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

作者：Shu, Chutian; Ge, Hu; Song, Michael; Chen, Jyun-hong; Zhou, Huimin; Qi, Qu; Wang, Feng; Ma, Xifeng; Yang, Xiaolei; Zhang, Genyan; Ding, Yanwei; Zhou, Dapeng; Peng, Peng; Shih, Cheng-kon; Xu, Jun; Wu, Frank^*

来源：ACS Medicinal Chemistry Letters, 2014, 5(8): 921-926.

DOI：10.1021/ml5001905

• Diabetes
• dipeptidyl peptidase IV (DPP-4)
• inhibitor
• scaffold-hopping
• imigliptin
• OGTT
• pyridinylimidazolone

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.

• 出版日期2014-8
• 单位中山大学