inhibitory properties of Src phosphorylation.
Syntheses of sphingosine-1-phosphate analogues and their interaction with EDG/S1P receptors.
Synthesis and structure-activity relationships of 1,5-diazaanthraquinones as antitumour compounds.
A library synthesis of 4-hydroxy-3-methyl-6-phenylbenzofuran-2-carboxylic acid ethyl ester derivatives as anti-tumor agents.
Antibacterial and antiproliferative activity of cationic fullerene derivatives.
Pulicatins A-E, neuroactive thiazoline metabolites from cone snail-associated bacteria.
Tuning hydrophobicity of highly cationic tetradecameric Gramicidin S analogues using adamantane amino acids.
Ipomotaosides A-D, resin glycosides from the aerial parts of Ipomoea batatas and their inhibitory activity against COX-1 and COX-2.
Synthesis of lakshminine and antiproliferative testing of related oxoisoaporphines.
Discovery of a potent tubulin polymerization inhibitor: synthesis and evaluation of water-soluble prodrugs of benzophenone analog.
Bioassay-guided isolation of the antidiabetic principle from Sorbus decora (Rosaceae) used traditionally by the Eeyou Istchee Cree First Nations.
Rubiyunnanins C-H, cytotoxic cyclic hexapeptides from Rubia yunnanensis inhibiting nitric oxide production and NF-B activation.
Novel 34 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation.
N6-Alkyladenosines: Synthesis and evaluation of in vitro anticancer activity.
Properties and synthesis of 2-{2-fluoro (or bromo)-4-[(2-oxocyclopentyl)methyl]phenyl}propanoic acid: nonsteroidal anti-inflammatory drugs with low membrane permeabilizing and gastric lesion-producing activities.
Development of 3-aryl-1-isoquinolinamines as potent antitumor agents based on CoMFA.
Imidazo[2,1-b]thiazole carbohydrate derivatives: Synthesis and antiviral activity against Junin virus, agent of Argentine hemorrhagic fever.
3-alkylthio-1,2,4-triazine dimers with potent antimalarial activity.
Synthesis and evaluation of indole, pyrazole, chromone and pyrimidine based conjugates for tumor growth inhibitory activities--development of highly efficacious cytotoxic agents.
Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors.
Novel alkyl- and arylcarbamate derivatives with N-benzylpiperidine and N-benzylpiperazine moieties as cholinesterases inhibitors.
Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools.
Synthesis and triplex-forming ability of oligonucleotides bearing 1-substituted 1H-1,2,3-triazole nucleobases.
Aminopyridinecarboxamide-based inhaled IKK-2 inhibitors for asthma and COPD: Structure-activity relationship.
Comparison of in vitro metabolism of ticlopidine by human cytochrome P450 2B6 and rabbit cytochrome P450 2B4.
Structure-activity relationship studies on isoindoline inhibitors of dipeptidyl peptidases 8 and 9 (DPP8, DPP9): is DPP8-selectivity an attainable goal?
Fused heterocyclic M1 positive allosteric modulators.
Structure-activity relationships of carboline and carbazole derivatives as a novel class of ATP-competitive kinesin spindle protein inhibitors.
Design, synthesis and potential 6 Hz psychomotor seizure test activity of some novel 2-(substituted)-3-{[substituted]amino}quinazolin-4(3H)-one.
Design and synthesis of novel tetrahydronaphthyl azoles and related cyclohexyl azoles as antileishmanial agents.
Discovery and preliminary SARs of keto-indoles as novel indoleamine 2,3-dioxygenase (IDO) inhibitors.
'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.
Tethered thiazolidinone dimers as inhibitors of the bacterial type III secretion system.
Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.
Pleuromutilin derivatives having a purine ring. Part 2: influence of the central spacer on the antibacterial activity against Gram-positive pathogens.
Synthesis and evaluation of novel phosphoramidate prodrugs of 2'-methyl cytidine as inhibitors of hepatitis C virus NS5B polymerase.
Pseurotin A and its analogues as inhibitors of immunoglobulin E [correction of immunoglobuline E] production.
Molecular recognition of a DNA:RNA hybrid: sub-nanomolar binding by a neomycin-methidium conjugate.
N-Acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines.
Selective androgen receptor modulators based on a series of 7H-[1,4]oxazino[3,2-g]quinolin-7-ones with improved in vivo activity.
Synthesis, SAR, and Evaluation of 4-[2,4-Difluoro-5-(cyclopropylcarbamoyl)phenylamino]pyrrolo[2,1-f][1,2,4]triazine-based VEGFR-2 kinase inhibitors.
Synthesis and antitumor activity of 4-phenyl-1-arylsulfonyl imidazolidinones.
Synthesis, anti-HIV activity, and resistance profiles of ribose modified nucleoside phosphonates.
N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease.
Synthesis and screening of 3-substituted thioxanthen-9-one-10,10-dioxides.
Synthesis of benzothiazole semicarbazones as novel anticonvulsants--the role of hydrophobic domain.
A novel arginine methyltransferase inhibitor with cellular activity.
Novel ebselen-porphyrin conjugates: synthesis and nucleic acid interaction study.
Formation of an enolate intermediate is required for the reaction catalyzed by 3-hydroxyacyl-CoA dehydrogenase.
Minimum structure requirement of immunomodulatory glycolipids for predominant Th2 cytokine induction and the discovery of non-linear phytosphingosine analogs.
Cyclocondensation reaction of heterocyclic carbonyl compounds. Part XIII: synthesis and cytotoxic activity of some 3,7-diaryl-5-(3,4,5-trimethoxyphenyl)pyrazolo[4,3-e][1,2,4]triazines.
Anti-trypanosomatid benzofuroxans and deoxygenated analogues: synthesis using polymer-supported triphenylphosphine, biological evaluation and mechanism of action studies.
Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors.
Synthesis, structure and biological activity of pseudopeptidic macrolides based on an amino alcohol.
Substituted 2-aminothiopen-derivatives: a potential new class of GluR6-antagonists.
Triazole incorporated thiazoles as a new class of anticonvulsants: design, synthesis and in vivo screening.
Synthesis and serotonin transporter activity of sulphur-substituted alpha-alkyl phenethylamines as a new class of anticancer agents.
Angiotensin II--AT1 receptor antagonists: design, synthesis and evaluation of substituted carboxamido benzimidazole derivatives.
Substituted quinolinyl chalcones and quinolinyl pyrimidines as a new class of anti-infective agents.
First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.
Anti-HSV-1 activity and mechanism of action of some new synthesized substituted pyrimidine, thiopyrimidine and thiazolopyrimidine derivatives.
Synthesis and anti-HIV-1 integrase activity of modified dinucleotides.
Synthesis, characterization and in vitro pharmacology of novel pregabalin derivatives.
New isatin derivatives with antioxidant activity.
Novel rhodanine derivatives induce growth inhibition followed by apoptosis.
Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells.
Synthesis and antiviral evaluation of -D-2',3'-didehydro-2',3'-dideoxy-3'-C-hydroxymethyl nucleosides.
Synthesis and antimicrobial activity of 2-substituted [4-(1,3,4-oxadiazol-2-yl methyl)] phthalazin-1(2H)-one derivatives.
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG.
Synthesis and evaluation of tumor cell growth inhibition of methyl 3-amino-6-[(hetero)arylethynyl]thieno[3,2-b]pyridine-2-carboxylates. Structure-activity relationships, effects on the cell cycle and apoptosis.
Synthesis, structural elucidation and DNA-dependant protein kinase and antiplatelet studies of 2-amino-[5, 6, 7, 8-mono and 7, 8-di-substituted]-1,3-benzoxazines.
A clickable inhibitor reveals context-dependent autoactivation of p90 RSK.
Antihypertensive activity of newer 1,4-dihydro-5-pyrimidine carboxamides: synthesis and pharmacological evaluation.
Synthesis, characterization and antimicrobial activity of some disubstituted 1,3,4-oxadiazoles carrying 2-(aryloxymethyl)phenyl moiety.
Methylantcinate A induces tumor specific growth inhibition in oral cancer cells via Bax-mediated mitochondrial apoptotic pathway.
Synthesis and molecular modeling of novel tetrahydro--carboline derivatives with phosphodiesterase 5 inhibitory and anticancer properties.
Structure-guided development of affinity probes for tyrosine kinases using chemical genetics.
P3 optimization of functional potency, in vivo efficacy and oral bioavailability in 3-aminopyrazinone thrombin inhibitors bearing non-charged groups at the P1 position.
Synthesis and anti-Trypanosoma cruzi activity of -lapachone analogues.
Identification of potent, soluble, and orally active TRPV1 antagonists.
Synthesis and evaluation of heterobivalent tacrine derivatives as potential multi-functional anti-Alzheimer agents.
Scaffold oriented synthesis. Part 4: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing heterocycle forming and multicomponent reactions.
Synthesis and evaluation of aroylthiourea derivatives of 4--amino-4'-O-demethyl-4-desoxypodophyllotoxin as novel topoisomerase II inhibitors.
Efficient microwave-assisted synthesis of novel 3-aminohexahydrocoumarin derivatives and evaluation on their cytotoxicity.
Structure-activity relationship studies to probe the phosphoprotein binding site on the carboxy terminal domains of the breast cancer susceptibility gene 1.
Synthesis and evaluation of arylquinones as BACE1 inhibitors, -amyloid peptide aggregation inhibitors, and destabilizers of preformed -amyloid fibrils.
Design and synthesis of AApeptides: a new class of peptide mimics.
Scaffold oriented synthesis. Part 3: design, synthesis and biological evaluation of novel 5-substituted indazoles as potent and selective kinase inhibitors employing [2+3] cycloadditions.
One-pot synthesis and anticancer studies of 2-arylamino-5-aryl-1,3,4-thiadiazoles.
Exploring subtype selectivity and metabolic stability of a novel series of ligands for the benzodiazepine binding site of the GABAA receptor.
Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors.
-Carbolines and their ring-opened analogs: synthesis and evaluation against fungal and bacterial opportunistic pathogens.
The identification of a selective dopamine D2 partial agonist, D3 antagonist displaying high levels of brain exposure.
Optimization of 5-vinylaryl-3-pyridinecarbonitriles as PKCtheta inhibitors.
Synthesis and characterization of a novel iNOS/Akt inhibitor Se,Se'-1,4-phenylenebis(1,2-ethanediyl)bisisoselenourea (PBISe)--against colon cancer.
SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors.
Novel thioamide derivatives as neutral CB1 receptor antagonists.
Novel N-(3-carboxyl-9-benzyl-beta-carboline-1-yl)ethylamino acids: synthesis, anti-tumor evaluation, intercalating determination, 3D QSAR analysis and docking investigation.
2,3,5-Substituted tetrahydrofurans: COX-2 inhibitory activities of 5-hydroxymethyl-/carboxyl-2,3-diaryl-tetrahydro-furan-3-ols.
Syntheses of sphingosine-1-phosphate stereoisomers and analogues and their interaction with EDG receptors.
N-Aroyl-L-phenylalanine derivatives as VCAM/VLA-4 antagonists.
Structure-activity relationship investigations of a potent and selective benzodiazepine oxytocin antagonist.
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes.
5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition.
Synthesis and AChE inhibitory activity of new chiral tetrahydroacridine analogues from terpenic cyclanones.
Design and synthesis of Pfmrk inhibitors as potential antimalarial agents.
Discovery of a nuclease-resistant, non-natural dinucleotide that inhibits HIV-1 integrase.
Basic 3-hydroxypyridin-4-ones: potential antimalarial agents.
N-{[(6-substituted-1,3-benzothiazole-2-yl)amino]carbonothioyl}-2/4-substituted benzamides: synthesis and pharmacological evaluation.
Visual detection of AMP and real-time monitoring of cyclic nucleotide phosphodiesterase (PDE) activity in neutral aqueous solution. Chemosensor-coupled assay of PDE and PDE inhibitors.
Alkylation of manganese(II) tetraphenylporphyrin by antimalarial fluorinated artemisinin derivatives.
Structure based design: novel spirocyclic ethers as nonpeptidal P2-ligands for HIV protease inhibitors.
N1-Alkylated 3,4-dihydropyrimidine-2(1H)-ones: Convenient one-pot selective synthesis and evaluation of their calcium channel blocking activity.
Synthesis and biological evaluation of benzenesulfonamide-substituted 4-(6-alkylpyridin-2-yl)-5-(quinoxalin-6-yl)imidazoles as transforming growth factor-beta type 1 receptor kinase inhibitors.
Structure-activity relationships of novel anti-malarial agents. Part 7: N-(3-benzoyl-4-tolylacetylaminophenyl)-3-(5-aryl-2-furyl)acrylic acid amides with polar moieties.
(+/-)-2-(3-Piperidyl)-1,2,3,4-tetrahydroisoquinolines as a new class of specific bradycardic agents.
Vitamin D(3): synthesis of seco C-9,11,21-trisnor-17-methyl-1 alpha, 25-dihydroxyvitamin D(3) analogues.
8-Methoxyquinoline-5-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 3: polar functionality and its effect on anti-HIV-1 activity.
Synthesis and bioactivities of novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
SAR and species/stereo-selective metabolism of the sorbitol dehydrogenase inhibitor, CP-470,711.
Synthesis of 4-(8-benzo[1,2,5]oxadiazol-5-yl-[1,7]naphthyridine-6-yl)-benzoic acid: a potent and selective phosphodiesterase type 4D inhibitor.
Biphenyls as potent vitronectin receptor antagonists.
The identification of 8,9-dimethoxy-5-(2-aminoalkoxy-pyridin-3-yl)-benzo[c][2,7]naphthyridin-4-ylamines as potent inhibitors of 3-phosphoinositide-dependent kinase-1 (PDK-1).
Synthesis and antimicrobial studies on novel sulfonamides containing 4-azidomethyl coumarin.
Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.
New generation dopaminergic agents. 7. Heterocyclic bioisosteres that exploit the 3-OH-phenoxyethylamine D2 template.
Acylcarnitine analogues as topical, microbicidal spermicides.
Novel euglycemic and hypolipidemic agents: Part-2. Antioxidant moiety as structural motif.
Nonsteroidal progesterone receptor antagonists based on a conformationally-restricted subseries of 6-aryl-1,2-dihydro-2,2,4-trimethylquinolines.
Synthesis and biological activity of novel thiazolidinediones.
Developing a new resource for drug discovery: marine actinomycete bacteria.
Biomimetic synthesis of the IDO inhibitors exiguamine A and B.
Ring B aromatic norpimarane glucoside from a Xylaria sp.
Oroidin inhibits the activity of the multidrug resistance target Pdr5p from yeast plasma membranes.
On resin amino acid side chain attachment strategy for the head to tail synthesis of new glutamine containing gramicidin-S analogs and their antimicrobial activity.
The structure and antimalarial activity of dispiro-1,2,4,5-tetraoxanes derived from (+)-dihydrocarvone.
Tri- and tetrasubstituted imidazoles as p38 mitogen-activated protein kinase inhibitors.
Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists.
Synthesis and SAR of 2-aryl-3-aminomethylquinolines as agonists of the bile acid receptor TGR5.
Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents.
Synthesis and biological evaluation of novel coumarin-based inhibitors of Cdc25 phosphatases.
N-Substituted acetamidines and 2-methylimidazole derivatives as selective inhibitors of neuronal nitric oxide synthase.
6-Alkoxyisoindolin-1-one based dopamine D2 partial agonists as potential antipsychotics.
Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold.
Synthesis, in vitro anti-inflammatory and cytotoxic evaluation, and mechanism of action studies of 1-benzoyl--carboline and 1-benzoyl-3-carboxy--carboline derivatives.
Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase.
Azaxanthene based selective glucocorticoid receptor modulators: design, synthesis, and pharmacological evaluation of (S)-4-(5-(1-((1,3,4-thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and its methylene homologue (BMS-791826).
Rapidly photoactivatable ATP probes for specific labeling of tropomyosin within the actomyosin protein complex.
Synthesis and SAR investigations of novel 2-arylbenzimidazole derivatives as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists.
6''-Azido-6''-deoxy-UDP-N-acetylglucosamine as a glycosyltransferase substrate.
Novel -carboline-tripeptide conjugates attenuate mesenteric ischemia/reperfusion injury in the rat.
Chemical and biological explorations of the electrophilic reactivity of the bioactive marine natural product halenaquinone with biomimetic nucleophiles.
Synthesis and in vitro antitumor activity of substituted quinazoline and quinoxaline derivatives: search for anticancer agent.
Synthesis of new 3,20-bispolyaminosteroid squalamine analogues and evaluation of their antimicrobial activities.
Decahydroquinoline amides as highly selective CB2 agonists: role of selectivity on in vivo efficacy in a rodent model of analgesia.
Phenoxyacetic acids as PPAR partial agonists: synthesis, optimization, and in vivo efficacy.
Structure and property based design, synthesis and biological evaluation of -lactam based HDAC inhibitors.
Design, synthesis and structure-activity relationship of novel [3.3.1] bicyclic sulfonamide-pyrazoles as potent -secretase inhibitors.
Prodrug and covalent linker strategies for the solubilization of dual-action antioxidants/iron chelators.
Constrained phytoestrogens and analogues as ERbeta selective ligands.
Advances Toward new antidepressants beyond SSRIs: 1-aryloxy-3-piperidinylpropan-2-ols with dual 5-HT(1A) receptor antagonism/SSRI activities. Part 2.
Structure-activity study and analgesic efficacy of amino acid derivatives as N-type calcium channel blockers.
Synthesis and photodynamic action of diphenyl-2,3-dihydroxychlorin: a potential tumor photosensitizer.
Synthetic analogues of SB-219383. Novel C-glycosyl peptides as inhibitors of tyrosyl tRNA synthetase.
Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.
7-Methoxyfuro[2,3-c]pyridine-4-carboxamides as PDE4 inhibitors: a potential treatment for asthma.
Reaction of Lys-Tyr-Lys triad mimics with benzylpenicillin: insight into the role of Tyr150 in class C beta-lactamase.
Discovery of novel low molecular weight inhibitors of IMPDH via virtual needle screening.
Diamino benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. Part 6: further focus on the contracted C4'-side chain analogues.
The basal SAR of a novel insulin receptor activator.
Synthesis of polyamine derivatives having non-hypotensive Ca2 +-permeable AMPA receptor antagonist activity.
Structure-activity relationship of short-chain sphingoid bases as inhibitors of sphingosine kinase.
Metallopeptide approach to the design of biologically active ligands: design of specific human neutrophil elastase inhibitors.
Synthesis and structure-activity relationship of novel glycylcycline derivatives leading to the discovery of GAR-936.
Heterocycle-peptide hybrid compounds. Aminotriazole-containing agonists of the thrombin receptor (PAR-1).
4,4,14 alpha-trimethyl 9 beta,19-cyclo-5 alpha-26-homocholesta-24,26-dien-3 beta-ol: a potent mechanism-based inactivator of delta 24(25)- to delta 25(27)-sterol methyl transferase.
Synthesis and evaluation of 4-amino-3,4-dihydro-2H-naphthalen-1-one derivatives as mast cell stabilising and anti-inflammatory compounds.
Synthesis and antibacterial study of 10, 15, 20-triphenyl-5-(4-hydroxy-3-(trimethylammonium)methyl)phenylporphyrin as models for combination of porphyrin and alkylating agent.
A three-step synthesis from rebeccamycin of an efficient checkpoint kinase 1 inhibitor.
Synthesis and bioassay of a new class of heterocycles pyrrolyl oxadiazoles/thiadiazoles/triazoles.
Dopamine- and tyramine-based derivatives of triazenes: activation by tyrosinase and implications for prodrug design.
Peptide inhibitors of N-succinyl diaminopimelic acid aminotransferase (DAP-AT): a novel class of antimicrobial compounds.
Design and synthesis of bicyclic pyrimidinone-based HCV NS3 protease inhibitors.
Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics.
Oximino-piperidino-piperidine-based CCR5 antagonists. Part 2: synthesis, SAR and biological evaluation of symmetrical heteroaryl carboxamides.
