Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease

被引：66
|
作者：
Shao, D [1 ]
Zou, CY [1 ]
Luo, C [1 ]
Tang, XC [1 ]
Li, YC [1 ]
机构：
[1] Chinese Acad Sci, Grad Sch, Shanghai Inst Biol Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 18期
关键词：
tacrine-E2020; hybrids; acetylcholinesterase inhibitor; Alzheimer's disease;
D O I：
10.1016/j.bmcl.2004.07.005
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Tacrine-E2020 hybrids and some related compounds were prepared and their bioactivities on the Alzheimer's disease were assayed. The optimum hybrid inhibitor 3 is 37-fold more potent and 31-fold more selective than tacrine in vitro. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4639 / 4642
页数：4
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