Open AccessNew sulfone and sulfanyl derivatives with antifungal activity
Author(s) -
Małgorzata Gizińska,
Marzena Połaska,
Zbigniew Ochal,
Monika Staniszewska
Publication year - 2018
Publication title -
medycyna doświadczalna i mikrobiologia
Language(s) - English
Resource type - Journals
eISSN - 2545-2517
pISSN - 0025-8601
DOI - 10.32394/mdm.70.2.7
Subject(s) - candida albicans , sulfanyl , sulfone , context (archaeology) , antifungal , broth microdilution , biology , corpus albicans , microbiology and biotechnology , in vitro , toxicity , chemistry , biochemistry , pharmacology , stereochemistry , minimum inhibitory concentration , organic chemistry , paleontology
Increasing occurrence of fungal infections raises the need to develop novel antifungal agents. In this context, an inhibition of morphological switch may provide an alternative approach to find compounds with a potential to control the Candida albicans infections.Methods: A series of 17 sulfone and sulfanyl derivatives was synthesized and evaluated for activity against the C. albicans wild type (SC5314, ATCC) and SAP-deficient mutant strains using the broth microdilution method M27-A3. Afterwards, phase-contrast microscopy was applied to evaluate the inhibition of fungal morphogenesis under the influence of randomly selected active compounds: 1, 5 and 6.Results: By in vitro susceptibility testing of C. albicans, we identified the effective antifungal agents displaying moderate-to-good activity. Newly synthesized sulfanyl and sulfone derivatives strongly inhibited the C. albicans morphogenetic transition under the hyphae inducing conditions.Conclusions: The leading compound 6 has the potential to be used as a base structure in antifungal drug development, however further structural optimalization and toxicity studies are required.