Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design
文献类型：期刊论文
| 作者 | Sheng, Ren2,4; Yang, Liu1,3; Zhang, Yanchun2,4; Xing, Enming2,4; Shi, Rui2,4; Wen, Xiaoan2,4; Wang, Heyao1 ; Sun, Hongbin2,4
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
 |
| 出版日期 | 2018-08-15 |
| 卷号 | 28期号:15页码:2599-2604 |
| 关键词 | GPR120 Agonist biphenyl derivatives OGTT Type 2 diabetes |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2018.06.047 |
| 文献子类 | Article |
| 英文摘要 | GPR120 is an attractive target for the treatment of type 2 diabetes. In this study, a series of biphenyl derivatives were designed, synthesized by hybrid design. The selected compound 6a exhibited potent GPR120 agonist activity (EC50 = 93 nM) and high selectivity over GPR40. The results of oral glucose tolerance test (OGTT) demonstrated that 6a exhibited significant glucose-lowering effect in glucose-loaded ICR male mice. Analysis of the structure-activity relationship is also presented. Compound 6a deserves further biological evaluation and structural modifications. |
| WOS关键词 | RECEPTOR 4 FFA4/GPR120 ; IDENTIFICATION ; SECRETION |
| 资助项目 | National Natural Science Foundation of China[81730094] ; National Natural Science Foundation of China[81473262] ; National Natural Science Foundation of China[81573299] ; "111 Project" from the Ministry of Education of China, the State Administration of Foreign Expert Affairs of China[111-2-07] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000440568900004 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279619]  |
| 专题 | 药理学第三研究室 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 | Wang, Heyao; Sun, Hongbin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Jiangsu Key Lab Drug Discovery Metab Dis, 24 Tongjia Xiang, Nanjing 210009, Jiangsu, Peoples R China; 3.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 4.China Pharmaceut Univ, State Key Lab Nat Med, 24 Tongjia Xiang, Nanjing 210009, Jiangsu, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Sheng, Ren,Yang, Liu,Zhang, Yanchun,et al. Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(15):2599-2604. |
| APA | Sheng, Ren.,Yang, Liu.,Zhang, Yanchun.,Xing, Enming.,Shi, Rui.,...&Sun, Hongbin.(2018).Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(15),2599-2604. |
| MLA | Sheng, Ren,et al."Discovery of novel selective GPR120 agonists with potent anti-diabetic activity by hybrid design".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.15(2018):2599-2604. |
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。