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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Synthesis of water-soluble prodrugs of 5-modified 2MODIFIER LETTER PRIME-deoxyuridines and their antibacterial activity
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Synthesis of water-soluble prodrugs of 5-modified 2MODIFIER LETTER PRIME-deoxyuridines and their antibacterial activity

机译：5-改性的2种过氧基尿苷和抗菌活性的水溶性前药的合成及其抗菌活性

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摘要

Recently we have synthesized a set of pyrimidine nucleoside derivatives bearing extended alkyltriazolylmethyl substituents at position 5 of the nucleic base, and showed their significant activity against Mycobacterium tuberculosis virulent laboratory strain H37Rv as well as drug-resistant MS-115 strain. The presence of a lengthy hydrophobic substituent leads to the reduction of nucleoside water solubility making their antibacterial activity troublesome to study. A series of water-soluble forms of 5-modified 2MODIFIER LETTER PRIME-deoxyuridines 4a-c and 8a-c were synthesized. They appeared at least two orders more soluble compared with the parent compounds 1a and 1b. Their half-hydrolysis time was 5-12 h, which can be considered optimal for prodrugs used in clinics. Obtained compounds showed moderate activity (MIC 48-95 mu g center dot ml(-1)) against some Gram-positive bacteria including resistant strains of Staphylococcus aureus and Mycobacterium smegmatis and were low cytotoxic for human cell lines (CD50 100 mu g center dot ml(-1)).
机译：最近，我们已经合成了一组嘧啶核苷衍生物，其在核基碱的第5位延伸延伸的烷基三唑基甲基取代基，并表明其对结核分枝杆菌病毒实验室菌株H37RV的显着活性以及耐药MS-115菌株。冗长的疏水性取代基的存在导致核苷水溶解度的减少，使其抗菌活性麻烦的研究。合成了一系列水溶性的5-改性的2种过氧基脲4a-C和8A-C的水溶性形式。与母体化合物1A和1B相比，它们似乎至少有两个溶解。它们的半水解时间为5-12小时，可以考虑诊所中使用的前药的最佳。得到的化合物显示出适度的活性（MIC48-95μg中心点M11（-1）），其针对一些革兰氏阳性细菌，包括金黄色葡萄球菌和分枝杆菌的抗性菌株，并且是人细胞系的低细胞毒性（CD50 100μg中心点M1（-1））。

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