Background: Over the last few years, fungal infections have emerged as a worrisome global
public health problem. Candidiasis is a disease caused by Candida species and has been a problem
worldwide mainly for immunosuppressed patients. Lately, the resistant strains and side effects have been
reported as important issues for treating Candidiasis, which have to be solved by identifying new drugs.
Objective: The goal of this work was to synthesize a series of 1,3-benzoxathiol-2-one derivatives, XYbenzo[
d][1,3]oxathiol-2-ones, and evaluate their antifungal activity against five Candida species.
Methods: In vitro antifungal screening test and minimum inhibitory concentration determination were
performed according to CLSI protocols using ketoconazole as the reference drug. The cytotoxicity of the
most active compounds was evaluated by hemolysis and MTT (Vero cells) assays.
Results: Compounds 2 (XY = 6-hydroxy-5-nitro, MIC = 4-32 µg/mL) and 7 (XY = 6-acetoxy-5-nitro,
MIC =16-64 µg/mL) showed good results when compared with current antifungals in CLSI values
(MIC = 0.04-250 µg/mL). These compounds exhibited a safer cytotoxicity as well as a lower hemolytic
profile than ketoconazole.
Conclusion: Overall, the in vitro results pointed to the potential of compounds 2 and 7 as new antifungal
prototypes to be further explored.