Design, synthesis and evaluation of flavonoid derivatives as potent AChE inhibitors

被引：73

作者：

Sheng, Rong ^{[1
]}

Lin, Xiao ^{[1
]}

Zhang, Jing ^{[2
]}

Chol, Kim Sun ^{[3
]}

Huang, Wenhai ^{[1
]}

Yang, Bo ^{[2
]}

He, Qiaojun ^{[2
]}

Hu, Yongzhou ^{[1
]}

机构：

[1] Zhejiang Univ, ZJU ENS Joint Lab Med Chem, Sch Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China

[2] Zhejiang Univ, Dept Pharmacol, Sch Pharmaceut Sci, Hangzhou 310058, Zhejiang, Peoples R China

[3] Pyongsong Med Univ, Dept Chem, Pyongsong, North Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 18期

基金：

中国国家自然科学基金;

关键词：

Flavonoid derivatives; Synthesis; AChE inhibitor; ACETYLCHOLINESTERASE INHIBITORS; HUPERZINE;

D O I：

10.1016/j.bmc.2009.07.072

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A new series of flavonoid derivatives have been designed, synthesized and evaluated as potent AChE inhibitors. Most of them showed more potent inhibitory activities to AChE than rivastigmine. The most potent inhibitor isoflavone derivative 10d inhibit AChE with a IC50 of 4 nM and showed high BChE/AChE inhibition ratio (4575-fold), superior to donepezil (IC50 = 12 nM, 389-fold). Molecular docking studies were also performed to explore the detailed interaction with AChE. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6692 / 6698

页数：7

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