| Chromone-2- and -3-carboxylic acids inhibit differently monoamine oxidases A and B. | |
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MedLine Citation:
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PMID: 20382016 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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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. |
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Authors:
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Stefano Alcaro; Alexandra Gaspar; Francesco Ortuso; Nuno Milhazes; Francisco Orallo; Eugenio Uriarte; Matilde Yáñez; Fernanda Borges |
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Publication Detail:
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Type: Journal Article; Research Support, Non-U.S. Gov't Date: 2010-03-27 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 20 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2010 May |
Date Detail:
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Created Date: 2010-04-20 Completed Date: 2010-07-27 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 2709-12 Citation Subset: IM |
Copyright Information:
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2010 Elsevier Ltd. All rights reserved. |
Affiliation:
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Dipartimento di Scienze Farmacobiologiche, Facoltà di Farmacia, Università Magna Graecia di Catanzaro, Campus Universitario S. Venuta, Viale Europa, 88100 Catanzaro, Italy. alcaro@unicz.it |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Binding Sites Chromones / chemistry*, pharmacology Computer Simulation Humans Monoamine Oxidase / chemistry*, metabolism Monoamine Oxidase Inhibitors / chemistry*, pharmacology Protein Isoforms / antagonists & inhibitors, metabolism |
| Chemical | |
Reg. No./Substance:
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0/Chromones; 0/Monoamine Oxidase Inhibitors; 0/Protein Isoforms; 4940-39-0/chromone-2-carboxylic acid; EC 1.4.3.4/Monoamine Oxidase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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