新型选择性二肽基肽酶-4抑制剂依米格列净用于治疗2型糖尿病的发现。
Discovery of Imigliptin, a Novel Selective DPP-4 Inhibitor for the Treatment of Type 2 Diabetes.
作者信息
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
机构信息
Department of Project Management, Medicinal Chemistry, Process, Pharmacology, Drug Metabolism and Pharmacokenetics, Toxicology, XuanZhu Pharma , 2518 Tianchen Street, Jinan, Shandong, The People's Republic of China.
School of Pharmaceutical Sciences & Institute of Human Virology, Sun Yat-Sen University , 132 East Circle Road at University City, Guangzhou, The People's Republic of China.
出版信息
ACS Med Chem Lett. 2014 Jun 16;5(8):921-6. doi: 10.1021/ml5001905. eCollection 2014 Aug 14.
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.
摘要
我们报告了我们发现的一系列新型强效且选择性的二肽基肽酶IV（DPP-4）抑制剂。从通过骨架跃迁方法确定的先导化合物开始，我们的发现和开发工作集中在探索构效关系、优化药代动力学特征、提高体外和体内疗效以及评估安全性方面。所选候选药物依米格列汀目前正在进行临床试验。
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