3-Acrylamide-4-aryloxyindoles: Synthesis, biological evaluation and metabolic stability of potent and selective EP3 receptor antagonists

A series of potent and selective EP3 receptor antagonists are described. Utilizing a pharmacophore model developed for the EP3 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 pro. le and potency in the functional rat and human platelet aggregation assays. (C) 2009 Elsevier Ltd. All rights reserved.