Yun Yinling, Yang Jie, Miao Yuhang, Wang Xiaojing, Sun Jie
School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, Jinan, Shandong, China; Institute of MateriaMedica, Shandong Academy of Medical Sciences, Jinan, Shandong, China; Key Laboratory for Biotech-Drugs Ministry of Health, Jinan, Shandong, China; Key Laboratory for Rare & Uncommon Diseases of Shandong Province, Jinan, Shandong, China.
School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, Jinan, Shandong, China; Institute of MateriaMedica, Shandong Academy of Medical Sciences, Jinan, Shandong, China; Key Laboratory for Biotech-Drugs Ministry of Health, Jinan, Shandong, China; Key Laboratory for Rare & Uncommon Diseases of Shandong Province, Jinan, Shandong, China.
Bioorg Med Chem Lett. 2020 Feb 15;30(4):126900. doi: 10.1016/j.bmcl.2019.126900. Epub 2019 Dec 19.
Alzheimer's disease (AD) is a progressive neurological degenerative disease that has complex pathogenesis. A variety of studies in humans indicate that several enzymes inhibitors can be useful in the treatment of AD, including acetylcholinesterase (AchE), butyrylcholinesterase (BuChE) and monoamine oxidase (MAO). Various substituted 4-arylcoumarin derivatives were synthesised, and their activity in vitro were investigated, including AChE/BuChE inhibitory activity, MAO inhibitory activity, and antioxidant activity. Most of the compounds were found to exhibit high inhibitory activity, and individual compounds have extremely excellent activities. Therefore 4-arylcoumarins provides an idea for drugs design for the development of therapeutic or preventive agents for AD.
阿尔茨海默病（AD）是一种具有复杂发病机制的进行性神经退行性疾病。多项人体研究表明，几种酶抑制剂可用于治疗AD，包括乙酰胆碱酯酶（AchE）、丁酰胆碱酯酶（BuChE）和单胺氧化酶（MAO）。合成了各种取代的4-芳基香豆素衍生物，并研究了它们的体外活性，包括AChE/BuChE抑制活性、MAO抑制活性和抗氧化活性。发现大多数化合物具有高抑制活性，个别化合物具有极其优异的活性。因此，4-芳基香豆素为开发AD治疗或预防药物的药物设计提供了思路。
