Document Report Card
Basic Information
ID: ALA1153263
Journal: Bioorg Med Chem Lett
Title: 3-Acrylamide-4-aryloxyindoles: synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists.
Authors: Zhou N, Zeller W, Zhang J, Onua E, Kiselyov AS, Ramirez J, Palsdottir G, 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 found to be efficient ligands for this target. These compounds showed high selectivity over IP, FP and other EP receptors. An optimized molecule 7c featured a sound profile and potency in the functional rat and human platelet aggregation assays.
CiteXplore: 19188065