Discovery of a novel indole series of EP1 receptor antagonists by scaffold hopping

We describe the medicinal chemistry approach that generated a novel indole series of EP1 receptor antagonists. The SAR of this new template was evaluated and culminated in the identification of compound 12g which demonstrated in vivo efficacy in a preclinical model of inflammatory pain.

Graphical abstractThe discovery, synthesis, and biological activity of a novel series of indole EP1 receptor antagonists is described, such as compounds 10a and 12g. Compound 12g demonstrated in vivo efficacy in a preclinical model of inflammatory pain.Figure optionsDownload full-size imageDownload as PowerPoint slide