文章基本信息

标题：Cholinesterase Inhibitory Activity, Kinetic and Molecular Docking Studies of N-(1-substituted-1H-1,2,3-triazole-4-yl)-aralkylamide Derivatives
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作者：Woralak PETRAT ; Chatchai WATTANAPIROMSAKUL ; Teerapat NUALNOI 等
期刊名称：Walailak Journal of Science and Technology (WJST)
印刷版ISSN：2228-835X
出版年度：2016
卷号：14
期号：9
页码：687-701
语种：English
出版社：Institute of Research and Development, Walailak University.
摘要：Acetylcholinesterase (AChE) inhibitors are widely used for treatment of Alzheimer’s disease (AD). With the ultimate goal of improving the efficiency of AChE inhibitors currently used in AD treatment, in this study, a total number of 14 compounds of N -(1-substituted-1 H -1,2,3-triazole-4-yl)-aralkylamide derivatives were designed, synthesized, and investigated for their AChE and butyrylcholinesterase (BuChE) inhibitory activities. The most potent AChE inhibitor in this series was 6e (IC 50 15.01 mM against human AChE). The inhibition kinetics of 6e indicated that the compound was a noncompetitive inhibitor of acetylcholinesterase. A molecular docking study supported the idea that the aromatic moieties of 6e interacted with both a catalytic anionic site and a peripheral anionic site of acetylcholinesterase, while the 1,2,3-triazole ring also formed van der Waals and hydrogen bond interactions with the amino acid residues in the mid-gorge of the enzyme.