Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators
文献类型：期刊论文
| 作者 | Mao, Weiwei1; Ning, Mengmeng2 ; Liu, Zhiqing1; Zhu, Qingzhang2; Leng, Ying2; Zhang, Ao1
|
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2012-05-01 |
| 卷号 | 20期号:9页码:2982-2991 |
| 关键词 | Type 2 diabetes (T2D) Glucokinase activator Benzamide derivatives Privileged-fragment-merging Aminothiazole |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2012.03.008 |
| 文献子类 | Article |
| 英文摘要 | A series of benzamide derivatives were assembled by using the privileged-fragment-merging (PFM) strategy and their SAR studies as glucokinase activators were described. Compounds 5 and 16b were identified having a suitable balance of potency and activation profile. They showed EC50 values of 28.3 and 44.8 nM, and activation folds of 2.4 and 2.2, respectively. However, both compounds displayed a minor reduction in plasma glucose levels on imprinting control region (ICR) mice. Unfavorable pharmacokinetic profiles (PK) were also observed on these two compounds. (C) 2012 Elsevier Ltd. All rights reserved. |
| WOS关键词 | INSULIN-RESISTANCE ; DIABETES THERAPY ; THIAZOL-2-YL)-2-ARYL-3-(TETRAHYDRO-2H-PYRAN-4-YL) PROPANAMIDES ; METABOLIC-REGULATION ; GLUCOSE ; SECRETION ; DISCOVERY ; PARADIGM ; EFFICACY ; DISEASE |
| 资助项目 | Chinese National Science Foundation[81125021] ; Chinese National Science Foundation[81072528] ; National Basic Research Program of China (973 Program)[2009CB522300] ; National Science & Technology Major Project on 'Key New Drug Creation and Manufacturing Program', China[2012ZX09103-101-035] ; Shanghai postdoctoral research funding program[11R21417900] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000303002100025 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278100]  |
| 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 药物化学研究室 |
| 通讯作者 | Leng, Ying |
| 作者单位 | 1.Chinese Acad Sci, Synthet Organ & Med Chem Lab, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China 2.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Mao, Weiwei,Ning, Mengmeng,Liu, Zhiqing,et al. Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2012,20(9):2982-2991. |
| APA | Mao, Weiwei,Ning, Mengmeng,Liu, Zhiqing,Zhu, Qingzhang,Leng, Ying,&Zhang, Ao.(2012).Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators.BIOORGANIC & MEDICINAL CHEMISTRY,20(9),2982-2991. |
| MLA | Mao, Weiwei,et al."Design, synthesis, and pharmacological evaluation of benzamide derivatives as glucokinase activators".BIOORGANIC & MEDICINAL CHEMISTRY 20.9(2012):2982-2991. |
入库方式： OAI收割
来源：上海药物研究所
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