Design and optimization of potent, selective antagonists of Oxytocin

A novel series of Oxytocin antagonists are described. This series was identified through pharmacophoric overlap of in-house and literature antagonists. Subsequent optimization led to a series of potent, selective antagonists. Several analogues displayed oral bioavailability in vivo in the rat.

Graphical abstractPharmacophoric overlap of a high throughput screening hit and published OT antagonists followed by subsequent optimization led to a series of potent, selective Oxytocin antagonists (X). Several of these analogues showed oral bioavailability in vivo.Figure optionsDownload full-size imageDownload as PowerPoint slide