Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.

Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore.

Bioorganic & medicinal chemistry letters (2010-11-16)

Yukihiro Nishio, Hidenori Kimura, Shinya Tosaki, Eiji Sugaru, Mutsuko Sakai, Masakuni Horiguchi, Yumi Masui, Michiko Ono, Tsutomu Nakagawa, Hiroyuki Nakahira

PMID21074430

摘要

Structures containing the (R)-3-amino-3-methyl piperidine unit as a new pharmacophore moiety have been shown to possess moderate inhibitory activity for DPP-4 with good pharmacokinetics profile. One of these compounds was found to have good oral bioavailability and PK/PD profile in ZF-rat.