色满酮-2-和-3-羧酸抑制单胺氧化酶 A 和 B 的方式不同。
Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B.
机构信息
Dipartimento di Scienze Farmacobiologiche, Facoltà di Farmacia, Università Magna Graecia di Catanzaro, Campus Universitario S. Venuta, Viale Europa, 88100 Catanzaro, Italy.
出版信息
Bioorg Med Chem Lett. 2010 May 1;20(9):2709-12. doi: 10.1016/j.bmcl.2010.03.081. Epub 2010 Mar 27.
Chromone carboxylic acids were evaluated as human monoamine oxidase A and B (hMAO-A and hMAO-B) inhibitors. The biological data indicated that only chromone-3-carboxylic acid is a potent hMAO-B inhibitor, with a high degree of selectivity for hMAO-B compared to hMAO-A. Conversely the chromone-2-carboxylic acid resulted almost inactive against both MAO isoforms. Docking experiments were performed to elucidate the reasons of the different MAO IC(50) data and to explain the absence of activity versus selectivity, respectively.
色酮羧酸类化合物被评估为人类单胺氧化酶 A 和 B（hMAO-A 和 hMAO-B）抑制剂。生物数据表明，只有色酮-3-羧酸是一种强效的 hMAO-B 抑制剂，与 hMAO-A 相比，对 hMAO-B 具有高度的选择性。相反，色酮-2-羧酸对两种 MAO 同工酶几乎没有活性。进行了对接实验，以阐明不同 MAO IC（50）数据的原因，并分别解释缺乏活性与选择性的原因。
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