The abyssomicin C family as in vitro inhibitors of Mycobacterium tuberculosis
- PMID: 20739223
- PMCID: PMC3213896
- DOI: 10.1016/j.tube.2010.08.002
The abyssomicin C family as in vitro inhibitors of Mycobacterium tuberculosis
Abstract
The antimycobacterial efficacy of the abyssomicin C family of natural products, in addition to a key synthetic intermediate, has been investigated given their reported inhibition of Bacillus subtilis p-aminobenzoate biosynthesis. The naturally occurring (-)-abyssomicin C and its atropisomer were found to exhibit low micromolar growth inhibition against the relatively fast-growing and non-virulent Mycobacterium smegmatis and the vaccine strain Mycobacterium bovis BCG, while their antipodes were slightly less active. (-)-abyssomicin C and its atropisomer were particularly efficacious against Mycobacterium tuberculosis H37Rv, exhibiting MIC values of 3.6 and 7.2 μM, respectively. More specifically, (-)-abyssomicin C was bactericidal. This complex natural product and its analogs, thus, hold promise as chemical tools in the study of M. tuberculosis metabolism.
Copyright © 2010 Elsevier Ltd. All rights reserved.
Conflict of interest statement
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References
-
- World Health Organization. Global tuberculosis control report. 2009.
-
- Sacchettini JC, Rubin EJ, Freundlich JS. Drugs versus bugs: in pursuit of the persistent predator Mycobacterium tuberculosis. Nat Rev Microbiol. 2008;6:41–52. - PubMed
-
- Jassal M, Bishai WR. Extensively drug-resistant tuberculosis. Lancet Infect Dis. 2009;9:19–30. - PubMed
-
- Andries K, Verhasselt P, Guillemont J, Gohlmann HWH, Neefs J-M, Winkler H, et al. A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis. Science. 2005;307:223–7. - PubMed
-
- Stover CK, Warrener P, VanDevanter DR, Sherman DR, Arain TM, Langhorne MH, et al. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature. 2000;405:962–6. - PubMed
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