Engelhardt Institute of Molecular Biology, Russian Academy of Sciences.
Acta Naturae. 2010 Apr;2(1):108-11.
The WHO has declared tuberculosis (TB) a global health emergency. Therefore, there is an urgent need to discover and develop new anti-TB drugs. Here we report on a new category of 5-substituted pyrimidine nucleosides as potent inhibitors of Myco-bacterium tuberculosis growth in vitro. A series of 2'-deoxy-, 3'-azido-2',3'-dideoxy-, and 3'-amino-2',3'-dideoxypyrimidine nucleoside analogues bearing lengthy flexible alkyloxymethyl substituents exhibited marked inhibitory activity against M. tuberculosis in vitro. 5-Dodecyloxymethyl-2'-deoxyuridine was found to be a potent inhibitor of M. tuberculosis propagation in vitro. In contrast, monophosphates of the tested nucleosides were devoid of antimycobacterial activity. This new class of inhibitors seems to be a promising chemotherapeutic agent against TB and merits further studies.
世界卫生组织已宣布结核病（TB）为全球卫生紧急情况。因此，迫切需要发现和开发新的抗结核药物。在这里，我们报告了一类新的 5-取代嘧啶核苷，它们是体外抑制结核分枝杆菌生长的有效抑制剂。一系列带有长链柔性烷氧基甲基取代基的 2'-脱氧、3'-叠氮-2'，3'-二脱氧和 3'-氨基-2'，3'-二脱氧嘧啶核苷类似物对结核分枝杆菌表现出显著的体外抑制活性。5-十二烷氧基甲基-2'-脱氧尿苷被发现是体外抑制结核分枝杆菌繁殖的有效抑制剂。相比之下，测试核苷的单磷酸盐没有抗分枝杆菌活性。这类新型抑制剂似乎是一种有前途的抗结核化疗药物，值得进一步研究。
