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Synthesis and biological evaluation of 3-arylbenzofuranone derivatives as potential anti-Alzheimer's disease agents.
Journal of Enzyme inhibition and Medicinal Chemistry ( IF 5.6 ) Pub Date : 2020-03-19 , DOI: 10.1080/14756366.2020.1740694
Jie Yang 1, 2, 3, 4 , Yinling Yun 1, 2, 3, 4 , Yuhang Miao 1, 2, 3, 4 , Jie Sun 2, 3, 4 , Xiaojing Wang 2, 3, 4
Affiliation  

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.

中文翻译:

3-芳基苯并呋喃酮衍生物作为潜在的抗阿尔茨海默氏病药物的合成和生物学评估。

与单独的胆碱酯酶抑制剂相比,多靶点药物可以更好地解决阿尔茨海默氏病中氧化应激和胆碱能传递减少所涉及的一系列事件。我们合成了一系列的3-芳基苯并呋喃酮衍生物,并评估了其抗氧化活性,胆碱酯酶抑制活性和单胺氧化酶抑制活性。3-芳基苯并呋喃酮化合物具有良好的抗氧化活性以及选择性的乙酰胆碱酯酶抑制活性。化合物20的抗乙酰胆碱酯酶抑制作用的IC50值(0.089±0.01μM)与阳性药物多奈哌齐(0.059±0.003μM)相似。根据实验结果,化合物7、13在进行的体外评估中显示出一定的效果,并且有可能作为治疗阿尔茨海默氏病的候选药物
更新日期:2020-04-20
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