Inhibition of glutathione S-transferase in rat hepatocytes by a glycine-tetrazole modified S-alkyl-GSH analogue.
A series of C-terminal amino alcohol dipeptide A beta inhibitors.
Exiguamide, a new spirocyclic sesquiterpene from the marine sponge Geodia exigua that inhibits cell fate specification during sea urchin embryogenesis.
Synthesis and biological activities of YkFA analogues: effects of position 4 substitutions and altered ring size on in vitro opioid activity.
Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.
Anthranilate sulfonamide hydroxamate TACE inhibitors. Part 1: Structure-based design of novel acetylenic P1' groups.
Anisylazoformylarginine: a superior assay substrate for carboxypeptidase B type enzymes.
Synthesis and structure-activity relationship study of 8-hydroxyquinoline-derived Mannich bases as anticancer agents.
Synthesis and pharmacological evaluation of novel N-alkyl/aryl substituted thiazolidinone arecoline analogues as muscarinic receptor 1 agonist in Alzheimer's dementia models.
Synthesis and bioassay of aminosulfonyl-1,3,4-oxadiazoles and their interconversion to 1,3,4-thiadiazoles.
Phenyloxazoles and phenylthiazoles as benzamide bioisosteres: synthesis and dopamine receptor binding profiles.
Use of proline bioisosteres in potential HIV protease inhibitors: phenylalanine-2-thiophenoxy-3-pyrrolidinone: synthesis and anti-HIV evaluation.
Natural product derived inhibitors of lipoprotein associated phospholipase A2, synthesis and activity of analogues of SB-253514.
Enantio- and diastereocontrolled dopamine D1, D2, D3 and D4 receptor binding of N-(3-pyrrolidinylmethyl)benzamides synthesized from aspartic acid.
2-aminomethylphenylamine as a novel scaffold for factor Xa inhibitor.
Design, synthesis and antimycobacterial activities of 1-methyl-2-alkenyl-4(1H)-quinolones.
Triterpene and sterol derivatives from the roots of Breynia fruticosa.
Design, synthesis and inhibition activity of a novel cyclic enediyne amino acid conjugates against MPtpA.
Thiazole-based chalcones as potent antimicrobial agents. Synthesis and biological evaluation.
A class of 5-benzylidene-2-phenylthiazolinones with high potency as direct 5-lipoxygenase inhibitors.
In vitro anti-rotavirus activity of polyphenol compounds isolated from the roots of Glycyrrhiza uralensis.
Design, synthesis, and evaluation of dibenzo[c,h][1,6]naphthyridines as topoisomerase I inhibitors and potential anticancer agents.
Triterpenoids from Aglaia abbreviata and their cytotoxic activities.
Synthesis and in vitro antibacterial activity of fluoroquinolone derivatives containing 3-(N'-alkoxycarbamimidoyl)-4-(alkoxyimino) pyrrolidines.
Discovery of novel GSK-3 inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening.
Parallel synthesis, evaluation, and preliminary structure-activity relationship of 2,5-diamino-1,4-benzoquinones as a novel class of bivalent anti-prion compound.
Synthesis of 4-N-polyaromatic substituted podophyllotoxins: DNA topoisomerase inhibition, anticancer and apoptosis-inducing activities.
Synthesis and structure-activity relationship of tetrahydropyrazolopyrimidine derivatives--a novel structural class of potent calcium-sensing receptor antagonists.
Structure-activity relationships of pyrrole based S-nitrosoglutathione reductase inhibitors: pyrrole regioisomers and propionic acid replacement.
7-Oxopyrrolopyridine-derived DPP4 inhibitors-mitigation of CYP and hERG liabilities via introduction of polar functionalities in the active site.
Synthesis and in vitro antiprotozoal activities of 5-phenyliminobenzo[a]phenoxazine derivatives.
The selective P-TEFb inhibitor CAN508 targets angiogenesis.
Synthesis and effects of some novel tetrahydronaphthalene derivatives on proliferation and nitric oxide production in lipopolysaccharide activated Raw 264.7 macrophages.
Triterpenoids with rare carbon skeletons from Salvia hydrangea: antiprotozoal activity and absolute configurations.
Synthesis, antimicrobial activity and possible mechanism of action of 9-bromo-substituted indolizinoquinoline-5,12-dione derivatives.
Simplification of the tetracyclic SIRT1-selective inhibitor MC2141: coumarin- and pyrimidine-based SIRT1/2 inhibitors with different selectivity profile.
4-Aminothiazolyl analogs of GE2270 A: design, synthesis and evaluation of imidazole analogs.
A new quinoline derivative with cytotoxic activity from Streptomyces sp. neau50.
Design and synthesis of pyridin-2-yloxymethylpiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Synthesis and antibacterial evaluation of novel clarithromycin derivatives with C-4 elongated arylalkyl groups against macrolide-resistant strains.
Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes.
Synthesis and structure-activity relationships of open D-Ring galanthamine analogues.
2,3,4,5-tetrahydro- and 2,3,4,5,11,11a-hexahydro-1H-[1,4]diazepino[1,7-a]indoles: new templates for 5-HT(2C) agonists.
Prodrugs to enhance central nervous system effects of the TRH-like peptide pGlu-Glu-Pro-NH2.
Cancer chemotherapy: a SN-38 (7-ethyl-10-hydroxycamptothecin) glucuronide prodrug for treatment by a PMT (Prodrug MonoTherapy) strategy.
4,4-Disubstituted cyclohexylamine NK(1) receptor antagonists II.
Acylcyclohexanedione derivatives as potential in vivo sequential inhibitors of 4-hydroxyphenylpyruvate dioxygenase and GA(20) 3beta-hydroxylase.
New leads for selective inhibitors of alpha-L-fucosidases. Synthesis and glycosidase inhibitory activities of [(2R,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]furan derivatives.
Two selective novel triterpene glycosides from sea cucumber, Telenata Ananas: inhibitors of chemokine receptor-5.
Potent in vitro methicillin-resistant Staphylococcus aureus activity of 2-(1H-indol-3-yl)quinoline derivatives.
Ester and hydroxamate analogues of methionyl and isoleucyl adenylates as inhibitors of methionyl-tRNA and isoleucyl-tRNA synthetases.
2,4,5-Trisubstituted imidazoles: novel nontoxic modulators of P-glycoprotein mediated multidrug resistance. Part 2.
Chlorophenylmethyl benzothiadiazine dioxides derivatives: potent human cytomegalovirus inhibitors.
Substituted piperidines--highly potent renin inhibitors due to induced fit adaptation of the active site.
Synthesis and antimicrobial activity of novel globomycin analogues.
Synthesis of the first examples of A-C8/C-C2 amide-Linked pyrrolo[2,1-c][1,4]benzodiazepine dimers.
A four component coupling strategy for the synthesis of D-phenylglycinamide-derived non-covalent factor Xa inhibitors.
Pyridopyrimidine analogues as novel adenosine kinase inhibitors.
Solid-phase synthesis of di- and tripeptidic hydroxamic acids as inhibitors of procollagen C-proteinase.
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Benzenesulfonamide derivatives of 2-substituted 4H-3,1-benzoxazin-4-ones and benzthiazin-4-ones as inhibitors of complement C1r protease.
Studies towards the identification of potent, selective and bioavailable thrombin inhibitors.
Membrane-permeant, bioactivatable analogues of cGMP as inducers of cell death in IPC-81 leukemia cells.
Exploration of beta-turn scaffolding motifs as components of sialyl Le(X) mimetics and their relevance to P-selectin.
Synthesis and immunosuppressant activity of pyrazole carboxamides.
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
Fecal excretion pattern of bile acids in rats fed high fat diets and neomycin in induced colon tumorigenesis.
Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives.
Synthesis and metabotropic glutamate receptor activity of a 2-aminobicyclo[3.2.0]heptane-2,5-dicarboxylic acid, a molecule possessing an extended glutamate conformation.
First hydroxamate inhibitors for carboxypeptidase A. N-acyl-N-hydroxy-beta-phenylalanines.
A macrolactone from benzo[a]phenazine with potent activity against Mycobacterium tuberculosis.
Sulfonamide-based hydroxamic acids as potent inhibitors of mouse macrophage metalloelastase.
Pyrazoles, 1,2,4-triazoles, and tetrazoles as surrogates for cis-amide bonds in boronate ester thrombin inhibitors.
Homoisofagomines: chemical-enzymatic synthesis and evaluation as alpha- and beta-glucosidase inhibitors.
Molecular design, synthesis, and structure-Activity relationships leading to the potent and selective p56(lck) inhibitor BMS-243117.
Substituted 4-(2,2-diphenylethyl)pyridine-N-oxides as phosphodiesterase-4 inhibitors: SAR study directed toward the improvement of pharmacokinetic parameters.
Inhibitors of human neutrophil elastase based on a highly functionalized N-amino-4-imidazolidinone scaffold.
Synthesis and pharmacological evaluation of 6-piperidino- and 6-piperazinoalkyl-2(3H)-benzothiazolones as mixed sigma/5-HT(1A) ligands.
Regioselective hydrostannation of diarylalkynes directed by a labile ortho bromine atom: an easy access to stereodefined triarylolefins, hybrids of combretastatin A-4 and isocombretastatin A-4.
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.
Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: discovery of potent ligands for a variety of G-protein coupled receptors.
Synthesis of essramycin and comparison of its antibacterial activity.
Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors.
Discovery of 4-(5-(cyclopropylcarbamoyl)-2-methylphenylamino)-5-methyl-N-propylpyrrolo[1,2-f][1,2,4]triazine-6-carboxamide (BMS-582949), a clinical p38 MAP kinase inhibitor for the treatment of inflammatory diseases.
Synthesis, in vitro and in vivo biological evaluation, and comprehensive understanding of structure-activity relationships of dipeptidyl boronic acid proteasome inhibitors constructed from -amino acids.
Electron density guided fragment-based lead discovery of ketohexokinase inhibitors.
Discovery of molecular switches within the ADX-47273 mGlu5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu5 NAMs, PAMs and partial antagonists.
Identification of the first non-peptidic small molecule inhibitor of the c-Abl/14-3-3 protein-protein interactions able to drive sensitive and Imatinib-resistant leukemia cells to apoptosis.
Development of molecular probes for the human 5-HT(6) receptor.
A stereo-controlled synthesis of 2,4-dimethyl-4-hydroxy-16-phenylhexadecanoic acid 1,4-lactone and its PPAR activities.
Design, synthesis and evaluation of novel tacrine-multialkoxybenzene hybrids as dual inhibitors for cholinesterases and amyloid beta aggregation.
Steroidal saponins from fresh stems of Dracaena angustifolia.
Identification of a specific inhibitor of the histone methyltransferase SU(VAR)3-9.
Targeted mutations of Bacillus anthracis dihydrofolate reductase condense complex structureactivity relationships.
blaROB-1 presence on pB1000 in Haemophilus influenzae is widespread, and variable cefaclor resistance is associated with altered penicillin-binding proteins.
Synthesis and biological evaluation of [D-lysine]8cyclosporin A analogs as potential anti-HCV agents.
Species independence in brain tissue binding using brain homogenates.
Design of HIV-1 protease inhibitors with C3-substituted hexahydrocyclopentafuranyl urethanes as P2-ligands: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.
Discovery of new inhibitor for PDE3 by virtual screening.
Synthesis and evaluation of monoamidoxime derivatives: toward new antileishmanial compounds.
SAR studies on dihydropyrimidinone antibiotics.
Efficient synthesis of triazole moiety-containing nucleotide analogs and their inhibitory effects on a malic enzyme.
Synthesis and evaluation of [(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]cyclohexanes and 4-[(1R)-1-amino-2-(2,5-difluorophenyl)ethyl]piperidines as DPP-4 inhibitors.
Synthesis and biological evaluation of a novel human stem/progenitor cells proliferation activator: 4-(4-(5-mercapto-1,3,4-oxadiazol-2-yl)phenyl) thiosemicarbazide (Stemazole).
Phenolic compounds from the roots of Jordanian viper's grass, Scorzonera judaica.
Synthesis and antiproliferative activity of new cytotoxic azanaphthoquinone pyrrolo-annelated derivatives: Part II.
Biological evaluation of 3'-O-alkylated analogs of salacinol, the role of hydrophobic alkyl group at 3' position in the side chain on the -glucosidase inhibitory activity.
Phellinstatin, a new inhibitor of enoyl-ACP reductase produced by the medicinal fungus Phellinus linteus.
Sorafenib derivatives induce apoptosis through inhibition of STAT3 independent of Raf.
Novel aminopeptidase N (APN/CD13) inhibitors derived from chloramphenicol amine.
Synthesis of 1-(2,6-dichlorophenyl)-3-methylene-1,3-dihydro-indol-2-one derivatives and in vitro anticancer evaluation against SW620 colon cancer cell line.
Synthesis and structure guided evaluation of estrogen agonist and antagonist activities of some new tetrazolyl indole derivatives.
Synthesis and biological activities of some new fluorinated coumarins and 1-aza coumarins.
Synthesis and cytotoxicity evaluation of some benzimidazole-4,7-diones as bioreductive anticancer agents.
Novel 8-deaza-5,6,7,8-tetrahydroaminopterin derivatives as dihydrofolate inhibitor: design, synthesis and antifolate activity.
Synthesis of 2-substituted-N-[4-(1-methyl-4,5-diphenyl-1H-imidazole-2-yl)phenyl]acetamide derivatives and evaluation of their anticancer activity.
Simple oxidation of pyrimidinylhydrazones to triazolopyrimidines and their inhibition of Shiga toxin trafficking.
Alkyl and dialkylaminoethyl derivatives of 5-amino-2-azabicyclo[3.2.2]nonanes and their antiplasmodial and antitrypanosomal activities.
Discovery of potential new InhA direct inhibitors based on pharmacophore and 3D-QSAR analysis followed by in silico screening.
Condensed bridgehead nitrogen heterocyclic system: synthesis and pharmacological activities of 1,2,4-triazolo-[3,4-b]-1,3,4-thiadiazole derivatives of ibuprofen and biphenyl-4-yloxy acetic acid.
Antiplasmodial and antitrypanosomal activities of aminobicyclo[2.2.2]octyl omega-aminoalkanoates.
Selenium containing heterocycles: synthesis, anti-inflammatory, analgesic and anti-microbial activities of some new 4-cyanopyridazine-3(2H)selenone derivatives.
Synthesis of N-(5,7-diamino-3-phenyl-quinoxalin-2-yl)-3,4,5-substituted anilines and N-[4[(5,7-diamino-3-phenylquinoxalin-2-yl)amino]benzoyl]-l-glutamic acid diethyl ester: evaluation of in vitro anti-cancer and anti-folate activities.
Design and synthesis of phosphotyrosine mimetics.
Studies towards the next generation of antidepressants. Part 1: Indolylcyclohexylamines as potent serotonin reuptake inhibitors.
The S-alkyl chain length as a determinant of the anti-leukemic activity of cysteine chloromethyl ketone compounds.
Synthesis and biological activity of novel macrocyclic antifungals. modification of the tyrosine moiety of the lipopeptidolactone FR901469.
Synthesis and biological activity of substituted bis-(4-hydroxyphenyl)methanes as N-type calcium channel blockers.
Molecular structure of FR901277, a novel inhibitor of human leukocyte elastase, and its binding mode simulation.
Modified synthesis and antiangiogenic activity of linomide.
1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.
Synthesis of glucuronides of multidrug resistance reversing drug MS-209.
Synthesis and antiviral evaluation of nucleic acid-based (NAB) libraries.
Anti-oxidant, anti-fungal and anti-leishmanial activities of novel 3-[4-(1H-imidazol-1-yl) phenyl]prop-2-en-1-ones.
Synthesis and biological evaluation of conformationally restricted Gabapentin analogues.
Synthesis and pharmacological activity of diarylindole derivatives. Cytotoxic agents based on combretastatins.
Solid-phase synthesis of novel inhibitors of farnesyl transferase.
Stereoselective synthesis and receptor activity of conformationally defined retinoid X receptor selective ligands.
Inhibition of 4-hydroxyphenylpyruvate dioxygenase by sethoxydim, a potent inhibitor of acetyl-coenzyme A carboxylase.
Benzylamine-based selective and orally bioavailable inhibitors of thrombin.
Design of novel tripeptides with macrophage migration-enhancing activity.
The development of novel and selective p56lck tyrosine kinase inhibitors.
Synthesis and antiviral activity of novel isodideoxy nucleosides with exocyclic methylene.
The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues.
Preparation of 9-deoxo-4"-deoxy-6,9-epoxyerythromycin lactams "motilactides": potent and orally active prokinetic agents.
New synthetic analogues of N-acyl homoserine lactones as agonists or antagonists of transcriptional regulators involved in bacterial quorum sensing.
Novel pyrimidines as acid pump antagonists (APAs).
2-, 3-, and 4-(1-Oxo-1H-2,3-dihydroisoindol-2-yl)benzoic acids and their corresponding organotin carboxylates: synthesis, characterization, fluorescent, and biological activities.
Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents.
Synthesis and in vitro anti-hepatitis B virus activity of six-membered azanucleoside analogues.
Cytotoxic isomalabaricane derivatives and a monocyclic triterpene glycoside from the sponge Rhabdastrella globostellata.
Indapamide-like benzenesulfonamides as inhibitors of carbonic anhydrases I, II, VII, and XIII.
Rational design and synthesis of potent aminoglycoside antibiotics against resistant bacterial strains.
Synthesis of sugar-amino acid-nucleosides as potential glycosyltransferase inhibitors.
Synthesis and pharmacological evaluation of 4-(3,4-dichlorophenyl)-N-methyl-1,2,3,4-tetrahydronaphthalenyl amines as triple reuptake inhibitors.
Rational design, synthesis, and evaluation of new selective inhibitors of microbial class II (zinc dependent) fructose bis-phosphate aldolases.
Direct renin inhibitors as a new therapy for hypertension.
Medicinal chemistry as a conduit for the modulation of quorum sensing.
Design, synthesis and biological evaluation of small molecule inhibitors of CD4-gp120 binding based on virtual screening.
NF kappa B inhibitors and antitrypanosomal metabolites from endophytic fungus Penicillium sp. isolated from Limonium tubiflorum.
Flow cytometry as a tool to determine the effects of cell wall-active antibiotics on vancomycin-susceptible and -resistant Enterococcus faecalis strains.
Evolution from a natural flavones nucleus to obtain 2-(4-Propoxyphenyl)quinoline derivatives as potent inhibitors of the S. aureus NorA efflux pump.
Mapping the intestinal alpha-glucogenic enzyme specificities of starch digesting maltase-glucoamylase and sucrase-isomaltase.
Synthesis of new vitamin K analogues as steroid and xenobiotic receptor (SXR) agonists: insights into the biological role of the side chain part of vitamin K.
Novel 3,5-bis(bromohydroxybenzylidene)piperidin-4-ones as coactivator-associated arginine methyltransferase 1 inhibitors: enzyme selectivity and cellular activity.
Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.
Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors.
Novel thiophenyl C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.
Synthesis of new six- and seven-membered 1-N-iminosugars as promising glycosidase inhibitors.
Engineering an antibiotic to fight cancer: optimization of the novobiocin scaffold to produce anti-proliferative agents.
Cytotoxic ring A-modified steroid analogues derived from Grundmann's ketone.
Thiazole- and imidazole-containing peptidomimetic inhibitors of protein farnesyltransferase.
Antifungal thiopeptide cyclothiazomycin B1 exhibits growth inhibition accompanying morphological changes via binding to fungal cell wall chitin.
Synthesis and in vitro evaluation of ambrisentan analogues as potential endothelin receptor antagonists.
Anticonvulsant 4-aminobenzenesulfonamide derivatives with branched-alkylamide moieties: X-ray crystallography and inhibition studies of human carbonic anhydrase isoforms I, II, VII, and XIV.
Synthesis and anti-inflammatory evaluation of some condensed [4-(3,4-dimethylphenyl)-1(2H)-oxo-phthalazin-2-yl]acetic acid hydrazide.
