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.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Chromones / chemistry*
  • Chromones / pharmacology
  • Computer Simulation
  • Humans
  • Monoamine Oxidase / chemistry*
  • Monoamine Oxidase / metabolism
  • Monoamine Oxidase Inhibitors / chemistry*
  • Monoamine Oxidase Inhibitors / pharmacology
  • Protein Isoforms / antagonists & inhibitors
  • Protein Isoforms / metabolism

Substances

  • Chromones
  • Monoamine Oxidase Inhibitors
  • Protein Isoforms
  • chromone-2-carboxylic acid
  • Monoamine Oxidase