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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Detalles Bibliográficos
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:
benzylphthalazinones
antifungal
Cryptococcus neoformans
dermatophytes structure–activity relationships
conformational study
Acceso en línea:http://hdl.handle.net/2133/2584
http://hdl.handle.net/2133/2584
Aporte de:
Repositorio Hipermedial de la Universidad Nacional de Rosario (UNR) de Universidad Nacional de Rosario
Descripción
Sumario: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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