Synthesis and in vitro microbiological evaluation of novel 4-aryl-5-isopropoxycarbonyl-6-methyl-3,4-dihydropyrimidinones.
Synthesis of glycose carbamides and evaluation of the induction of erythroid differentiation of human erythroleukemic K562 cells.
Knowledge based identification of MAO-B selective inhibitors using pharmacophore and structure based virtual screening models.
Computational modeling and surface plasmon resonance analyses in the assessment of peptide ligands interacting with fibrin gamma(312-324) epitope.
Design, synthesis and biological evaluation of novel fluorinated docetaxel analogues.
Synthesis, antileukemic and antiplatelet activities of 2,3-diaryl-6,7-dihydro-5H-1,4-diazepines.
QSAR analysis of PPAR-gamma agonists as anti-diabetic agents.
Lead discovery of alpha,beta-unsaturated sulfones from a combinatorial library as inhibitors of inducible VCAM-1 expression.
Functional expression and characterization of EryA, the erythritol kinase of Brucella abortus, and enzymatic synthesis of L-erythritol-4-phosphate.
Inhibition of inosine monophosphate dehydrogenase (IMPDH) by 2-[2-(Z)-fluorovinyl]inosine 5'-monophosphate.
Synthesis and muscarinic M2 subtype antagonistic activity of unnatural ent-himbacine and an enantiomeric pair of (2'S,6'R)-diepihimbacine.
Anti-tubercular agents. Part 5: synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners.
Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Structure-based design, chemistry and activity evaluation. II.
Synthesis and evaluation of some new benzothiazole derivatives as potential antimicrobial agents.
N-acyloxymethyl carbamate linked prodrugs of pseudomycins are novel antifungal agents.
Diaminopurine-acridine heterodimers for specific recognition of abasic site containing DNA. Influence on the biological activity of the position of the linker on the purine ring.
Identification of potent and selective oxytocin antagonists. Part 2: further investigation of benzofuran derivatives.
Antifungal sordarins. part 3: synthesis and structure-activity relationships of 2',3'-fused oxirane derivatives.
Synthesis of analogues of the O-beta-D-ribofuranosyl nucleoside moiety of liposidomycins. Part 1: contribution of the amino group and the uracil moiety upon the inhibition of MraY.
Identification and characterization of a potential ischemia-selective N-methyl-D-aspartate (NMDA) receptor ion-channel blocker, CNS 5788.
Synthesis of substituted 4(Z)-(methoxyimino)pentyl-1-piperidines as dual NK1/NK2 inhibitors.
The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.
Novel and potent tacrine-related hetero- and homobivalent ligands for acetylcholinesterase and butyrylcholinesterase.
Solid phase synthesis of diamides as potential bone resorption inhibitors.
Bifunctional alkylating agents derived from duocarmycin SA: potent antitumor activity with altered sequence selectivity.
The design, synthesis and activity of non-ATP competitive inhibitors of pp60(c-src) tyrosine kinase. Part 2: hydroxyindole derivatives.
Non-peptidic, non-prenylic inhibitors of the prenyl protein-specific protease Rce1.
Synthesis, characterization and biological activity of some new 1,3,4-oxadiazole bearing 2-flouro-4-methoxy phenyl moiety.
Mechanism-based inactivation of thymidylate synthase by 5-(3-fluoropropyn-1-yl)-2'-deoxyuridine 5'-phosphate.
Construction of HIV Rev peptides containing peptide nucleic acid that bind HIV RRE IIB RNA.
Design and biological evaluation of non-peptide analogues of omega-conotoxin MVIIA.
Human chymase inhibitors based on the 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold.
Novel quinolinequinone antitumor agents: structure-metabolism studies with NAD(P)H:quinone oxidoreductase (NQO1).
6-Bicyclopiperazinyl-1-arylsulfonylindoles and 6-bicyclopiperidinyl-1-arylsulfonylindoles derivatives as novel, potent, and selective 5-HT6 receptor antagonists.
(3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents.
Update on fusidic acid (CEM-102) tested against Neisseria gonorrhoeae and Chlamydia trachomatis.
Synthesis and characterization of novel indole derivatives reveal improved therapeutic agents for treatment of ischemia/reperfusion (I/R) injury.
Orally active MMP-1 sparing -tetrahydropyranyl and -piperidinyl sulfone matrix metalloproteinase (MMP) inhibitors with efficacy in cancer, arthritis, and cardiovascular disease.
Oritavancin disrupts membrane integrity of Staphylococcus aureus and vancomycin-resistant enterococci to effect rapid bacterial killing.
A systematic protocol for the characterization of Hsp90 modulators.
Reservoir of antimicrobial resistance determinants associated with horizontal gene transfer in clinical isolates of the genus Shewanella.
Synthesis and biological evaluation of diastereoisomerically pure N,O-nucleosides.
Lysyl-phosphatidylglycerol attenuates membrane perturbation rather than surface association of the cationic antimicrobial peptide 6W-RP-1 in a model membrane system: implications for daptomycin resistance.
Synthesis and biological evaluation of 7-substituted-1-(3-bromophenylamino)isoquinoline-4-carbonitriles as inhibitors of myosin light chain kinase and epidermal growth factor receptor.
1,6-AnhMurNAc derivatives for assay development of amidase AmiD.
The ABC transporter AnrAB contributes to the innate resistance of Listeria monocytogenes to nisin, bacitracin, and various beta-lactam antibiotics.
Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer.
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
Effect of carbohydrate amino group modifications on the cytotoxicity of glycosylated 2-phenyl-benzo[b]thiophenes and 2-phenyl-benzo[b]furans.
Design and synthesis of novel CCR2 antagonists: investigation of non-aryl/heteroaryl binding motifs.
Novel imidazo[4,5-b]pyridine and triaza-benzo[c]fluorene derivatives: synthesis, antiproliferative activity and DNA binding studies.
I. Novel HCV NS5B polymerase inhibitors: discovery of indole 2-carboxylic acids with C3-heterocycles.
Positive GABA(A) receptor modulators from Acorus calamus and structural analysis of (+)-dioxosarcoguaiacol by 1D and 2D NMR and molecular modeling.
Synthesis and SERCA activities of structurally simplified cyclopiazonic acid analogues.
Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.
Coprismycins A and B, neuroprotective phenylpyridines from the dung beetle-associated bacterium, Streptomyces sp.
Design of benzimidazole- and benzoxazole-2-thione derivatives as inhibitors of bacterial hyaluronan lyase.
Effect of 4-aryl-2-methyl-5-nitro-1,4-dihydropyridine-3-carboxylates on the guinea pig papillary muscle and isolated human vena saphena magna that is used for coronary artery bypass grafting.
Discovery of a series of imidazo[4,5-b]pyridines with dual activity at angiotensin II type 1 receptor and peroxisome proliferator-activated receptor-.
Synthesis and anticonvulsant activity of new N-Mannich bases derived from 5-cyclopropyl-5-phenyl- and 5-cyclopropyl-5-(4-chlorophenyl)-imidazolidine-2,4-diones.
6-Substituted imidazo[1,2-a]pyridines: synthesis and biological activity against colon cancer cell lines HT-29 and Caco-2.
From benzimidazole to indole-5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase. Part 1: indole C-2 SAR and discovery of diamide derivatives with nanomolar potency in cell-based subgenomic replicons.
Inhibition of the cellular function of perforin by 1-amino-2,4-dicyanopyrido[1,2-a]benzimidazoles.
5a-Carba--D-glucopyranose derivatives as novel sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Novel derivatives of 6-mercaptopurine: synthesis, characterization and antiproliferative activities of S-allylthio-mercaptopurines.
Classification of estrogen receptor-beta ligands on the basis of their binding affinities using support vector machine and linear discriminant analysis.
Synthesis of non-natural C2-homo-ceramide and its apoptotic activity against HL-60 cells.
Synthesis and activity of a novel class of tribasic macrocyclic antibiotics: the triamilides.
Inhibitors of the RET tyrosine kinase based on a 2-(alkylsulfanyl)-4-(3-thienyl)nicotinonitrile scaffold.
Captopril and 6-mercaptopurine: whose SH possesses higher antioxidant ability?
Enaminonitrile in heterocyclic synthesis: synthesis and antimicrobial evaluation of some new pyrazole, isoxazole and pyrimidine derivatives incorporating a benzothiazole moiety.
Novel 4H-1,3,4-oxadiazin-5(6H)-ones with hydrophobic and long alkyl chains: design, synthesis, and bioactive diversity on inhibition of monoamine oxidase, chitin biosynthesis and tumor cell.
Flexible computational docking studies of new aminoglycosides targeting RNA 16S bacterial ribosome site.
The novel phosphoramidate derivatives of NSAID 3-hydroxypropylamides: synthesis, cytostatic and antiviral activity evaluations.
Regiospecific microwave-assisted synthesis and cytotoxic activity against human breast cancer cells of (RS)-6-substituted-7- or 9-(2,3-dihydro-5H-1,4-benzodioxepin-3-yl)-7H- or -9H-purines.
Development of a phosphatase-stable phosphotyrosyl mimetic suitably protected for the synthesis of high-affinity Grb2 SH2 domain-binding ligands.
Synthesis and evaluation of novel pyrrolidinyl sordaricin derivatives as antifungal agents.
Synthesis and antioxidant activity of quinolinobenzothiazinones.
On the relationship of OSW-1 to the cephalostatins.
Simplification of adenophostin A defines a minimal structure for potent glucopyranoside-based mimics of D-myo-inositol 1,4,5-trisphosphate.
Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists.
NMR and topochemical studies of peptidomimetic HIV-I protease inhibitors containing a cis-epoxide amide isostere.
Synthesis, SAR and pharmacology of CP-293,019: a potent, selective dopamine D4 receptor antagonist.
Potent HIV protease inhibitors incorporating high-affinity P2-ligands and (R)-(hydroxyethylamino)sulfonamide isostere.
Solid phase organic synthesis of polyamine derivatives and initial biological evaluation of their antitumoral activity.
1-[omega-(4-arylpiperazin-1-yl)alkyl]-3-diphenylmethylene-2,5- pyrrolidinediones as 5-HT1A receptor ligands: study of the steric requirements of the terminal amide fragment on 5-HT1A affinity/selectivity.
Use of the 1,2,5-thiadiazolidin-3-one 1,1 dioxide and isothiazolidin-3-one 1,1 dioxide scaffolds in the design of potent inhibitors of serine proteinases.
DNA cleavage by 7-methylbenzopentathiepin: a simple analog of the antitumor antibiotic varacin.
Novel quinolone derivatives as potent antibacterials.
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 1.
Phenylcyanoguanidines as inhibitors of glucose-induced insulin secretion from beta cells.
A mechanism-based affinity-labeling agent for possible use in isolating N-acetylglucosaminidase.
Anti-Helicobacter pylori agents endowed with H2-antagonist properties.
Novel bicyclic lactam inhibitors of thrombin: potency and selectivity optimization through P1 residues.
Effect of C2/C3-endo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines.
Effect of C2-exo unsaturation on the cytotoxicity and DNA-binding reactivity of pyrrolo[2,1-c][1,4]benzodiazepines.
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones.
Amino acid phosphoramidate nucleosides: potential ADEPT/GDEPT substrates.
Total synthesis and antifungal activity of 9-methoxystrobilurin L as the originally proposed 1,4-benzodioxan structure.
Identification of a reduction product of aristolochic acid: implications for the metabolic activation of carcinogenic aristolochic acid.
Cytotoxic triterpenoids from Maytenus retusa.
Acylideneoxoindoles: a new class of reversible inhibitors of human transglutaminase 2.
Synthesis of chroman aldehydes that inhibit HIV.
(R)-/(S)-10-camphorsulfonyl-substituted aromatic/heterocyclic sulfonamides selectively inhibit mitochondrial over cytosolic carbonic anhydrases.
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
Synthesis, biological evaluation and molecular modeling of novel triazole-containing berberine derivatives as acetylcholinesterase and -amyloid aggregation inhibitors.
Dihydro--agarofuran sesquiterpenes isolated from Celastrus vulcanicola as potential anti-Mycobacterium tuberculosis multidrug-resistant agents.
Synthesis and pharmacological characterization of bicyclic triple reuptake inhibitor 3-aryl octahydrocyclopenta[c]pyrrole analogues.
Discovery of non-peptide, small molecule antagonists of 910 nicotinic acetylcholine receptors as novel analgesics for the treatment of neuropathic and tonic inflammatory pain.
Synthesis and biological evaluation of 4-styrylcoumarin derivatives as inhibitors of TNF- and IL-6 with anti-tubercular activity.
Synthesis and proteasome inhibition of lithocholic acid derivatives.
Synthesis of antimitotic thioglycosides: in vitro and in vivo evaluation of their anticancer activity.
6-Benzoyl-3-hydroxypyrimidine-2,4-diones as dual inhibitors of HIV reverse transcriptase and integrase.
Synthesis and biological evaluation of ()-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.
2-Arylimidazo[2,1-b]benzothiazoles: a new family of amyloid binding agents with potential for PET and SPECT imaging of Alzheimer's brain.
Revisiting glitazars: thiophene substituted oxazole containing -ethoxy phenylpropanoic acid derivatives as highly potent PPAR/ dual agonists devoid of adverse effects in rodents.
Maintaining potent HTLV-I protease inhibition without the P3-cap moiety in small tetrapeptidic inhibitors.
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Oxadiazole derivatives containing 1,4-benzodioxan as potential immunosuppressive agents against RAW264.7 cells.
Identification of ostruthin from Peucedanum ostruthium rhizomes as an inhibitor of vascular smooth muscle cell proliferation.
Identification of 3-aminomethyl-1,2-dihydro-4-phenyl-1-isoquinolones: a new class of potent, selective, and orally active non-peptide dipeptidyl peptidase IV inhibitors that form a unique interaction with Lys554.
Synthesis and biological activity of optically active phenylbutenoid dimers.
Sesquiterpene and xanthone derivatives from the sea fan-derived fungus Aspergillus sydowii PSU-F154.
The combination of 4-anilinoquinazoline and cinnamic acid: a novel mode of binding to the epidermal growth factor receptor tyrosine kinase.
Discovery of potent, selective, and orally bioavailable quinoline-based dipeptidyl peptidase IV inhibitors targeting Lys554.
Ieodomycins A-D, antimicrobial fatty acids from a marine Bacillus sp.
Design and synthesis of simplified taxol analogs based on the T-Taxol bioactive conformation.
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
Synthesis, anti-tuberculosis activity and 3D-QSAR study of amino acid conjugates of 4-(adamantan-1-yl) group containing quinolines.
Synthesis and antimalarial activity of new atovaquone derivatives.
Synthesis and antiproliferative activity of oxazinocarbazole and N,N-bis(carbazolylmethyl)amine derivatives.
Pyrimido[1,2-a]quinoxaline 6-oxide and phenazine 5,10-dioxide derivatives and related compounds as growth inhibitors of Trypanosoma cruzi.
Bioactivities of a series of phosphodiesterase type 5 (PDE-5) inhibitors as modelled by MIA-QSAR.
Novel 2-aryl-naphtho[1,2-d]oxazole derivatives as potential PTP-1B inhibitors showing antihyperglycemic activities.
Solvatochromism, DNA binding, antitumor activity and molecular modeling study of mixed-ligand copper(II) complexes containing the bulky ligand: bis[N-(p-tolyl)imino]acenaphthene.
Synthesis and antiviral/antiproliferative activity of some N-sulphonylbenzimidazoles.
Synthesis and evaluation of the alpha-glucosidase inhibitory activity of 3-[4-(phenylsulfonamido)benzoyl]-2H-1-benzopyran-2-one derivatives.
Synthesis and biological evaluation of dialkylaminoalkylamino benzo[c][1,7] and [1,8]phenanthrolines as antiproliferative agents.
Synthesis and in vivo antidiabetic activity of novel dispiropyrrolidines through [3+2] cycloaddition reactions with thiazolidinedione and rhodanine derivatives.
Discovery of selective hydroxamic acid inhibitors of tumor necrosis factor-alpha converting enzyme.
The cytotoxic properties and preferential toxicity to tumour cells displayed by some 2,4-bis(benzylidene)-8-methyl-8-azabicyclo[3.2.1] octan-3-ones and 3,5-bis(benzylidene)-1-methyl-4-piperidones.
Nucleoside analogues as highly potent and selective inhibitors of herpes simplex virus thymidine kinase.
Antihypertensive activity of substituted 2,3,8,8a-tetrahydro-7H-oxazolo[3,2-a]pyridinedicarboxylate enantiomers.
Synthesis and antitumor activities of 5-methyl-1- and 2-[[2-dimethylaminoethyl]amino]-aza-thiopyranoindazoles.
Probing the extended binding determinants of oligosaccharyl transferase with synthetic inhibitors of asparagine-linked glycosylation.
Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT.
Bioisosteric modification of PETT-HIV-1 RT-inhibitors: synthesis and biological evaluation.
Novel conformationally restricted tetracyclic analogs of delta8-tetrahydrocannabinol.
Tetrapeptide derived inhibitors of complexation of a class II MHC: the peptide backbone is not inviolate.
Novel benzopyrano[3,4-c]pyrrole derivatives as potent and selective dopamine D3 receptor antagonist.
Synthesis of an array of potential matrix metalloproteinase inhibitors using a sequence of polymer-supported reagents.
Symmetrical anhydride-type serine protease inhibitors: structure-activity relationship studies of human chymase inhibitors.
Periodinates: a new class of protein tyrosine phosphatase inhibitors.
Highly efficient and versatile synthesis of libraries of constrained beta-strand mimetics.
N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists.
RNA-aminoglycoside antibiotic interactions: fluorescence detection of binding and conformational change.
Synthesis of a paclitaxel isomer: C-2-acetoxy-C-4-benzoate paclitaxel.
Design and synthesis of 2-oxo-imidazolidine-4-carboxylic acid hydroxyamides as potent matrix metalloproteinase-13 inhibitors.
Structure-based optimisation of 2-aminobenzylstatine derivatives: potent and selective inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Discovery of 3-amino-4-chlorophenyl P1 as a novel and potent benzamidine mimic via solid-phase synthesis of an isoxazoline library.
Synthesis of a molecular mimic of the Glc1Man9 oligoside as potential inhibitor of calnexin binding to DeltaF508 CFTR protein.
Synthesis of a novel fluorescent probe for estrogen receptor.
2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents: design, synthesis, biological evaluation and SAR studies.
Design, synthesis and biological evaluation of new arylpiperazine derivatives bearing a flavone moiety as 1-adrenoceptor antagonists.
New positive allosteric modulators of the metabotropic glutamate receptor 2 (mGluR2): identification and synthesis of N-propyl-8-chloro-6-substituted isoquinolones.
Modulation of GABAA-receptors by honokiol and derivatives: subtype selectivity and structure-activity relationship.
Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties.
Novel 12-membered non-antibiotic macrolides from erythromycin A; EM900 series as novel leads for anti-inflammatory and/or immunomodulatory agents.
Synthesis and evaluation of new furanyl and thiophenyl azoles as antileishmanial agents.
Pharmacophore-based virtual screening and Bayesian model for the identification of potential human leukotriene A4 hydrolase inhibitors.
Two dimeric lignans with an unusual ,-unsaturated ketone motif from Zanthoxylum podocarpum and their inhibitory effects on nitric oxide production.
The identification of novel orally active mGluR5 antagonist GSK2210875.
Synthesis and evaluation of indole-based new scaffolds for antimicrobial activities--identification of promising candidates.
Synthesis and pharmacological characterization of 5-phenyl-2-[2-(1-piperidinylcarbonyl)phenyl]-2,3-dihydro-1H-pyrrolo[1,2-c]imidazol-1-ones: a new class of Neuropeptide S antagonists.
Changes in flavonoid content and tyrosinase inhibitory activity in kenaf leaf extract after far-infrared treatment.
Receptor agonists of macrophage migration inhibitory factor.
Pyrimidinylmethylphenyl glucoside as novel C-aryl glucoside SGLT2 inhibitors.
One-pot syntheses of pseudopteroxazoles from pseudopterosins: a rapid route to non-natural congeners with improved antimicrobial activity.
