(MDPI Open Access Publishing, 2013-03) Derita, Marcos; del Olmo, Esther; Barboza, Bianca; García-Cadenas, Ana E.; López-Pérez, José L.; Andújar, Sebastián; Enriz, Daniel; Zacchino, Susana; San Feliciano, Arturo
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.