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 IC(50) data and to explain the absence of activity versus selectivity, respectively.
Alcaro
Stefano
S
Dipartimento di Scienze Farmacobiologiche, Facoltà di Farmacia, Università Magna Graecia di Catanzaro, Campus Universitario S. Venuta, Viale Europa, 88100 Catanzaro, Italy. alcaro@unicz.it
Gaspar
Alexandra
A
Ortuso
Francesco
F
Milhazes
Nuno
N
Orallo
Francisco
F
Uriarte
Eugenio
E
Yáñez
Matilde
M
Borges
Fernanda
F
D001665:Binding Sites; D002867:Chromones / Q000737:chemistry* / Q000494:pharmacology; D003198:Computer Simulation; D006801:Humans; D008995:Monoamine Oxidase / Q000737:chemistry* / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000737:chemistry* / Q000494:pharmacology; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism
D002867:Chromones; D008996:Monoamine Oxidase Inhibitors; D020033:Protein Isoforms; C043668:chromone-2-carboxylic acid; D008995:Monoamine Oxidase