Synthesis, structure-activity relationship and in vitro biological evaluation of N-arylethyl isoquinoline derivatives as Coxsackievirus B3 inhibitors.
Psilostachyin, acetylated pseudoguaianolides and their analogues: preparation and evaluation of their anti-inflammatory potential.
Synthesis of novel fluconazoliums and their evaluation for antibacterial and antifungal activities.
Synthesis and evaluation of the anti parasitic activity of aromatic nitro compounds.
Synthesis, characterization and biological evaluation of some 16-azolyl-3-amino-5-androstane derivatives as potential anticancer agents.
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
Design, synthesis and docking studies on benzamide derivatives as histone deacetylase inhibitors.
Antitumor agents 288: design, synthesis, SAR, and biological studies of novel heteroatom-incorporated antofine and cryptopleurine analogues as potent and selective antitumor agents.
Discovery and SAR of methylated tetrahydropyranyl derivatives as inhibitors of isoprenylcysteine carboxyl methyltransferase (ICMT).
Identification of 2-(4-pyridyl)thienopyridinones as GSK-3 inhibitors.
Novel imidazo[1,2-a]pyridine based inhibitors of the IGF-1 receptor tyrosine kinase: optimization of the aniline.
New betulinic acid derivatives as potent proteasome inhibitors.
Novel lipophilic acetohydroxamic acid derivatives based on conformationally constrained spiro carbocyclic 2,6-diketopiperazine scaffolds with potent trypanocidal activity.
Cytotoxicity and TOP1-targeting activity of 8- and 9-amino derivatives of 5-butyl- and 5-(2-N,N-dimethylamino)ethyl-5H-dibenzo[c,h][1,6]naphthyridin-6-ones.
Chemotherapy of leishmaniasis. Part VII: synthesis and bioevaluation of substituted terpenyl pyrimidines.
Synthesis of novel 3-amino-2-(4-chloro-2-mercaptobenzenesulfonyl)-guanidine derivatives as potential antitumor agents.
Design, synthesis and biological evaluation of cyclic angiotensin II analogues with 3,5 side-chain bridges. Role of C-terminal aromatic residue and ring cluster for activity and implications in the drug design of AT1 non-peptide antagonists.
Synthesis and cytotoxic activity of pyridazino[1',6':1,2]pyrido[3,4-b]indol-5-inium derivatives as anti-cancer agents.
Synthesis, photobiological activity and photoreactivity of methyl-thieno-8-azacoumarins, novel bioisosters of psoralen.
Anchoring and bola cationic amphiphiles for nucleotide delivery. Effects of orientation and extension of hydrophobic regions.
Synthesis, anticancer and antioxidant activities of 7-methoxyisoflavanone and 2,3-diarylchromanones.
Synthesis of new chiral 2,5-disubstituted 1,3,4-thiadiazoles possessing gamma-butenolide moiety and preliminary evaluation of in vitro anticancer activity.
Hydroxychalcones induce apoptosis in B16-F10 melanoma cells via GSH and ATP depletion.
Synthesis, antimicrobial and antioxidant activities of substituted pyrazoles, isoxazoles, pyrimidine and thioxopyrimidine derivatives.
Synthesis and anti-HIV studies of 2- and 3-adamantyl-substituted thiazolidin-4-ones.
Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro.
2-[2-Substituted-3-(3,4-dichlorobenzylamino)propylamino]-1H-quinolin-4-ones as Staphylococcus aureus methionyl-tRNA synthetase inhibitors.
Synthesis of 6- and 9-alkylaminomethyl furoflavones as gastroprotective agents.
Synthesis, antimicrobial activities and cytogenetic studies of newer diazepino quinoline derivatives via Vilsmeier-Haack reaction.
Biological activity in human neutrophils of di-tripeptides, analogues of the chemotactic fMLP.
Synthesis and anti-HIV activity of oleanolic acid derivatives.
Synthesis of substituted 5[H]phenanthridin-6-ones as potent poly(ADP-ribose)polymerase-1 (PARP1) inhibitors.
Enantioselective synthesis and complement inhibitory assay of A/B-ring partial analogues of oleanolic acid.
A practical synthesis of (S) 3-tert-butoxycarbonylamino-2-oxo-2,3,4,5-tetrahydro-1,5-benzodiazepine-1-acetic acid methyl ester as a conformationally restricted dipeptido-mimetic for caspase-1 (ICE) inhibitors.
Synthesis and in vitro and in vivo evaluation of the 2-(6'methoxy-3',4'-dihydro-1'-naphtyl)-4H-3,1-benzoxazin-4- one as a new potent substrate inhibitor of human leukocyte elastase.
Cathepsin B-sensitive dipeptide prodrugs. 1. A model study of structural requirements for efficient release of doxorubicin.
Thio-sugars. IV: Design and synthesis of S-linked fucoside analogs as a new class of alpha-L-fucosidase inhibitors.
Expedited discovery of second generation NK-1 antagonists: identification of a nonbasic aryloxy substituent.
The cyclohexene ring as bioisostere of a furanose ring: synthesis and antiviral activity of cyclohexenyl nucleosides.
Arylalkylidene rhodanine with bulky and hydrophobic functional group as selective HCV NS3 protease inhibitor.
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
Heteroaryl and cycloalkyl sulfonamide hydroxamic acid inhibitors of matrix metalloproteinases.
Design and synthesis of potent and selective inhibitors of integrin VLA-4.
Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones.
Synthesis of novel ferrocenyl sugars and their antimalarial activities.
Selective alpha1a adrenergic receptor antagonists based on 4-aryl-3,4-dihydropyridine-2-ones.
Mechanistic studies on type I and type II dehydroquinase with (6R)- and (6S)-6-fluoro-3-dehydroquinic acids.
Amido-(propyl and allyl)-hydroxybenzamidines: development of achiral inhibitors of factor Xa.
Synthesis of dolichyl phosphate derivatives with fluorescent label at the omega-end of the chain, new tools to study protein glycosylation.
Polyunsaturated fatty acid anilides as inhibitors of acyl-coA: cholesterol acyltransferase (ACAT).
Design and synthesis of a novel synthetic NAPAP-penta-saccharide conjugate displaying a dual antithrombotic action.
A novel ring-expanded product with enhanced tyrosinase inhibitory activity from classical Fe-catalyzed oxidation of rosmarinic acid, a potent antioxidative Lamiaceae polyphenol.
Second generation analogs of rigid 6,7-spiro scaffolds targeting the bacterial ribosome.
Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa.
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Interaction of 3'-azido-3'-deamino daunorubicin with human serum albumin: investigation by fluorescence spectroscopy and molecular modeling methods.
Discovery of novel, potent, selective, and orally active human glucagon receptor antagonists containing a pyrazole core.
Pyridyl amides as potent inhibitors of T-type calcium channels.
Synthesis, biological evaluation and radiolabelling by 18F-fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET.
Substituted spiro [2.3'] oxindolespiro [3.2]-5,6-dimethoxy-indane-1-one-pyrrolidine analogue as inhibitors of acetylcholinesterase.
6-Benzylamino 4-oxo-1,4-dihydro-1,8-naphthyridines and 4-oxo-1,4-dihydroquinolines as HIV integrase inhibitors.
New furin inhibitors based on weakly basic amidinohydrazones.
The discovery and structure-activity relationships leading to CE-156811, a difluorophenyl cyclopropyl fluoroether: a novel potent antibacterial analog derived from hygromycin A.
Design, synthesis, and structure-activity relationship study of bicyclic piperazine analogs of indole-3-carboxamides as novel cannabinoid CB1 receptor agonists.
Synthesis, antimicrobial and antioxidant evaluation of quinolines and bis(indolyl)methanes.
Stereoselective synthesis of hexahydro-3-methyl-1-arylchromeno[3,4-b]pyrrole and its annulated heterocycles as potent antimicrobial agents for human pathogens.
N,N'-methyleno-didemnin A from the ascidian Trididemnum solidum. Complete NMR assignments and confirmation of the imidazolidinone ring by strategic analysis of 1J(CH).
Antiproliferative triterpenes from the leaves and twigs of Juglans sinensis on HSC-T6 cells.
Discovery of 4-[4-({(3R)-1-butyl-3-[(R)-cyclohexyl(hydroxy)methyl]-2,5-dioxo-1,4,9-triazaspiro[5.5]undec-9-yl}methyl)phenoxy]benzoic acid hydrochloride: a highly potent orally available CCR5 selective antagonist.
Novel macrocyclic C-aryl glucoside SGLT2 inhibitors as potential antidiabetic agents.
Preliminary evaluation of a 3H imidazoquinoline library as dual TLR7/TLR8 antagonists.
Design, synthesis, and biological evaluation of curcumin analogues as multifunctional agents for the treatment of Alzheimer's disease.
Assessment of dopamine D1 receptor affinity and efficacy of three tetracyclic conformationally-restricted analogs of SKF38393.
Glionitrin B, a cancer invasion inhibitory diketopiperazine produced by microbial coculture.
Design, synthesis, and biological evaluation of imidazoline derivatives as p53-MDM2 binding inhibitors.
Extended targeting potential and improved synthesis of Microcin C analogs as antibacterials.
Synthesis and antimalarial evaluation of novel benzopyrano[4,3-b]benzopyran derivatives.
Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.
Investigation of chalcones as selective inhibitors of the breast cancer resistance protein: critical role of methoxylation in both inhibition potency and cytotoxicity.
Novel (S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acids: peroxisome proliferator-activated receptor selective agonists with protein-tyrosine phosphatase 1B inhibition.
Pyrrolo[1,2-b]pyridazines, pyrrolo[2,1-f]triazin-4(3H)-ones, and related compounds as novel corticotropin-releasing factor 1 (CRF1) receptor antagonists.
Synthesis and biological activities of a series of 4,5-diaryl-3-hydroxy-2(5H)-furanones.
Antitumor agents 200. Cytotoxicity of naturally occurring resveratrol oligomers and their acetate derivatives.
Antinociceptive properties of caffeic acid derivatives in mice.
4,1-Benzoxazepinone analogues of efavirenz (Sustiva) as HIV-1 reverse transcriptase inhibitors.
Synthesis and morphological reversion activity on srctsNRK cells of pyrimidinylpropanamide antibiotics, sparsomycin, sparoxomycin A1, A2, and their analogues.
A new series of C3-aza carbocyclic influenza neuraminidase inhibitors: synthesis and inhibitory activity.
Synthesis and anti-VZV activity of 6-heteroaryl derivatives of tricyclic acyclovir and 9-{[cis-1',2'-bis(hydroxymethyl)cycloprop-1'-yl]methyl}guanine analogues.
Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors.
Synthesis and antibacterial activity of some new thiadiaza/triazaphospholes, thiadiaza/triaza/tetrazaphosphinines and thiadiaza/tetrazaphosphepines containing 1,2,4-triazinone moiety.
Design and in silico screening of combinatorial library of antimalarial analogs of triclosan inhibiting Plasmodium falciparum enoyl-acyl carrier protein reductase.
Design and evaluation of anacardic acid derivatives as anticavity agents.
Synthesis and antibacterial activity of levofloxacin derivatives with certain bulky residues on piperazine ring.
Asymmetric synthesis of chiral piperazinylpropylisoxazoline ligands for dopamine receptors.
Synthesis, spectral studies and antiamoebic activity of new 1-N-substituted thiocarbamoyl-3-phenyl-2-pyrazolines.
Synthesis of N-methyl-bisindolylmaleimide amino acid methyl ester conjugates and cytotoxicity study.
Acyl-CoA: cholesterol acyltransferase inhibitory activity of ginseng sapogenins, produced from the ginseng saponins.
4-Alkyl- and 3,4-dialkyl-1,2,3,4-tetrahydro-8-pyridono[5,6-g]quinolines: potent, nonsteroidal androgen receptor agonists.
Enzymatic synthesis of a modified phospholipid and its evaluation as a substrate for B. cereus phospholipase C.
C32-O-imidazol-2-yl-methyl ether derivatives of the immunosuppressant ascomycin with improved therapeutic potential.
Identification of (-)-cis-6-acetyl-4S-(3-chloro-4-fluoro-benzoylamino)- 3,4-dihydro-2,2-dimethyl-2H-benzo[b]pyran-3S-ol as a potential antimigraine agent.
Modeling directed design and biological evaluation of quinazolinones as non-peptidic growth hormone secretagogues.
Novel synthetic oleanane triterpenoids: a series of highly active inhibitors of nitric oxide production in mouse macrophages.
Synthesis and evaluation of potential complement inhibitory semisynthetic analogs of oleanolic acid.
6,6'-Bis(2-hydroxyphenyl)-2,2'-bipyridine manganese(III) complexes: a novel series of superoxide dismutase and catalase mimetics.
Synthesis and antiviral activities of the major metabolites of the HIV protease inhibitor ABT-378 (Lopinavir).
Heterocyclic derivatives of 2-(3,5-dimethylphenyl)tryptamine as GnRH receptor antagonists.
Synthesis and biological evaluation of novel 1 beta-methylcarbapenems with isothiazoloethenyl side chains.
A series of 2(Z)-2-benzylidene-6,7-dihydroxybenzofuran-3[2H]-ones as inhibitors of chorismate synthase.
Efficient liquid-phase synthesis of 2'-hydroxychalcones.
Facile synthesis of high affinity styrylpyridine systems as inherently fluorescent ligands for the estrogen receptor.
Synthesis of P(1)-Citronellyl-P(2)-alpha-D-pyranosyl pyrophosphates as potential substrates for the E. coli undecaprenyl-pyrophosphoryl-N-acetylglucoseaminyl transferase MurG.
Serine derived NK1 antagonists. 2: A pharmacophore model for arylsulfonamide binding.
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
Identification of 2-aminobenzimidazole dimers as antibacterial agents.
Substituted 2-(R)-methyl piperazines as muscarinic M(2) selective ligands.
Synthesis, topoisomerase I inhibition and antitumor cytotoxicity of 2,2':6',2"-, 2,2':6',3"- and 2,2':6',4"-terpyridine derivatives.
New inhibitors of the thioredoxin-thioredoxin reductase system based on a naphthoquinone spiroketal natural product lead.
Inhibition of Wnt signaling by Dishevelled PDZ peptides.
Design and synthesis of aryl ether and sulfone hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
Indium(III) chloride catalyzed three-component coupling reaction: a novel synthesis of 2-substituted aryl(indolyl)kojic acid derivatives as potent antifungal and antibacterial agents.
Design, synthesis, and structure-activity relationship of Trypanosoma brucei leucyl-tRNA synthetase inhibitors as antitrypanosomal agents.
Pentasaccharide resin glycosides from Ipomoea pes-caprae.
17-Hydroxycyclooctatin, a fused 5-8-5 ring diterpene, from Streptomyces sp. MTE4a.
Potent and selective phosphopeptide mimetic prodrugs targeted to the Src homology 2 (SH2) domain of signal transducer and activator of transcription 3.
Discovery of sulfated sterols from marine invertebrates as a new class of marine natural antagonists of farnesoid-X-receptor.
Structures, synthesis, and human Nod1 stimulation of immunostimulatory bacterial peptidoglycan fragments in the environment.
Inhibition of amyloid- aggregation by coumarin analogs can be manipulated by functionalization of the aromatic center.
8-Azatetracyclines: synthesis and evaluation of a novel class of tetracycline antibacterial agents.
Inhibitors of the oncogenic transcription factor AP-1 from Podocarpus latifolius.
Trigonosins A-F, daphnane diterpenoids from Trigonostemon thyrsoideum.
Absolute configuration of (-)-gambogic acid, an antitumor agent.
Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents.
Quinazolinedione sulfonamides: a novel class of competitive AMPA receptor antagonists with oral activity.
Expeditious synthesis and biological evaluation of novel 2,N6-disubstituted 1,2-dihydro-1,3,5-triazine-4,6-diamines as potential antimalarials.
Synthesis, biological evaluation, and molecular docking study of 3-(3'-heteroatom substituted-2'-hydroxy-1'-propyloxy) xanthone analogues as novel topoisomerase II catalytic inhibitor.
Naphthol derivatives as TRPV1 inhibitors for the treatment of urinary incontinence.
NMR evaluation of interactions between substituted-indole and PDZ1 domain of PSD-95.
Synthesis and SAR study of tricyclic sulfones as -secretase inhibitors: C-6 and C-8 positions.
A novel, broad-spectrum antitumor compound containing the 1-hydroxycyclohexa-2,5-dien-4-one group: the disclosure of a new antitumor pharmacophore in protoapigenone 1.
Biological evaluation of KRIBB3 analogs as a microtubule polymerization inhibitor.
Studying synergism of methyl linked cyclohexyl thiophenes with triazole: synthesis and their cdk5/p25 inhibition activity.
SPF32629A and SPF32629B: enantioselective synthesis, determination of absolute configuration, cytotoxicity and antibacterial evaluation.
Synthesis, spectral, crystal structure and in vitro antimicrobial evaluation of imidazole/benzotriazole substituted piperidin-4-one derivatives.
Quinolino-benzo-[5, 6]-dihydroisoquindolium compounds derived from berberine: a new class of highly selective ligands for G-quadruplex DNA in c-myc oncogene.
Synthesis and in vitro anti-HIV activity of N-1,3-benzo[d]thiazol-2-yl-2-(2-oxo-2H-chromen-4-yl)acetamide derivatives using MTT method.
Pharmacophore-based design, synthesis, and biological evaluation of novel chloro-pyridazine piperazines as human rhinovirus (HRV-3) inhibitors.
Synthesis and antifungal activity of furo[2,3-f]quinolin-5-ols.
Design, synthesis and antibacterial activity of 3-methylenepyrrolidine formyl hydroxyamino derivatives as novel peptide deformylase inhibitors.
8-Hydroxynaphthalene-1,4-dione derivative as novel compound for glioma treatment.
Conventional and microwave assisted synthesis of small molecule based biologically active heterocyclic amidine derivatives.
Synthesis, characterization and evaluation of antibacterial activity of some thiazolo[3,2-b][1,2,4]triazole incorporating diphenylsulfone moieties.
N-[4-(1,1'-biphenyl)methyl]-4-(4-thiomorpholinylmethyl) benzenamines as non-oxazolidinone analogues of antimycobacterial U-100480.
Synthesis and biological evaluation of 3,6-disubstituted [1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives as a novel class of potential anti-tumor agents.
Synthesis and in vitro antitumor activity of new quinoxaline derivatives.
Pharmacophore modeling of diverse classes of p38 MAP kinase inhibitors.
Synthesis, radiolabelling and biological characterization of (D)-7-iodo-N-(1-phosphonoethyl)-5-aminomethylquinoxaline-2,3-dione, a glycine-binding site antagonist of NMDA receptors.
Synthesis and antioxidant activity evaluation of new hexahydropyrimido[5,4-c]quinoline-2,5-diones and 2-thioxohexahydropyrimido[5,4-c]quinoline-5-ones obtained by Biginelli reaction in two steps.
Mechanistic studies on prolyl-4-hydroxylase: the vitamin C requiring uncoupled oxidation.
A novel class of inhibitors for steroid 5alpha-reductase: synthesis and evaluation of umbelliferone derivatives.
The discovery of RFI-641 as a potent and selective inhibitor of the respiratory syncytial virus.
Structure and antimalarial activity of adducts of 11-azaartemisinin with conjugated terminal acetylenes.
Guanidine-substituted imidazoles as inhibitors of nitric oxide synthase.
Unique spirocyclopiperazinium salt. Part 2: synthesis and structure-activity relationship of dispirocyclopiperazinium salts as analgesics.
Structure-activity relationships of novel anti-malarial agents: part 5. N-(4-acylamino-3-benzoylphenyl)-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides.
Bioreductively-activated prodrugs for targeting hypoxic tissues: elimination of aspirin from 2-nitroimidazole derivatives.
Design and semisynthesis of spermine-sensitive Ribonuclease S'.
Genetic mapping of targets mediating differential chemical phenotypes in Plasmodium falciparum.
Pyrazolo[1,5-a]pyrimidine acetamides: 4-Phenyl alkyl ether derivatives as potent ligands for the 18 kDa translocator protein (TSPO).
