title: A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
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.
authors.affiliation: Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma La Sapienza, Ple A Moro 5, 00185 Roma, Italy.
authors.forename: Franco
authors.initials: F
authors.lastname: Chimenti
authors.forename: Rossella
authors.initials: R
authors.lastname: Fioravanti
authors.forename: Adriana
authors.initials: A
authors.lastname: Bolasco
authors.forename: Paola
authors.initials: P
authors.lastname: Chimenti
authors.forename: Daniela
authors.initials: D
authors.lastname: Secci
authors.forename: Francesca
authors.initials: F
authors.lastname: Rossi
authors.forename: Matilde
authors.initials: M
authors.lastname: Yáñez
authors.forename: Francisco
authors.initials: F
authors.lastname: Orallo
authors.forename: Francesco
authors.initials: F
authors.lastname: Ortuso
authors.forename: Stefano
authors.initials: S
authors.lastname: Alcaro
authors.forename: Roberto
authors.initials: R
authors.lastname: Cirilli
authors.forename: Rosella
authors.initials: R
authors.lastname: Ferretti
authors.forename: M Luisa
authors.initials: ML
authors.lastname: Sanna
mesh_terms: D044950:Flavanones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D047309:Flavones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D008995:Monoamine Oxidase / Q000737:chemistry / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013237:Stereoisomerism; D013438:Sulfhydryl Compounds / Q000737:chemistry
chemical_list: D044950:Flavanones; D047309:Flavones; D008996:Monoamine Oxidase Inhibitors; D013438:Sulfhydryl Compounds; D008995:Monoamine Oxidase