N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators
文献类型：期刊论文
| 作者 | Liu, Zhiqing2; Zhu, Qingzhang1; Li, Fuying2; Zhang, Lina1; Leng, Ying1 ; Zhang, Ao2
|
| 刊名 | MEDCHEMCOMM
 |
| 出版日期 | 2011-06 |
| 卷号 | 2期号:6页码:531-535 |
| ISSN号 | 2040-2503 |
| DOI | 10.1039/c1md00002k |
| 文献子类 | Article |
| 英文摘要 | A series of novel arylacetamides were designed to further explore the GK binding property at the aminothiazole C5 position. The C5-amide substituted aminothiazoles 7a-f generally displayed decreased potency, whereas most of the C5-triazole substituted aminothiazoles retained good GK potency. Triazole 15 with a hydroxyethyl side chain was the most potent among the current series possessing an EC50 value of 0.18 mu M. Its R-enantiomer R-15 showed similar potency (0.22 mu M) that deserves for further evaluation. |
| WOS关键词 | DIABETES THERAPY ; METABOLIC-REGULATION ; GLUCOSE ; DISCOVERY ; PARADIGM ; PSN-GK1 ; ABILITY ; AGENTS |
| 资助项目 | 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"[2009ZX09301-001] ; National Science & Technology Major Project on "Key New Drug Creation and Manufacturing Program"[2009ZX09103-062] ; Shanghai Commission of Science and Technology[10410702600] ; Shanghai Commission of Science and Technology[10JC1417100] ; Shanghai Commission of Science and Technology[10dz1910104] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000292953500011 |
| 出版者 | ROYAL SOC CHEMISTRY |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/278508]  |
| 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, Shanghai Inst Mat Med SIMM, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med SIMM, Synthet Organ & Med Chem Lab SOMCL, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Liu, Zhiqing,Zhu, Qingzhang,Li, Fuying,et al. N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators[J]. MEDCHEMCOMM,2011,2(6):531-535. |
| APA | Liu, Zhiqing,Zhu, Qingzhang,Li, Fuying,Zhang, Lina,Leng, Ying,&Zhang, Ao.(2011).N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators.MEDCHEMCOMM,2(6),531-535. |
| MLA | Liu, Zhiqing,et al."N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators".MEDCHEMCOMM 2.6(2011):531-535. |
入库方式： OAI收割
来源：上海药物研究所
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