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Future Med Chem. 2011 Sep;3(11):1427-54. doi: 10.4155/fmc.11.90.

Nitroimidazoles for the treatment of TB: past, present and future.

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Tuberculosis Research Section, LCID, NIAID, NIH, Room 2W20G, Building 33, 9000 Rockville Pike, Bethesda, MD 20892, USA.


Tuberculosis remains a leading cause of death resulting from an infectious agent, and the spread of multi- and extensively drug-resistant strains of Mycobacterium tuberculosis poses a threat to management of global health. New drugs that effectively shorten the duration of treatment and are active against drug-resistant strains of this pathogen are urgently required to develop effective chemotherapies to combat this disease. Two nitroimidazoles, PA-824 and OPC-67683, are currently in Phase II clinical trials for the treatment of TB and the outcome of these may determine the future directions of drug development for anti-tubercular nitroimidazoles. In this review we summarize the development of these nitroimidazoles and alternative analogs in these series that may offer attractive alternatives to PA-824 and OPC-67683 for further development in the drug-discovery pipeline. Lastly, the potential pitfalls in the development of nitroimidazoles as drugs for TB are discussed.

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