Amino-substituted thalidomide analogs: potent inhibitors of TNF-alpha production.
Design of scytalone dehydratase inhibitors as rice blast fungicides: derivatives of norephedrine.
Synthesis and structure-activity relationships of pyridine-modified analogs of 3-[2-((S)-pyrrolidinyl)methoxy]pyridine, A-84543, a potent nicotinic acetylcholine receptor agonist.
Synthesis, DNA-damaging and cytotoxic properties of novel topoisomerase II-directed bisantrene analogues.
Unique spirocyclopiperazinium salt I: synthesis and structure-activity relationship of spirocyclopiperazinium salts as analgesics.
Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones.
Synthesis and biological evaluation of novel D-2'-azido-2',3'-dideoxyarabinofuranosyl-4'-thiopyrimidines and purines.
Benzimidazole-4,7-diones as inhibitors of protozoal (Toxoplasma gondii) purine nucleoside phosphorylase.
Novel N-[1-(1-substituted 4-piperidinylmethyl)-4-piperidinyl]benzamides as potent colonic prokinetic agents.
Synthesis and activity of selective MMP inhibitors with an aryl backbone.
Inhibition of Escherichia coli glucosamine synthetase by novel electrophilic analogues of glutamine--comparison with 6-diazo-5-oxo-norleucine.
Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy.
Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists.
SAR of 4-hydroxypiperidine and hydroxyalkyl substituted heterocycles as novel p38 map kinase inhibitors.
Synthesis of 6(alpha, beta)-aminocholestanols as ergosterol biosynthesis inhibitors.
Ascorbic acid-based inhibitors of alpha-amylases.
Nonpeptide RGD antagonists: a novel class of mimetics, the 5,8-disubstituted 1-azabicyclo[5.2.0]nonan-2-one lactam.
Chiral sulfoxides as metabolites of 2-thioimidazole-based p38 mitogen-activated protein kinase inhibitors: enantioselective synthesis and biological evaluation.
Synthesis and biological activity of 22-deoxo-23-oxa analogues of saponin OSW-1.
Discovery of indeno[1,2-c]quinoline derivatives as inhibitors of osteoclastogenesis induced by receptor activator of NF-B ligand (RANKL).
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
3-Thiomorpholin-8-oxo-8H-acenaphtho[1,2-b]pyrrole-9-carbonitrile (S1) based molecules as potent, dual inhibitors of B-cell lymphoma 2 (Bcl-2) and myeloid cell leukemia sequence 1 (Mcl-1): structure-based design and structure-activity relationship studies.
Pestaloquinols A and B, isoprenylated epoxyquinols from Pestalotiopsis sp.
Synthesis and biological evaluation of novel irreversible serine protease inhibitors using amino acid based sulfonyl fluorides as an electrophilic trap.
Contribution of cinnamic acid analogues in rosmarinic acid to inhibition of snake venom induced hemorrhage.
Syntheses of 2-deoxy-2,3-didehydro-N-acetylneuraminic acid analogues modified by N-sulfonylamidino groups at the C-4 position and biological evaluation as inhibitors of human parainfluenza virus type 1.
Phragmalin- and mexicanolide-type limonoids from the leaves of Trichilia connaroides.
Cycloartane triterpenes isolated from Combretum quadrangulare in a screening program for death-receptor expression enhancing activity.
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket.
Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues.
Synthesis of a novel ester of hydroxytyrosol and -lipoic acid exhibiting an antiproliferative effect on human colon cancer HT-29 cells.
Structure-activity relationship and pharmacokinetic studies of sotrastaurin (AEB071), a promising novel medicine for prevention of graft rejection and treatment of psoriasis.
Discovery of 1,2,4-thiadiazolidine-3,5-dione analogs that exhibit unusual and selective rapid cell death kinetics against acute myelogenous leukemia cells in culture.
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.
Selenocyanates and diselenides: a new class of potent antileishmanial agents.
Selective cytotoxicity of oxysterols through structural modulation on rings A and B. Synthesis, in vitro evaluation, and SAR.
MMP-13 selective alpha-sulfone hydroxamates: identification of selective P1' amides.
Toxic polyketides produced by Fusarium sp., an endophytic fungus isolated from Melia azedarach.
Synthesis and biological evaluation of 4-quinazolinones as Rho kinase inhibitors.
Discovery of small molecule human FPR1 receptor antagonists.
Design and synthesis of C35-fluorinated solamins and their growth inhibitory activities against human cancer cell lines.
Synthesis and structure-activity relationship of 4-quinolone-3-carboxylic acid based inhibitors of glycogen synthase kinase-3.
Cyathane diterpenes from Chinese mushroom Sarcodon scabrosus and their neurite outgrowth-promoting activity.
Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain.
Design and synthesis of benzoxazole containing indole analogs as peroxisome proliferator-activated receptor-/ dual agonists.
Towards rational design of cannabinoid receptor 1 (CB1) antagonists for peripheral selectivity.
Evaluation of a structure-based statine cyclic diamino amide encoded combinatorial library against plasmepsin II and cathepsin D.
Broad spectrum matrix metalloproteinase inhibitors: an examination of succinamide hydroxamate inhibitors with P1 C alpha gem-disubstitution.
Synthesis and biological activities of hapalosin derivatives with modification at the C12 position.
Solution-phase combinatorial synthesis and evaluation of piperazine-2,5-dione derivatives.
Prodrugs of CL316243: a selective beta3-adrenergic receptor agonist for treating obesity and diabetes.
Potent, elective human beta3 adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore.
Cell adhesion antagonists: synthesis and evaluation of a novel series of phenylalanine based inhibitors.
Synthesis of new (difluoromethylphosphono)azadisaccharides designed as bisubstrate analogue inhibitors for GlcNAc:beta-1,4 glycosyltransferases.
Structure-activity relationships of non-imidazole H(3) receptor ligands. Part 2: binding preference for D-amino acids motifs.
4-Aminoarylguanidine and 4-aminobenzamidine derivatives as potent and selective urokinase-type plasminogen activator inhibitors.
Synthesis and antithrombotic activity of carbolinecarboxyl RGD sequence.
A new class of type I protein geranylgeranyltransferase (GGTase I) inhibitor.
Synthesis and bioactivities of novel 5,6-bis(4-methoxyphenyl)-2H-pyridazin-3-one derivatives: inhibitors of interleukin-1 beta (IL-1beta) production.
Synthesis and bioactivities of novel pyridazine derivatives: inhibitors of interleukin-1 beta (IL-1beta) production.
Solution-Phase parallel synthesis of 5-carboxamido 1-benzyl-3-(3-dimethylaminopropyloxy)-1H-pyrazoles as activators of soluble guanylate cyclase with improved oral bioavailability.
Design, synthesis and stability of N-acyloxymethyl- and N-aminocarbonyloxymethyl-2-azetidinones as human leukocyte elastase inhibitors.
Thienopyridines: nitric oxide synthase inhibitors with potent in vivo activity.
3,4-Dihydro-1-isoquinolinamines: a novel class of nitric oxide synthase inhibitors with a range of isoform selectivity and potency.
4-(3,4-dihydro-1H-isoquinolin-2yl)-pyridines and 4-(3,4-dihydro-1H-isoquinolin-2-yl)-quinolines as potent NR1/2B subtype selective NMDA receptor antagonists.
New minimal substrate structural requirements in the enzymatic peroxidation of alkenes with soybean lipoxygenase.
Synthesis and methemoglobin toxicity of the amides of 6/7 mono or disubstituted quinolone.
High-throughput synthesis and optimization of thrombin inhibitors via urazole alpha-addition and Michael addition.
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists: modifications of the arylpropylpiperidine side chains.
Identification of TNF-alpha inhibitors from a split-pool library based on a tyrosine-proline peptidomimetic scaffold.
Synthesis and SAR of azalide 3,6-ketal aromatic derivatives as potent Gram-positive and Gram-negative antibacterial agents.
Indinavir analogues with blocked metabolism sites as HIV protease inhibitors with improved pharmacological profiles and high potency against PI-resistant viral strains.
Substituted 3-amino biaryl propionic acids as potent VLA-4 antagonists.
Novel inhibitors of plasminogen activator inhibitor-1: development of new templates from diketopiperazines.
Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives.
Synthesis of N-propargylphenelzine and analogues as neuroprotective agents.
Synthesis of diaminobutane derivatives as potent Ca(2+)-permeable AMPA receptor antagonists.
Synthesis of L-(+)-3-(3-hydroxy-4-pivaloyloxybenzyl)-2,5-diketomorpholine as potential prodrug of L-dopa.
Synthesis and uptake of nitric oxide-releasing drugs by the P2 nucleoside transporter in Trypanosoma equiperdum.
Proteasome inhibition by the natural products epoxomicin and dihydroeponemycin: insights into specificity and potency.
Peptidic immunosuppressants from the fungus Trichoderma polysporum.
Picking the S1, S1' and S2' pockets of matrix metalloproteinases. A niche for potent acyclic sulfonamide inhibitors.
Novel C-ring analogues of 20(S)-camptothecin-part-2: synthesis and in vitro cytotoxicity of 5-C-substituted 20(S)-camptothecin analogues.
Total synthesis of pyrrolizidines 223H', 239K', 265H', and 267H' found in Madagascan frogs (Mantella) and their affinities for nicotinic acetylcholine receptor.
Cytotoxic, antifouling bromotyramines: a synthetic study on simple marine natural products and Their analogues.
Synthesis and vasorelaxant activity of new coumarin and furocoumarin derivatives.
Substituted 3-(2-benzoxazyl)-benzimidazol-2-(1H)-ones: a new class of GABA(A) brain receptor ligands.
Design, synthesis and characterisation of a peptide with oxaloacetate decarboxylase activity.
Malyngamide 2, an oxidized lipopeptide with nitric oxide inhibiting activity from a Papua New Guinea marine cyanobacterium.
Synthesis and in vitro cytotoxic evaluation of some thiazolylbenzimidazole derivatives.
The highly potent and selective dipeptidyl peptidase IV inhibitors bearing a thienopyrimidine scaffold effectively treat type 2 diabetes.
Synthesis and antiprotozoal activity of N-alkoxy analogues of the trypanocidal lead compound 4,4'-bis(imidazolinylamino)diphenylamine with improved human blood-brain barrier permeability.
Radical scavenging and antioxidant activities of isocoumarins and a phthalide from the endophytic fungus Colletotrichum sp.
Isolation, structure elucidation, and cytotoxic evaluation of furanonaphthoquinones from in vitro plantlets and cultures of Streptocarpus dunnii.
Sesquiterpenes from Chloranthus japonicus.
Receptor-dependent (RD) 3D-QSAR approach of a series of benzylpiperidine inhibitors of human acetylcholinesterase (HuAChE).
4-[1-(Substituted aryl/alkyl carbonyl)-benzoimidazol-2-yl]-benzenesulfonic acids: synthesis, antimicrobial activity, QSAR studies, and antiviral evaluation.
Human cytochrome P450 liability studies of trans-dihydronarciclasine: a readily available, potent, and selective cancer cell growth inhibitor.
Metachromins U-W: cytotoxic merosesquiterpenoids from an Australian specimen of the sponge Thorecta reticulata.
Cytotoxic veraguamides, alkynyl bromide-containing cyclic depsipeptides from the marine cyanobacterium cf. Oscillatoria margaritifera.
A neuroprotective sulfone of marine origin and the in vivo anti-inflammatory activity of an analogue.
Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class.
1,4-dioxane, a suitable scaffold for the development of novel M3 muscarinic receptor antagonists.
Toward the definition of stereochemical requirements for MT2-selective antagonists and partial agonists by studying 4-phenyl-2-propionamidotetralin derivatives.
C-Aryl 5a-carba--d-glucopyranosides as novel sodium glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes.
Perturbing pro-survival proteins using quinoxaline derivatives: a structure-activity relationship study.
Novel 3-phenylpiperidine-4-carboxamides as highly potent and orally long-acting neurokinin-1 receptor antagonists with reduced CYP3A induction.
Design, synthesis and biological evaluation of peptidyl-vinylaminophosphonates as novel cysteine protease inhibitors.
Discovery and pharmacological characterization of N-[2-({2-[(2S)-2-cyanopyrrolidin-1-yl]-2-oxoethyl}amino)-2-methylpropyl]-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxamide hydrochloride (anagliptin hydrochloride salt) as a potent and selective DPP-IV inhibitor.
Toll-like receptor (TLR)-7 and -8 modulatory activities of dimeric imidazoquinolines.
Synthesis and antifungal activity of natural product-based 6-alkyl-2,3,4,5-tetrahydropyridines.
Synthesis of novel mast cell-stabilising and anti-allergic 1,2,3,4-tetrahydro-1-naphthalenols and related compounds.
Diverse metabolic profiles of a Streptomyces strain isolated from a hyper-arid environment.
Non-competitive and selective dipeptidyl peptidase IV inhibitors with phenethylphenylphthalimide skeleton derived from thalidomide-related -glucosidase inhibitors and liver X receptor antagonists.
Design and synthesis of potent and selective aldose reductase inhibitors based on pyridylthiadiazine scaffold.
2-Acylamino-5-chlorobenzophenones with enhanced selectivity towards malaria parasites.
DNA binding ligands with excellent antibiotic potency against drug-resistant gram-positive bacteria.
Conformationally restricted 3,4-diarylfuranones (2,3a,4,5-tetrahydronaphthofuranones) as selective cyclooxygenase-2 inhibitors.
Novel spermine-amino acid conjugates and basic tripeptides enhance cleavage of the hairpin ribozyme at low magnesium ion concentration.
p38MAP kinase inhibitors. Part 1: design and development of a new class of potent and highly selective inhibitors based on 3,4-dihydropyrido[3,2-d]pyrimidone scaffold.
Parallel solution- and solid-phase synthesis of spirohydantoin derivatives as neurokinin-1 receptor ligands.
Spirocyclic NK(1) antagonists I: [4.5] and [5.5]-spiroketals.
An improved synthesis of the C-linked glucuronide of N-(4-hydroxyphenyl)retinamide.
Aromatic inhibitors of dehydroquinate synthase: synthesis, evaluation and implications for gallic acid biosynthesis.
3,3a-Dihydropyrano[4,3,2-de]quinazolin-2(1H)-ones are potent non-nucleoside reverse transcriptase inhibitors.
A new C-nucleoside analogue of tiazofurin: synthesis and biological evaluation of 2-beta-D-ribofuranosylimidazole-4-carboxamide (imidazofurin).
The design and synthesis of thrombin inhibitors: analogues of MD805 containing non-polar surrogates for arginine at the P1 position.
Fine Tuning of physico-chemical parameters to optimise a new series of novobiocin analogues.
Broad spectrum antiprotozoal agents that inhibit histone deacetylase: structure-activity relationships of apicidin. Part 2.
B-ring substituted 5,7-dihydroxyflavonols with high-affinity binding to P-glycoprotein responsible for cell multidrug resistance.
Design, synthesis, and biological evaluation of fluoronitrophenyl substituted folate analogues as potential inhibitors of GAR transformylase and AICAR transformylase.
Syntheses and antifilarial profile of 7-chloro-4-(substituted amino) quinolines: a new class of antifilarial agents.
Purpurinimides as photosensitizers: effect of the presence and position of the substituents in the in vivo photodynamic efficacy.
Novel 2,5-dideoxystreptamine derivatives targeting the ribosomal decoding site RNA.
Modification of the pyridine moiety of non-peptidyl indole GnRH receptor antagonists.
G-quadruplex DNA binding by a series of carbocyanine dyes.
Synthesis and biological testing of non-fluorinated analogues of levofloxacin.
Thiosugars. Part 5: synthesis and biological activity of 1-(4-thio-L-arabinofuranosyl)-5-halopyrimidine nucleosides.
Structure-activity relationships study at the 3'-N position of paclitaxel. Part 2: synthesis and biological evaluation of 3'-N-thiourea- and 3'-N-thiocarbamate-bearing paclitaxel analogues.
Cytotoxic halogenoacrylic derivatives of distamycin A.
Synthesis of phosphatidylinositol 3-kinase (PI3K) inhibitory analogues of the sponge meroterpenoid liphagal.
Discovery of novel benzopyranyl tetracycles that act as inhibitors of osteoclastogenesis induced by receptor activator of NF-B ligand.
Design, synthesis, and evaluation of an -tocopherol analogue as a mitochondrial antioxidant.
Environmental study of azole-resistant Aspergillus fumigatus and other aspergilli in Austria, Denmark, and Spain.
2-Aryl indole NK1 receptor antagonists: optimisation of the 2-aryl ring and the indole nitrogen substituent.
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1.
4-Hydroxy-1-[3-(5-(1,2,4-triazol-4-yl)-1H-indol-3-yl)propyl]piperidines: selective h5-HT1D agonists for the treatment of migraine.
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Synthesis and evaluation of 5-substituted 9-hydroxypyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones as check point 1 kinase inhibitors.
In vitro antitumor activity of N-glycosyl sulfonamides.
Synthesis and anticancer evaluation of thiazolyl-chalcones.
Synthetic analogues of the microtubule-stabilizing sponge alkaloid ceratamine A are more active than the natural product.
Gusanlungionosides A-D, potential tyrosinase inhibitors from Arcangelisia gusanlung.
Structural basis for the interaction between carbonic anhydrase and 1,2,3,4-tetrahydroisoquinolin-2-ylsulfonamides.
Molluscicidal metabolites from an assemblage of Palmyra Atoll cyanobacteria.
Structure-based design, synthesis, and nonalcoholic steatohepatitis (NASH)-preventive effect of phenylpropanoic acid peroxisome proliferator-activated receptor (PPAR) -selective agonists.
2-Hydroxypropyl--cyclodextrin strongly improves water solubility and anti-proliferative activity of pyrazolo[3,4-d]pyrimidines Src-Abl dual inhibitors.
Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.
Peptide deformylase inhibitors with non-peptide scaffold: synthesis and structure-activity relationships.
Bitriazolyl acyclonucleosides synthesized via Huisgen reaction using internal alkynes show antiviral activity against tobacco mosaic virus.
Synthesis and hydrolytic evaluation of acid-labile imine-linked cytotoxic isatin model systems.
Regiospecific synthesis and biological evaluation of spirooxindolopyrrolizidines via [3+2] cycloaddition of azomethine ylide.
Role of metalation in the topoisomerase II inhibition and antiproliferation activity of a series of -heterocyclic-N4-substituted thiosemicarbazones and their Cu(II) complexes.
Aspergilones A and B, two benzylazaphilones with an unprecedented carbon skeleton from the gorgonian-derived fungus Aspergillus sp.
Indole-3-piperazinyl derivatives: novel chemical class of 5-HT(6) receptor antagonists.
Click chemistry inspired one-pot synthesis of 1,4-disubstituted 1,2,3-triazoles and their Src kinase inhibitory activity.
Design and evaluation of fragment-like estrogen receptor tetrahydroisoquinoline ligands from a scaffold-detection approach.
Spirocyclic lignans from Guaiacum (Zygophyllaceae) induce apoptosis in human breast cancer cell lines.
Bioactive compounds from the scale insect pathogenic fungus Conoideocrella tenuis BCC 18627.
Antimalarial activities of new guanidylimidazole and guanidylimidazoline derivatives.
Dual function inhibitors of relevance to chronic obstructive pulmonary disease.
Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties.
Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.
Onoceranoid-type triterpenoids from Lansium domesticum.
Briarane diterpenes diminish COX-2 expression in human colon adenocarcinoma cells.
Regioselective Suzuki coupling of dihaloheteroaromatic compounds as a rapid strategy to synthesize potent rigid combretastatin analogues.
The synthesis and evaluation of a novel class of (E)-3-(1-cyclohexyl-1H-pyrazol-3-yl)-2-methylacrylic acid hepatitis C virus polymerase NS5B inhibitors.
MMP-13 selective -sulfone hydroxamates: a survey of P1' heterocyclic amide isosteres.
PNA containing isocytidine nucleobase: synthesis and recognition of double helical RNA.
