【摘要】：單胺氧化酶(MAO)在維持大腦和哺乳動物組織中神經(jīng)遞質(zhì)和生物胺的正常水平中起著重要的作用.MAO-B是治療阿爾茲海默癥(AD)的一個重要靶點,而MAO-A主要用于治療抑郁癥.第一代、第二代MAO-B不可逆抑制劑毒副作用大,臨床應(yīng)用受到限制.隨著老齡化進程加劇,尋找一種高效、可逆的MAO-B選擇性抑制劑已迫在眉睫.香豆素類物質(zhì)由于其較強的MAO-B抑制活性近年來得到廣泛的研究,在此回顧近20年香豆素類MAO-B抑制劑的研究進展,對它們的構(gòu)效關(guān)系進行了闡述和總結(jié).
[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.
【作者單位】： 浙江工業(yè)大學長三角綠色制藥協(xié)同創(chuàng)新中心;
【分類號】：R914

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