Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective huma...

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Heterocyclic 1,7-disubstituted indole sulfonamides are potent and selective human EP3 receptor antagonists.
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We have developed a pharmacophore model for the EP(3) receptor antagonists based on its endogenous ligand PGE(2). This ligand-based design yielded a series of novel peri-substituted [4.3.0] bicyclic aromatics featuring 1-alklyaryl 7-heterocyclic sulfonamide substituents. The synthesized molecules are potent antagonists of human EP(3) receptor in vitro and show inhibition of rat platelets aggregation. Optimized derivatives display high selectivity over IP, FP, and other EP receptor panels.
Bioorganic & medicinal chemistry letters 19(23):6797-800, 2009 Dec 1 - Who cited this? | PubMed ID: 19836233 | Fulltext
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