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  • 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
ABSTRACT

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.