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

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 ant...

Full description

Bibliographic Details
Main Authors: Susana Zacchino, Daniel Enriz, Sebastián Andújar, José Luis López-Pérez, Bianca Barboza, Ana Esther García-Cadenas, Esther del Olmo, Marcos Derita, Arturo San Feliciano
Format: Article
Language:English
Published: MDPI AG 2013-03-01
Series:Molecules
Subjects:
benzylphthalazinones
antifungal
Cryptococcus neoformans
dermatophytes structure–activity relationships
conformational study
Online Access:http://www.mdpi.com/1420-3049/18/3/3479
Description
Summary: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.
ISSN:1420-3049

Similar Items