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

• Type: Article in International Scientific Journal
• Date: 2010

Authors

Stefano Alcaro (Author) Other; Alexandra Gaspar (Author) Other; Francesco Ortuso (Author) Other; Nuno Milhazes (Author) Other; Francisco Orallo (Author) Other; Eugenio Uriarte (Author) Other; Matilde Yáñez (Author) Other; Fernanda Borges (Author) FCUP

Journal

Title: Bioorganic and Medicinal Chemistry Letters

Vol. 20 No. 9

Pages: 2709-2712

ISSN: 0960-894X

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 49 Citations

Scopus - 54 Citations

Scientific classification

FOS: Engineering and technology > Chemical engineering

CORDIS: Physical sciences > Chemistry > Organic chemistry

Other information

Authenticus ID: P-003-6W2

Abstract (EN): Chromone carboxylic acids were evaluated as human monoamine oxidase A and B (hMAO-A and hMAOB) 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 IC50 data and to explain the absence of activity versus selectivity, respectively.

Language: English

Type (Professor's evaluation): Scientific