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

被引：53

作者：

Alcaro, Stefano ^{[1
]}

Gaspar, Alexandra ^{[2
,3
]}

Ortuso, Francesco ^{[1
]}

Milhazes, Nuno ^{[3
]}

Orallo, Francisco ^{[4
]}

Uriarte, Eugenio ^{[5
]}

Yanez, Matilde ^{[4
]}

Borges, Fernanda ^{[2
]}

机构：

[1] Magna Graecia Univ Catanzaro, Dipartimento Sci Farmacobiol, Fac Farm, I-88100 Catanzaro, Italy

[2] Univ Porto, CIQUP, Dept Quim, Fac Ciencias, P-4169007 Oporto, Portugal

[3] Inst Super Ciencias Saude Norte, P-4585116 Gandra Prd, Portugal

[4] Univ Santiago de Compostela, Dept Farmacol, Fac Farm, Santiago De Compostela 15782, Spain

[5] Univ Santiago de Compostela, Dept Quim Organ, Fac Farm, Santiago De Compostela 15782, Spain

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 09期

关键词：

Chromones; Docking; Monoamine oxidase; Inhibitors; DERIVATIVES; COUMARINS; ANALOGS;

D O I：

10.1016/j.bmcl.2010.03.081

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2709 / 2712

页数：4

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