1,2,3-Triazole-Isoxazole Based Acetylcholinesterase Inhibitors: Synthesis, Biological Evaluation and Docking Study

Author(s): Zahra Najafi, Mohammad Mahdavi, Mina Saeedi, Reyhaneh Sabourian, Mahnaz Khanavi, Maliheh Safavi, Maliheh Barazandeh Tehrani, Abbas Shafiee, Alireza Foroumadi, Tahmineh Akbarzadeh.

Journal Name: Letters in Drug Design & Discovery

Volume 14 , Issue 1 , 2017

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Abstract:

In this work, a series of derivatives containing 1,2,3-triazole and isoxazole were synthesized. All of them were evaluated as novel dual AChE inhibitors. Most of synthesized compounds showed moderate to good inhibitory potency toward AChE. Among them, N-((1-(4-methylbenzyl)- 1H-1,2,3-triazol-4-yl)methyl)-5-(p-tolyl)isoxazole-3-carboxamide (5m) was the most potent AChE inhibitor, being 12-fold more potent than rivastigmine, as the reference drug. Also, molecular modeling revealed that compound 5m targeted both the catalytic anionic site (CAS) and the peripheral anionic site (PAS) of AChE.

Keywords: Alzheimer’s disease, acetylcholinesterase, butyrylcholinesterase, 1, 2, 3-triazole-isoxazole, docking study.

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Article Details

VOLUME: 14
ISSUE: 1
Year: 2017
Page: [58 - 65]
Pages: 8
DOI: 10.2174/1570180813666160628085515
Price: $58

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