Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida. (1st November 2016)

• Record Type: Journal Article
• Authors: Meleddu, Rita; Distinto, Simona; Corona, Angela; Maccioni, Elias; Arridu, Antonella; Melis, Claudia; Bianco, Giulia; Matyus, Peter; Cottiglia, Filippo; Sanna, Adriana; De Logu, Alessandro
• Is Part Of: Journal of enzyme inhibition and medicinal chemistry. Volume 31:Number 6(2016:Dec.)
• Page Start: 1672
• Page End: 1677
• Publication Date: 2016-11-01
• Subjects: Fungicidal activity -- heterocyclic antifungal agents -- iron (III) chelators; Enzyme inhibitors -- Periodicals; Enzyme Inhibitors -- periodicals; Biochemistry -- periodicals; 572.7
• DOI: 10.3109/14756366.2015.1113171
• Languages: English
• ISSNs: 1475-6366

Abstract

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 .