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

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.

Graphical abstractThe new chemotype DPP-IV inhibitors, such as compound 7c (IC50 = 27 nM), is herein reported.Figure optionsDownload full-size imageDownload as PowerPoint slide