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. 1990 Jul;34(7):1323–1325. doi: 10.1128/aac.34.7.1323

Activity of KB-5246 against outer membrane mutants of Escherichia coli and Salmonella typhimurium.

Y Kotera 1, M Inoue 1, S Mitsuhashi 1
PMCID: PMC175974  PMID: 2167038

Abstract

The inhibitory activity of KB-5246 against Escherichia coli DNA gyrase and the antibacterial activity and apparent uptake in E. coli and Salmonella typhimurium outer membrane mutants of KB-5246 were measured. The 50% inhibitory concentrations of KB-5246, ciprofloxacin, oflaxacin, and norfloxacin for E. coli KL-16 DNA gyrase were 0.72, 0.62, 0.84, and 1.16 micrograms/ml, respectively. The activity of KB-5246 was twofold lower against an OmpF-deficient mutant and twofold higher against a mutant which produced OmpF constitutively than against the parent with osmoregulated OmpF production. KB-5246 had twofold-higher activity against a deep rough mutant of S. typhimurium than against the parent. The apparent uptake of KB-5246 in the OmpF-deficient mutant was decreased and its uptake in the deep rough mutant was increased when compared with those in the parents. These results suggest that KB-5246 is taken up by porin and nonporin pathways and has strong inhibitory activity against DNA gyrase, resulting in potent antibacterial activity.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Aoyama H., Sato K., Kato T., Hirai K., Mitsuhashi S. Norfloxacin resistance in a clinical isolate of Escherichia coli. Antimicrob Agents Chemother. 1987 Oct;31(10):1640–1641. doi: 10.1128/aac.31.10.1640. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Bedard J., Wong S., Bryan L. E. Accumulation of enoxacin by Escherichia coli and Bacillus subtilis. Antimicrob Agents Chemother. 1987 Sep;31(9):1348–1354. doi: 10.1128/aac.31.9.1348. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. Chapman J. S., Georgopapadakou N. H. Routes of quinolone permeation in Escherichia coli. Antimicrob Agents Chemother. 1988 Apr;32(4):438–442. doi: 10.1128/aac.32.4.438. [DOI] [PMC free article] [PubMed] [Google Scholar]
  4. Cohen S. P., Hooper D. C., Wolfson J. S., Souza K. S., McMurry L. M., Levy S. B. Endogenous active efflux of norfloxacin in susceptible Escherichia coli. Antimicrob Agents Chemother. 1988 Aug;32(8):1187–1191. doi: 10.1128/aac.32.8.1187. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Fujimaki K., Noumi T., Saikawa I., Inoue M., Mitsuhashi S. In vitro and in vivo antibacterial activities of T-3262, a new fluoroquinolone. Antimicrob Agents Chemother. 1988 Jun;32(6):827–833. doi: 10.1128/aac.32.6.827. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Gutmann L., Williamson R., Moreau N., Kitzis M. D., Collatz E., Acar J. F., Goldstein F. W. Cross-resistance to nalidixic acid, trimethoprim, and chloramphenicol associated with alterations in outer membrane proteins of Klebsiella, Enterobacter, and Serratia. J Infect Dis. 1985 Mar;151(3):501–507. doi: 10.1093/infdis/151.3.501. [DOI] [PubMed] [Google Scholar]
  7. Hirai K., Aoyama H., Irikura T., Iyobe S., Mitsuhashi S. Differences in susceptibility to quinolones of outer membrane mutants of Salmonella typhimurium and Escherichia coli. Antimicrob Agents Chemother. 1986 Mar;29(3):535–538. doi: 10.1128/aac.29.3.535. [DOI] [PMC free article] [PubMed] [Google Scholar]
  8. Hirai K., Aoyama H., Suzue S., Irikura T., Iyobe S., Mitsuhashi S. Isolation and characterization of norfloxacin-resistant mutants of Escherichia coli K-12. Antimicrob Agents Chemother. 1986 Aug;30(2):248–253. doi: 10.1128/aac.30.2.248. [DOI] [PMC free article] [PubMed] [Google Scholar]
  9. Hooper D. C., Wolfson J. S., Souza K. S., Tung C., McHugh G. L., Swartz M. N. Genetic and biochemical characterization of norfloxacin resistance in Escherichia coli. Antimicrob Agents Chemother. 1986 Apr;29(4):639–644. doi: 10.1128/aac.29.4.639. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. Kotera Y., Mitsuhashi S. In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone. Antimicrob Agents Chemother. 1989 Nov;33(11):1896–1900. doi: 10.1128/aac.33.11.1896. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Mitsuhashi S. Comparative antibacterial activity of new quinolone-carboxylic acid derivatives. Rev Infect Dis. 1988 Jan-Feb;10 (Suppl 1):S27–S31. doi: 10.1093/clinids/10.supplement_1.s27. [DOI] [PubMed] [Google Scholar]
  12. Sato K., Inoue Y., Fujii T., Aoyama H., Inoue M., Mitsuhashi S. Purification and properties of DNA gyrase from a fluoroquinolone-resistant strain of Escherichia coli. Antimicrob Agents Chemother. 1986 Nov;30(5):777–780. doi: 10.1128/aac.30.5.777. [DOI] [PMC free article] [PubMed] [Google Scholar]

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