Department of Laboratory Medicine and Pathology, 1-71 Medical Sciences Building, Edmonton, AB, Canada T6G 2H7.
Bioorg Med Chem Lett. 2012 Jan 15;22(2):1091-4. doi: 10.1016/j.bmcl.2011.11.114. Epub 2011 Dec 4.
Several 5-alkyl (or halo)-3'-azido (amino or halo) analogs of pyrimidine nucleosides have been synthesized and evaluated against Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium. Among these compounds, 3'-azido-5-ethyl-2',3'-dideoxyuridine (3) was found to have significant antimycobacterial activities against M. bovis (MIC(50)=1μg/mL), M. tuberculosis (MIC(50)=10μg/mL) and M. avium (MIC(50)=10μg/mL).
已经合成了几种嘧啶核苷的 5-烷基（或卤代）-3'-叠氮化物（氨基或卤代）类似物，并对牛分枝杆菌、结核分枝杆菌和鸟分枝杆菌进行了评估。在这些化合物中，发现 3'-叠氮-5-乙基-2'，3'-二脱氧尿苷（3）对牛分枝杆菌（MIC（50）=1μg/mL）、结核分枝杆菌（MIC（50）=10μg/mL）和鸟分枝杆菌（MIC（50）=10μg/mL）具有显著的抗分枝杆菌活性。
