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Design, synthesis and biological evaluation of novel 2-methylpyrimidine-4-ylamine derivatives as inhibitors of Escherichia coli pyruvate dehydrogenase complex E1

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成果类型:
期刊论文
作者:
He, Junbo;Feng, Lingling(冯玲玲);Li, Jing;Tao, Ruijuan;Wang, Fang;...
通讯作者:
Wan, Jian
作者机构:
[Feng, Lingling; He, Hongwu; Sun, Qiushuang; He, Junbo; Long, Qingwu; Wan, Jian; Li, Jing; Tao, Ruijuan; Wang, Fang; Ren, Yanliang; Liao, Xun] Cent China Normal Univ, Dept Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Peoples R China.
通讯机构:
[Wan, Jian] C
Cent China Normal Univ, Dept Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Peoples R China.
语种:
英文
关键词:
2-Methylpyrimidine-4-ylamine;Antifungal activity;Click chemistry;PDHc E1 inhibitor
期刊:
Bioorganic & Medicinal Chemistry
ISSN:
0968-0896
年:
2012
卷:
20
期:
5
页码:
1665-1670
基金类别:
National Basic Research Program of ChinaNational Basic Research Program of China [2010CB126100]; Natural Science Foundation of ChinaNational Natural Science Foundation of China (NSFC) [20772042, 21172090]; PCSIRTProgram for Changjiang Scholars & Innovative Research Team in University (PCSIRT) [IRT0953]
机构署名:
本校为第一且通讯机构
院系归属:
化学学院
摘要:
As potential inhibitors of Escherichia coli pyruvate dehydrogenase complex E1 (PDHc E1), a series of novel 2-methylpyrimidine-4-ylamine derivatives were designed based on the structure of the active site of PDHc E1 and synthesized using 'click chemistry'. Their inhibitory activity in vitro against PDHc E1 and fungicidal activity were examined. Some of these compounds such as 3g, 3l, 3n, 3o, and 5b demonstrated to be effective inhibitors of PDHc E1 from E. coli and exhibited antifungal activity. SAR analysis indicated that both, the inhibitory p...

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