3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists

Yue H Li; Pei-San Tseng; Karen A Evans; Jon-Paul Jaworski; Dwight M Morrow; Harvey E Fries; Charlene W Wu; Richard M Edwards; Jian Jin

doi:10.1016/j.bmcl.2010.08.137

3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP3 receptor antagonists

Bioorg Med Chem Lett. 2010 Nov 15;20(22):6744-7. doi: 10.1016/j.bmcl.2010.08.137.

Authors

Yue H Li¹, Pei-San Tseng, Karen A Evans, Jon-Paul Jaworski, Dwight M Morrow, Harvey E Fries, Charlene W Wu, Richard M Edwards, Jian Jin

Affiliation

¹ Discovery Medicinal Chemistry, Discovery Research, GlaxoSmithKline Pharmaceuticals, 1250 South Collegeville Road, PO Box 5089, Collegeville, PA 19426-0989, United States. [email protected]

PMID: 20926294
DOI: 10.1016/j.bmcl.2010.08.137

Abstract

A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP(3) antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP(3) receptor antagonists such as 11g are described.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Humans
Pyridones / chemistry
Pyridones / pharmacology*
Rats
Receptors, Prostaglandin E, EP3 Subtype / antagonists & inhibitors*
Structure-Activity Relationship

Substances

Pyridones
Receptors, Prostaglandin E, EP3 Subtype