Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375595 | Bioorganic & Medicinal Chemistry Letters | 2009 | 4 Pages |
Abstract
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 profile and potency in the functional rat and human platelet aggregation assays.
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Authors
Nian Zhou, Wayne Zeller, Jun Zhang, Emmanuel Onua, Alex S. Kiselyov, Jose Ramirez, Guðrún Palsdottir, Guðrún Halldorsdottir, Ãorkell Andrésson, Mark E. Gurney, Jasbir Singh,