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.

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