摘要
单胺氧化酶(MAO)在维持大脑和哺乳动物组织中神经递质和生物胺的正常水平中起着重要的作用.MAO-B是治疗阿尔兹海默症(AD)的一个重要靶点,而MAO-A主要用于治疗抑郁症.第一代、第二代MAO-B不可逆抑制剂毒副作用大,临床应用受到限制.随着老龄化进程加剧,寻找一种高效、可逆的MAO-B选择性抑制剂已迫在眉睫.香豆素类物质由于其较强的MAO-B抑制活性近年来得到广泛的研究,在此回顾近20年香豆素类MAO-B抑制剂的研究进展,对它们的构效关系进行了阐述和总结.
Monoamine oxidase（MAO） plays a critical role in regulating intracellular levels of neurotransmitters and biogenic amines in brain and peripheral tissues. MAO-B is one of the crucial targets for the treatment of Alzheimer＇s diseases, and MAO-A is for depression. However, earlier MAO-B inhibitors are almost irreversible and limited in clinical application because of their side effects. With the acceleration of aging process, it has been extremely urgent to seek efficient, selective MAO-B inhibitors with less side effects. This review highlights recent major advances in studying coumarin derivatives as MAO-B inhibitors and salient findings related to structure-activity relationship（SAR）.
作者
谢媛媛
黄应益
米治胜
XIE Yuanyuan HUANG Yingyi MI Zhisheng(Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceutical, Zhejiang University of Technology, Hangzb, ou 310014, China)
出处
《浙江工业大学学报》
CAS
北大核心
2017年第4期394-400,共7页
Journal of Zhejiang University of Technology
基金
国家自然科学基金资助项目(21576239)
作者简介
谢媛嫒（1976-），女，安徽宿州人，教授，博士生导师，主要从事药物及中间体的绿色合成新方法、新技术工艺研究，E-mail：xyycz@ziut．edu．cn．
