| Tryptophan-containing dipeptide derivatives as potent ppar gamma antagonists: design, synthesis, biological evaluation, and molecular modeling | |
| Deng, Guanghui1; Liu, Zhiguo1; Ye, Fei1; Luo, Xiaomin1; Zhu, Weiliang1; Shen, Xu1,2; Liu, Hong1; Jiang, Hualiang1,2 | |
| 刊名 | European journal of medicinal chemistry
 |
| 2008-12-01 | |
| 卷号 | 43期号:12页码:2699-2716 |
| 关键词 | Difficult sequence Dipeptide Ppar Sar Tryptophan |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2008.01.032 |
| 通讯作者 | Liu, hong(hliu@mail.shcnc.ac.cn) |
| 英文摘要 | The discovery of peroxisome proliferator-activated receptor gamma (ppar gamma) antagonists (also termed "selective ppar gamma modulators, sppar gamma m") is now of a great interest in the treatment of diabetes and obesity. the structure of compound la (g3335, fig. 1), a novel class of ppar gamma antagonist, is entirely different from that of other reported ppar gamma antagonists. a series of 35 novel analogues (1b-1, 9a-d, 13a-t) were designed, synthesized and evaluated against the agonistic effects exerted by rosiglitazone. these results indicated that most functional groups of la were conserved, and six new compounds (1b, 1c, and 9a-d) exhibited strong ppar gamma antagonistic activities (ic(50) values of 5.2-25.8 mu m) against 10 mu m rosiglitazone in the promotion of the ppar gamma-lbd-cbp (ligand-binding domain and camp-response-element binding protein) interaction as investigated by yeast two-hybrid technology based assay. molecular modeling studies for compounds 1a-d, 1h, 9c-d, and 13a were also presented. (c) 2008 elsevier masson sas. all rights reserved. |
| WOS关键词 | ACTIVATED-RECEPTOR-GAMMA ; ADIPOCYTE DIFFERENTIATION ; ANTIDIABETIC ACTIVITY ; INSULIN SENSITIZER ; GENE-EXPRESSION ; LIGAND-BINDING ; IN-VITRO ; MODULATOR ; AGONISTS ; OBESITY |
| WOS研究方向 | Pharmacology & Pharmacy |
| WOS类目 | Chemistry, Medicinal |
| 语种 | 英语 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| WOS记录号 | WOS:000261984000008 |
| 内容类型 | 期刊论文 |
| URI标识 | http://www.corc.org.cn/handle/1471x/2388929 |
| 专题 | 中国科学院大学 |
| 通讯作者 | Liu, Hong |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Grad Sch, State Key Lab Drug Res,Shanghai Inst Mat Med,Drug, Shanghai 201203, Peoples R China 2.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Deng, Guanghui,Liu, Zhiguo,Ye, Fei,et al. Tryptophan-containing dipeptide derivatives as potent ppar gamma antagonists: design, synthesis, biological evaluation, and molecular modeling[J]. European journal of medicinal chemistry,2008,43(12):2699-2716. |
| APA | Deng, Guanghui.,Liu, Zhiguo.,Ye, Fei.,Luo, Xiaomin.,Zhu, Weiliang.,...&Jiang, Hualiang.(2008).Tryptophan-containing dipeptide derivatives as potent ppar gamma antagonists: design, synthesis, biological evaluation, and molecular modeling.European journal of medicinal chemistry,43(12),2699-2716. |
| MLA | Deng, Guanghui,et al."Tryptophan-containing dipeptide derivatives as potent ppar gamma antagonists: design, synthesis, biological evaluation, and molecular modeling".European journal of medicinal chemistry 43.12(2008):2699-2716. |
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