1. Academic Validation
  2. A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors

A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors

  • Bioorg Med Chem. 2010 Feb;18(3):1273-9. doi: 10.1016/j.bmc.2009.12.029.
Franco Chimenti 1 Rossella Fioravanti Adriana Bolasco Paola Chimenti Daniela Secci Francesca Rossi Matilde Yáñez Francisco Orallo Francesco Ortuso Stefano Alcaro Roberto Cirilli Rosella Ferretti M Luisa Sanna
Affiliations

Affiliation

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma La Sapienza, Ple A Moro 5, 00185 Roma, Italy.
Abstract

A new series of synthetic Flavones, thioflavones, and flavanones has been synthesized and evaluated as potential inhibitors of Monoamine Oxidase isoforms (MAO-A and -B). The most active series is the flavanone one with higher selective inhibitory activity against MAO-B. Some of these flavanones (mainly the most effective) have been separated and tested as single enantiomers. In order to investigate the MAOs recognition of the most active and selective compounds, a molecular modeling study has been performed using available Protein Data Bank (PDB) structures as receptor models for docking experiments.

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