Abstract To obtain nucleoside derivatives with antibacterial activity, we have proposed three ways of the synthesis of 5-alkylthiomethyl-2'-deoxyuridines, which was based on the condensation of 3',5'-diacetyl-5-bromomethyl-2'-deoxyuridine with the corresponding 1-mercaptans. 5-Hexylthiomethyl-, 5-octylthiomethyl-, 5-bis(octylthio)methyl-2'-deoxyuridine and α and β anomers of 5-decylthiomethyl-2'-deoxyuridine have been synthesized. The notable cytotoxicity of a number of the synthesized compounds in the A549 cell culture has been shown. 5-Hexylthiomethyl-2'-deoxyuridine has been shown to inhibit the in vitro growth of the Mycobacterium smegmatis mc 2 155 strain with the MIC value of 200 μg/mL. The other compounds have not inhibited the growth of the Mycobacterium smegmatis and Staphylococcus aureus strains.

中文翻译：

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2'-脱氧尿苷的 5-烷基硫甲基衍生物：合成和抗菌活性

摘要 为了获得具有抗菌活性的核苷衍生物，我们提出了 3',5'-二乙酰-5-溴甲基-2'-脱氧尿苷缩合的 3 种合成 5-烷硫基甲基-2'-脱氧尿苷的方法。与相应的1-硫醇。已经合成了 5-Hexylthiomethyl-, 5-octylthiomethyl-, 5-bis(octylthio)methyl-2'-deoxyuridine 和 5-decylthiomethyl-2'-deoxyuridine 的 α 和 β 端基异构体。许多合成化合物在 A549 细胞培养物中具有显着的细胞毒性。5-Hexylthiomethyl-2'-deoxyuridine 已显示抑制耻垢分枝杆菌 mc 2 155 菌株的体外生长，MIC 值为 200 μg/mL。其他化合物没有抑制耻垢分枝杆菌和金黄色葡萄球菌菌株的生长。