Discovering benzamide derivatives as glycogen phosphorylase inhibitors and their binding site at the enzyme
文献类型：期刊论文
| 作者 | Chen, Ling; Li, Honglin; Liu, Jun; Zhang, Luyong; Liu, Hong ; Jiang, Hualiang
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2007-11-01 |
| 卷号 | 15期号:21页码:6763-6774 |
| 关键词 | glycogen phosphorylase (GP) inhibitors binding site structure-based pharmacophore molecular docking |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2007.08.003 |
| 文献子类 | Article |
| 英文摘要 | A series of novel benzamide derivatives was designed, synthesized, and their inhibitory activities against glycogen phosphorylase (GP) in the direction of glycogen synthesis by the release of phosphate from glucose-1-phosphate were evaluated. The structure-activity relationships (SAR) of these compounds are also presented. Within this series of compounds, 4m is the most potent GPa inhibitor (IC50 = 2.68 mu M), which is nearly 100 times more potent than the initial compound 1. Analysis of mapping between pharmacophores of different binding sites and each compound demonstrated that these benzamide derivatives bind at the dimer interface of the rabbit muscle enzyme, and possible docking modes of compound 4m were explored by molecular docking simulation. (C) 2007 Elsevier Ltd. All rights reserved. |
| WOS关键词 | POTENTIAL ANTIDIABETIC DRUG ; IN-VITRO ; GLUCOSE ; TARGETS ; VIVO |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000250179600016 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/273118]  |
| 专题 | 新药研究国家重点实验室 中科院受体结构与功能重点实验室 |
| 通讯作者 | Li, Honglin |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Drug Discovery & Design Ctr, Shanghai Inst Mat Med,State Key Lab Drug Res, Shanghai 201203, Peoples R China 2.Dalian Univ Technol, Dept Mech Engn, State Key Lab Struct Anal Ind Equipment, Dalian 116023, Peoples R China 3.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Peoples R China 4.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Chen, Ling,Li, Honglin,Liu, Jun,et al. Discovering benzamide derivatives as glycogen phosphorylase inhibitors and their binding site at the enzyme[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2007,15(21):6763-6774. |
| APA | Chen, Ling,Li, Honglin,Liu, Jun,Zhang, Luyong,Liu, Hong,&Jiang, Hualiang.(2007).Discovering benzamide derivatives as glycogen phosphorylase inhibitors and their binding site at the enzyme.BIOORGANIC & MEDICINAL CHEMISTRY,15(21),6763-6774. |
| MLA | Chen, Ling,et al."Discovering benzamide derivatives as glycogen phosphorylase inhibitors and their binding site at the enzyme".BIOORGANIC & MEDICINAL CHEMISTRY 15.21(2007):6763-6774. |
入库方式： OAI收割
来源：上海药物研究所
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