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

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

Volume: 14 Issue: 1

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

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

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.

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Najafi Zahra, Mahdavi Mohammad, Saeedi Mina, Sabourian Reyhaneh, Khanavi Mahnaz, Safavi Maliheh, Tehrani Barazandeh Maliheh, Shafiee Abbas, Foroumadi Alireza and Akbarzadeh Tahmineh, 1,2,3-Triazole-Isoxazole Based Acetylcholinesterase Inhibitors: Synthesis, Biological Evaluation and Docking Study, Letters in Drug Design & Discovery 2017; 14 (1) . https://dx.doi.org/10.2174/1570180813666160628085515