Synthesis and Biological Evaluation of Genistein Carbamate Derivatives

被引：6

作者：

Qiang, Xiaoming ^{[1
]}

Yuan, Wen ^{[1
]}

Sang, Zhipei ^{[1
]}

Deng, Yong ^{[1
,2
]}

机构：

[1] Sichuan Univ, Dept Med Chem, West China Sch Pharm, Chengdu 610041, Peoples R China

[2] Sichuan Univ, Key Lab Drug Targeting & Drug Delivery Syst, Minist Educ, West China Sch Pharm, Chengdu 610041, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2013年 / 33卷 / 03期

基金：

中国国家自然科学基金;

关键词：

alzheimer's disease; mud-target therapeutics; genistein carbamate derivatives; synthesis; AChE inhibitors; neuroprotective agents; ACID; TACRINE;

D O I：

10.6023/cjoc201210042

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

With genistein as lead compound, twenty-four genistein carbamate derivatives were synthesized from genistein with the structural modification of 7-OH and 4'-OH based on the muti-target-directed drug design strategy. The chemical structures of target compounds were confirmed by H-1 NMR and HRMS techniques. Their acetylcholinesterase and butylcholinesterase inhibitory activity and neuroprotective effects against hydrogen peroxide induced PC12 cell injury were evaluated in vitro. The results indicated that some compounds exhibited the most potent acetylcholinesterase inhibitory activity and neuroprotective effects.

引用

页码：621 / 629

页数：9

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