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 an...

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Detalhes bibliográficos
Autores: Derita, Marcos Gabriel, del Olmo, Esther, Barboza, Bianca, García Cadenas, Ana Esther, López Pérez, José Luis, Andújar, Sebastián Antonio, Daniel Enriz, Zacchino, Susana Alicia Stella, San Feliciano, Arturo
Formato: artículo
Estado:Versión publicada
Fecha de publicación:2013
País:Argentina
Recursos:Consejo Nacional de Investigaciones Científicas y Técnicas
Repositorio:CONICET Digital (CONICET)
Idioma:inglés
OAI Identifier:oai:ri.conicet.gov.ar:11336/1545
Acesso em linha:http://hdl.handle.net/11336/1545
Access Level:acceso abierto
Palavra-chave:Benzylphthalazinones
Antifungal
Cryptococcus neoformans
Dermatophytes structure–activity relationships
Conformational study
https://purl.org/becyt/ford/1.6
https://purl.org/becyt/ford/1
Descrição
Resumo: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.