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. (C) 2009 Elsevier Ltd. All rights reserved.
A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors / Chimenti, Franco; Fioravanti, Rossella; Bolasco, Adriana; Chimenti, Paola; Secci, Daniela; Rossi, Francesca; Matilde, Yanez; Francisco, Orallo; Francesco, Ortuso; Stefano, Alcaro; Roberto, Cirilli; Rosella, Ferretti; M., Luisa Sanna. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 18:3(2010), pp. 1273-1279. [10.1016/j.bmc.2009.12.029]
A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors
CHIMENTI, Franco;FIORAVANTI, Rossella;BOLASCO, Adriana;CHIMENTI, Paola;SECCI, DANIELA;ROSSI, FRANCESCA;
2010
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. (C) 2009 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
