Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B.
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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
Drug Target Property Measurement pH Temperature (°C) Clorgiline Amine oxidase [flavin-containing] A IC 50 (nM) 5.2 N/A N/A Details Iproniazid Amine oxidase [flavin-containing] B IC 50 (nM) 7540 N/A N/A Details Moclobemide Amine oxidase [flavin-containing] A IC 50 (nM) 361380 N/A N/A Details Selegiline Amine oxidase [flavin-containing] A IC 50 (nM) 68730 N/A N/A Details Selegiline Amine oxidase [flavin-containing] B IC 50 (nM) 17 N/A N/A Details