Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics

We successfully discovered peptidomimetic motilin antagonists (17c and 17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs.

Peptidomimetic motilin antagonists (17c and 17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs.Figure optionsDownload as PowerPoint slide