2,5-Diketopiperazines as potent and selective oxytocin antagonists 1: identification, stereochemistry and initial SAR

This paper covers efforts to discover orally active potent and selective oxytocin antagonists. Screening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure–activity relationship investigations and the determination of the stereochemistry of the most potent compounds.

Graphical abstractScreening pooled libraries identified a novel series of 2,5-diketopiperazine derivatives with antagonist activity at the human oxytocin receptor. We report the initial structure activity relationship investigations and the determination of the stereochemistry of a series of potent and selective oxytocin antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide