Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists
文献类型：期刊论文
| 作者 | Huang, Jing1; Guo, Bin2 ; Chu, Wen-Jing2; Xie, Xin3; Yang, Yu-She2; Zhou, Xian-Li1
|
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2016-01 |
| 卷号 | 27期号:1页码:159-162 |
| 关键词 | GPR40 Anti-diabetic Agonist Phenylpropionic acid derivative |
| ISSN号 | 1001-8417 |
| DOI | 10.1016/j.cclet.2015.09.002 |
| 文献子类 | Article |
| 英文摘要 | 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 22g and 23e as potent GPR40 agonists with moderate liver microsomal stability. All the discovery supported further exploration surrounding this scaffold. (C) 2015 Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences. Published by Elsevier B.V. All rights reserved. |
| WOS关键词 | DISCOVERY ; GPR40 |
| 资助项目 | National Natural Science Foundation of China[2140222] |
| WOS研究方向 | Chemistry |
| 语种 | 英语 |
| CSCD记录号 | CSCD:5623721 |
| WOS记录号 | WOS:000369458700034 |
| 出版者 | ELSEVIER SCIENCE INC |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/276251]  |
| 专题 | 药物化学研究室 中科院受体结构与功能重点实验室 新药研究国家重点实验室 |
| 通讯作者 | Yang, Yu-She; Zhou, Xian-Li |
| 作者单位 | 1.Southwest Jiao Tong Univ, Sch Life Sci & Engn, Chengdu 610031, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Mat Med, Natl Ctr Drug Screening, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Huang, Jing,Guo, Bin,Chu, Wen-Jing,et al. Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists[J]. CHINESE CHEMICAL LETTERS,2016,27(1):159-162. |
| APA | Huang, Jing,Guo, Bin,Chu, Wen-Jing,Xie, Xin,Yang, Yu-She,&Zhou, Xian-Li.(2016).Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists.CHINESE CHEMICAL LETTERS,27(1),159-162. |
| MLA | Huang, Jing,et al."Design, synthesis and evaluation of potent G-protein coupled receptor 40 agonists".CHINESE CHEMICAL LETTERS 27.1(2016):159-162. |
入库方式： OAI收割
来源：上海药物研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。