Azoles are generally fungistatic, and resistance to fluconazole is emerging in several fungal pathogens. We designed a series of cinnamaldehyde based sulfonyl tetrazole derivatives. To further explore the antifungal activity, in vitro studies were conducted against 60 clinical isolates and 6 standard laboratory strains of Candida. The rapid irreversible action of these compounds on fungal cells suggested a membrane-located target for their action. Results obtained indicate plasma membrane H +-ATPase as site of action of the synthesized compounds. Inhibition of H +-ATPase leads to intracellular acidification and cell death. Presence of chloro and nitro groups on the sulfonyl pendant has been demonstrated to be a key structural element of antifungal potency. SEM micrographs of treated Candida cells showed severe cell breakage and alterations in morphology. © 2011 Elsevier Ltd. All rights reserved.
CITATION STYLE
Shreaz, S., Wani, M. Y., Ahmad, S. R., Ahmad, S. I., Bhatia, R., Athar, F., … Khan, L. A. (2012). Proton-pumping-ATPase-targeted antifungal activity of cinnamaldehyde based sulfonyl tetrazoles. European Journal of Medicinal Chemistry, 48, 363–370. https://doi.org/10.1016/j.ejmech.2011.12.007
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