Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists
Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists作者机构：School of Life Science and Engineering Southwest Jiao Tong University State Key Laboratory of Drug Research Shanghai Institute of Materia Medica Chinese Academy of Sciences CAS Key Laboratory of Receptor Research The National Center for Drug Screening Shanghai Institute of Materia Medica Chinese Academy of Sciences
出 版 物：《Chinese Chemical Letters》 (中国化学快报（英文版）)
年 卷 期：2016年第27卷第1期
页 面：159-162页
核心收录：
学科分类：1007[医学-药学(可授医学、理学学位)] 100701[医学-药物化学] 10[医学]
基 金：supported by grants from the National Natural Science Foundation of China (No. 2140222)
主 题：GPR40 Anti-diabetic Agonist Phenylpropionic acid derivative
摘 要：GPR40 has emerged as an attractive drug target for the treatment of type 2 diabetes due to its role in the enhancement of insulin secretion with glucose dependency. With the aim to improve the metabolic and safety profiles, a series of novel phenylpropionic acid derivatives were synthesized. Extensive structural optimization led to identification of compounds 22 g and 23 e as potent GPR40 agonists with moderate liver microsomal stability. All the discovery supported further exploration surrounding this scaffold.
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