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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.
[Box: see text].
[Box: see text].
摘要：
目的：设计并合成一系列新的1-芳基多奈哌齐类似物。材料和方法：通过钯/PCy3催化的Suzuki反应合成了1-芳基多奈哌齐类似物，并评估了胆碱酯酶抑制活性和神经保护作用。进行最有效化合物的硅对接。结果：4-叔丁基苯基类似物对乙酰胆碱酯酶和丁酰胆碱酯酶具有良好的抑制作用，对H2O2诱导的SH-SY5Y细胞损伤具有良好的神经保护作用。结论:4-叔丁基苯基衍生物是一种有前景的抗阿尔茨海默病药物开发的先导化合物。
[方框：见正文]。
[方框：见正文]。
