Synthesis, bioevaluation and structural study of substituted phthalazin-1(2H)-ones acting as antifungal agents

M.DERITA; E. DEL OLMO; B.BARBOZA; A.GARCIA CARDENAS; J. LOPEZ PEREZ; S.ANDUJAR; ENRIZ R; S.SACCHINO; A.SAN FELICIANO

MOLECULES

MOLECULAR DIVERSITY PRESERVATION INTERNATIONAL-MDPI

Lugar: Basel; Año: 2013 vol. 18 p. 3479 - 3501

1420-3049

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.