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Published on: July 14, 2010
Design, synthesis and biological evaluation of 1-aryldonepezil analogues as anti-Alzheimer's disease agents
Jiao Luo1, Jing-Jing Xu1, Hui-Jun Ren1
1Department of Pharmacy, The Third People's Hospital of Chengdu, Chengdu, 610041, PR China.
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.
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