PDF(Pubmed)
Abstract：
Heterocyclic compounds, particularly those containing azole rings, have shown extensive biological activity, including anticancer, antibacterial, and antifungal properties. Among these, the imidazole ring stands out due to its diverse therapeutic potential. In the presented study, we designed and synthesized a series of imidazole derivatives to identify compounds with high biological potential. We focused on two groups: thiosemicarbazide derivatives and hydrazone derivatives. We synthesized these compounds using conventional methods and confirmed their structures via nuclear magnetic resonance spectroscopy (NMR), MS, and elemental analysis, and then assessed their antibacterial and antifungal activities in vitro using the broth microdilution method against Gram-positive and Gram-negative bacteria, as well as Candida spp. strains. Our results showed that thiosemicarbazide derivatives exhibited varied activity against Gram-positive bacteria, with MIC values ranging from 31.25 to 1000 µg/mL. The hydrazone derivatives, however, did not display significant antibacterial activity. These findings suggest that structural modifications can significantly influence the antimicrobial efficacy of imidazole derivatives, highlighting the potential of thiosemicarbazide derivatives as promising candidates for further development in antibacterial therapies. Additionally, the cytotoxic activity against four cancer cell lines was evaluated. Two derivatives of hydrazide-hydrazone showed moderate anticancer activity.
摘要：
杂环化合物,特别是那些含有唑环的，已经显示出广泛的生物活性，包括抗癌，抗菌，和抗真菌特性。其中,咪唑环因其多样化的治疗潜力而脱颖而出。在提出的研究中，我们设计并合成了一系列咪唑衍生物，以鉴定具有高生物潜力的化合物。我们专注于两组：氨基硫脲衍生物和腙衍生物。我们使用常规方法合成了这些化合物，并通过核磁共振波谱（NMR）证实了它们的结构，MS,和元素分析，然后使用肉汤微量稀释法对革兰氏阳性和革兰氏阴性细菌进行体外抗菌和抗真菌活性的评估，以及念珠菌属。菌株。我们的结果表明，氨基硫脲衍生物对革兰氏阳性细菌表现出不同的活性，MIC值范围为31.25至1000µg/mL。腙衍生物，然而,没有显示出显著的抗菌活性。这些发现表明，结构修饰可以显着影响咪唑衍生物的抗菌功效，强调氨基硫脲衍生物作为抗菌疗法进一步发展的有希望的候选药物的潜力。此外,评估了对四种癌细胞系的细胞毒活性。酰肼-腙的两种衍生物显示出中等的抗癌活性。
