%0 Journal Article
%T Design, synthesis and biological evaluation of 1-aryldonepezil analogues as anti-Alzheimer's disease agents.
%A Luo J
%A Xu JJ
%A Ren HJ
%A Xu JB
%A Gao F
%A Fang DM
%A Wan LX
%J Future Med Chem
%V 16
%N 10
%D 2024
%M 38910574
%F 4.767
%R 10.4155/fmc-2023-0369
%X Aim: To design and synthesize a novel series of 1-aryldonepezil analogues. Materials & methods: The 1-aryldonepezil analogues were synthesized through palladium/PCy3-catalyzed Suzuki reaction and were evaluated for cholinesterase inhibitory activities and neuroprotective effects. In silico docking of the most effective compound was conducted. Results: The 4-tert-butylphenyl analogue exhibited good inhibitory potency against acetylcholinesterase and butyrylcholinesterase and had a favorable neuroprotective effect on H2O2-induced SH-SY5Y cell injury. Conclusion: The 4-tert-butylphenyl derivative is a promising lead compound for anti-Alzheimer's disease drug development.<BR>[Box: see text].