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.
J Enzyme Inhib Med Chem. 2020 Dec;35(1):805-814. doi: 10.1080/14756366.2020.1740694.
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 IC value of anti-acetylcholinesterase inhibition of Compound (0.089 ± 0.01 μM) is similar to the positive drug donepezil (0.059 ± 0.003 μM). According to the experimental results, Compounds , show a certain effect in the evaluation performed and have the potential as drug candidates for the treatment of Alzheimer's disease.
多靶标药物在应对阿尔茨海默病中氧化应激级联反应和胆碱能传递减少方面比单独使用胆碱酯酶抑制剂更为有效。我们合成了一系列 3-芳基苯并呋喃酮衍生物，并评估了它们的抗氧化活性、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和选择性乙酰胆碱酯酶抑制活性。化合物 （0.089 ± 0.01 μM）的抗乙酰胆碱酯酶抑制 IC 值与阳性药物多奈哌齐（0.059 ± 0.003 μM）相似。根据实验结果，化合物 、 在评价中表现出一定的效果，具有作为治疗阿尔茨海默病药物候选物的潜力。
