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

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.

Graphical abstractA 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.Figure optionsDownload full-size imageDownload as PowerPoint slide