882996-45-4Relevant academic research and scientific papers
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
Singh, Jasbir,Zeller, Wayne,Zhou, Nian,Hategan, Georgeta,Mishra, Rama K.,Polozov, Alex,Yu, Peng,Onua, Emmanuel,Zhang, Jun,Ramírez, José L.,Sigthorsson, Gudmundur,Thorsteinnsdottir, Margret,Kiselyov, Alex S.,Zembower, David E.,Andrésson, Thorkell,Gurney, Mark E.
supporting information; experimental part, p. 18 - 36 (2010/04/26)
The EP3 receptor on the platelet mediates prostaglandin E 2 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 displayed favorable in vitro and functional activities as an inhibitor of human platelet aggregation. This agent is currently in human clinical trials for the treatment of atherothrombosis.
Sulfonamide peri-substituted bicyclics for occlusive artery disease
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Page/Page column 59, (2008/06/13)
Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
