Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents

Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one (5) exhibited a remarkable ant...

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Autores principales: Derita, Marcos, del Olmo, Esther, Barboza, Bianca, García-Cadenas, Ana Esther, López-Pérez, José Luis, Andújar, Sebastián, Enriz, Daniel, Zacchino, Susana, San Feliciano, Arturo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270128/
https://www.ncbi.nlm.nih.gov/pubmed/23507777
http://dx.doi.org/10.3390/molecules18033479
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author Derita, Marcos
del Olmo, Esther
Barboza, Bianca
García-Cadenas, Ana Esther
López-Pérez, José Luis
Andújar, Sebastián
Enriz, Daniel
Zacchino, Susana
San Feliciano, Arturo
author_facet Derita, Marcos
del Olmo, Esther
Barboza, Bianca
García-Cadenas, Ana Esther
López-Pérez, José Luis
Andújar, Sebastián
Enriz, Daniel
Zacchino, Susana
San Feliciano, Arturo
author_sort Derita, Marcos
collection PubMed
description Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues.
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spelling pubmed-62701282018-12-20 Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents Derita, Marcos del Olmo, Esther Barboza, Bianca García-Cadenas, Ana Esther López-Pérez, José Luis Andújar, Sebastián Enriz, Daniel Zacchino, Susana San Feliciano, Arturo Molecules Article Twenty-five polysubstituted phthalazinone derivatives were synthesized and tested for their antifungal activity against a panel of pathogenic and clinically important yeasts and filamentous fungi. Among them, the compound 4-(4-chlorobenzyl)-2-methylphthalazin-1(2H)-one (5) exhibited a remarkable antifungal activity against standardised strains of dermatophytes and Cryptococcus neoformans, as well as against some clinical isolates. A physicochemical study performed on compound 5 revealed its conformational and electronic characteristics, providing us with useful data for the future design of novel related antifungal analogues. MDPI 2013-03-18 /pmc/articles/PMC6270128/ /pubmed/23507777 http://dx.doi.org/10.3390/molecules18033479 Text en © 2013 by the authors; licensee MDPI, Basel, Switzerland. http://creativecommons.org/licenses/by/3.0/ This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Derita, Marcos
del Olmo, Esther
Barboza, Bianca
García-Cadenas, Ana Esther
López-Pérez, José Luis
Andújar, Sebastián
Enriz, Daniel
Zacchino, Susana
San Feliciano, Arturo
Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
title Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
title_full Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
title_fullStr Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
title_full_unstemmed Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
title_short Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
title_sort synthesis, bioevaluation and structural study of substituted phthalazin-1(2h)-ones acting as antifungal agents
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6270128/
https://www.ncbi.nlm.nih.gov/pubmed/23507777
http://dx.doi.org/10.3390/molecules18033479
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