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J Enzyme Inhib Med Chem. 2020 Dec;35(1):805-814. doi: 10.1080/14756366.2020.1740694.

Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer's disease agents.

Yang J1,2,3,4, Yun Y1,2,3,4, Miao Y1,2,3,4, Sun J2,3,4, Wang X2,3,4.

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School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, Shandong, Jinan, China.
Institute of Materia Medica, Shandong First Medical University and Shandong Academy of Medical Sciences, Shandong, Jinan, China.
Key Laboratory for Biotech-Drugs Ministry of Health, Shandong, Jinan, China.
Key Laboratory for Rare and Uncommon Diseases of Shandong Province, Shandong, Jinan, China.


Multi-target drugs can better address the cascade of events involved in oxidative stress and the reduction in cholinergic transmission that occur in Alzheimer's disease than cholinesterase inhibitors alone. We synthesised a series of 3-arylbenzofuranone derivatives and evaluated their antioxidant activity, cholinesterase inhibitory activity, and monoamine oxidase inhibitory activity. 3-Arylbenzofuranone compounds exhibit good antioxidant activity as well as selective acetylcholinesterase inhibitory activity. The IC50 value of anti-acetylcholinesterase inhibition of Compound 20 (0.089 ± 0.01 μM) is similar to the positive drug donepezil (0.059 ± 0.003 μM). According to the experimental results, Compounds 7, 13 show a certain effect in the in vitro evaluation performed and have the potential as drug candidates for the treatment of Alzheimer's disease.


3-Arylbenzofuranone derivatives; Alzheimer’s disease; antioxidant activity; cholinesterase inhibitors; monoamine oxidase inhibitors

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