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Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents.
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2019-12-19 , DOI: 10.1016/j.bmcl.2019.126900
Yinling Yun 1 , Jie Yang 1 , Yuhang Miao 1 , Xiaojing Wang 1 , Jie Sun 1
Affiliation  

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.

中文翻译:

4-芳基香豆素作为潜在的抗阿尔茨海默氏病药物的合成和生物学评估。

阿尔茨海默氏病(AD)是一种具有复杂发病机制的进行性神经退行性疾病。人类的各种研究表明,多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,并研究了它们在体外的活性,包括AChE / BuChE抑制活性,MAO抑制活性和抗氧化活性。发现大多数化合物表现出高抑制活性,并且各个化​​合物具有极其优异的活性。因此4-芳基香豆素为药物设计提供了一种思路,以开发用于AD的治疗剂或预防剂。
更新日期:2019-12-20
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