115 articles for thisTarget
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The crystal structure, absolute configuration, and phosphodiesterase inhibitory activity of (+)-1-(4-bromobenzyl)-4-(3-(cyclopentyloxy)- 4-methoxyphenyl)-pyrrolidin-2-one.
Smithkline Beecham Pharmaceuticals
(+/-) 3-Amino-6-carboxamido-1,2,3,4-tetrahydrocarbazole: a conformationally restricted analogue of 5-carboxamidotryptamine with selectivity for the serotonin 5-HT1D receptor.
Smithkline Beecham Pharmaceuticals
Potent nonpeptide angiotensin II receptor antagonists. 2. 1-(Carboxybenzyl)imidazole-5-acrylic acids.
Smithkline Beecham Pharmaceuticals
Synthesis and muscarinic activities of quinuclidin-3-yltriazole and -tetrazole derivatives.
Smithkline Beecham Pharmaceuticals
Substituent variation in azabicyclic triazole- and tetrazole-based muscarinic receptor ligands.
Smithkline Beecham Pharmaceuticals
Comparison of azabicyclic esters and oxadiazoles as ligands for the muscarinic receptor.
Smithkline Beecham Pharmaceuticals
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
Smithkline Beecham Pharmaceuticals
Design and synthesis of novel 2,3-dihydro-1H-isoindoles with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
Novel 2,3,4,5-tetrahydro-1H-3-benzazepines with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
1-[2-[(Heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT2C receptor inverse agonists.
Smithkline Beecham Pharmaceuticals
1-[2-[(Heteroaryloxy)heteroaryl]carbamoyl]indolines: novel and selective 5-HT2C receptor inverse agonists with potential as antidepressant/anxiolytic agents.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
Novel 1,2,3,4-tetrahydroisoquinolines with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
Heterocyclic analogues of 2-aminotetralins with high affinity and selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
Pyrimidinylimidazole inhibitors of CSBP/p38 kinase demonstrating decreased inhibition of hepatic cytochrome P450 enzymes.
Smithkline Beecham Pharmaceuticals
Fused aminotetralins: novel antagonists with high selectivity for the dopamine D3 receptor.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
(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.
Smithkline Beecham Pharmaceuticals
The selective 5-HT1B receptor inverse agonist 1'-methyl-5-[[2'-methyl-4'-(5-methyl-1,2, 4-oxadiazol-3-yl)biphenyl-4-yl]carbonyl]-2,3,6,7-tetrahydro- spiro[furo[2,3-f]indole-3,4'-piperidine] (SB-224289) potently blocks terminal 5-HT autoreceptor function both in vitro and in vivo.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
Structure-based design of cathepsin K inhibitors containing a benzyloxy-substituted benzoyl peptidomimetic.
Smithkline Beecham Pharmaceuticals
Synthesis, biological activity, and molecular modeling of selective 5-HT(2C/2B) receptor antagonists.
Smithkline Beecham Pharmaceuticals
Benzophenone- and indolecarboxylic acids: potent type-2 specific inhibitors of human steroid 5 alpha-reductase.
Smithkline Beecham Pharmaceuticals
Synthesis, specificity, and antifungal activity of inhibitors of the Candida albicans delta 24-sterol methyltransferase.
Smithkline Beecham Pharmaceuticals
Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134).
Smithkline Beecham Pharmaceuticals
Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
1-substituted 4-aryl-5-pyridinylimidazoles: a new class of cytokine suppressive drugs with low 5-lipoxygenase and cyclooxygenase inhibitory potency.
Smithkline Beecham Pharmaceuticals
Alpha- and beta-adrenoceptors: from the gene to the clinic. 2. Structure-activity relationships and therapeutic applications.
Smithkline Beecham Pharmaceuticals
Synthesis of structural analogs of leukotriene B4 and their receptor binding activity.
Smithkline Beecham Pharmaceuticals
Cyclic nucleotide phosphodiesterase inhibition by imidazopyridines: analogues of sulmazole and isomazole as inhibitors of the cGMP specific phosphodiesterase.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
Aminoalkyl adenylate and aminoacyl sulfamate intermediate analogues differing greatly in affinity for their cognate Staphylococcus aureus aminoacyl tRNA synthetases.
Smithkline Beecham Pharmaceuticals
Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of four stereoisomeric analogues of the natural product SB-219383.
Smithkline Beecham Pharmaceuticals
The inhibition of human cytomegalovirus (hCMV) protease by hydroxylamine derivatives.
Smithkline Beecham Pharmaceuticals
Rigidone, a sesquiterpene o-quinone from the gorgonian Pseudopterogorgia rigida.
Smithkline Beecham Pharmaceuticals
Discovery of potent and selective phenylalanine derived CCR3 receptor antagonists. Part 2.
