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Objective . Tuberculosis is a serious problem of public health. The increase on the number of clinical cases of tuberculosis infected with multidrug resistant (MDR)  M. tuberculosis  calls for the development of novel therapy.  Design . We investigated the effect of mefloquine and two enantiomers, (+)erythro-mefloquine and (+)threo-mefloquine against  M. tuberculosis  strains in the environment resembling the aspects of the granuloma environment and in macrophages.  Results . The results suggest that mefloquine (racemic mixture) and (+)erythro-mefloquine have bactericidal activity against  M. tuberculosis  strains both in acidic, low oxygen tension and in macrophages. The activity, however, was impaired under increased osmolarity.  Conclusion . Identification of the target for mefloquine in the pathogen will allow for the development of novel drugs with antituberculosis activity.

Mefloquine and Its Enantiomers Are Active againstMycobacterium tuberculosisIn Vitro and in Macrophages