Prospective acetylcholinesterase inhibitory activity of indole and its analogs

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• 作者：Nantaka Khorana^a ; ^{nantakak@nu.ac.th} ; ^{nantaka@hotmail.com} ; Kanokwan Changwichit^a ; Kornkanok Ingkaninan^a ; Maleeruk Utsintong^b
• 关键词：Indoles ; 尾-Carbolines ; Quinolines ; Acetylcholinesterase inhibitory activity ; Alzheimer&rsquo ; s disease
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 April, 2012
• 卷：22
• 期：8
• 页码：2885-2888
• 文件大小：866 K

摘要

Acetylcholinesterase (AChE) inhibitory activity is one of the proposed targets for indole analogs. Simple indoles with substitution of methoxy, carboxy or hydroxy at the benzene ring showed a low percent of inhibitory activity in eel-AChE. Adding a side chain at the pyrrole ring, such as serotonin, 尾-carbolines and quinolines (the bioisostere of indole), improved the inhibitory activity significantly. However, proper substitution and conformation of the ring were required for good binding. The result of inhibition in human-AChE of serotonin, 尾-carbolines and quinolines showed similar profile as eel-AChE with lower magnitude. The data from molecular docking showed that they shared the same binding site as galantamine.