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标题：Synthesis, characterization, biological evaluation, and kinetic study of indole base sulfonamide derivatives as acetylcholinesterase inhibitors in search of potent anti-Alzheimer agent
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作者：Muhammad Taha ; Foziah J. Alshamrani ; Fazal Rahim 等
期刊名称：Journal of King Saud University - Science
印刷版ISSN：1018-3647
出版年度：2021
卷号：33
期号：3
页码：1-8
DOI：10.1016/j.jksus.2021.101401
语种：English
出版社：Elsevier
摘要：Graphical abstractDisplay OmittedAbstractAlzheimer is a prolonged neurodegenerative disease which degenerate the brain cells and particularly affects the person ability to function independently. Despite of dynamic research, there is no proper treatment but can limit their persistent effect in early stages. In search of more potent drug for Alzheimer treatment, we have synthesized indole-based sulfonamide derivatives (1–17). All analogs were screened to find out lead candidate against acetylcholinesterase enzyme under positive control of donepezil as standard drug. Herein this study, analogs1–4,6–9, and13–15showed potent inhibition while kinetic studies further confirmed their mode of inhibition. All the synthesized analogs were characterized through HR-EI-MS,1H NMR and13C NMR spectroscopic techniques.
关键词：Alzheimer;Sulfonamide derivatives;Acetylcholinesterase enzyme;Kinetic study