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Chemical Compound Review

CHEMBL507853     7-ethyl-3-nitro-6-oxa-1,4...

Synonyms: AG-K-81062, ACMC-20as7x, CGI-17341, LS-80036, CTK4B5688, ...
 
 
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Disease relevance of Cgi 17341

  • At concentrations ranging from 0.1 to 0.3 micrograms/ml, CGI 17341 inhibited the drug-susceptible and multi-drug-resistant strains of Mycobacterium tuberculosis [1].
  • In mice infected with M. tuberculosis, the 50% effective dose for CGI 17341 was 7.7 mg/kg of body weight (95% confidence limits, 3.5 and 10.27) when administered on days 11 and 12 postinfection [1].
 

High impact information on Cgi 17341

  • We have confirmed that resistance to PA-824 (a nitroimidazo-oxazine) and CGI-17341 (a nitroimidazo-oxazole) is most commonly mediated by loss of a specific glucose-6-phosphate dehydrogenase (FGD1) or its deazaflavin cofactor F420, which together provide electrons for the reductive activation of this class of molecules [2].

References

  1. In vitro and in vivo activities of the nitroimidazole CGI 17341 against Mycobacterium tuberculosis. Ashtekar, D.R., Costa-Perira, R., Nagrajan, K., Vishvanathan, N., Bhatt, A.D., Rittel, W. Antimicrob. Agents Chemother. (1993) [Pubmed]
  2. Identification of a nitroimidazo-oxazine-specific protein involved in PA-824 resistance in Mycobacterium tuberculosis. Manjunatha, U.H., Boshoff, H., Dowd, C.S., Zhang, L., Albert, T.J., Norton, J.E., Daniels, L., Dick, T., Pang, S.S., Barry, C.E. Proc. Natl. Acad. Sci. U.S.A. (2006) [Pubmed]
 
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