Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists
文献类型：期刊论文
| 作者 | Yu, Juanhong1; Tang, Lei2; Yang, Yushe1 ; Ji, Ruyun1
|
| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2008-11 |
| 卷号 | 43期号:11页码:2428-2435 |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2008.01.029 |
| 文献子类 | Article |
| 英文摘要 | A series of benzopyran derivatives were synthesized and evaluated for PPAR alpha/gamma agonist activities. Most of the compounds exhibit reasonable PPAR alpha and PPAR gamma agonist activities. In particular, compounds 7b, 8b, 8e and 8h with remarkable PPARg EC50 values of 0.001 mu M are excellent full PPAR gamma agonists; with the functional potency about 130, 20 times stronger than that of leading compound 5 and rosiglitazone, respectively. Compounds 7a, 7c, 7d and 8a are dual PPAR alpha/gamma agonists, and all of them gave comparable or stronger PPAR alpha/gamma agonist efficacy than that of the corresponding positive control. (C) 2008 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | ACTIVATED RECEPTOR-ALPHA ; GAMMA ; ACIDS ; DESIGN ; METABOLISM ; DISCOVERY ; AGENTS |
| 资助项目 | Shenzhen Chipscreen Biosciences Ltd[00000000] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000261157100019 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279450]  |
| 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, Yushe |
| 作者单位 | 1.Chinese Acad Sci, Grad Sch, Shanghai Inst Biol Sci, Shanghai Inst Mat Med,State Key Lab Drug Res,CAS, Shanghai 201203, Peoples R China; 2.Guiyang Med Coll, Sch Pharm, Guiyang 550004, Peoples R China |
| 推荐引用方式 GB/T 7714 | Yu, Juanhong,Tang, Lei,Yang, Yushe,et al. Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2008,43(11):2428-2435. |
| APA | Yu, Juanhong,Tang, Lei,Yang, Yushe,&Ji, Ruyun.(2008).Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,43(11),2428-2435. |
| MLA | Yu, Juanhong,et al."Synthesis and evaluation of a series of benzopyran derivatives as PPAR alpha/gamma agonists".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 43.11(2008):2428-2435. |
入库方式： OAI收割
来源：上海药物研究所
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