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

ID: ALA1137004

Journal: Bioorg Med Chem Lett

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

Authors: Taka N, Matsuoka H, Sato T, Yoshino H, Imaoka I, Sato H, Kotake K, Kumagai Y, Kamei K, Ozaki K, Higashida A, Kuroki T.

Abstract: 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.

CiteXplore: 19481451

DOI: 10.1016/j.bmcl.2009.05.059

Patent ID: ┄