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...

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Autores principales: Derita, Marcos, del Olmo, Esther, Barboza, Bianca, García-Cadenas, Ana E., López-Pérez, José L., Andújar, Sebastián, Enriz, Daniel, Zacchino, Susana, San Feliciano, Arturo
Formato: article artículo publishedVersion
Lenguaje:Inglés
Publicado: MDPI Open Access Publishing 2013
Materias:
Acceso en línea:http://hdl.handle.net/2133/2584
http://hdl.handle.net/2133/2584
Aporte de:
id I15-R121-2133-2584
record_format dspace
institution Universidad Nacional de Rosario
institution_str I-15
repository_str R-121
collection Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR)
language Inglés
orig_language_str_mv en
topic benzylphthalazinones
antifungal
Cryptococcus neoformans
dermatophytes structure–activity relationships
conformational study
spellingShingle benzylphthalazinones
antifungal
Cryptococcus neoformans
dermatophytes structure–activity relationships
conformational study
Derita, Marcos
del Olmo, Esther
Barboza, Bianca
García-Cadenas, Ana E.
López-Pérez, José L.
Andújar, Sebastián
Enriz, Daniel
Zacchino, Susana
San Feliciano, Arturo
Synthesis, Bioevaluation and Structural Study of Substituted Phthalazin-1(2H)-ones Acting as Antifungal Agents
topic_facet benzylphthalazinones
antifungal
Cryptococcus neoformans
dermatophytes structure–activity relationships
conformational study
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.
format article
artículo
publishedVersion
author Derita, Marcos
del Olmo, Esther
Barboza, Bianca
García-Cadenas, Ana E.
López-Pérez, José L.
Andújar, Sebastián
Enriz, Daniel
Zacchino, Susana
San Feliciano, Arturo
author_facet Derita, Marcos
del Olmo, Esther
Barboza, Bianca
García-Cadenas, Ana E.
López-Pérez, José L.
Andújar, Sebastián
Enriz, Daniel
Zacchino, Susana
San Feliciano, Arturo
author_sort Derita, Marcos
title 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_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_sort synthesis, bioevaluation and structural study of substituted phthalazin-1(2h)-ones acting as antifungal agents
publisher MDPI Open Access Publishing
publishDate 2013
url http://hdl.handle.net/2133/2584
http://hdl.handle.net/2133/2584
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