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

Article Details

Citation

Alcaro S, Gaspar A, Ortuso F, Milhazes N, Orallo F, Uriarte E, Yanez M, Borges F

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

Bioorg Med Chem Lett. 2010 May 1;20(9):2709-12. doi: 10.1016/j.bmcl.2010.03.081. Epub 2010 Mar 27.

PubMed ID
20382016 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
ClorgilineAmine oxidase [flavin-containing] AIC 50 (nM)5.2N/AN/ADetails
IproniazidAmine oxidase [flavin-containing] BIC 50 (nM)7540N/AN/ADetails
MoclobemideAmine oxidase [flavin-containing] AIC 50 (nM)361380N/AN/ADetails
SelegilineAmine oxidase [flavin-containing] AIC 50 (nM)68730N/AN/ADetails
SelegilineAmine oxidase [flavin-containing] BIC 50 (nM)17N/AN/ADetails