Synthesis and cytotoxicity of novel (thiazol-2-yl)hydrazine derivatives as promising anti-Candida agents

•Synthesis and selective anti-Candida activity of new 2,4-disubstituted-thiazoles.•They represent lead compounds for the development of new broad anti-Candida agents.•They could be used in association with azoles to improve antifungal activity.•They displayed a good safety profile with lower cytotoxicity than clotrimazole.

Thirty-eight new (4-(4-substituted-phenyl/2,4-disubstituted-phenyl)-thiazol-2-yl)hydrazine derivatives were synthesized in good yield and assayed for their in vitro anti-Candida activity, compared to topical and systemic antifungal drugs, against twenty-two clinical isolates of Candida spp. The concurrent presence of aliphatic chains or cycloaliphatic rings at N1-hydrazine and a 4-methyl/4-methoxyphenyl at C4 position of the thiazole nucleus exhibited an interesting anti-Candida inhibitory activity. Moreover, some of the most active compounds showed synergistic antifungal effects and lower cell toxicity when combined with clotrimazole.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide