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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