Synthesis of Some New 3-Coumaranone and Coumarin Derivatives as Dual Inhibitors of Acetyl- and Butyrylcholinesterase

被引：33

作者：

Alipour, Masoumeh ^{[1
]}

Khoobi, Mehdi ^{[2
]}

Nadri, Hamid ^{[3
]}

Sakhteman, Amirhossein ^{[3
]}

Moradi, Alireza ^{[3
]}

Ghandi, Mehdi ^{[1
]}

Foroumadi, Alireza ^{[2
]}

Shafiee, Abbas ^{[2
]}

机构：

[1] Univ Tehran, Univ Coll Sci, Sch Chem, Tehran, Iran

[2] Univ Tehran Med Sci, Dept Med Chem, Fac Pharm & Pharmaceut Sci, Res Ctr, Tehran 14176, Iran

[3] Shahid Sadoughi Univ Med Sci, Fac Pharm, Dept Med Chem, Yazd, Iran

来源：

ARCHIV DER PHARMAZIE | 2013年 / 346卷 / 08期

基金：

美国国家科学基金会;

关键词：

Actylcholinesterase; Butyrylcholinesterase; Coumarin; 3-Coumaranone; Docking study; Phenacyl pyridinium; MILD COGNITIVE IMPAIRMENT; BINDING-SITE INHIBITORS; BIOLOGICAL EVALUATION; ACETYLCHOLINESTERASE INHIBITORS; ALZHEIMERS-DISEASE; DESIGN; HYBRIDS; AGENTS; E2020; CHOLINESTERASE;

D O I：

10.1002/ardp.201300080

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A novel series of coumarin and 3-coumaranone derivatives encompassing the phenacyl pyridinium moiety were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity using Ellman's method. All compounds presented inhibitory activity against both AChE and BuChE in the micromolar range. The molecular docking simulations revealed that all compounds were dual binding site inhibitors of AChE. A kinetic study was performed and the mechanism of enzyme inhibition was proved to be of mixed type. All compounds were tested for their antioxidant activity and no significant activity was observed.

引用

收藏

页码：577 / 587

页数：11

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