Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase
文献类型：期刊论文
| 作者 | Zhang, Lei2; Li, Honglin1; Zhu, Qingzhang2; Liu, Jun3; Chen, Ling2; Leng, Ying2 ; Jiang, Hualiang1,2; Liu, Hong2
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2009-10-15 |
| 卷号 | 17期号:20页码:7301-7312 |
| 关键词 | Glucokinase (GK) activators Glycogen phosphorylase (GP) inhibitors Type 2 diabetes Dual action |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2009.08.045 |
| 文献子类 | Article |
| 英文摘要 | A series of benzamide derivatives which can simultaneously inhibit glycogen phosphorylase (GP) and activate glucokinase (GK) were prepared and evaluated. The structure-activity relationships (SAR) of these compounds were also presented. Among these, compounds 12, 13l, 13q, and 13v showed moderate activities towards both GK and GP. Compound 13h inhibited hLGP with an IC50 of 8.95 mu M and activated GK with an EC50 of 1.87 mu M. The possible binding modes of compounds 12, 13l, 13h, and 13q with GP and GK were also explored by molecular docking simulation. (C) 2009 Elsevier Ltd. All rights reserved. |
| WOS关键词 | GLUCOSE-METABOLISM ; SITE ; PARADIGM ; BINDING ; PROTEIN ; ENZYME |
| 资助项目 | National Natural Science Foundation of China[20372069] ; National Natural Science Foundation of China[29725203] ; National Natural Science Foundation of China[20803022] ; National Natural Science Foundation of China[20472094] ; Shanghai Science and Technology Commission[02DJ14006] ; CAS[00000000] ; 863 Hi-Tech Program of China[2006AA020402] ; 863 Hi-Tech Program of China[2006AA020602] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000270434000024 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279100]  |
| 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 药理学第二研究室 |
| 通讯作者 | Liu, Hong |
| 作者单位 | 1.E China Univ Sci & Technol, Sch Pharm, Shanghai 200237, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 3.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Lei,Li, Honglin,Zhu, Qingzhang,et al. Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2009,17(20):7301-7312. |
| APA | Zhang, Lei.,Li, Honglin.,Zhu, Qingzhang.,Liu, Jun.,Chen, Ling.,...&Liu, Hong.(2009).Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase.BIOORGANIC & MEDICINAL CHEMISTRY,17(20),7301-7312. |
| MLA | Zhang, Lei,et al."Benzamide derivatives as dual-action hypoglycemic agents that inhibit glycogen phosphorylase and activate glucokinase".BIOORGANIC & MEDICINAL CHEMISTRY 17.20(2009):7301-7312. |
入库方式： OAI收割
来源：上海药物研究所
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