- Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B.
Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B.
Bioorganic & medicinal chemistry letters (2010-04-13)
Stefano Alcaro, Alexandra Gaspar, Francesco Ortuso, Nuno Milhazes, Francisco Orallo, Eugenio Uriarte, Matilde Yáñez, Fernanda Borges
PMID20382016
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.
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