Synthesis of New Indole Derivatives Structurally Related to Donepezil and Their Biological Evaluation as Acetylcholinesterase Inhibitors

被引：46

作者：

Ismail, Mohamed M. ^{[1
]}

Kamel, Mona M. ^{[1
]}

Mohamed, Lamia W. ^{[1
]}

Faggal, Samar I. ^{[1
]}

机构：

[1] Cairo Univ, Fac Pharm, Dept Organ Pharmaceut Chem, Cairo 11562, Egypt

来源：

MOLECULES | 2012年 / 17卷 / 05期

关键词：

indole; isatin; oxindole; acetylcholinesterase inhibitors; Alzheimer; donepezil; E2020; DESIGN;

D O I：

10.3390/molecules17054811

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：

New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compared to donepezil as standard. The compound 1-(2-(4-(2-fluorobenzyl) piperazin-1-yl)acetyl)indoline-2,3-dione (IIId) was found to be the most potent.

引用

页码：4811 / 4823

页数：13

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