Smithkline Beecham Pharmaceuticals
Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1.
Smithkline Beecham Pharmaceuticals
Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.
Smithkline Beecham Pharmaceuticals
Diastereoselective synthesis, activity and chiral stability of cyclic alkoxyketone inhibitors of cathepsin K.
Smithkline Beecham Pharmaceuticals
Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
N-1 substituted pyrimidin-4-ones: novel, orally active inhibitors of lipoprotein-associated phospholipase A2.
Smithkline Beecham Pharmaceuticals
Metal mediated protease inhibition: design and synthesis of inhibitors of the human cytomegalovirus (hCMV) protease.
Smithkline Beecham Pharmaceuticals
CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.
Smithkline Beecham Pharmaceuticals
Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent.
Smithkline Beecham Pharmaceuticals
2-(Alkylthio)pyrimidin-4-ones as novel, reversible inhibitors of lipoprotein-associated phospholipase A2.
Smithkline Beecham Pharmaceuticals
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.
Smithkline Beecham Pharmaceuticals
Selective inhibition of low affinity IgE receptor (CD23) processing: P1' bicyclomethyl substituents.
Smithkline Beecham Pharmaceuticals
Interaction of tyrosyl aryl dipeptides with S. aureus tyrosyl tRNA synthetase: inhibition and crystal structure of a complex.
Smithkline Beecham Pharmaceuticals
Design and synthesis of diaminopyrrolidinone inhibitors of human osteoclast cathepsin K.
Smithkline Beecham Pharmaceuticals
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.
Smithkline Beecham Pharmaceuticals
Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.
Smithkline Beecham Pharmaceuticals
Inhibition of human cytomegalovirus protease by enedione derivatives of thieno[2,3-d]oxazinones through a novel dual acylation/alkylation mechanism.
Smithkline Beecham Pharmaceuticals
Inhibition of herpes proteases and antiviral activity of 2-substituted thieno[2,3-d]oxazinones.
Smithkline Beecham Pharmaceuticals
Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.
Smithkline Beecham Pharmaceuticals
Benzothiopyran-4-one based reversible inhibitors of the human cytomegalovirus (HCMV) protease.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Smithkline Beecham Pharmaceuticals
Selective inhibition of low affinity IgE receptor (CD23) processing.
Smithkline Beecham Pharmaceuticals
Hydroxamate-based inhibitors of low affinity IgE receptor (CD23) processing.
Smithkline Beecham Pharmaceuticals
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.
Smithkline Beecham Pharmaceuticals
Conformationally constrained 1,3-diamino ketones: a series of potent inhibitors of the cysteine protease cathepsin K.
Smithkline Beecham Pharmaceuticals
Design of [R-(Z)]-(+)-alpha-(methoxyimino)-1-azabicyclo[2.2.2]octane-3-acetonitri le (SB 202026), a functionally selective azabicyclic muscarinic M1 agonist incorporating the N-methoxy imidoyl nitrile group as a novel ester bioisostere.
Smithkline Beecham Pharmaceuticals
6-Chloro-5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]- indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist.
Smithkline Beecham Pharmaceuticals
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Smithkline Beecham Pharmaceuticals
Bicyclic N-hydroxyurea inhibitors of 5-lipoxygenase: pharmacodynamic, pharmacokinetic, and in vitro metabolic studies characterizing N-hydroxy-N-(2,3-dihydro-6-(phenylmethoxy)-3-benzofuranyl)urea.
Smithkline Beecham Pharmaceuticals
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
Smithkline Beecham Pharmaceuticals
(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.
Smithkline Beecham Pharmaceuticals
ATP-citrate lyase as a target for hypolipidemic intervention. Design and synthesis of 2-substituted butanedioic acids as novel, potent inhibitors of the enzyme.
Smithkline Beecham Pharmaceuticals
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid: a novel high-affinity leukotriene B4 receptor antagonist.
Smithkline Beecham Pharmaceuticals
A novel constrained reduced-amide inhibitor of HIV-1 protease derived from the sequential incorporation of gamma-turn mimetics into a model substrate.
Smithkline Beecham Pharmaceuticals
Synthesis of novel N-phosphonoalkyl dipeptide inhibitors of human collagenase.
Smithkline Beecham Pharmaceuticals
Synthesis of novel modified dipeptide inhibitors of human collagenase: beta-mercapto carboxylic acid derivatives.
Smithkline Beecham Pharmaceuticals
Synthesis and LTB4 receptor antagonist activities of the naturally occurring LTB4 receptor antagonist Leucettamine A and related analogues.
Smithkline Beecham Pharmaceuticals
Trisubstituted pyridine leukotriene B4 receptor antagonists: synthesis and structure-activity relationships.
