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Novel Tacrine-Coumarin Hybrids Linked to 1,2,3-Triazole As Anti-Alzheimer's Compounds: In Vitro and in Vivo Biological Evaluation and Docking Study Publisher Pubmed



Najafi Z1, 2 ; Mahdavi M3 ; Saeedi M4, 5 ; Karimpourrazkenari E5 ; Edraki N6 ; Sharifzadeh M7 ; Khanavi M8 ; Akbarzadeh T1, 5
Authors

Source: Bioorganic Chemistry Published:2019


Abstract

A new series of tacrine-coumarin hybrids linked to 1,2,3-triazole were designed, synthesized, and tested as potent dual binding site cholinesterase inhibitors (ChEIs) for the treatment of Alzheimer's disease (AD). Among them, compound 8e was the most potent anti-AChE derivative (IC 50 = 27 nM) and compound 8m displayed the best anti-BChE activity (IC 50 = 6 nM) much more active than tacrine and donepezil as the reference drugs. Compound 8e was also evaluated for its BACE1 inhibitory activity and neuroprotectivity against PC12 cells exposed to Aβ 25-35 which indicated low activity. Finally, in vivo studies by Morris water maze task showed that compound 8e significantly reversed scopolamine-induced memory deficit in rats. © 2018
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