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Chromone derivatives bearing pyridinium moiety as multi-target-directed ligands against Alzheimer's disease
Authors
S. Abdpour
S.N.A. Bukhari
+7 more
S.E.S. Ebrahimi
H. Forootanfar
A. Foroumadi
L. Jalili-Baleh
M. Khoobi
H. Nadri
A. Ramazani
Publication date
1 January 2021
Publisher
Abstract
A new serise of 7-hydroxy-chromone derivatives bearing pyridine moiety were synthesized, and evaluated as multifunctional agents against Alzheimer's disease (AD). Most of the compounds were good AChE inhibitors (IC50 = 9.8�0.71 µM) and showed remarkable BuChE inhibition activity (IC50 = 1.9�0.006 µM) compared with donepezil as the standard drug (IC50 = 0.023 and 3.4 µM). Compounds 14 and 10 showed the best inhibitory activity toward AChE (IC50 = 0.71 µM) and BuChE (IC50 = 0.006 µM), respectively. The ligand�protein docking simulations and kinetic studies revealed that compound 14 and 10 could bind effectively to the peripheral anionic binding site (PAS) of the AChE and BuChE through mixed-type inhibition. In addition, the most potent compounds showed acceptable neuroprotective activity on H2O2- and Aβ-induced.neurotoxicity in PC12 cells, more than standard drugs. The compounds could block effectively self- and AChE-induced Aβ aggregation. All the results suggest that compounds 14 and 10 could be considered as promising multi-target-directed ligands against AD. © 2021 Elsevier Inc
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Last time updated on 14/10/2021