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Synthesis and Bio-Evaluation of New Multifunctional Methylindolinone-1,2,3-Triazole Hybrids As Anti-Alzheimer's Agents Publisher



Saeedi M1, 2 ; Maleki A3 ; Iraji A4 ; Hariri R5 ; Akbarzadeh T2, 5 ; Edraki N4 ; Firuzi O4 ; Mirfazli SS6
Authors
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Authors Affiliations
  1. 1. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  2. 2. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
  3. 3. Department of Chemistry, North Tehran Branch, Islamic Azad University, Tehran, Iran
  4. 4. Medicinal and Natural Products Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran
  5. 5. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Department of Medicinal Chemistry, School of Pharmacy, Iran University of Medical Sciences, Tehran, Iran

Source: Journal of Molecular Structure Published:2021


Abstract

In view of the multifactorial nature of Alzheimer's disease, a new series of methylindolinone-1,2,3-triazole derivatives (7a-n) were efficiently prepared and evaluated for their in vitro cholinesterase inhibitory activity. Although most synthesized compounds showed weak acetylcholinesterase inhibitory activity, they depicted moderate to good activity against butyrylcholinesterase. The IC50 value for anti-BuChE activity of compound 7k was calculated as 4.78 μM which was more potent than the reference drug donepezil (5.19 μM). Based on the molecular docking evaluation, it was found that compound 7k could bind simultaneously to the peripheral and catalytic sites of BuChE. Also, the optimal compound 7k was further assessed as a BACE1 inhibitor and neuroprotective agent. © 2020
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