New 5-Modified Pyrimidine Nucleoside Inhibitors of Mycobacterial Growth

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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 a new category of 5-substituted pyrimidine nucleosides as potent inhibitors of Mycobacterium 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.

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New 5-Modified Pyrimidine Nucleoside Inhibitors of Mycobacterial Growth
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© Alexandrova L.A., Shmalenyuk E.R., Kochetkov S.N., Erokhin V.V., Smirnova T.G., Andreevskaia S.N., Chernousova L.N., 2010

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