香豆素类单胺氧化酶B抑制剂的研究进展

发布时间：2019-01-27 14:23

【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.
[Abstract]:Monoamine oxidase (MAO) plays an important role in maintaining normal levels of neurotransmitters and biogenic amines in brain and mammalian tissues. MAO-B is an important target in the treatment of Alzheimer's disease (AD). MAO-A is mainly used to treat depression. The first generation, second generation MAO-B irreversible inhibitor has great toxicity and side effect, and its clinical application is limited. With the aggravation of aging, it is urgent to find an efficient and reversible MAO-B selective inhibitor. Coumarins have been widely studied in recent years because of their strong MAO-B inhibitory activity. In this paper, the recent advances in the studies of coumarin MAO-B inhibitors are reviewed, and their structure-activity relationships are summarized.
【作者单位】：浙江工业大学长三角绿色制药协同创新中心;
【分类号】：R914

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