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

Rita Meleddu, Simona Distinto, Angela Corona, Elias Maccioni, Antonella Arridu, Claudia Melis, Giulia Bianco, P. Mátyus, Filippo Cottiglia, Adriana Sanna, Alessandro De Logu

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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.

Original languageEnglish
Pages (from-to)1-6
Number of pages6
JournalJournal of Enzyme Inhibition and Medicinal Chemistry
DOIs
Publication statusAccepted/In press - Jan 7 2016

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Keywords

  • Fungicidal activity
  • heterocyclic antifungal agents
  • iron (III) chelators

ASJC Scopus subject areas

  • Drug Discovery
  • Pharmacology

Cite this

Meleddu, R., Distinto, S., Corona, A., Maccioni, E., Arridu, A., Melis, C., Bianco, G., Mátyus, P., Cottiglia, F., Sanna, A., & De Logu, A. (Accepted/In press). Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida. Journal of Enzyme Inhibition and Medicinal Chemistry, 1-6. https://doi.org/10.3109/14756366.2015.1113171