N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators
N-(5-substituted thiazol-2-yl)-2-aryl-3-(tetrahydro-2H-pyran-4-yl) propanamides as glucokinase activators
复制标题
N-(5-取代的噻唑-2-基)-2-芳基-3-(四氢-2H-吡喃-4-基)丙酰胺作为葡萄糖激酶激活剂
DOI：
10.1039/c1md00002k
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发表时间：
2011-06-01
期刊：
影响因子：
--
通讯作者：
Zhang, Ao
中科院分区：
文献类型：
--
作者：
Liu, Zhiqing;Zhu, Qingzhang;Zhang, Ao
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.
