Discovery of novel protease activated receptors 1 antagonists with potent antithrombotic activity in vivo

Journal of Medicinal Chemistry

Volumn 52, Issue 19, 2009, Pages 5826-5836

  Perez, Michel ^a   Lamothe, Marie ^a   Maraval, Catherine ^a   Mirabel, Etienne ^a   Loubat, Chantal ^a   Planty, Bruno ^a   Horn, Clemens ^a   Michaux, Julien ^a   Marrot, Sebastien ^a   Letienne, Robert ^a   Pignier, Christophe ^a   Bocquet, Arnaud ^a   Nadal Wollbold, Florence ^a   Cussac, Didier ^a   De Vries, Luc ^a   Le Grand, Bruno ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

[No Author keywords available]

Indexed keywords

1 (4 (4 FLUOROBENZYL)PIPERAZIN 1 YL) 3 (2 NITROPHENYL)PROP 2 YN 1 ONE; 1 (4 CYCLOHEPTANECARBONYLPIPERAZIN 1 YL) 3 (2 NITROPHENYL)PROPENONE; 1 (4 CYCLOHEPTANECARBONYLPIPERAZIN 1 YL) 3 (2,6 DIFLUOROPHENYL)PROPENONE; 1 (4 CYCLOHEXYLMETHYLPIPERAZIN 1 YL) 3 (2 NITROPHENYL) PROPENONE; 1 (4 CYCLOPENTYLPIPERAZIN 1 YL) 5 (2 NITROPHENYL)PENTA 2,4 DIEN 1 ONE; 1 (4 FLUOROBENZYL) 4 [3 (2 NITROPHENYL)ACRYLOYL]PIPERAZIN 2 ONE; 1 (4 FLUOROBENZYL) N METHOXY N METHYLPIPERIDINE 4 CARBOXAMIDE; 1 [4 (2 FLUOROBENZENESULFONYL)PIPERAZIN 1 YL] 3 (2 NITROPHENYL)PROPENONE; 1 [4 (3 CHLOROPHENYL)PIPERAZIN 1 YL] 3 (2 NITROPHENYL)PROPENONE; 1 [4 (4 FLUOROBENZYL) 1,4 DIAZEPAN 1 YL] 3 (2 NITROPHENYL)PROP 2 EN 1 ONE; 1 [4 (4 FLUOROBENZYL)PIPERAZIN 1 YL] 3 (2 NITROPHENYL)PROPAN 1 ONE; 1 [4 (4 FLUOROBENZYL)PIPERAZIN 1 YL] 5 (2 NITROPHENYL)PENTA 2,4 DIEN 1 ONE; 1 [4 (4 FLUOROBENZYLAMINO)PIPERIDIN 1 YL] 3 (2 NITROPHENYL)PROP 2 EN 1 ONE; 2 [ 3 (4 CYCLOHEPTANECARBONYLPIPERAZIN 1 YL) 3 OXOPROPENYL]BENZONITRILE; 2 [ 3 [4 (4 FLUOROBENZYL)PIPERAZIN 1 YL] 3 OXOPROPENYL]BENZONITRILE; 2 [5 OXO 5 (4 PYRIDIN 2 YLPIPERAZIN 1 YL)PENTA 1,3 DIENYL]BENZONITRILE; 3 (2 CHLOROPHENYL) 1 [1 (4 FLUOROBENZYL)PIPERIDIN 4 YL]PROP 2 EN 1 ONE; 3 (2 CHLOROPHENYL) 1 [4 (4 FLUOROBENZYL)PIPERAZIN 1 YL]PROPENONE; 3 (2 NITROPHENYL) 1 (4 PYRIDIN 4 YLMETHYLPIPERAZIN 1 YL)PROPENONE; 3 (2 NITROPHENYL) 1 [4 (4 CYANOPHENYL)PIPERAZIN 1 YL]PROPENONE; 3 (2,6 DIFLUOROPHENYL) 1 [4 (3 METHYLBENZYL)PIPERAZIN 1 YL]PROPENONE; 3 (2,6 DIFLUOROPHENYL) 1 [4 (3,4 DIMETHYLBENZYL)PIPERAZIN 1 YL]PROPENONE; 3 (2,6 DIFLUOROPHENYL) 1 [4 (4 FLUOROBENZYL) 2,5 DIMETHYLPIPERAZIN 1 YL]PROP 2 EN 1 ONE; 4 [3 (2 NITROPHENYL)ACRYLOYL]PIPERAZINE 1 CARBOXYLIC ACID CYCLOHEXYLAMIDE; 5 (2 NITROPHENYL) 1 (4 PHENYLPIPERAZIN 1 YL)PENTA 2,4 DIEN 1 ONE; 5 (2 NITROPHENYL)PENTA 2,4 DIENOIC ACID; ANTICOAGULANT AGENT; F 16357; F 16618; PROTEASE ACTIVATED RECEPTOR 1 ANTAGONIST; TERT BUTYL 4 [METHOXY(METHYL)CARBAMOYL]PIPERIDINE 1 CARBOXYLATE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTICOAGULATION; ARTERIOVENOUS SHUNT; ARTICLE; CALCIUM TRANSPORT; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG HALF LIFE; HUMAN; IN VIVO STUDY; MALE; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; RAT; SERUM RESPONSIVE ELEMENT; STRUCTURE ACTIVITY RELATION; SUBSTITUTION REACTION; THROMBOCYTE AGGREGATION;

ANIMALS; DRUG DISCOVERY; DRUG TOXICITY; FIBRINOLYTIC AGENTS; HUMANS; PIPERAZINES; PLATELET AGGREGATION INHIBITORS; PYRIDINES; RATS; RECEPTOR, PAR-1; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 70349640055     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900553j     Document Type: Article

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