Benzimidazole inhibitors induce a DFG-out conformation of never in mitosis gene A-related kinase 2 (Nek2) without binding to the back pocket and reveal a nonlinear structure-activity relationship.
Isoprenylated flavonoids and adipogenesis-promoting constituents from Morus nigra.
2,4-Disubstituted pyrroles: synthesis, traceless linking and pharmacological investigations leading to the dopamine D4 receptor partial agonist FAUC 356.
Design and synthesis of novel benzofurans as a new class of antifungal agents targeting fungal N-myristoyltransferase. Part 2.
Structure-based design of cyclooxygenase-2 selectivity into ketoprofen.
Synthesis of an alpha-aminophosphonate nucleoside as an inhibitor of S-adenosyl-L-homocysteine hydrolase.
Design and synthesis of glycolic and mandelic acid derivatives as factor Xa inhibitors.
Design and synthesis of a highly selective EP4-receptor agonist. Part 1: 3,7-dithiaPG derivatives with high selectivity.
Substituent effects within the DNA binding subunit of CBI analogues of the duocarmycins and CC-1065.
Inhibition of HIV-1 infection by synthetic peptide analogues derived from the NH(2)-Terminal extracellular region of GPR1.
Pyridazine based inhibitors of p38 MAPK.
Serotonin transporter inhibitors: synthesis and binding potency of 2'-methyl- and 3'-methyl-6-nitroquipazine.
Design and synthesis of spiro-cyclopentenyl and spiro-[1,3]-dithiolanyl substituted pyrrolidine-5,5-trans-lactams as inhibitors of hepatitis C virus NS3/4A protease.
CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine.
Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.
A unique ring-expanded acyclic nucleoside analogue that inhibits both adenosine deaminase (ADA) and guanine deaminase (GDA; guanase): synthesis and enzyme inhibition studies of 4,6-diamino-8H-1-hydroxyethoxymethyl-8-iminoimidazo[4,5-e][1,3]diazepine.
Structure-activity relationship studies of chloromethyl ketone derivatives for selective human chymase inhibitors.
Design and synthesis of sialyl Lewis x mimics as E-selectin inhibitors.
Structure-based design of inhibitors of human L-xylulose reductase modelled into the active site of the enzyme.
Structure-based design of a non-peptidic antagonist of the SH2 domain of GRB2.
Kinetic characterisation of ene-diol-based inhibitors of alpha-amylase.
Trifluoromethyl ketone inhibitors of fatty acid amide hydrolase: a probe of structural and conformational features contributing to inhibition.
Azole derivatives as histamine H3 receptor antagonists, part I: thiazol-2-yl ethers.
Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.
Identification of non-peptide malignant brain tumor (MBT) repeat antagonists by virtual screening of commercially available compounds.
Antitumor Agents. 282. 2'-(R)-O-acetylglaucarubinone, a quassinoid from Odyendyea gabonensis as a potential anti-breast and anti-ovarian cancer agent.
Positive allosteric modulators of the -amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor.
ATPases as drug targets: insights from heat shock proteins 70 and 90.
Novel 1',1'-chain substituted hexahydrocannabinols: 9-hydroxy-3-(1-hexyl-cyclobut-1-yl)-hexahydrocannabinol (AM2389) a highly potent cannabinoid receptor 1 (CB1) agonist.
(R,S)-anti-1-amino-2-[18F]fluorocyclopentyl-1-carboxylic acid: synthesis from racemic 2-benzyloxycyclopentanone and biological evaluation for brain tumor imaging with positron emission tomography.
Anthraquinone, cyclopentanone, and naphthoquinone derivatives from the sea fan-derived fungi Fusarium spp. PSU-F14 and PSU-F135.
Synthesis and cytotoxicity evaluation of novel 1,4-disubstituted 1,2,3-triazoles via CuI catalysed 1,3-dipolar cycloaddition.
Structure activity relationship studies of imidazo[1,2-a]pyrazine derivatives against cancer cell lines.
Indole alkaloids from Ervatamia hainanensis with potent acetylcholinesterase inhibition activities.
Synthesis and vasodilation activity of some novel bis(3-pyridinecarbonitrile) derivatives.
CYP1A2-mediated biotransformation of cardioactive 2-thienylidene-3,4-methylenedioxybenzoylhydrazine (LASSBio-294) by rat liver microsomes and human recombinant CYP enzymes.
Purmorphamine activates the Hedgehog pathway by targeting Smoothened.
2-Acetylpyridine thiosemicarbazones: cytotoxic activity in nanomolar doses against malignant gliomas.
Synthesis and structure-activity relationships of novel benzoxaboroles as a new class of antimalarial agents.
Inhibition of P-glycoprotein-mediated Multidrug Resistance (MDR) by N,N-bis(cyclohexanol)amine aryl esters: further restriction of molecular flexibility maintains high potency and efficacy.
Synthesis, hypolipidemic and hypoglycemic activity of some novel 2-(4-(2-substituted aminothiazole-4-yl) phenoxy)-2-methyl propanoic acid derivatives.
A novel series of potent and selective EP(4) receptor ligands: facile modulation of agonism and antagonism.
Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models.
Synthesis of bi-substrate state mimics of dihydropteroate synthase as potential inhibitors and molecular probes.
An efficient one-pot synthesis of benzothiazolo-4-anilino-podophyllotoxin congeners: DNA topoisomerase-II inhibition and anticancer activity.
A novel transition state analog inhibitor of guanase based on azepinomycin ring structure: Synthesis and biochemical assessment of enzyme inhibition.
Discovery of novel class 1 phosphatidylinositide 3-kinases (PI3K) fragment inhibitors through structure-based virtual screening.
Asymmetric synthesis of phenanthroindolizidine alkaloids with hydroxyl group at the C14 position and evaluation of their antitumor activities.
Design, synthesis and SAR of thienopyridines as potent CHK1 inhibitors.
The antibacterial ent-eusynstyelamide B and eusynstyelamides D, E, and F from the Arctic bryozoan Tegella cf. spitzbergensis.
An efficient synthesis of the precursor of AI-2, the signalling molecule for inter-species quorum sensing.
Extending SAR of bile acids as FXR ligands: discovery of 23-N-(carbocinnamyloxy)-3,7-dihydroxy-6-ethyl-24-nor-5-cholan-23-amine.
Quinonoid and phenazine compounds: synthesis and evaluation against H37Rv, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis.
Design, synthesis and cytotoxicity of a new series of isoxazolidines derived from substituted chalcones.
Antiplasmodial sesquiterpene alkaloids from the roots of Maytenus mekongensis.
1,1-Diarylalkenes as anticancer agents: dual inhibitors of tubulin polymerization and phosphodiesterase 4.
Identification of 4H,6H-[2]benzoxepino[4,5-c][1,2]oxazoles as novel squalene synthase inhibitors.
Amino-caprolactam -secretase inhibitors showing potential for the treatment of Alzheimer's disease.
Synthesis, in vitro evaluation and molecular docking studies of new triazole derivatives as antifungal agents.
Synthesis and biological evaluation of 4-acrylamidopodophyllotoxin congeners as DNA damaging agents.
Aminomethyltetrazoles as potential inhibitors of the -aminobutyric acid transporters mGAT1-mGAT4: synthesis and biological evaluation.
A facile synthesis of 1,5-disubstituted-2-aminoimidazoles: antibiotic activity of a first generation library.
Sulfonamides as selective oestrogen receptor agonists.
Arthrobotrisins A-C, oligosporons from the nematode-trapping fungus Arthrobotrys oligospora.
Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors.
Synthesis of -functionalized temoporfin derivatives for an application in photodynamic therapy.
A mechanism-based potent sirtuin inhibitor containing N-thiocarbamoyl-lysine (TuAcK).
The role of the 4''-hydroxyl on motilin agonist potency in the 9-dihydroerythromycin series.
3'-Beta-ethynyl and 2'-deoxy-3'-beta-ethynyl adenosines: first 3'-beta-branched-adenosines substrates of adenosine deaminase.
Quantum chemical- and 3-D-QSAR (CoMFA) studies of benzalacetones and 1,1,1-trifluoro-4-phenyl-3-buten-2-ones.
Oxal hydroxamic acid derivatives with inhibitory activity against matrix metalloproteinases.
Structure-activity study of L-cysteine-based N-type calcium channel blockers: optimization of N- and C-terminal substituents.
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Pharmacological evaluation of a diarylmethylene-piperidine derivative: a new potent atypical antipsychotic?
Potent second generation vinyl sulfonamide inhibitors of the trypanosomal cysteine protease cruzain.
Butyrophenone analogues in the carbazole series: synthesis and determination of affinities at D2 and 5-HT2A receptors.
Syntheses and evaluation of amidinobenzofuran derivatives as tryptase inhibitors.
SAR studies of diaryltriazoles against bacterial two-component regulatory systems and their antibacterial activities.
Discovery of a novel benzyloxyisoquinoline derivative with potent anti-Helicobacter pylori activity.
An efficient stereoselective synthesis of [3S(1S,9S)]-3-[[[9-(benzoylamino) octahydro-6,10-dioxo-6H-pyridazino-(1,2-a)(1,2)-diazepin-1-yl]-carbonyl ]amino]-4-oxobutanoic acid, an interleukin converting enzyme (ICE) inhibitor.
A novel and practical route to A-ring enyne synthon for 1 alpha,25-dihydroxyvitamin D3 analogs: synthesis of A-ring diastereomers of 1 alpha,25-dihydroxyvitamin D2 and 3-methyl-1,25-dihydroxyvitamin D3.
Highly specific inhibitory effect of three-component hybrid liposomes including sugar surfactants on the growth of glioma cells.
Synthesis of a heterocyclic aza-enediyne and its DNA-cleavage properties.
Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard.
A free energy calculation can be used to predict K(+)-binding constants for new macrotetrolide antibiotics.
Design of novel N-(2,4-dioxo-1,2,3,4-tetrahydro-thieno[3,2-d]pyrimidin-7-yl)-guanidines as thymidine phosphorylase inhibitors, and flexible docking to a homology model.
Synthesis of [(2S,3S,4R)-3,4-dihydroxypyrrolidin-2-yl]-5-methylfuran-4-carboxylic acid derivatives: new leads as selective beta-galactosidase inhibitors.
Azalide 3,6-ketals: antibacterial activity and structure-activity relationships of aryl and hetero aryl substituted analogues.
QSAR study on adenosine kinase inhibition of pyrrolo[2,3-d]pyrimidine nucleoside analogues using the hansch approach.
Investigation of 4-piperidinols as novel H3 antagonists.
Design, synthesis and in vitro evaluation of antitubercular and antimicrobial activity of some novel pyranopyrimidines.
Identification of a new biaryl scaffold generating potent renin inhibitors.
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.
Novel amides and esters prodrugs of olmesartan: Synthesis, bioconversion, and pharmacokinetic evaluation.
Cytotoxic cycloartane triterpene and rare isomeric bisclerodane diterpenes from the leaves of Polyalthia longifolia var. pendula.
Design and synthesis of novel pyrimidine hydroxamic acid inhibitors of histone deacetylases.
Identification of a sulfonoquinovosyldiacylglyceride from Azadirachta indica and studies on its cytotoxic activity and DNA binding properties.
Identification of 2,3,6-trisubstituted quinoxaline derivatives as a Wnt2/-catenin pathway inhibitor in non-small-cell lung cancer cell lines.
Rational design of inhibitors that bind to inactive kinase conformations.
Optimization of a series of dipeptides with a P3 threonine residue as non-covalent inhibitors of the chymotrypsin-like activity of the human 20S proteasome.
Azole derivatives as histamine H3 receptor antagonists, part 2: C-C and C-S coupled heterocycles.
Phage-encoded combinatorial chemical libraries based on bicyclic peptides.
Discovery of 1H-benzo[d][1,2,3]triazol-1-yl 3,4,5-trimethoxybenzoate as a potential antiproliferative agent by inhibiting histone deacetylase.
Nasal carriage of methicillin-resistant and methicillin-sensitive strains of Staphylococcus sciuri in the Indonesian population.
The synthesis and biological evaluation of 1-C-alkyl-L-arabinoiminofuranoses, a novel class of -glucosidase inhibitors.
Inhibitory effects of hybrid liposomes on the growth of synoviocyte causing rheumatoid arthritis.
Synthesis and anti-HCV activity of a new 2'-deoxy-2'-fluoro-2'-C-methyl nucleoside analogue.
Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors.
In silico identification and biochemical evaluation of novel inhibitors of NRH:quinone oxidoreductase 2 (NQO2).
A novel application of DDQ as electrophile in the Nenitzescu reaction.
Synthesis and biological evaluation of N-substituted benzo[c]phenanthrolines and benzo[c]phenanthrolinones as antiproliferative agents.
Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.
Synthesis and biological assay of 4-aryl-6-chloro-quinoline derivatives as novel non-nucleoside anti-HBV agents.
Synthesis and SAR of 3-arylsulfonyl-pyrazolo[1,5-a]pyrimidines as potent serotonin 5-HT6 receptor antagonists.
A regio- and stereoselective 1,3-dipolar cycloaddition for the synthesis of novel spiro-pyrrolothiazolyloxindoles and their antitubercular evaluation.
Chisopanins A-K, 11 new protolimonoids from Chisocheton paniculatus and their anti-inflammatory activities.
Modelling topoisomerase I inhibition by minor groove binders.
Molecular docking and QSAR study on steroidal compounds as aromatase inhibitors.
Synthesis and biological evaluation of novel quinazoline-derived human Pin1 inhibitors.
Conformationally restricted homotryptamines 3. Indole tetrahydropyridines and cyclohexenylamines as selective serotonin reuptake inhibitors.
Synthesis and biological evaluation of 5-substituted 1,4-dihydroindeno[1,2-c]pyrazoles as multitargeted receptor tyrosine kinase inhibitors.
2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors.
The design and development of 2-aryl-2-hydroxy ethylamine substituted 1H,7H-pyrido[1,2,3-de]quinoxaline-6-carboxamides as inhibitors of human cytomegalovirus polymerase.
Discovery of substituted biphenyl imidazoles as potent, bioavailable bombesin receptor subtype-3 agonists.
Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.
Microwave assisted synthesis and in vitro cytotoxicities of substituted (Z)-2-amino-5-(1-benzyl-1H-indol-3-yl)methylene-1-methyl-1H-imidazol-4(5H)-ones against human tumor cell lines.
Novel substituted (Z)-5-((N-benzyl-1H-indol-3-yl)methylene)imidazolidine-2,4-diones and 5-((N-benzyl-1H-indol-3-yl)methylene)pyrimidine-2,4,6(1H,3H,5H)-triones as potent radio-sensitizing agents.
Histone deacetylase and microtubules as targets for the synthesis of releasable conjugate compounds.
Synthesis of the new pseudo-symmetrical tamoxifen derivatives and their anti-tumor activity.
Synthesis of soluble multivalent glycoconjugates that target the Hc region of botulinum neurotoxin A.
Synthesis and biological evaluation of nucleoside analogues having 6-chloropurine as anti-SARS-CoV agents.
Characterization of lassa virus cell entry inhibitors: determination of the active enantiomer by asymmetric synthesis.
Two novel monoterpene-chalcone conjugates isolated from the seeds of Alpinia katsumadai.
Lys17 in the 'lasso' peptide lariatin A is responsible for anti-mycobacterial activity.
4-Piperidines and 3-pyrrolidines as dual serotonin and noradrenaline reuptake inhibitors: design, synthesis and structure-activity relationships.
Calculation of binding free energies for non-zinc chelating pyrimidine dicarboxamide inhibitors with MMP-13.
Design, synthesis and biological activity of carbohydrate-containing peptidomimetics as new ligands for the human tachykinin NK-2 receptor.
Synthesis and structure-activity relationships of thiotetronic acid analogues of thiolactomycin.
1,3,4-Trisubstituted pyrrolidine CCR5 receptor antagonists. Part 2: lead optimization affording selective, orally bioavailable compounds with potent anti-HIV activity.
Discovery of potent, selective human granzyme B inhibitors that inhibit CTL mediated apoptosis.
Blockers of human T cell Kv1.3 potassium channels using de novo ligand design and solid-phase parallel combinatorial chemistry.
Unsymmetrical cyclic ureas as HIV-1 protease inhibitors: novel biaryl indazoles as P2/P2' substituents.
Isolation and synthesis of a novel immunosuppressive 17alpha-substituted dammarane from the flour of the Palmyrah palm (Borassus flabellifer).
Synthesis and phototoxic property of tetra- and octa-glycoconjugated tetraphenylchlorins.
Synthesis and structure-activity relationships of adenosine analogs as inhibitors of trypanosomal glyceraldehyde-3-phosphate dehydrogenase. Modifications at positions 5' and 8.
C-alkylated spiro[benzofuran-3(2H),4'-1'-methyl-piperidine-7-ols] as potent opioids: a conformation-activity study.
Bicyclic nucleoside inhibitors of Varicella-Zoster Virus (VZV): the effect of a terminal halogen substitution in the side-chain.
The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic.
Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors.
Siphonols A-E: novel nitric oxide inhibitors from Orthosiphon stamineus of Indonesia.
Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the metal binding group.
Synthesis and antifungal activity of 2,5-disubstituted-6-arylamino-4,7-benzimidazolediones.
Borrelidin induces the transcription of amino acid biosynthetic enzymes via a GCN4-dependent pathway.
Synthesis and antinociceptive activities of some pyrazoline derivatives.
Discovery of a potent and selective series of pyrazole bacterial methionyl-tRNA synthetase inhibitors.
4-Amino-2-(aryl)-butylbenzamides and Their conformationally constrained analogues. Potent antagonists of the human neurokinin-2 (NK(2)) receptor.
Synthesis and evaluation of the quorum sensing inhibitory effect of substituted triazolyldihydrofuranones.
Antibacterial butenolides from the Korean tunicate Pseudodistoma antinboja.
Structure-activity relationships in 1,4-benzodioxan-related compounds. 11. (1) reversed enantioselectivity of 1,4-dioxane derivatives in 1-adrenergic and 5-HT1A receptor binding sites recognition.
Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity.
Alkylsulfanyl-1,2,4-triazoles, a new class of allosteric valosine containing protein inhibitors. Synthesis and structure-activity relationships.
Novel hybrids of optically active ring-opened 3-n-butylphthalide derivative and isosorbide as potential anti-ischemic stroke agents.
Design and synthesis of new bifunctional sigma-1 selective ligands with antioxidant activity.
Sulfonylureas have antifungal activity and are potent inhibitors of Candida albicans acetohydroxyacid synthase.
Development of dual PLD1/2 and PLD2 selective inhibitors from a common 1,3,8-Triazaspiro[4.5]decane Core: discovery of Ml298 and Ml299 that decrease invasive migration in U87-MG glioblastoma cells.
Alpha-heteroatom derivatized analogues of 3-(acetylhydroxyamino)propyl phosphonic acid (FR900098) as antimalarials.
Optimizing solubility and permeability of a biopharmaceutics classification system (BCS) class 4 antibiotic drug using lipophilic fragments disturbing the crystal lattice.
Synthesis, biological evaluation, and molecular modeling of glycyrrhizin derivatives as potent high-mobility group box-1 inhibitors with anti-heart-failure activity in vivo.
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Wake-promoting agents: search for next generation modafinil: part IV.
Synthesis and biological evaluation of novel 2-(2-arylmethylene)hydrazinyl-4-aminoquinazoline derivatives as potent antitumor agents.
Interference Competition Among Natural Fungal Competitors: an Antifungal Metabolite from the Coprophilous Fungus Preussia fleischhakii.
Kinetics and docking studies of two potential new inhibitors of the nucleoside hydrolase from Leishmania donovani.
JD-5006 and JD-5037: peripherally restricted (PR) cannabinoid-1 receptor blockers related to SLV-319 (Ibipinabant) as metabolic disorder therapeutics devoid of CNS liabilities.
Synthesis, biological evaluation, and molecular docking studies of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives as novel anticancer agents.
New oxirane derivatives of 1,4-naphthoquinones and their evaluation against T. cruzi epimastigote forms.
