Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase
文献类型：期刊论文
| 作者 | Zhang, Lei1; Chen, Xiaojie1; Liu, Jun2; Zhu, Qingzhang1; Leng, Ying1 ; Luo, Xiaomin1; Jiang, Hualiang1; Liu, Hong1
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| 刊名 | EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-12 |
| 卷号 | 58页码:624-639 |
| 关键词 | Glycogen phosphorylase inhibitors Glucokinase activators Type 2 diabetes Dual-target-directed Hybrid |
| ISSN号 | 0223-5234 |
| DOI | 10.1016/j.ejmech.2012.06.020 |
| 文献子类 | Article |
| 英文摘要 | Dual-target-directed agents simultaneously inhibiting glycogen phosphorylase (GP) and activating glucokinase (GK) could decelerate the inflow of glucose from glycogenolysis and accelerate the outflow of glucose in the liver, therefore allow for a better control over hyperglycaemia in a synergetic manner. A series of hybrid compounds were designed by structure-assisted and ligand-based strategies. In vitro bioassays found two novel compounds (1j, 6g) worthy of further optimization on balance of dual action to GP and GK. In addition, for single-target activity, two compounds exhibited more potent GP inhibitory activity and four compounds showed better GK activation than their corresponding references. (C) 2012 Elsevier Masson SAS. All rights reserved. |
| WOS关键词 | PPAR-ALPHA/GAMMA-AGONISTS ; DESIGNING MULTIPLE LIGANDS ; HEPATIC GLUCOSE-PRODUCTION ; TYPE-2 DIABETES THERAPY ; DRUG DISCOVERY ; LIVER ; METABOLISM ; PARADIGM ; ACIDS ; DERIVATIVES |
| 资助项目 | National Basic Research Program of China[2009CB940903] ; National Basic Research Program of China[2012CB518000] ; National Natural Science Foundation of China[20721003] ; National Natural Science Foundation of China[81025017] ; National S&T Major Projects[2012ZX09103-101-072] ; Silver Project[260644] |
| WOS研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000312745100064 |
| 出版者 | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277854]  |
| 专题 | 药理学第一研究室 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 药物化学研究室 |
| 通讯作者 | Leng, Ying |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.China Pharmaceut Univ, Jiangsu Ctr Drug Screening, Nanjing 210038, Jiangsu, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Lei,Chen, Xiaojie,Liu, Jun,et al. Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase[J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,2012,58:624-639. |
| APA | Zhang, Lei.,Chen, Xiaojie.,Liu, Jun.,Zhu, Qingzhang.,Leng, Ying.,...&Liu, Hong.(2012).Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase.EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY,58,624-639. |
| MLA | Zhang, Lei,et al."Discovery of novel dual-action antidiabetic agents that inhibit glycogen phosphorylase and activate glucokinase".EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 58(2012):624-639. |
入库方式： OAI收割
来源：上海药物研究所
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