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

Author： Derita Marcos   del Olmo Esther   Barboza Bianca   García-Cadenas Ana Esther   López-Pérez José Luis   Andújar Sebastián   Enriz Daniel   Zacchino Susana   San Feliciano Arturo  

Publisher： MDPI

E-ISSN： 1420-3049|18|3|3479-3501

ISSN： 1420-3049

Source： Molecules, Vol.18, Iss.3, 2013-03, pp. : 3479-3501

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Abstract

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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