Azide-alkyne cycloaddition en route to novel 1H-1,2,3-triazole tethered isatin conjugates with in vitro cytotoxic evaluation.
Elucidation of New Binding Interactions with the Tumor Susceptibility Gene 101 (Tsg101) Protein Using Modified HIV-1 Gag-p6 Derived Peptide Ligands.
Synthesis, biological evaluation and molecular modeling of 4,6-diarylpyrimidines and diarylbenzenes as novel non-nucleosides HIV-1 reverse transcriptase inhibitors.
Discovery and optimization of a series of 2-aminothiazole-oxazoles as potent phosphoinositide 3-kinase inhibitors.
Ureido-substituted sulfamates show potent carbonic anhydrase IX inhibitory and antiproliferative activities against breast cancer cell lines.
Synthesis of novel 7-oxo and 7-hydroxy trifluoroallocolchicinoids with cytotoxic effect.
Synthesis and antimalarial evaluation of novel isocryptolepine derivatives.
Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists.
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms.
Dithiocarbamates strongly inhibit carbonic anhydrases and show antiglaucoma action in vivo.
Rapid development of piperidine carboxamides as potent and selective anaplastic lymphoma kinase inhibitors.
Cycloartane and friedelane triterpenoids from the leaves of Caloncoba glauca and their evaluation for inhibition of 11-hydroxysteroid dehydrogenases.
Synthesis and structure elucidation of novel fused 1,2,4-triazine derivatives as potent inhibitors targeting CYP1A1 activity.
Benzenepolycarboxylic acids with potential anti-hemorrhagic properties and structure-activity relationships.
Synthesis and in vitro evaluation of analogues of avocado-produced toxin (+)-(R)-persin in human breast cancer cells.
Synthesis and activity of new macrolones: conjugates between 6(7)-(2'-aminoethyl)-amino-1-cyclopropyl-3-carboxylic acid (2'-hydroxyethyl) amides and 4-propenoyl-azithromycin.
Design and synthesis of active site inhibitors of the human farnesyl pyrophosphate synthase: apoptosis and inhibition of ERK phosphorylation in multiple myeloma cells.
Synthesis and structure-activity relationship study of antimicrotubule agents phenylahistin derivatives with a didehydropiperazine-2,5-dione structure.
Design, synthesis, molecular docking and biological evaluation of new dithiocarbamates substituted benzimidazole and chalcones as possible chemotherapeutic agents.
Design, synthesis, and evaluation of novel 4-thiazolylimidazoles as inhibitors of transforming growth factor- type I receptor kinase.
Synthesis and structure-activity relationship of 5-pyridazin-3-one phenoxypiperidines as potent, selective histamine H(3) receptor inverse agonists.
-PNA: peptide nucleic acid (PNA) with a chiral center at the -position of the PNA backbone.
Synthesis and in vitro characterization of trans- and cis-[(18)F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoropiperidine-1-carboxylates as new potential PET radiotracer candidates for the NR2B subtype N-methyl-D-aspartate receptor.
Synthesis, antitumor activity and SAR study of novel [1,2,4]triazino[4,5-a]benzimidazole derivatives.
Bakuchiol derivatives as novel and potent cytotoxic agents: a report.
Quinazolino-benzothiazoles: fused pharmacophores as anticonvulsant agents.
Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-yl)-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones.
Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) derived from a closely related mGlu5 PAM.
Synthesis of [Tyr-5-(CH2NMe)-Tyr-6]RA-VII, a reduced peptide bond analogue of RA-VII, an antitumor bicyclic hexapeptide.
Design and synthesis of thiourea derivatives containing a benzo[5,6]cyclohepta[1,2-b]pyridine moiety as potential antitumor and anti-inflammatory agents.
Synthesis and evaluation of cytotoxic effects of novel -methylenelactone tetracyclic diterpenoids.
Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.
Orally active zwitterionic factor Xa inhibitors with long duration of action.
Quinazoline-tyrphostin as a new class of antitumor agents, molecular properties prediction, synthesis and biological testing.
Identification, synthesis, and biological evaluation of metabolites of the experimental cancer treatment drugs indotecan (LMP400) and indimitecan (LMP776) and investigation of isomerically hydroxylated indenoisoquinoline analogues as topoisomerase I poisons.
Development of N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-methyl-4-[11C]methylbenzamide for positron emission tomography imaging of metabotropic glutamate 1 receptor in monkey brain.
Discovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Synthesis and biological evaluation of colchicine B-ring analogues tethered with halogenated benzyl moieties.
Bicyclic peptidomimetics targeting secreted aspartic protease 2 (SAP2) from Candida albicans reveal a constrained inhibitory chemotype.
Isolation and structures of axistatins 1-3 from the Republic of Palau marine sponge Agelas axifera Hentschel .
Structures and cytotoxic evaluation of new and known acyclic Ene-Ynes from an American Samoa Petrosia sp. Sponge.
Microwave assisted synthesis and anti-influenza virus activity of 1-adamantyl substituted N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide derivatives.
Identification of novel D-amino acid oxidase inhibitors by in silico screening and their functional characterization in vitro.
Discovery of novel 2-(3-(2-chlorophenyl)pyrazin-2-ylthio)-N-arylacetamides as potent HIV-1 inhibitors using a structure-based bioisosterism approach.
Synthesis and biological evaluation of a fluorescent analog of phenytoin as a potential inhibitor of neuropathic pain and imaging agent.
The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
The cell adhesion and proliferation activities of a peptide derived from human tenascin-C are dependent on two Ile residues.
Design, synthesis and SAR investigation of thienosultam derivatives as ADAMTS-5 (aggrecanase-2) inhibitors.
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
The first total synthesis and biological evaluation of marine natural products ma'edamines A and B.
A novel series of tacrine-selegiline hybrids with cholinesterase and monoamine oxidase inhibition activities for the treatment of Alzheimer's disease.
Discovery of 4-alkylamino-7-aryl-3-cyanoquinoline LRRK2 kinase inhibitors.
Synthesis and biological evaluation of 1-(6-methylpyridin-2-yl)-5-(quinoxalin-6-yl)-1,2,3-triazoles as transforming growth factor- type 1 receptor kinase inhibitors.
Rational design and synthesis of 4-substituted 2-pyridin-2-ylamides with inhibitory effects on SH2 domain-containing inositol 5'-phosphatase 2 (SHIP2).
A new cytotoxic quinolone alkaloid and a pentacyclic steroidal glycoside from the stem bark of Crataeva nurvala: study of anti-proliferative and apoptosis inducing property.
Luteolin suppresses the differentiation of THP-1 cells through the Inhibition of NOX2 mRNA expression and the membrane translocation of p47phox.
Identification and characterization of small molecule inhibitors of signal transducer and activator of transcription 3 (STAT3) signaling pathway by virtual screening.
In vitro efficiency of 9-(N-cinnamoylbutyl)aminoacridines against blood- and liver-stage malaria parasites.
Design, synthesis, biological evaluation and molecular modeling studies of 1-aryl-6-(3,4,5-trimethoxyphenyl)-3(Z)-hexen-1,5-diynes as a new class of potent antitumor agents.
Chemical constituents from the aerial parts of Aster koraiensis with protein glycation and aldose reductase inhibitory activities.
Alstiphyllanines I-O, ajmaline type alkaloids from Alstonia macrophylla showing vasorelaxant activity.
Synthesis, biological evaluation and molecular investigation of fluorinated peroxisome proliferator-activated receptors / dual agonists.
Synthesis and biological activities of 2-[(heteroaryl)methyl]imidazolines.
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.
Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.
Discovery of a novel class of potent human deoxyuridine triphosphatase inhibitors remarkably enhancing the antitumor activity of thymidylate synthase inhibitors.
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.
Drug-like properties: guiding principles for the design of natural product libraries.
Dihydroagarofuran derivatives from the dried roots of Tripterygium wilfordii.
Bidirectional fluorescence properties of pyrene-based peroxisome proliferator-activated receptor (PPAR) / dual agonist.
Marine sponge Hymeniacidon sp. amphilectane metabolites potently inhibit rat brain microglia thromboxane B2 generation.
Structural modifications that alter the P-glycoprotein efflux properties of compounds.
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
Design, synthesis and biological evaluation of pyrazole derivatives as potential multi-kinase inhibitors in hepatocellular carcinoma.
Pre-steady state kinetic analysis of cyclobutyl derivatives of 2'-deoxyadenosine 5'-triphosphate as inhibitors of HIV-1 reverse transcriptase.
Synthesis and structure-activity relationship of aminopyridines with substituted benzoxazoles as c-Met kinase inhibitors.
In vivo evaluation of oral anti-tumoral effect of 3,4-dihydroquinazoline derivative on solid tumor.
Design, synthesis, and antitumor evaluation of 2,4,6-triaryl pyridines containing chlorophenyl and phenolic moiety.
Design and synthesis of pyridin-2-ylmethylaminopiperidin-1-ylbutyl amide CCR5 antagonists that are potent inhibitors of M-tropic (R5) HIV-1 replication.
Discovery of AZD2932, a new Quinazoline Ether Inhibitor with high affinity for VEGFR-2 and PDGFR tyrosine kinases.
AChE inhibitor: a regio- and stereo-selective 1,3-dipolar cycloaddition for the synthesis of novel substituted 5,6-dimethoxy spiro[5.3']-oxindole-spiro-[6.3]-2,3-dihydro-1H-inden-1-one-7-(substituted aryl)-tetrahydro-1H-pyrrolo[1,2-c][1,3]thiazole.
Synthesis and cytotoxic evaluation of novel paraconic acid analogs.
Synthesis and biological evaluation of salicylate-based compounds as a novel class of methionine aminopeptidase inhibitors.
Synthesis and in vitro antimycobacterial activity of compounds derived from (R)- and (S)-2-amino-1-butanol - The crucial role of the configuration.
New potent 5-HT(2A) receptor ligands containing an N'-cyanopicolinamidine nucleus: Synthesis and in vitro pharmacological evaluation.
Synthesis and antimicrobial activities of structurally novel S,S'-bis(heterosubstituted) disulfides.
Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors.
Tubulin inhibitors from an endophytic fungus isolated from Cedrus deodara.
Synthesis and evaluation of apoptosis induction of thienopyrimidine compounds on KRAS and BRAF mutated colorectal cancer cell lines.
Design, synthesis, and pharmacological properties of new heteroarylpyridine/heteroarylpyrimidine derivatives as CB(2) cannabinoid receptor partial agonists.
Bioactive sesterterpenoids from a Korean sponge Monanchora sp.
Dimeric Smac mimetics/IAP inhibitors as in vivo-active pro-apoptotic agents. Part II: Structural and biological characterization.
Discovery of a class of novel tankyrase inhibitors that bind to both the nicotinamide pocket and the induced pocket.
Dibenzocyclooctadiene lignans and norlignans from fruits of Schisandra wilsoniana.
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, A aggregation, and -secretase.
Hypoxia-selective O6-alkylguanine-DNA alkyltransferase inhibitors: design, synthesis, and evaluation of 6-(benzyloxy)-2-(aryldiazenyl)-9H-purines as prodrugs of O6-benzylguanine.
Neolignanamides, lignanamides, and other phenolic compounds from the root bark of Lycium chinense.
Isobutylhydroxyamides from the pericarp of Nepalese Zanthoxylum armatum inhibit NF1-defective tumor cell line growth.
Role of the side chain stereochemistry in the -glucosidase inhibitory activity of kotalanol, a potent natural -glucosidase inhibitor. Part 2.
Cyanide antidotes for mass casualties: water-soluble salts of the dithiane (sulfanegen) from 3-mercaptopyruvate for intramuscular administration.
First synthesis and biological evaluation of indeno[2,1-e]pyrazolo[3,4-b]pyrazin-5-one and related derivatives.
Antimicrobial activity of various 4- and 5-substituted 1-phenylnaphthalenes.
Monocyclic -lactams as antibacterial agents: facing antioxidant activity of N-methylthio-azetidinones.
Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.
Asperterrestide A, a cytotoxic cyclic tetrapeptide from the marine-derived fungus Aspergillus terreus SCSGAF0162.
Abietane diterpenoids and a sesquiterpene pyridine alkaloid from Euonymus lutchuensis.
Triazole derivatives: a series of Darapladib analogues as orally active Lp-PLA2 inhibitors.
Design and synthesis of thiophene dihydroisoquinolines as novel BACE1 inhibitors.
3D-QSAR studies of 1,2-diaryl-1H-benzimidazole derivatives as JNK3 inhibitors with protective effects in neuronal cells.
Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors.
New annelated thieno[2,3-e][1,2,3]triazolo[1,5-a]pyrimidines, with potent anticancer activity, designed through VLAK protocol.
Bioactive barrigenol type triterpenoids from the leaves of Xanthoceras sorbifolia Bunge.
Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a -sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.
Synthesis and evaluation of 2,3-dinorprostaglandins: Dinor-PGD1 and 13-epi-dinor-PGD1 are peroxisome proliferator-activated receptor / dual agonists.
Dynamic modeling of human 5-lipoxygenase-inhibitor interactions helps to discover novel inhibitors.
From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists.
Tri- and tetrasubstituted pyrazole derivates: regioisomerism switches activity from p38MAP kinase to important cancer kinases.
Peroxisome proliferator-activated receptors (PPARs) have multiple binding points that accommodate ligands in various conformations: phenylpropanoic acid-type PPAR ligands bind to PPAR in different conformations, depending on the subtype.
Antiandrogenic, maspin induction, and antiprostate cancer activities of tanshinone IIA and its novel derivatives with modification in ring A.
Rational design of phosphoinositide 3-kinase inhibitors that exhibit selectivity over the phosphoinositide 3-kinase isoform.
Secondary metabolites from the roots of Neolitsea daibuensis and their anti-inflammatory activity.
Naphthoquinone-like polyketide isolated from Streptomyces sp. RI-77 and its predicted biosynthetic pathway.
Discovery of novel indane derivatives as liver-selective thyroid hormone receptor (TR) agonists for the treatment of dyslipidemia.
Phosphodiesterase inhibitors. Part 3: Design, synthesis and structure-activity relationships of dual PDE3/4-inhibitory fused bicyclic heteroaromatic-dihydropyridazinones with anti-inflammatory and bronchodilatory activity.
Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1.
Synthesis and anti-HIV activities of glutamate and peptide conjugates of nucleoside reverse transcriptase inhibitors.
Substituted chromones as highly potent nontoxic inhibitors, specific for the breast cancer resistance protein.
Synthesis and SAR study of imidazoquinolines as a novel structural class of microsomal prostaglandin E2 synthase-1 inhibitors.
Synthesis and antitumor activity of 5,6-dihydro-17-hydroxy icogenin analogs.
Design and synthesis of novel magnolol derivatives as potential antimicrobial and antiproliferative compounds.
PEG-SO(3)H catalyzed synthesis and cytotoxicity of -aminophosphonates.
Novel 1,3,4-heterodiazole analogues: synthesis and in-vitro antitumor activity.
Synthetic menthyl /-(16)-diglucopyranosides-induced cell death in human leukemia cells is dependent on caspases.
Fluorometric detection of adenine in target DNA by exciplex formation with fluorescent 8-arylethynylated deoxyguanosine.
Discovery of nor-seco himbacine analogs as thrombin receptor antagonists.
Synthesis and biological activity of 23-ethylidene-26-hydroxy-22-oxocholestane derivatives from spirostanic sapogenins.
Design, synthesis and in vitro antitumour activity of new heteroaryl ethylenes.
A new high-yield synthetic route to PET CB1 radioligands [11C]OMAR and its analogs.
Derivatives of 8-hydroxyquinoline--antibacterial agents that target intra- and extracellular Gram-negative pathogens.
Human kallikrein 6 inhibitors with a para-amidobenzylanmine P1 group identified through virtual screening.
Synthesis and biological evaluation of piperidine-substituted triazine derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors.
CK2 and CK2' subunits differ in their sensitivity to 4,5,6,7-tetrabromo- and 4,5,6,7-tetraiodo-1H-benzimidazole derivatives.
Nerve growth factor-potentiating benzofuran derivatives from the medicinal fungus Phellinus ribis.
Antimycobacterial activity: a facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines.
Synthesis and structure-activity relationships of pyrido[3,2-b]pyrazin-3(4H)-ones and pteridin-7(8H)-ones as corticotropin-releasing factor-1 receptor antagonists.
Practical synthesis of bredemolic acid, a natural inhibitor of glycogen phosphorylase.
Inhibition of P-glycoprotein activity and reversal of multidrug resistance in vitro by rosemary extract.
Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase.
The Use of 3,5,4'-Tri-O-acetylresveratrol as a Potential Pro-drug for Resveratrol Protects Mice from -Irradiation-Induced Death.
Synthesis of novel pyrazolo[3,4-d]pyrimidine derivatives as potential anti-breast cancer agents.
Synthesis and in vitro and in vivo anticancer activity of novel 3-methyl-5H-isoxazolo[5',4':5,6]pyrido[2,3-b]indoles.
Identification of a glutathione peroxidase inhibitor that reverses resistance to anticancer drugs in human B-cell lymphoma cell lines.
Design, synthesis, and structural analysis of phenylpropanoic acid-type PPAR-selective agonists: discovery of reversed stereochemistry-activity relationship.
Human organic anion transporter 3 (hOAT3) can operate as an exchanger and mediate secretory urate flux.
Secretion of sparfloxacin from the human intestinal Caco-2 cell line is altered by P-glycoprotein inhibitors.
Inhibition of HIV-1 capsid assembly: optimization of the antiviral potency by site selective modifications at N1, C2 and C16 of a 5-(5-furan-2-yl-pyrazol-1-yl)-1H-benzimidazole scaffold.
Synthesis, antimycobacterial and antibacterial activity of ciprofloxacin derivatives containing a N-substituted benzyl moiety.
Synthesis and evaluation of methylsulfonylnitrobenzamides (MSNBAs) as inhibitors of the thyroid hormone receptor-coactivator interaction.
Design and synthesis of novel 2-methyl-4,5-substitutedbenzo[f]-3,3a,4,5-tetrahydro-pyrazolo[1,5-d][1,4]oxazepin-8(7H)-one derivatives as telomerase inhibitors.
Synthesis and evaluation of 8-oxoadenine derivatives as potent Toll-like receptor 7 agonists with high water solubility.
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.
Synthesis and biological evaluation of novel coumarin-pyrazoline hybrids endowed with phenylsulfonyl moiety as antitumor agents.
Sulphonamides: Deserving class as MMP inhibitors?
Design and selection parameters to accelerate the discovery of novel central nervous system positron emission tomography (PET) ligands and their application in the development of a novel phosphodiesterase 2A PET ligand.
Discovery of ML326: The first sub-micromolar, selective M5 PAM.
Synthesis and SAR study of pyrrolo[3,4-b]pyridin-7(6H)-one derivatives as melanin concentrating hormone receptor 1 (MCH-R1) antagonists.
A facile synthesis, antibacterial activity of pulvinone and its derivatives.
Discovery of nosokophic acid, a predicted intermediate of moenomycins, from nosokomycin-producing Streptomyces sp. K04-0144.
Synthesis and evaluation of novel sulfenamides as novel anti Methicillin-resistant Staphylococcus aureus agents.
Synthesis and biological evaluation of novel neuroprotective agents for paraquat-induced apoptosis in human neuronal SH-SY5Y cells.
Synthesis and biological activity against Trypanosoma cruzi of substituted 1,4-naphthoquinones.
Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent 42 nicotinic acetylcholine receptor ligands.
ent-Kaurane diterpenoids from Croton tonkinensis stimulate osteoblast differentiation.
Cellular uptake of covalent conjugates of oligonucleotide with membrane-modifying peptide, peptaibol.
Investigating the activity of quinine analogues versus chloroquine resistant Plasmodium falciparum.
A fluorous and click approach for screening potential PET probes: Evaluation of potential hypoxia biomarkers.
Antiadhesion therapy for urinary tract infections--a balanced PK/PD profile proved to be key for success.
Nitro seco analogues of the duocarmycins containing sulfonate leaving groups as hypoxia-activated prodrugs for cancer therapy.
