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ID: ALA1139279

Journal: Bioorg Med Chem Lett

Title: 3,4-Disubstituted indole acylsulfonamides: a novel series of potent and selective human EP3 receptor antagonists.

Authors: Zhou N, Zeller W, Krohn M, Anderson H, Zhang J, Onua E, Kiselyov AS, Ramirez J, Halldorsdottir G, Andrésson T, Gurney ME, Singh J.

Abstract: A series of potent and selective EP(3) receptor antagonists are described. Utilizing a pharmacophore model developed for the EP(3) receptor, a series of 3,4-disubstituted indoles were shown to be high affinity ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors and are potent antagonists in functional assays.

CiteXplore: 19022669

DOI: 10.1016/j.bmcl.2008.11.007