Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B
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Título: | Through scaffold modification to 3,5-diaryl-4,5-dihydroisoxazoles: new potent and selective inhibitors of monoamine oxidase B |
Autor/a: | Meleddu, Rita Distinto, Simona Cirilli, Roberto Alcaro, Stefano Yañez Jato, Matilde Sanna, María Luisa Corona, Ángela Melis, Claudia Bianco, Giulia Matyus, Peter Cottiglia, Filippo Maccioni, Elias |
Centro/Departamento: | Universidade de Santiago de Compostela. Departamento de Farmacoloxía, Farmacia e Tecnoloxía Farmacéutica |
Palabras chave: | 3,5-diaryl-dihydroisosxazoles | MAO B selective inhibitors | Neuroprotective agents | |
Data: | 2017 |
Editor: | Taylor & Francis |
Cita bibliográfica: | 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 |
Resumo: | 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. |
Versión do editor: | https://doi.org/10.1080/14756366.2016.1247061 |
URI: | http://hdl.handle.net/10347/22808 |
DOI: | 10.1080/14756366.2016.1247061 |
ISSN: | 1475-6366 |
E-ISSN: | 1475-6374 |
Dereitos: | © 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 |
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© 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
© 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