Design, synthesis and anticholinesterase activity of a novel series of 1-benzyl-4-((6-alkoxy-3-oxobenzofuran-2(3H)-ylidene) methyl) pyridinium derivatives

被引：65

作者：

Nadri, Hamid ^{[1
]}

Pirali-Hamedani, Morteza ^{[1
]}

Shekarchi, Maryam ^{[2
]}

Abdollahi, Mohammad ^{[3
]}

Sheibani, Vahid ^{[4
]}

Amanlou, Massoud ^{[1
]}

Shafiee, Abbas ^{[1
]}

Foroumadi, Alireza ^{[1
,4
]}

机构：

[1] Univ Tehran Med Sci, Dept Med Chem, Fac Pharm & Pharmaceut Sci, Res Ctr, Tehran 14174, Iran

[2] Res Ctr, Food & Drug Control Labs, Tehran, Iran

[3] Univ Tehran Med Sci, Dept Toxicol, Fac Pharm, Tehran 14174, Iran

[4] Kerman Univ Med Sci, Kerman Neurosci Res Ctr, Kerman, Iran

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2010年 / 18卷 / 17期

基金：

美国国家科学基金会;

关键词：

Benzofuranone; Benzylpyridinium; Cholinesterase inhibitor; Ellman's method; BETA-AMYLOID AGGREGATION; ACETYLCHOLINESTERASE INHIBITORS; ALZHEIMERS-DISEASE; HYDROCHLORIDE;

D O I：

10.1016/j.bmc.2010.07.012

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 novel series of benzofuranone-ylidene-methyl benzylpyridinium derivatives (6a-u) were synthesized as acetylcholinesterase inhibitors. The anticholinesterase activity of synthesized compounds was measured using colorimetric Ellman's method. It was revealed that some synthesized compounds exhibited high anticholinesterase activity, among them compound 6b was the most active compound (IC(50) = 10 +/- 6.87 nM). (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6360 / 6366

页数：7

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