Anti- Candida albicans Activity of Thiazolylhydrazone Derivatives in Invertebrate and Murine Models

• Published in: Journal of fungi (Basel) 2018-12, Vol.4 (4), p.134
• Main Authors: Cruz, Lana Ivone Barreto, Lopes, Larissa Ferreira Finamore, de Camargo Ribeiro, Felipe, de Sá, Nívea Pereira, Lino, Cleudiomar Inácio, Tharmalingam, Nagendran, de Oliveira, Renata Barbosa, Rosa, Carlos Augusto, Mylonakis, Eleftherios, Fuchs, Beth Burgwyn, Johann, Susana
• Format: Article
• Language: English
• Subjects: Animal models; Animals; antifungal; Antifungal activity; Candida albicans; Candidiasis; Cytotoxicity; Erythrocytes; Fluconazole; Fungal infections; Invertebrates; Kidneys; Public health; thiazolylhydrazone derivatives; Toxicity; Vagina
• ISSN: 2309-608X; 2309-608X
• DOI: 10.3390/jof4040134

Candidiasis is an opportunistic fungal infection with being the most frequently isolated species. Treatment of these infections is challenging due to resistance that can develop during therapy, and the limited number of available antifungal compounds. Given this situation, the aim of this study was to evaluate the antifungal activity of four thiazolylhydrazone compounds against . Thiazolylhydrazone compounds , , , and were found to exert antifungal activity, with MICs of 0.125⁻16.0 μg/mL against . . The toxicity of the compounds was evaluated using human erythrocytes and yielded LC > 64 μg/mL. The compounds were further evaluated using the greater wax moth as an in vivo model. The compounds prolonged larval survival when tested between 5 and 15 mg/kg, performing as well as fluconazole. Compound was evaluated in murine models of oral and systemic candidiasis. In the oral model, compound reduced the fungal load on the mouse tongue; and in the systemic model it reduced the fungal burden found in the kidney when tested at 10 mg/kg. These results show that thiazolylhydrazones are an antifungal towards with in vivo efficacy.