Structure - activity relationship studies leading to the identification of (2E)-3-[l-[(2,4-dichlorophenyl)methyl]-5-fluoro-3-methyl-lH-indol-7-yl]-N-[(4, 5-dichloro-2-thienyl)sulfonyl]-2-propenamide (DG-041), a potent and selective prostanoid EP3 receptor antagonist, as a novel antiplatelet agent that does not prolong bleeding

Journal of Medicinal Chemistry

Volumn 53, Issue 1, 2010, Pages 18-36

  Singh, Jasbir ^a   Zeller, Wayne ^a   Zhou, Nian ^a   Hategan, Georgeta ^a   Mishra, Rama K ^a   Polozov, Alex ^a   Yu, Peng ^a   Onua, Emmanuel ^a   Zhang, Jun ^a   Ramírez, José L ^b   Sigthorsson, Gudmundur ^b   Thorsteinnsdottir, Margret ^b   Kiselyov, Alex S ^a   Zembower, David E ^a   Andrésson, Thorkell ^b   Gurney, Mark E ^a,b  

^a DeCODE Chemistry & Biostructures   (United States)

^b DECODE GENETICS   (Iceland)

Author keywords

[No Author keywords available]

Indexed keywords

3 [1 [(2,4 DICHLOROPHENYL)METHYL] 5 FLUORO 3 METHYL 1H INDOL 7 YL] N [(4,5 DICHLORO 2 THIENYL)SULFONYL] 2 PROPENAMIDE; ANTITHROMBOCYTIC AGENT; CYTOCHROME P450 2C9; CYTOCHROME P450 3A4; DG 041; PROSTAGLANDIN E2; PROSTAGLANDIN RECEPTOR BLOCKING AGENT; UNCLASSIFIED DRUG;

ANTICOAGULATION; ARTICLE; BLEEDING TIME; DRUG HALF LIFE; DRUG METABOLISM; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; GENOTOXICITY; HUMAN; IC 50; MAXIMUM PLASMA CONCENTRATION; MOLECULAR STABILITY; NONHUMAN; REACTION ANALYSIS; STRUCTURE ACTIVITY RELATION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOSIS;

ACRYLAMIDES; BLOOD COAGULATION; DRUG DISCOVERY; HEMORRHAGE; HUMANS; LIGANDS; MOLECULAR STRUCTURE; PLATELET AGGREGATION; PLATELET AGGREGATION INHIBITORS; RECEPTORS, PROSTAGLANDIN E; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP; SULFONES;

EID: 74849116661     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm9005912     Document Type: Article

References (23)

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