Literature DB >> 19188065

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

Nian Zhou1, Wayne Zeller, Jun Zhang, Emmanuel Onua, Alex S Kiselyov, Jose Ramirez, Gudrún Palsdottir, Gudrún Halldorsdottir, Thornorkell Andrésson, Mark E Gurney, Jasbir Singh.   

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.

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Year:  2009        PMID: 19188065     DOI: 10.1016/j.bmcl.2008.12.112

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.

Authors:  Jian Jin; Angel Morales-Ramos; Patrick Eidam; John Mecom; Yue Li; Carl Brooks; Mark Hilfiker; David Zhang; Ning Wang; Dongchuan Shi; Pei-San Tseng; Karen Wheless; Brian Budzik; Karen Evans; Jon-Paul Jaworski; Jack Jugus; Lisa Leon; Charlene Wu; Mark Pullen; Bhumika Karamshi; Parvathi Rao; Emma Ward; Nicholas Laping; Christopher Evans; Colin Leach; Dennis Holt; Xin Su; Dwight Morrow; Harvey Fries; Kevin Thorneloe; Richard Edwards
Journal:  ACS Med Chem Lett       Date:  2010-05-14       Impact factor: 4.345

Review 2.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

  2 in total

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