1H-benzimidazole derivatives as butyrylcholinesterase inhibitors: synthesis and molecular modeling studies

被引:0
作者
Gunes Coban
Luca Carlino
Ayse Hande Tarikogullari
Sülünay Parlar
Görkem Sarıkaya
Vildan Alptüzün
Ayşe Selcen Alpan
Hasan Semih Güneş
Erçin Erciyas
机构
[1] Ege University,Department of Pharmaceutical Chemistry, Faculty of Pharmacy
[2] Martin-Luther University of Halle-Wittenberg,Department of Pharmaceutical Chemistry, Institute of Pharmacy
来源
Medicinal Chemistry Research | 2016年 / 25卷
关键词
Alzheimer’s disease; 1; -Benzimidazole; Acetylcholinesterase inhibitor; Butyrylcholinesterase inhibitor; Ellman’s method; Molecular modeling;
D O I
暂无
中图分类号
学科分类号
摘要
A series of N-{2-[2-(1H-benzimidazole-2-yl)phenoxy]ethyl} substituted amine derivatives were synthesized and tested for their cholinesterase inhibitor activity. Acetylcholinesterase and butyrylcholinesterase inhibitor activities were evaluated in vitro by using Ellman’s method. According to the activity results, all of the compounds displayed moderate acetylcholinesterase inhibitory activity and most of the compounds displayed remarkable butyrylcholinesterase inhibitory activity. Compound 3d was the most active compound in the series and also a selective butyrylcholinesterase inhibitor. Molecular docking studies and molecular dynamic simulations were also carried out.
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页码:2005 / 2014
页数:9
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