Synthesis and Biological Activities of Novel GPR40 Agonists
文献类型：期刊论文
| 作者 | Huang Jing2; Guo Bin1 ; Zhou Xianli2
|
| 刊名 | Chinese Journal of Synthetic Chemistry
 |
| 出版日期 | 2016 |
| 卷号 | 24期号:1页码:1-5 |
| 关键词 | 2-butyne-1,4-diol GPR40 agonist benzo-dihydrofuran derivative synthesis biological activity |
| ISSN号 | 1005-1511 |
| 其他题名 | 新型GPR40激动剂的合成及其生物活性 |
| 文献子类 | Article |
| 英文摘要 | Methyl 2-{ 6-[4-(tert-butyldimethylsilyloxy) but-2-ynyloxy]-2,3-dihydrobenzofuran-3-yl} acetate(3) was prepared by protection of 2-butyne-1,4 -diol with tert-butyldimethylsilyl chloride,then Mitsunobu reaction with methyl 2-(6-hydroxy-2,3 -dihydrobenzofuran-3-yl) acetate. Six novel benzo-dihydrofuran derivatives(7a ~ 7f) were synthesized by deprotection,Mitsunobu reaction with phenol derivatives and hydrolysis from 3. The structures were characterized by ~1H NMR,~(13)C NMR and HR-EIMS. The activities of 7a ~ 7f were tested in GPR40-transfected HEK293 cells. The results showed that 7a ~ 7f all exhibited agonistic activities on GPR40,7e and 7f were the most potent componds,with the EC_(50) of 0.593 mumol?L~(-1) and 0.596 mumol?L~(-1),respectively. |
| 资助项目 | 国家自然科学基金资助项目[00000000] |
| WOS研究方向 | Chemistry ; Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5775406 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269242]  |
| 专题 | 药物化学研究室 |
| 作者单位 | 1.Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China. 2.School of Life Science and Engineering,Southwest Jiaotong University, Chengdu, Sichuan 610031, China.; |
| 推荐引用方式 GB/T 7714 | Huang Jing,Guo Bin,Zhou Xianli. Synthesis and Biological Activities of Novel GPR40 Agonists[J]. Chinese Journal of Synthetic Chemistry,2016,24(1):1-5. |
| APA | Huang Jing,Guo Bin,&Zhou Xianli.(2016).Synthesis and Biological Activities of Novel GPR40 Agonists.Chinese Journal of Synthetic Chemistry,24(1),1-5. |
| MLA | Huang Jing,et al."Synthesis and Biological Activities of Novel GPR40 Agonists".Chinese Journal of Synthetic Chemistry 24.1(2016):1-5. |
入库方式： OAI收割
来源：上海药物研究所
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