期刊
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
卷 50, 期 10, 页码 3350-3354出版社
AMER SOC MICROBIOLOGY
DOI: 10.1128/AAC.00488-06
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资金
- Intramural NIH HHS [Z01 AI000783-11] Funding Source: Medline
- NIAID NIH HHS [Y1-AI-2004] Funding Source: Medline
Leprosy responds very slowly to the current multidrug therapy, and hence there is a need for novel drugs with potent bactericidal activity. PA-824 is a 4-nitroimidazo-oxazine that is currently undergoing phase I clinical trials for the treatment of tuberculosis. The activity of PA-824 against Mycobacterium leprae was tested and compared with that of rifampin in axenic cultures, macrophages, and two different animal models. Our results conclusively demonstrate that PA-824 has no effect on the viability of M. leprae in all three models, consistent with the lack of the nitroimidazo-oxazine-specific nitroreductase, encoded by Rv3547 in the M. leprae genome, which is essential for activation of this molecule.
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