Smithkline Beecham Pharmaceuticals
1,3-Diarylindan-2-carboxylic acids, potent and selective non-peptide endothelin receptor antagonists.
Smithkline Beecham Pharmaceuticals
Inhibition of cyclic nucleotide phosphodiesterase by derivatives of 1,3-bis(cyclopropylmethyl)xanthine.
Smithkline Beecham Pharmaceuticals
(E)-3-[[[[6-(2-carboxyethenyl)-5-[[8-(4- methoxyphenyl)octyl]oxy]-2-pyridinyl]-methyl]thio]methyl]benzoic acid and related compounds: high affinity leukotriene B4 receptor antagonists.
Smithkline Beecham Pharmaceuticals
Rational design, synthesis, and crystallographic analysis of a hydroxyethylene-based HIV-1 protease inhibitor containing a heterocyclic P1'--P2' amide bond isostere.
Smithkline Beecham Pharmaceuticals
Synthesis of novel thiol-containing citric acid analogues. Kinetic evaluation of these and other potential active-site-directed and mechanism-based inhibitors of ATP citrate lyase.
Smithkline Beecham Pharmaceuticals
Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore.
Smithkline Beecham Pharmaceuticals
Alpha- and beta-adrenoceptors: from the gene to the clinic. 1. Molecular biology and adrenoceptor subclassification.
Smithkline Beecham Pharmaceuticals
A check on rational drug design: crystal structure of a complex of human immunodeficiency virus type 1 protease with a novel gamma-turn mimetic inhibitor.
Smithkline Beecham Pharmaceuticals
Brominated polyacetylenic acids from the marine sponge Xestospongia muta: inhibitors of HIV protease.
Smithkline Beecham Pharmaceuticals
SB-202742, a novel beta-lactamase inhibitor isolated from Spondias mombin.
Smithkline Beecham Pharmaceuticals
1,4-Cyclohexanecarboxylates: potent and selective inhibitors of phosophodiesterase 4 for the treatment of asthma.
Smithkline Beecham Pharmaceuticals
Novel and selective 5-HT2C/2B receptor antagonists as potential anxiolytic agents: synthesis, quantitative structure-activity relationships, and molecular modeling of substituted 1-(3-pyridylcarbamoyl)indolines.
Smithkline Beecham Pharmaceuticals
The chemistry of pseudomonic acid. 18. Heterocyclic replacement of the alpha,beta-unsaturated ester: synthesis, molecular modeling, and antibacterial activity.
Smithkline Beecham Pharmaceuticals
The chemistry of pseudomonic acid. 17. Dual-action C-1 oxazole derivatives of pseudomonic acid having an extended spectrum of antibacterial activity.
Smithkline Beecham Pharmaceuticals
Design and synthesis of 2-naphthoate esters as selective dopamine D4 antagonists.
Smithkline Beecham Pharmaceuticals
1-(carboxybenzyl)imidazole-5-acrylic acids: potent and selective angiotensin II receptor antagonists.
Smithkline Beecham Pharmaceuticals
Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists.
Smithkline Beecham Pharmaceuticals
Investigation of conformational specificity at GPIIb/IIIa: evaluation of conformationally constrained RGD peptides.
Smithkline Beecham Pharmaceuticals
Imidazole-5-acrylic acids: potent nonpeptide angiotensin II receptor antagonists designed using a novel peptide pharmacophore model.
Smithkline Beecham Pharmaceuticals
Combination Alzheimer therapy using anti-N3pGlu Abeta antibodies + a BACE inhibitor
Eli Lilly
Rho-associated protein kinase inhibitor, pharmaceutical composition comprising the same, as well as preparation method and use thereof
Beijing Tide Pharmaceutical
N-acyl-(3-substituted)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor-mediated disorders
Ogeda
Quinazoline derivatives, compositions thereof, and use as pharmaceuticals
Shanghai Fochon Pharmaceutical
Carbonic anhydrase inhibitors. Comparison of aliphatic sulfamate/bis-sulfamate adducts with isozymes II and IX as a platform for designing tight-binding, more isoform-selective inhibitors.
Cnr
Structure-Based Design, Synthesis, and Biological Evaluation of a Series of Novel and Reversible Inhibitors for the Severe Acute Respiratory Syndrome-Coronavirus Papain-Like Protease.
Purdue University
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents.
Yale University
Terephthalamide derivatives as mimetics of helical peptides: disruption of the Bcl-x(L)/Bak interaction.
Yale University
Enantiomerically pure 1,4-benzodiazepine-2,5-diones as Hdm2 antagonists.
Johnson & Johnson Pharmaceutical
Chalcones: a valid scaffold for monoamine oxidases inhibitors.
Sapienza University of Rome
Conformationally constrained fatty acid ethanolamides as cannabinoid and vanilloid receptor probes.
Universita Del Piemonte Orientale