Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida

J Enzyme Inhib Med Chem. 2016 Dec;31(6):1672-7. doi: 10.3109/14756366.2015.1113171. Epub 2016 Jan 8.

Abstract

Cyclohexyliden- and 2-methylcyclohexyliden-hydrazo-4-arylthiazoles were synthesized and tested as antifungal agents. All compounds exhibited minimal inhibitory concentration (MIC) values comparable with those of fluconazole (FLC). Moreover, some compounds showed fungicidal activity at low concentration. Worth noting five out of nine compounds were active towards Candida albicans 25 FLC resistant isolated from clinical specimens. The cellular toxicity was evaluated and none of the compounds is toxic at the MIC. On the basis of our data we can conclude that these derivatives are promising agents for the treatment of resistant C. albicans.

Keywords: Fungicidal activity; heterocyclic antifungal agents; iron (III) chelators.

MeSH terms

  • Animals
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology
  • Antifungal Agents / therapeutic use*
  • Candida albicans / drug effects*
  • Candidiasis / drug therapy*
  • Candidiasis / microbiology
  • Chlorocebus aethiops
  • Drug Resistance, Fungal
  • Fluconazole / therapeutic use*
  • Microbial Sensitivity Tests
  • Thiazoles / chemistry*
  • Vero Cells

Substances

  • Antifungal Agents
  • Thiazoles
  • Fluconazole