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

MARCOS DERITA; ESTHER DEL OLMO; BIANCA BARBOZA; ANA ESTHER GARCÍA-CADENAS; OSÉ LUIS LÓPEZ-PÉREZ; SEBASTIÁN ANDÚJAR; DANIEL ENRIZ; SUSANA ZACCHINO; ARTURO SAN FELICIANO

MOLECULES

MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI

Lugar: Basel; Año: 2013 p. 3479 - 3501

1420-3049

wenty-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.