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.
第一作者:
Jasbir,Singh
第一单位:
deCODE Chemistry, Inc., 2501 Davey Road, Woodridge, Illinois 60517, USA. JSingh@decode.com
作者:
医学主题词
丙烯酰胺类(Acrylamides);血液凝固(Blood Coagulation);药物发现(Drug Discovery);出血(Hemorrhage);人类(Humans);配体(Ligands);分子结构(Molecular Structure);血小板聚集(Platelet Aggregation);血小板聚集抑制剂(Platelet Aggregation Inhibitors);受体, 前列腺素E(Receptors, Prostaglandin E);受体, 前列腺素E, EP3亚型(Receptors, Prostaglandin E, EP3 Subtype);立体异构现象(Stereoisomerism);构效关系(Structure-Activity Relationship);砜类(Sulfones)
DOI
10.1021/jm9005912
PMID
19957930
发布时间
2010-11-18
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