Department of Pathobiochemistry and Interdisciplinary Applications of Ion Chromatography, Biomedical Sciences, Medical University of Lublin, 1 Chodzki Street, 20-093 Lublin, Poland.
Department of Pharmaceutical Microbiology, Centre for Preclinical Research, Medical University of Warsaw, Banacha 1B Street, 02-097 Warsaw, Poland.
Molecules. 2024 Mar 17;29(6):1333. doi: 10.3390/molecules29061333.
The search for new antibacterial compounds is still a huge challenge for scientists. Each new chemotherapy drug is not 100% effective when introduced into treatment. Bacteria quickly become resistant to known structures. One promising group of new compounds is thiosemicarbazides. In the presented work, we looked for the relationship between structure and antibacterial activity within the group of thiosemicarbazide derivatives. This is a continuation of our previous work. Here, we decided to check to what extent the position of the 3-methoxyphenyl substituent affects potency. We obtained new structures that differ in the positions of the substituent in the thiosemicarbazide skeleton. Based on the obtained results of the biological tests, it can be concluded that the substituent in position 1 of thiosemicarbazide derivatives significantly determines their activity. Generally, among the substituents used, trifluoromethylphenyl turned out to be the most promising. The MIC values for compounds with this substituent are 64 µg/mL towards sp. Using molecular docking, we tried to explain the mechanism behind the antibacterial activity of the tested compounds.
寻找新的抗菌化合物仍然是科学家面临的巨大挑战。每一种新的化疗药物在引入治疗时并非 100%有效。细菌很快就对已知结构产生了耐药性。一类有前途的新化合物是硫代氨基脲。在本工作中，我们在硫代氨基脲衍生物组内寻找结构与抗菌活性之间的关系。这是我们之前工作的延续。在这里，我们决定检查 3-甲氧基苯基取代基的位置在多大程度上影响其效力。我们获得了在硫代氨基脲骨架中取代基位置不同的新结构。基于生物测试的结果，可以得出结论，取代基在硫代氨基脲衍生物的 1 位显著决定了它们的活性。一般来说，在所使用的取代基中，三氟甲基苯基是最有前途的。带有该取代基的化合物对 sp 的 MIC 值为 64 µg/mL。通过分子对接，我们试图解释测试化合物抗菌活性的背后机制。
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