Show simple item record

dc.contributor.authorMeleddu, Rita
dc.contributor.authorDistinto, Simona
dc.contributor.authorCirilli, Roberto
dc.contributor.authorAlcaro, Stefano
dc.contributor.authorYañez Jato, Matilde
dc.contributor.authorSanna, María Luisa
dc.contributor.authorCorona, Ángela
dc.contributor.authorMelis, Claudia
dc.contributor.authorBianco, Giulia
dc.contributor.authorMatyus, Peter
dc.contributor.authorCottiglia, Filippo
dc.contributor.authorMaccioni, Elias
dc.date.accessioned2020-06-05T19:24:21Z
dc.date.available2020-06-05T19:24:21Z
dc.date.issued2017
dc.identifier.citationRita 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
dc.identifier.issn1475-6366
dc.identifier.urihttp://hdl.handle.net/10347/22808
dc.description.abstract3,5-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.
dc.language.isoeng
dc.publisherTaylor & Francis
dc.rights© 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
dc.rights.urihttp://creativecommons.org/licenses/by/4.0/
dc.subject3,5-diaryl-dihydroisosxazoles
dc.subjectMAO B selective inhibitors
dc.subjectNeuroprotective agents
dc.titleThrough scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B
dc.typeinfo:eu-repo/semantics/article
dc.identifier.DOI10.1080/14756366.2016.1247061
dc.relation.publisherversionhttps://doi.org/10.1080/14756366.2016.1247061
dc.type.versioninfo:eu-repo/semantics/publishedVersion
dc.identifier.e-issn1475-6374
dc.rights.accessrightsinfo:eu-repo/semantics/openAccess
dc.contributor.affiliationUniversidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica
dc.description.peerreviewedSI


Files in this item

application/pdf
Name: 2017_jofenzinhandmedchem_meleddu_through.pdf
Size: 1.513 Mb
Format: PDF


Thumbnail

This item appears in the following Collection(s)

Show simple item record

©  2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited
Except where otherwise noted, this item's license is described as  © 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited





Harvesters:Useful links:
Universidade de Santiago de Compostela | Teléfonos: +34 881 811 000 e +34 982 820 000 | Contact Us | Send Feedback