Synthesis of glucoconjugates of oleanolic acid as inhibitors of glycogen phosphorylase
文献类型：期刊论文
| 作者 | Cheng, Keguang1,5; Liu, Jun4; Liu, Xiaofeng2; Li, Honglin2,3; Sun, Hongbin5; Xie, Juan1 |
| 刊名 | CARBOHYDRATE RESEARCH
 |
| 出版日期 | 2009-05-12 |
| 卷号 | 344期号:7页码:841-850 |
| 关键词 | Glycogen phosphorylase Oleanolic acid Glucoconjugate Inhibitor Diabetes Click chemistry |
| ISSN号 | 0008-6215 |
| DOI | 10.1016/j.carres.2009.02.012 |
| 文献子类 | Article |
| 英文摘要 | Synthesis and biological evaluation of glucoconjugates of oleanolic acid, linked by either a triazole moiety or an ester function, as novel inhibitors of glycogen phosphorylase have been described. Several triterpene-glycoside conjugates exhibited moderate-to-good inhibitory activity against rabbit muscle GPa. Compound 12 showed the best inhibition with an IC50 value of 1.14 mu M. Structure-activity relationship (SAR) analysis of these inhibitors is also discussed. Possible binding modes of compound 12 were explored by molecular docking simulations. (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | GLUCOSE ANALOG INHIBITORS ; PENTACYCLIC TRITERPENES ; CLICK CHEMISTRY ; IN-VIVO ; DERIVATIVES ; BINDING ; DESIGN ; DISCOVERY ; TARGET ; SITE |
| 资助项目 | National Natural Science Foundation of China[30672523] ; National Natural Science Foundation of China[90713037] ; Chinese ministry of Education[706030] ; Chinese ministry of Education[20050316008] ; New Century Excellent Talents in University[NCET-05-0495] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000266192500001 |
| 出版者 | ELSEVIER SCI LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279243]  |
| 专题 | 药物发现与设计中心 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 | Sun, Hongbin |
| 作者单位 | 1.UniverSud, CNRS, ENS Cachan, PPSM, F-94230 Cachan, France; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Drug Discovery & Design Ctr, Shanghai 201203, Peoples R China; 3.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China 4.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Peoples R China; 5.China Pharmaceut Univ, Coll Pharm, Ctr Drug Discovery, Nanjing 210009, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Cheng, Keguang,Liu, Jun,Liu, Xiaofeng,et al. Synthesis of glucoconjugates of oleanolic acid as inhibitors of glycogen phosphorylase[J]. CARBOHYDRATE RESEARCH,2009,344(7):841-850. |
| APA | Cheng, Keguang,Liu, Jun,Liu, Xiaofeng,Li, Honglin,Sun, Hongbin,&Xie, Juan.(2009).Synthesis of glucoconjugates of oleanolic acid as inhibitors of glycogen phosphorylase.CARBOHYDRATE RESEARCH,344(7),841-850. |
| MLA | Cheng, Keguang,et al."Synthesis of glucoconjugates of oleanolic acid as inhibitors of glycogen phosphorylase".CARBOHYDRATE RESEARCH 344.7(2009):841-850. |
入库方式： OAI收割
来源：上海药物研究所
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