Design, synthesis, and structure-activity relationship studies of highly potent novel benzoxazinyl-oxazolidinone antibacterial agents.
Alkylated flavanones from the bark of Cryptocarya chartacea as dengue virus NS5 polymerase inhibitors.
Cytotoxic bistetrahydrofuran annonaceous acetogenins from the seeds of Annona squamosa.
Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus.
Synthesis, molecular docking and biological evaluation of 1,3,4-oxadiazole derivatives as potential immunosuppressive agents.
A novel pyrimidine derivatives with aryl urea, thiourea and sulfonamide moieties: synthesis, anti-inflammatory and antimicrobial evaluation.
Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Synthesis and cytotoxicity evaluation of biaryl-based chalcones and their potential in TNF-induced nuclear factor-B activation inhibition.
Structure-activity studies on the anti-proliferation activity of ajoene analogues in WHCO1 oesophageal cancer cells.
Synthesis and antitumor activity of conjugates of 5-Fluorouracil and emodin.
Synthesis and biological activity of dihydroimidazole and 3,4-dihydrobenzo[4,5]imidazo[1,2-a][1,3,5]triazins.
The discovery of 2-fluoro-N-(3-fluoro-4-(5-((4-morpholinobutyl)amino)-1,3,4-oxadiazol-2-yl)phenyl)benzamide, a full agonist of the alpha-7 nicotinic acetylcholine receptor showing efficacy in the novel object recognition model of cognition enhancement.
Biological evaluation and docking studies of recently identified inhibitors of phosphoinositide-3-kinases.
Antimicrobial activity of sulfonamides containing 5-chloro-2-hydroxybenzaldehyde and 5-chloro-2-hydroxybenzoic acid scaffold.
Molecular docking of -sitosterol with some targets related to diabetes.
Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds.
Relationship between structure and P-glycoprotein inhibitory activity of dimeric peptides related to the Dmt-Tic pharmacophore.
Synthesis and antifungal activity of 6,7-bis(arylthio)-quinazoline-5,8-diones and furo[2,3-f]quinazolin-5-ols.
Novel series of 3-amino-N-(4-aryl-1,1-dioxothian-4-yl)butanamides as potent and selective dipeptidyl peptidase IV inhibitors.
Synthesis and biological evaluation of 4,4-dimethyl lithocholic acid derivatives as novel inhibitors of protein tyrosine phosphatase 1B.
Synthetic bicyclic iminosugar derivatives fused thiazolidin-4-one as new potential HIV-RT inhibitors.
Modulation of nitrated lipid signaling by multidrug resistance protein 1 (MRP1): glutathione conjugation and MRP1-mediated efflux inhibit nitrolinoleic acid-induced, PPARgamma-dependent transcription activation.
Transport characteristics of fexofenadine in the Caco-2 cell model.
Broad-spectrum modulation of ATP-binding cassette transport proteins by the taxane derivatives ortataxel (IDN-5109, BAY 59-8862) and tRA96023.
Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum.
One-pot synthesis of novel isoindoline-1,3-dione derivatives bearing 1,2,4-triazole moiety and their preliminary biological evaluation.
Triazolbenzo[d]thiazoles: efficient synthesis and biological evaluation as neuroprotective agents.
Synthesis and structure-activity relationship of 4-(1,3-benzothiazol-2-yl)-thiophene-2-sulfonamides as cyclin-dependent kinase 5 (cdk5)/p25 inhibitors.
Multidrug resistance protein 2 (MRP2) transports HIV protease inhibitors, and transport can be enhanced by other drugs.
Haloenol pyranones and morpholinones as antineoplastic agents of prostate cancer.
Discovery of di-indolinone as a novel scaffold for protein tyrosine phosphatase 1B inhibitors.
Design, synthesis, and structure-activity relationship studies of novel millepachine derivatives as potent antiproliferative agents.
Experimental and 'in silico' analysis of the effect of pH on HIV-1 protease inhibitor affinity: implications for the charge state of the protein ionogenic groups.
Synthesis and biological evaluation of new homocamptothecin analogs.
Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.
Cloning, characterization, and sulfonamide and thiol inhibition studies of an -carbonic anhydrase from Trypanosoma cruzi, the causative agent of Chagas disease.
Anti-neuroinflammatory diarylheptanoids from the rhizomes of Dioscorea nipponica.
Synthesis and anticancer activity of aminodihydroquinoline analogs: identification of novel proapoptotic agents.
Synthesis and study of 1-ethyl-3-carbohydrazide and 3-[1-oxo-2-hydrazino-3-{p-toluenesulfon}]quinolone derivatives against bacterial infections.
Regioselective synthesis of 6-substituted-2-amino-5-bromo-4(3H)-pyrimidinones and evaluation of their antiviral activity.
Design and synthesis of novel quinazoline nitrogen mustard derivatives as potential therapeutic agents for cancer.
An expedient, ionic liquid mediated multi-component synthesis of novel piperidone grafted cholinesterase enzymes inhibitors and their molecular modeling study.
A structure-activity relationship study of 1,2,4-triazolo[1,5-a][1,3,5]triazin-5,7-dione and its 5-thioxo analogues on anti-thymidine phosphorylase and associated anti-angiogenic activities.
Design and synthesis of novel 2'-hydroxy group substituted 2-pyridone derivatives as anticancer agents.
Cytotoxic triterpenoids from Lysimachia parvifolia.
Synthesis of 3'-azido-2',3'-dideoxy-5-fluorouridine phosphoramidates and evaluation of their anticancer activity.
Lessons from (S)-6-(1-(6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)ethyl)quinoline (PF-04254644), an inhibitor of receptor tyrosine kinase c-Met with high protein kinase selectivity but broad phosphodiesterase family inhibition leading to myocardial degeneration in rats.
Discovery, synthesis, and biological evaluation of a novel group of selective inhibitors of filoviral entry.
A novel necroptosis inhibitor-necrostatin-21 and its SAR study.
Search for a novel SIRT1 activator: structural modification of SRT1720 and biological evaluation.
Spongiacidin C, a pyrrole alkaloid from the marine sponge Stylissa massa, functions as a USP7 inhibitor.
Synthesis and evaluation of 8-amino-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives as glycogen synthase kinase-3 (GSK-3) inhibitors.
Low toxicity and unprecedented anti-osteoclast activity of a simple sulfur-containing gem-bisphosphonate: a comparative study.
Modern phenotypic drug discovery is a viable, neoclassic pharma strategy.
Bruton's tyrosine kinase inhibitors: approaches to potent and selective inhibition, preclinical and clinical evaluation for inflammatory diseases and B cell malignancies.
Synthesis and biological evaluation of the first dual tyrosyl-DNA phosphodiesterase I (Tdp1)-topoisomerase I (Top1) inhibitors.
Inhibitors of human immunodeficiency virus type 1 (HIV-1) attachment 6. Preclinical and human pharmacokinetic profiling of BMS-663749, a phosphonooxymethyl prodrug of the HIV-1 attachment inhibitor 2-(4-benzoyl-1-piperazinyl)-1-(4,7-dimethoxy-1H-pyrrolo[2,3-c]pyridin-3-yl)-2-oxoethanone (BMS-488043).
Design, synthesis, and biological evaluation of potent quinoline and pyrroloquinoline ammosamide analogues as inhibitors of quinone reductase 2.
Bivalent Smac mimetics with a diazabicyclic core as highly potent antagonists of XIAP and cIAP1/2 and novel anticancer agents.
Regulators of G protein signaling (RGS) proteins as drug targets: modulating G-protein-coupled receptor (GPCR) signal transduction.
Cytotoxic metabolites from the antarctic psychrophilic fungus Oidiodendron truncatum.
Jomthonic acid , a modified amino acid from a soil-derived Streptomyces.
The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization.
Design, synthesis, and evaluation of novel small molecule inhibitors of the influenza virus protein NS1.
Design, synthesis and in vitro evaluation of novel chroman-4-one, chroman, and 2H-chromene derivatives as human rhinovirus capsid-binding inhibitors.
Novel 1,2,4-triazolo[1,5-a]pyridines and their fused ring systems attenuate oxidative stress and prolong lifespan of Caenorhabiditis elegans.
Structure-based design of novel class II c-Met inhibitors: 1. Identification of pyrazolone-based derivatives.
Strategies to mitigate the bioactivation of 2-anilino-7-aryl-pyrrolo[2,1-f][1,2,4]triazines: identification of orally bioavailable, efficacious ALK inhibitors.
Design, synthesis, theoretical calculations and biological evaluation of new non-symmetrical choline kinase inhibitors.
Total synthesis and bioactivity of the marine alkaloid pityriacitrin and some of its derivatives.
Preparation, antibacterial evaluation and preliminary structure-activity relationship (SAR) study of benzothiazol- and benzoxazol-2-amine derivatives.
Pyronepolyene C-glucosides with NF-B inhibitory and anti-influenza A viral (H1N1) activities from the sponge-associated fungus Epicoccum sp. JJY40.
SAR and biological evaluation of 3-azabicyclo[3.1.0]hexane derivatives as opioid ligands.
Novel hepatitis C virus replicon inhibitors: synthesis and structure-activity relationships of fused pyrimidine derivatives.
A novel franchetine type norditerpenoid isolated from the roots of Aconitum carmichaeli Debx. with potential analgesic activity and less toxicity.
Click chemistry-derived bivalent quinine inhibitors of P-glycoprotein-mediated cellular efflux.
Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists.
The discovery of N-cyclopropyl-4-methyl-3-[6-(4-methylpiperazin-1-yl)-4-oxoquinazolin-3(4H)-yl]benzamide (AZD6703), a clinical p38 MAP kinase inhibitor for the treatment of inflammatory diseases.
Synthesis and cytotoxicity of 3,4-disubstituted-5-(3,4,5-trimethoxyphenyl)-4H-1,2,4-triazoles and novel 5,6-dihydro-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazole derivatives bearing 3,4,5-trimethoxyphenyl moiety.
Small molecule tertiary amines as agonists of the nuclear hormone receptor Rev-erb.
Montmorillonite K-10 mediated green synthesis of cyano pyridines: Their evaluation as potential inhibitors of PDE4.
Antibacterial and antitubercular activity of fosmidomycin, FR900098, and their lipophilic analogs.
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.
Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium.
Novel antiviral C5-substituted pyrimidine acyclic nucleoside phosphonates selected as human thymidylate kinase substrates.
Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver.
Inhibition of P-glycoprotein by flavonoid derivatives in adriamycin-resistant human myelogenous leukemia (K562/ADM) cells.
Biliary transport of irinotecan and metabolites in normal and P-glycoprotein-deficient mice.
Discovery and evolution of phenoxypiperidine hydroxyamide dual CCR3/H1 antagonists. Part I.
Synthesis and antibacterial activity of novel modified 5-O-desosamine ketolides.
Hit-to-lead investigation of a series of novel combined dopamine D2 and muscarinic M1 receptor ligands with putative antipsychotic and pro-cognitive potential.
Design, synthesis, and structure-activity-relationship of phenyl imidazoles as potent Smoothened antagonists.
VX-710 (biricodar) increases drug retention and enhances chemosensitivity in resistant cells overexpressing P-glycoprotein, multidrug resistance protein, and breast cancer resistance protein.
In vivo imaging of hepatobiliary transport function mediated by multidrug resistance associated protein and P-glycoprotein.
Compound instability in dimethyl sulphoxide, case studies with 5-aminopyrimidines and the implications for compound storage and screening.
Role of organic anion transporter OATP1B1 (OATP-C) in hepatic uptake of irinotecan and its active metabolite, 7-ethyl-10-hydroxycamptothecin: in vitro evidence and effect of single nucleotide polymorphisms.
Reversal of multidrug resistance of cancer through inhibition of P-glycoprotein by 5-bromotetrandrine.
Synthesis and antiviral activity of novel HCV NS3 protease inhibitors with P4 capping groups.
Novel quinolone substituted thiazolidin-4-ones as anti-inflammatory, anticancer agents: design, synthesis and biological screening.
Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit.
Fragment-based drug discovery of 2-thiazolidinones as inhibitors of the histone reader BRD4 bromodomain.
Design, synthesis and evaluation of flavonoid derivatives as potential multifunctional acetylcholinesterase inhibitors against Alzheimer's disease.
Discovery and structure-activity relationships of small molecules that block the human immunoglobulin G-human neonatal Fc receptor (hIgG-hFcRn) protein-protein interaction.
Potent and selective tariquidar bioisosters as potential PET radiotracers for imaging P-gp.
Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin.
Heterocyclic bismuth carboxylates based on a diphenyl sulfone scaffold: synthesis and antifungal activity against Saccharomyces cerevisiae.
Structure-based fragment screening is demonstrated to be a practical lead discovery method for a representative G-protein-coupled receptor.
Development of a selective peptide macrocycle inhibitor of coagulation factor XII toward the generation of a safe antithrombotic therapy.
Synthesis, preliminary structure-activity relationships, and in vitro biological evaluation of 6-aryl-3-amino-thieno[2,3-b]pyridine derivatives as potential anti-inflammatory agents.
Identification and synthesis of N-(thiophen-2-yl) benzamide derivatives as BRAF(V600E) inhibitors.
Inhibitory effect on NO production of triterpenes from the fruiting bodies of Ganoderma lucidum.
Structure-activity relationship study on benzoic acid part of diphenylamine-based retinoids.
Enantiomeric derivatives of tokinolide B: absolute configuration and biological properties.
Structural modifications modulate stability of glutathione-activated arylated diazeniumdiolate prodrugs.
Photoaffinity labeling of Ras converting enzyme using peptide substrates that incorporate benzoylphenylalanine (Bpa) residues: improved labeling and structural implications.
Novel nanomolar imidazo[4,5-b]pyridines as selective nitric oxide synthase (iNOS) inhibitors: SAR and structural insights.
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.
Malaria-infected mice are completely cured by one 6 mg/kg oral dose of a new monomeric trioxane sulfide combined with mefloquine.
In silico assay for assessing phospholipidosis potential of small druglike molecules: training, validation, and refinement using several data sets.
Ianthelliformisamines A-C, antibacterial bromotyrosine-derived metabolites from the marine sponge Suberea ianthelliformis.
Identification of pyridazin-3-one derivatives as potent, selective histamine H3 receptor inverse agonists with robust wake activity.
Discovery of 1-arylcarbonyl-6,7-dimethoxyisoquinoline derivatives as glutamine fructose-6-phosphate amidotransferase (GFAT) inhibitors.
Synthesis and anti-inflammatory activity of some new 4,5-dihydro-1,5-diaryl-1H-pyrazole-3-substituted-heteroazole derivatives.
Diarylheptanoids from Curcuma kwangsiensis and their inhibitory activity on nitric oxide production in lipopolysaccharide-activated macrophages.
Design and synthesis of a biotinylated probe of COX-2 inhibitor nimesulide analog JCC76.
Structure and property based design, synthesis and biological evaluation of -lactam based HDAC inhibitors: part II.
Synthesis, docking and in vitro antimalarial evaluation of bifunctional hybrids derived from -lactams and 7-chloroquinoline using click chemistry.
A three-step protocol for lead optimization: quick identification of key conformational features and functional groups in the SAR studies of non-ATP competitive MK2 (MAPKAPK2) inhibitors.
Structure-based design of isoindoline-1,3-diones and 2,3-dihydrophthalazine-1,4-diones as novel B-Raf inhibitors.
Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
On the search for potential anti-Trypanosoma cruzi drugs: synthesis and biological evaluation of 2-hydroxy-3-methylamino and 1,2,3-triazolic naphthoquinoidal compounds obtained by click chemistry reactions.
Synthesis and cytotoxicity of O,O'-dialkyl {[2-(substituted phenoxy)acetamido](substituted phenyl)methyl}phosphonates.
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targeting 51: part 1.
Combination of two chromophores: synthesis and PDT application of porphyrin-pentamethinium conjugate.
Novel antileukemic agents derived from tamibarotene and nitric oxide donors.
Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives.
Structure-based design, synthesis and biological evaluation of N-pyrazole, N'-thiazole urea inhibitors of MAP kinase p38.
Design, synthesis, and structure-activity relationships of novel spiro-piperidines as acetyl-CoA carboxylase inhibitors.
[18F](R)-5-chloro-1-(1-cyclopropyl-2-methoxyethyl)-3-(4-(2-fluoroethoxy)-2,5-dimethyl phenylamino)pyrazin-2(1H)-one: introduction of N3-phenylpyrazinones as potential CRF-R1 PET imaging agents.
Structure-guided design, synthesis and biological evaluation of novel DNA ligase inhibitors with in vitro and in vivo anti-staphylococcal activity.
Lignans from Schisandra sphenathera Rehd. et Wils. and semisynthetic schisantherin A analogues: absolute configuration, and their estrogenic and anti-proliferative activity.
Design and synthesis of 1H-1,2,3-triazoles derived from econazole as antitubercular agents.
Increase in bile flow and biliary excretion of glutathione-derived sulfhydryls in rats by drug-metabolizing enzyme inducers is mediated by multidrug resistance protein 2.
Design and synthesis of Pictet-Spengler condensation products that exhibit oncogenic-RAS synthetic lethality and induce non-apoptotic cell death.
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as -secretase inhibitors.
Identification and development of the 1,4-benzodiazepin-2-one and quinazoline-2,4-dione scaffolds as submicromolar inhibitors of HAT.
Design, synthesis and antimicrobial activities of nitroimidazole derivatives containing 1,3,4-oxadiazole scaffold as FabH inhibitors.
Inhibition of P-glycoprotein activity and reversal of cancer multidrug resistance by Momordica charantia extract.
Role of organic anion transporter 1 (OAT1) in cephaloridine (CER)-induced nephrotoxicity.
Uptake and efflux of the peptidic delta-opioid receptor agonist.
Chemoenzymatic synthesis and evaluation of 3-azabicyclo[3.2.0]heptane derivatives as dopaminergic ligands.
Armeniaspiroles, a new class of antibacterials: Antibacterial activities and total synthesis of 5-chloro-Armeniaspirole A.
Structure-activity relationship of benzodiazepine derivatives as LXXLL peptide mimetics that inhibit the interaction of vitamin D receptor with coactivators.
Discovery of thienopyrimidine-based inhibitors of the human farnesyl pyrophosphate synthase--parallel synthesis of analogs via a trimethylsilyl ylidene intermediate.
Small-molecular, non-peptide, non-ATP-competitive polo-like kinase 1 (Plk1) inhibitors with a terphenyl skeleton.
Discovery of disubstituted piperidines and homopiperidines as potent dual NK1 receptor antagonists-serotonin reuptake transporter inhibitors for the treatment of depression.
Synthesis and evaluation of quinazoline derivatives as phosphodiesterase 7 inhibitors.
Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors.
Biocatalytic synthesis, structural elucidation, antioxidant capacity and tyrosinase inhibition activity of long chain fatty acid acylated derivatives of phloridzin and isoquercitrin.
Exploration of 1-(3-chloro-4-(4-oxo-4H-chromen-2-yl)phenyl)-3-phenylurea derivatives as selective dual inhibitors of Raf1 and JNK1 kinases for anti-tumor treatment.
Substituted indolin-2-ones as p90 ribosomal S6 protein kinase 2 (RSK2) inhibitors: Molecular docking simulation and structure-activity relationship analysis.
Synthesis, molecular docking and evaluation of thiazolyl-pyrazoline derivatives containing benzodioxole as potential anticancer agents.
Design, synthesis and molecular docking of ,-unsaturated cyclohexanone analogous of curcumin as potent EGFR inhibitors with antiproliferative activity.
Stereoselective synthesis of a new class of potent and selective inhibitors of human 8,7-sterol isomerase.
Search for new tools to combat Gram-negative resistant bacteria among amine derivatives of 5-arylidenehydantoin.
Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors.
Gold(III) chloride catalyzed regioselective synthesis of pyrano[3,4-b]indol-1(9H)-ones and evaluation of anticancer potential towards human cervix adenocarcinoma.
SAR studies of 9-norbornylpurines as Coxsackievirus B3 inhibitors.