Bioorg Med Chem. 2010 Feb;18(3):1273-9. Epub 2010 Jan 4.

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

Chimenti F, Fioravanti R, Bolasco A, Chimenti P, Secci D, Rossi F, Yáñez M, Orallo F, Ortuso F, Alcaro S, Cirilli R, Ferretti R, Sanna ML.

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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.

PMID:: 20045650; [PubMed - indexed for MEDLINE]

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

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