{Reference Type}: Journal Article
{Title}: Design, synthesis and biological evaluation of 1-aryldonepezil analogues as anti-Alzheimer's disease agents.
{Author}: Luo J;Xu JJ;Ren HJ;Xu JB;Gao F;Fang DM;Wan LX;
{Journal}: Future Med Chem
{Volume}: 16
{Issue}: 10
{Year}: 2024
{Factor}: 4.767
{DOI}: 10.4155/fmc-2023-0369
{Abstract}: 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].