Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.

Abstract

We report our discovery of a novel series of potent and selective dipeptidyl peptidase IV (DPP-4) inhibitors. Starting from a lead identified by scaffold-hopping approach, our discovery and development efforts were focused on exploring structure-activity relationships, optimizing pharmacokinetic profile, improving in vitro and in vivo efficacy, and evaluating safety profile. The selected candidate, Imigliptin, is now undergoing clinical trial.

DOI: 10.1021/ml5001905

Cite this paper

@article{Shu2014DiscoveryOI, title={Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.}, author={Chutian Shu and Hu Ge and Michael Song and Jyun-Hong Chen and Huimin Zhou and Qu Qi and Feng Wang and Xifeng Ma and Xiaolei Yang and Genyan Zhang and Yanwei Ding and Dapeng Zhou and Peng Peng and Cheng-Kon Shih and Jun Xu and Frank Wu}, journal={ACS medicinal chemistry letters}, year={2014}, volume={5 8}, pages={921-6} }