Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors

被引：62

作者：

Jia, Ping ^{[1
]}

Sheng, Rong ^{[1
]}

Zhang, Jing ^{[2
]}

Fang, Liang ^{[2
]}

He, Qiaojun ^{[2
]}

Yang, Bo ^{[2
]}

Hu, Yongzhou ^{[1
]}

机构：

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

[2] Zhejiang Univ, Coll Pharmaceut Sci, Inst Pharmacol & Toxicol, Hangzhou 310058, Zhejiang, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 02期

基金：

中国国家自然科学基金;

关键词：

Galanthamine derivative; Synthesis; Cholinesterase inhibitor; ALZHEIMERS-DISEASE; MOLECULAR DOCKING; ACTIVE-SITE; DONEPEZIL; TACRINE; ANALOG;

D O I：

10.1016/j.ejmech.2008.04.018

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of galanthamine derivatives have been designed, synthesized and evaluated as acetylcholinesterase inhibitors. All of the new compounds prepared showed high AChE inhibitory activities, with compound 3e that has an N-hexyl-benzyl piperidine substituent on the nitrogen atom reaching the best inhibitory activity for AChE (IC50 = 5.62 nM). The docking study performed with AutoDock demonstrated that 3e was nicely accommodated by AChE. (c) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：772 / 784

页数：13

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