a School of Medicine and Life Sciences , University of Jinan-Shandong Academy of Medical Sciences , Jinan , PR China.
b Institute of Materia Medica , Shandong Academy of Medical Sciences , Jinan , PR China.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):1083-1092. doi: 10.1080/14756366.2019.1615484.
The work is focused on the design of drugs that prevent and treat Alzheimer's disease (AD) and its complications. A series of 3-(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated /. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound exhibited the highest AChE inhibition with an IC value of 0.091 ± 0.011 µM and compound exhibited the highest BuChE inhibition with an IC value of 0.559 ± 0.017 µM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.
本工作集中于设计预防和治疗阿尔茨海默病（AD）及其并发症的药物。设计、合成、充分表征和评估了一系列 3-(4-氨基苯基)-香豆素衍生物。生物测定实验表明，一些化合物对乙酰胆碱酯酶（AChE）和丁酰胆碱酯酶（BuChE）具有明显的选择性抑制作用。在所有化合物中，化合物 对 AChE 的抑制作用最强，IC 值为 0.091 ± 0.011 μM，化合物 对 BuChE 的抑制作用最强，IC 值为 0.559 ± 0.017 μM。使用斑马鱼行为分析仪（Zebrobox）确定活性化合物对氯化铝诱导的斑马鱼运动距离的行为影响。化合物 为开发 AD 及其并发症的治疗或预防药物提供了潜在的药物设计概念。
