A new series of flavones, thioflavones, and flavanones as selective monoamine oxidase-B inhibitors.
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.
Chimenti
Franco
F
Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma La Sapienza, Ple A Moro 5, 00185 Roma, Italy.
Fioravanti
Rossella
R
Bolasco
Adriana
A
Chimenti
Paola
P
Secci
Daniela
D
Rossi
Francesca
F
Yáñez
Matilde
M
Orallo
Francisco
F
Ortuso
Francesco
F
Alcaro
Stefano
S
Cirilli
Roberto
R
Ferretti
Rosella
R
Sanna
M Luisa
ML
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
D044950:Flavanones; D047309:Flavones; D008996:Monoamine Oxidase Inhibitors; D013438:Sulfhydryl Compounds; D008995:Monoamine Oxidase