Synthesis of PA-824

M. A. Marsini; P. J. Reider; E. J. Sorensen

doi:10.1055/s-0030-1258978

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Synfacts 2011(1): 0001-0001
DOI: 10.1055/s-0030-1258978

Synthesis of Natural Products and Potential Drugs

Synthesis of PA-824

Contributor(s): Philip Kocienski
M. A. Marsini, P. J. Reider*, E. J. Sorensen*
Princeton University, USA

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Publication History

Publication Date:
21 December 2010 (online)

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Significance

PA-824 is in phase II clinical trials for the treatment of tuberculosis. It inhibits cell wall formation by disrupting mycolic acid synthesis in Mycobacterium tuberculosis. The mechanism of action entails reduction of the nitroimidazole ring by Fgd1, an F₄₂₀-dependent glucose-6-phosphate dehydrogenase, and Rv3547, a deazaflavin-dependent nitroreductase, to afford the des-nitro compound and nitric oxide.