PMID

Data

Article Title

Organization

Discovery of 5-aryl-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-ones as positive allosteric modulators of metabotropic glutamate subtype-2 (mGlu2) receptors with efficacy in a preclinical model of psychosis.

Merck Research Laboratories

Discovery of 2-[5-(4-Fluorophenylcarbamoyl)pyridin-2-ylsulfanylmethyl]phenylboronic Acid (SX-517): Noncompetitive Boronic Acid Antagonist of CXCR1 and CXCR2.

Syntrix Biosystems

Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.

Glaxosmithkline

Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.

Broad Institute of Mit and Harvard

Novel phomactin analogues as PAF receptor ligands.

The University of Nottingham

Designed multiple ligands. An emerging drug discovery paradigm.

Organon Laboratories

Structure-activity relationships of phomactin derivatives as platelet activating factor antagonists.

Sankyo

Synthesis of alkyl chain-modified ether lipids and evaluation of their in vitro cytotoxicity.

Laboratorios Menarini

Novel antagonists of platelet-activating factor. 2. Synthesis and structure-activity relationships of potent and long-acting heterofused [1,5]benzodiazepine and [1,4]diazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.

Pfizer

Novel antagonists of platelet-activating factor. 1. Synthesis and structure-activity relationships of benzodiazepine and benzazepine derivatives of 2-methyl-1-phenylimidazo[4,5-c]pyridine.

Pfizer

3-(2-(3-Pyridinyl)thiazolidin-4-oyl)indoles, a novel series of platelet activating factor antagonists.

Abbott Laboratories

Design and modeling of new platelet-activating factor antagonists. 1. Synthesis and biological activity of 1,4-bis(3',4',5'-trimethoxybenzoyl)-2-[[(substituted carbonyl and carbamoyl)oxy]methyl]piperazines.

Universit£

Analogues of platelet activating factor. 6. Mono- and bis-aryl phosphate antagonists of platelet activating factor.

American Cyanamid

(Pyridylcyanomethyl)piperazines as orally active PAF antagonists.

J. Uriach & C£A.S.A.

Development, synthesis, and biological evaluation of (-)-trans-(2S,5S)-2-[3-[(2-oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)-phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran, a potent orally active platelet-activating factor (PAF) antagonist and its water-soluble prodrug phosphate ester.

Merck Research Laboratories

1,4-Dihydropyridines as antagonists of platelet activating factor. 1. Synthesis and structure-activity relationships of 2-(4-heterocyclyl)phenyl derivatives.

Pfizer

4-Alkyl-1,4-dihydropyridines derivatives as specific PAF-acether antagonists.

Alter

Platelet activating factor antagonists: synthesis and structure-activity studies of novel PAF analogues modified in the phosphorylcholine moiety.

Takeda Chemical Industries

Structure-activity relationships of kadsurenone analogues.

TBA

A 3D-QSAR study on ginkgolides and their analogues with comparative molecular field analysis.

Chinese Academy of Sciences

 

Cyclic ether acetal platelet activating factor (PAF) receptor antagonists II: imidazo[4,5-c]pyridyl derivatives

TBA

 

Cyclic ether acetal platelet activating factor (PAF) receptor antagonists I: 3-pyridyl derivatives

TBA

 

A partial pharmacophore for the platelet activating factor (PAF) receptor

TBA

 

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

TBA

 

Synthesis and biological activity of MK 287 (L-680,573): a potent, specific and orally active paf receptor antagonist

TBA

 

Cmi-206: A potent dual platelet activating factor antagonist and 5-lipoxygenase inhibitor

TBA

 

Enantiodifferentiation of dihydropyridine PAF antagonists

TBA

 

Synthesis and evaluation of water soluble indole pyrrolothiazole paf antagonists

TBA

 

Discovery and optimization of indole pyrrolothiazole paf antagonists

TBA

 

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.

TBA

 

Synthesis and bioactivities of heterocyclic lipids as PAF antagonists. 2

TBA

 

Synthesis and bioactivities of heterocyclic lipids as PAF antagonists. 1

TBA

 

Synthesis of bicyclic thiazolidine PAF antagonists

TBA

Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.

Pfizer

Chemistry, biosynthesis and biological activity of terpenoids and meroterpenoids in bacteria and fungi isolated from different marine habitats.

Iranian Fisheries Science Research Institute

Preparation of 7-substituted ginkgolide derivatives: potent platelet activating factor (PAF) receptor antagonists.

Columbia University

Ginkgolide derivatives for photolabeling studies: preparation and pharmacological evaluation.

Columbia University

In vitro platelet-activating factor receptor binding inhibitory activity of pinusolide derivatives: a structure-activity study.

Seoul National University

(+/-)-trans-2-[3-methoxy-4-(4-chlorophenylthioethoxy)-5-(N-methyl-N- hydroxyureidyl)methylphenyl]-5-(3,4, 5-trimethoxyphenyl)tetrahydrofuran (CMI-392), a potent dual 5-lipoxygenase inhibitor and platelet-activating factor receptor antagonist.

University of Virginia

Discovery and evaluation of a series of 3-acylindole imidazopyridine platelet-activating factor antagonists.

Abbott Laboratories

Analogues of platelet activating factor. 8. Antagonists of PAF containing an aromatic ring linked to a pyridinium ring.

American Cyanamid

Synthesis and structure-activity relationships of 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF antagonists.

J. Uriach & CíA.

Structural modification of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinoline platelet activating factor receptor antagonists.

Sandoz Research Institute

Antitumor activity of 5-aryl-2,3-dihydroimidazo[2,1-a]isoquinolines.

Sandoz Research Institute

Development of a novel series of trialkoxyaryl derivatives as specific and competitive antagonists of platelet activating factor.

Wellcome Research Laboratories

Pyrido[2,1-b]quinazolinecarboxamide derivatives as platelet activating factor antagonists.

Hoffmann-La Roche

Conformation and activity of tetrahydrofuran lignans and analogues as specific platelet activating factor antagonists.

TBA

Pentadienyl carboxamide derivatives as antagonists of platelet-activating factor.

Roche Research Center

Biphenylcarboxamide derivatives as antagonists of platelet-activating factor.

Roche Research Center

Propenyl carboxamide derivatives as antagonists of platelet activating factor.

Hoffmann-La Roche

Thienotriazolodiazepines as platelet-activating factor antagonists. Steric limitations for the substituent in position 2.

Roche Research Center

Triazolobenzo- and triazolothienodiazepines as potent antagonists of platelet activating factor.

Roche Research Center

Disubstituted tetrahydrofurans and dioxolanes and PAF antagonists.

J. Uriach & CíA.

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.

Schering-Plough

4-substituted 2-alkoxytetrahydrofurans as potent and long-lasting PAF antagonists.

J. Uriach & CíA.

Synthesis and structure-activity relationships of a series of novel benzopyran-containing platelet activating factor antagonists.

Abbott Laboratories

Inhibitory effect of the 4-aminotetrahydroquinoline derivatives, selective chemoattractant receptor-homologous molecule expressed on T helper 2 cell antagonists, on eosinophil migration induced by prostaglandin D2.

Kyowa Hakko Kogyo

SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.

Sanofi-Synthelabo Recherche

SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.

Sanofi Recherche

Biochemical and pharmacological characterization of L-659,989: an extremely potent, selective and competitive receptor antagonist of platelet-activating factor.

Merck Sharp & Dohme Research Laboratories

Functional validation of platelet-activating factor receptor sites characterized biochemically by a specific and reproducible [3H]platelet-activating factor binding in human platelets.

Rhone-Poulenc Sante