Literature DB >> 19022669

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

Nian Zhou1, Wayne Zeller, Michael Krohn, Herb Anderson, Jun Zhang, Emmanuel Onua, Alex S Kiselyov, Jose Ramirez, Gułrún 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 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.

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Year:  2008        PMID: 19022669     DOI: 10.1016/j.bmcl.2008.11.007

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


  4 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

3.  Synthesis of C3,C4-Disubstituted Indoles via the Palladium/Norbornene-Catalyzed ortho-Amination/ipso-Heck Cyclization.

Authors:  Alexander J Rago; Guangbin Dong
Journal:  Org Lett       Date:  2021-04-26       Impact factor: 6.072

Review 4.  Mapping PTGERs to the Ovulatory Follicle: Regional Responses to the Ovulatory PGE2 Signal.

Authors:  Soon Ok Kim; Diane M Duffy
Journal:  Biol Reprod       Date:  2016-06-15       Impact factor: 4.285

  4 in total

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