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

Molecules

Marcos Derita³  Esther del Olmo²  Bianca Barboza²  Ana Esther Garc໚-Cadenas²  José Luis López-Pérez²  Sebastián Andújar¹  Daniel Enriz¹  Susana Zacchino³ 

[1] Faculty of Chemistry, Biochemistry and Pharmacy, National University of San Luis (UNSL), Chacabuco 917, 5700 San Luis, Argentine; E-Mails:;Department of Pharmaceutical Chemistry, Faculty of Pharmacy, CIETUS-IBSAL, University of Salamanca, Campus Miguel de Unamuno, 37007 Salamanca, Spain; E-Mails:;Pharmacognosy Department, Faculty of Biochemical and Pharmaceutical Sciences, National University of Rosario, Suipacha 531, 2000 Rosario, Argentine; E-Mail:

关键词: benzylphthalazinones;    antifungal;    Cryptococcus neoformans;    dermatophytes structure-activity relationships;    conformational study;   

DOI  :  10.3390/molecules18033479

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.