4.5 Article

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

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 9, 页码 2709-2712

出版社

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.03.081

关键词

Chromones; Docking; Monoamine oxidase; Inhibitors

资金

  1. Fundacao para a Ciencia e a Tecnologia (FCT) [PTDC/QUI/70359/2006]
  2. A.G. doctoral Grant [SFRH/BD/43531/2008]
  3. Ministerio de Sanidad y Consumo (Spain) [FISS PI061537, FISS PI061457]
  4. Fundação para a Ciência e a Tecnologia [PTDC/QUI/70359/2006] Funding Source: FCT

向作者/读者索取更多资源

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. (C) 2010 Elsevier Ltd. All rights reserved.

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