含1,2,4-恶二唑片段硫醚及其氧化产物的合成与生物活性

IF 0.9 4区化学 Q4 CHEMISTRY, MULTIDISCIPLINARY

Russian Journal of General Chemistry Pub Date : 2025-02-27 DOI:10.1134/S107036322461189X

E. A. Vasilieva, I. K. Proskurina, A. D. Kotov, E. O. Sidorenko, L. M. Yablokova, M. K. Korsakov, S. A. Ivanovskii

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引用次数: 0

摘要

以4-氟噻吩、2-巯基苯并恶唑和5-甲氧基-2-巯基苯并咪唑为原料，与3-芳基-5-（氯甲基）-1,2,4-恶二唑反应，合成了一系列具有医学化学意义的新型硫醚。对所得的硫醚氧化成相应砜的条件进行了选择。对大肠杆菌、荧光假单胞菌、金黄色葡萄球菌、蜡样芽孢杆菌和白色念珠菌等敏感菌的抑菌活性进行了筛选，结果表明，在250 μg/mL以下的浓度下，化合物具有较高和中等的抑菌活性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Synthesis and Biological Activity of Thioethers Containing 1,2,4-Oxadiazole Fragment and Their Oxidation Products

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Synthesis and Biological Activity of Thioethers Containing 1,2,4-Oxadiazole Fragment and Their Oxidation Products

Methods were developed for the synthesis of a series of new thioethers, interesting for medical chemistry, by reacting 4-fluorothiophenol, 2-mercaptobenzoxazole and 5-methoxy-2-mercaptobenzimidazole with 3-aryl-5-(chloromethyl)-1,2,4-oxadiazoles. The conditions for the oxidation of the obtained thioethers into the corresponding sulfones were selected. Analysis of the results of screening of the prepared derivatives against sensitive strains of Escherichia coli, Pseudomonas fluorescens, Staphylococcus aureus, Bacillus cereus and Candida albicans showed the presence of high and moderate antibacterial activity in a number of compounds in drug concentrations up to 250 μg/mL.

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来源期刊

Russian Journal of General Chemistry 化学-化学综合

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.