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

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.

Docking experiments were carried out to explain the quite different inhibition activities of two carboxylic chromone isomers against A and B isoforms of monoamine oxidases.Figure optionsDownload as PowerPoint slide