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

Abstract

A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP3 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 EP3 receptor antagonists such as 11g are described.