Structure− Activity Relationship Studies Leading to the Identification of (2 E)-3-[l-[(2, 4-Dichlorophenyl) methyl]-5-fluoro-3-methyl-l H-indol-7-yl]-N-[(4, 5-dichloro-2- …
…, G Sigthorsson, M Thorsteinnsdottir…
文献索引：Singh, Jasbir; Zeller, Wayne; Zhou, Nian; Hategan, Georgeta; Mishra, Rama K.; Polozov, Alex; Yu, Peng; Onua, Emmanuel; Zhang, Jun; Ramirez, Jose L.; Sigthorsson, Gudmundur; Thorsteinnsdottir, Margret; Kiselyov, Alex S.; Zembower, David E.; Andresson, Thorkell; Gurney, Mark E. Journal of Medicinal Chemistry, 2010 , vol. 53, # 1 p. 18 - 36
The EP3 receptor on the platelet mediates prostaglandin E2 potentiation of thrombogenic coagonists including collagen and adenosine diphosphate (ADP). A pharmacophore driven approach led to the identification of diverse peri-substituted heterocycles as potent and selective EP3 receptor antagonists. A simultaneous chemical optimization and druglike assessment of prioritized molecules converged on a lead compound 50 (DG-041) that ...
