新型磺酰基-1H-1,2,3-三唑并-1H-咪唑-2-磺酰胺的合成、抗菌和抗生物膜活性

IF 0.9 4区 化学 Q4 CHEMISTRY, MULTIDISCIPLINARY Russian Journal of General Chemistry Pub Date : 2024-10-04 DOI:10.1134/S1070363224080280
Botla Durga Varaprasadu, Sharath Babu Haridasyam, Shiva Kumar Koppula
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引用次数: 0

摘要

提出了一种高效的一锅法合成新型磺酰基-1H-1,2,3-三唑-1H-咪唑-2-磺酰胺类化合物。对新合成的衍生物进行了体外抗菌筛选,以检测其对革兰氏阳性菌株的抑菌效力。在测试的化合物中,N-({1-[(4-氯苯基)磺酰基]-1H-1,2,3-三唑-4-基}甲基)-1-甲基-1H-咪唑-2-磺酰胺和 N-({1-[(4-氰基苯基)磺酰基]-1H-1,2,3-三唑-4-基}甲基)-1-甲基-1H-咪唑-2-磺酰胺的最低抑菌浓度(MIC)为 3.12 μg/mL,是普通链霉素(6.25 μg/mL)的两倍。它对金黄色葡萄球菌的 MIC 值也为 6.25 μg/mL,与阳性对照相同。此外,强效化合物的抗生物膜谱显示,这些活性衍生物不仅能很好地杀死细菌,还能很好地阻止枯草杆菌生物膜的生长。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Synthesis, Antibacterial, and Antibiofilm Activity of Novel Sulfonyl-1H-1,2,3-triazolo-1H-imidazole-2-sulfonamides

An efficient one-pot approach was proposed for the synthesis of novel sulfonyl-1H-1,2,3-triazolo-1H-imidazole-2-sulfonamides. The newly synthesized derivatives were screened for in vitro antibacterial inhibition potency against gram-positive strains. Among the tested compounds, N-({1-[(4-chlorophenyl)sulfonyl]-1H-1,2,3-triazol-4-yl}methyl)-1-methyl-1H-imidazole-2-sulfonamide and N-({1-[(4-cyanophenyl)sulfonyl]-1H-1,2,3-triazol-4-yl}methyl)-1-methyl-1H-imidazole-2-sulfonamide had a minimum inhibitory concentration (MIC) of 3.12 μg/mL against B. subtilis, which is two times higher than the normal streptomycin (6.25 μg/mL). It also had a MIC value of 6.25 μg/mL against S. aureus that was the same as the positive control. Also the antibiofilm profiles for the potent compounds showed that the active derivatives were not only very good at killing bacteria, but they were also very good at stopping the growth of B. subtilis biofilm.

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来源期刊
CiteScore
1.40
自引率
22.20%
发文量
252
审稿时长
2-4 weeks
期刊介绍: Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.
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