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.

译文

:通过2-[((1-甲基-1H-四唑-5-基)硫基)]乙酰肼与芳香族醛/酮的亲核加成消除反应合成了新的衍生物。该化合物在体外针对各种念珠菌进行了测试,并与酮康唑进行了比较。通过umuC和Ames分析评估了最有效的抗候选化合物的基因毒性。还研究了所有化合物对NIH3T3和A549细胞系的细胞毒性作用。化合物8是针对白色念珠菌的最有效的抗真菌衍生物(ATCC-90028),MIC值为0.05 mg / mL。化合物5由于其对A549细胞系的抑制作用和对NIH3T3细胞的低毒性而可以被确定为最有前途的针对A549癌细胞系的抗癌剂。

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