Literature DB >> 20382016

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

Stefano Alcaro1, Alexandra Gaspar, Francesco Ortuso, Nuno Milhazes, Francisco Orallo, Eugenio Uriarte, Matilde Yáñez, Fernanda Borges.   

Abstract

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. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20382016     DOI: 10.1016/j.bmcl.2010.03.081

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

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