New 5-Modified Pyrimidine Nucleoside Inhibitors of Mycobacterial Growth
| Autor: | Sergey N. Kochetkov, Eduard R. Shmalenyuk, Andreevskaia Sn, V V Erokhin, Larisa Chernousova, Tatiana Smirnova, L. A. Alexandrova |
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| Rok vydání: | 2010 |
| Předmět: |
Tuberculosis
Pyrimidine biology medicine.drug_class business.industry Pharmacology Antimycobacterial medicine.disease biology.organism_classification Biochemistry In vitro Mycobacterium tuberculosis chemistry.chemical_compound chemistry medicine Molecular Medicine business Nucleoside Molecular Biology Biotechnology |
| Zdroj: | Acta Naturae. 2:108-110 |
| ISSN: | 2075-8251 |
| DOI: | 10.32607/actanaturae.10780 |
| Popis: | 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 2ʹ–deoxy–, 3ʹ–azido–2ʹ,3ʹ–dideoxy–, and 3ʹ–amino–2ʹ,3ʹ–dideoxypyrimidine nucleoside analogues bearing lengthy flexible alkyloxymethyl substituents exhibited marked inhibitory activity against M. tuberculosis in vitro. 5–Dodecyloxymethyl–2ʹ–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. |
| Databáze: | OpenAIRE |
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