Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B

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• 作者：Stefano Alcaro ; Alex ; ra Gaspar ; Francesco Ortuso ; Nuno Milhazes ; Francisco Orallo ; Eugenio Uriarte ; Matilde Yá ; ñ ; ez ; Fern ; a Borges
• 关键词：Chromones ; Docking ; Monoamine oxidase ; Inhibitors
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 May 2010
• 年：2010
• 卷：20
• 期：9
• 页码：2709-2712
• 全文大小：264 K

文摘

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 IC₅₀ data and to explain the absence of activity versus selectivity, respectively.