Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B

Autor: 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
Jazyk: angličtina
Rok vydání: 2017
Předmět:
Zdroj: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 32, Iss 1, Pp 264-270 (2017)
Druh dokumentu: article
ISSN: 1475-6366
1475-6374
14756366
DOI: 10.1080/14756366.2016.1247061
Popis: 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.
Databáze: Directory of Open Access Journals
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