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

Nian Zhou; Wayne Zeller; Michael Krohn; Herb Anderson; Jun Zhang; Emmanuel Onua; Alex S Kiselyov; Jose Ramirez; Gułrún Halldorsdottir; Thornorkell Andrésson; Mark E Gurney; Jasbir Singh

doi:10.1016/j.bmcl.2008.11.007

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

Bioorg Med Chem Lett. 2009 Jan 1;19(1):123-6. doi: 10.1016/j.bmcl.2008.11.007. Epub 2008 Nov 6.

Authors

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

Affiliation

¹ Medicinal Chemistry Department, deCODE Chemistry, Inc, Woodridge, IL 60517, USA.

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

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.

MeSH terms

Humans
Indoles
Ligands
Receptors, Prostaglandin E / antagonists & inhibitors*
Receptors, Prostaglandin E, EP3 Subtype
Structure-Activity Relationship
Sulfonamides / chemical synthesis*
Sulfonamides / pharmacology

Substances

Indoles
Ligands
PTGER3 protein, human
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP3 Subtype
Sulfonamides