title: Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B.
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.
authors.affiliation: Dipartimento di Scienze Farmacobiologiche, Facoltà di Farmacia, Università Magna Graecia di Catanzaro, Campus Universitario S. Venuta, Viale Europa, 88100 Catanzaro, Italy. alcaro@unicz.it
authors.forename: Stefano
authors.initials: S
authors.lastname: Alcaro
authors.forename: Alexandra
authors.initials: A
authors.lastname: Gaspar
authors.forename: Francesco
authors.initials: F
authors.lastname: Ortuso
authors.forename: Nuno
authors.initials: N
authors.lastname: Milhazes
authors.forename: Francisco
authors.initials: F
authors.lastname: Orallo
authors.forename: Eugenio
authors.initials: E
authors.lastname: Uriarte
authors.forename: Matilde
authors.initials: M
authors.lastname: Yáñez
authors.forename: Fernanda
authors.initials: F
authors.lastname: Borges
mesh_terms: 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
chemical_list: D002867:Chromones; D008996:Monoamine Oxidase Inhibitors; D020033:Protein Isoforms; C043668:chromone-2-carboxylic acid; D008995:Monoamine Oxidase