@article{7166, keywords = {Animals, Culture Media, Disease Models, Animal, Drug Resistance, Bacterial, leprosy, Macrophages, Peritoneal, Mice, Mice, Inbred BALB C, Mice, Nude, Microbial Sensitivity Tests, Mycobacterium leprae, Nitroimidazoles}, author = {Manjunatha UH and Lahiri R and Randhawa B and Dowd C and Krahenbuhl JL and Barry C}, title = {Mycobacterium leprae is naturally resistant to PA-824.}, abstract = {
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.
}, year = {2006}, journal = {Antimicrobial agents and chemotherapy}, volume = {50}, pages = {3350-4}, month = {2006 Oct}, issn = {0066-4804}, url = {https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1610092/pdf/0488-06.pdf}, doi = {10.1128/AAC.00488-06}, language = {eng}, }