title: Exploring the thiazole scaffold for the identification of new agents for the treatment of fluconazole resistant Candida.
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.
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Rita
authors.initials: R
authors.lastname: Meleddu
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Simona
authors.initials: S
authors.lastname: Distinto
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Angela
authors.initials: A
authors.lastname: Corona
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Elias
authors.initials: E
authors.lastname: Maccioni
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Antonella
authors.initials: A
authors.lastname: Arridu
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Claudia
authors.initials: C
authors.lastname: Melis
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Giulia
authors.initials: G
authors.lastname: Bianco
authors.affiliation: b Department of Organic Chemistry , Semmelweis University Hogyes Endre U , Budapest , Hungary , and.
authors.forename: Peter
authors.initials: P
authors.lastname: Matyus
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Filippo
authors.initials: F
authors.lastname: Cottiglia
authors.affiliation: c Department of Public Health , Clinical and Molecular Medicine, University of Cagliari, Cittadella Universitaria , Monserrato , Italy.
authors.forename: Adriana
authors.initials: A
authors.lastname: Sanna
authors.affiliation: a Department of Life and Environmental Sciences , University of Cagliari , Cagliari , Italy .
authors.forename: Alessandro
authors.initials: A
authors.lastname: De Logu
mesh_terms: D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D002176:Candida albicans / Q000187:drug effects*; D002177:Candidiasis / Q000188:drug therapy* / Q000382:microbiology; D002522:Chlorocebus aethiops; D025141:Drug Resistance, Fungal; D015725:Fluconazole / Q000627:therapeutic use*; D008826:Microbial Sensitivity Tests; D013844:Thiazoles / Q000737:chemistry*; D014709:Vero Cells
chemical_list: D000935:Antifungal Agents; D013844:Thiazoles; D015725:Fluconazole
keywords: Fungicidal activity; heterocyclic antifungal agents; iron (III) chelators