RT Journal Article
T1 Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B
A1 Meleddu, Rita
A1 Distinto, Simona
A1 Cirilli, Roberto
A1 Alcaro, Stefano
A1 Yáñez Jato, Matilde
A1 Sanna, María Luisa
A1 Corona, Ángela
A1 Melis, Claudia
A1 Bianco, Giulia
A1 Matyus, Peter
A1 Cottiglia, Filippo
A1 Maccioni, Elias
K1 3,5-diaryl-dihydroisosxazoles
K1 MAO B selective inhibitors
K1 Neuroprotective agents
AB 3,5-Diaryl-4,5-dihydroisoxazoles were synthesized and evaluated as monoamine oxidase (MAO) enzyme inhibitors and iron chelators. All compounds exhibited selective inhibitory activity towards the B isoform of MAO in the nanomolar concentration range. The best performing compound was preliminarily evaluated for its ability to bind iron II and III cations, indicating that neither iron II nor iron III is coordinated. The best compounds racemic mixtures were separated and single enantiomers inhibitory activity evaluated. Furthermore, none of the synthesised compounds exhibited activity towards MAO A. Overall, these data support our hypothesis that 3,5-diaryl-4,5-dihydroisoxazoles are promising scaffolds for the design of neuroprotective agents.
PB Taylor & Francis
SN 1475-6366
YR 2017
FD 2017
LK http://hdl.handle.net/10347/22808
UL http://hdl.handle.net/10347/22808
LA eng
NO Rita Meleddu, Simona Distinto, Roberto Cirilli, Stefano Alcaro, Matilde Yanez, Maria Luisa Sanna, Angela Corona, Claudia Melis, Giulia Bianco, Peter Matyus, Filippo Cottiglia & Elias Maccioni (2017) Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B, Journal of Enzyme Inhibition and Medicinal Chemistry, 32:1, 264-270, DOI: 10.1080/14756366.2016.1247061
DS Minerva
RD 28 abr 2026