Synthesis and biological evaluation of some hydrazone derivatives as new anticandidal and anticancer agents

New hydrazone derivatives were synthesized via the nucleophilic addition–elimination reaction of 2-[(1-methyl-1H-tetrazol-5-yl)thio)]acetohydrazide with aromatic aldehydes/ketones. The compounds were tested in vitro against various Candida species and compared with ketoconazole. Genotoxicity of the most effective anticandidal compounds was evaluated by umuC and Ames assays. All compounds were also investigated for their cytotoxic effects on NIH3T3 and A549 cell lines. Compound 8 was the most effective antifungal derivative against C. albicans (ATCC-90028) with a MIC value of 0.05 mg/mL. Compound 5 can be identified as the most promising anticancer agent against A549 cancer cell lines due to its inhibitory effect on A549 cell lines and low toxicity to NIH3T3 cells.

The reaction of 2-[(1-methyl-1H-tetrazol-5-yl)thio)]acetohydrazide with appropriate aldehydes/ketones gave novel hydrazone derivatives, which were tested for anticandidal and anticancer effects. Genotoxicity of the most effective anticandidal compounds was also evaluated.Figure optionsDownload as PowerPoint slideHighlights
► The compounds were tested in vitro against various Candida species.
► Genotoxicity of the most effective anticandidal agents was evaluated.
►  Each derivative was evaluated for its anticancer activity against A549 cell lines.
► Compound 8 was the most effective anticandidal derivative.
►  Compound 5 was the most promising anticancer agent against A549 cell lines.