Advertisement

Springer Nature is making SARS-CoV-2 and COVID-19 research free. View research | View latest news | Sign up for updates

Factors affectingin vitro activity of LB20304, a new fluoroquinolone

Abstract

LB20304 is a novel fluoroquinolone that exhibits a potent broad spectrum antibacterial activity against both gram-positve and gram-negative bacteria. The MICs (Minimal Inhibitory Concentration) of LB20304 were determined against both gram-positve and gram-negative bacteria under various conditions including several media, pHs, and inoculum concentrations. Thein vitro activity of LB20304 was not significantly affected by the changes in testing conditions such as components of media and inoculum concentrations, but it was slightly reduced by acid condition. The MICs and MBCs (Minimal Bactericidal Concentration) of LB20304 againstStaphylococcus aureus, Escherichia coli andPseudomonas aeruginosa were hardly affected by the presence of 50% human serum, mouse serum, guinea pig serum or horse serum, and the MBCs were equal to or at most four-times higher than the MICs. The activities of LB20304 were decreased by the presence of high concentraion of Mg++ or human urine (pH, 5.5) in the test media. The frequencies of mutants resistant to LB20304 were similar to or lower than those found in ciprofloxacin and sparfloxacin.

This is a preview of subscription content, log in to check access.

References Cited

  1. Blumberg, H. M., Caroll, D. D. J., Terry, P. and Wachsmuth, I. K., Rapid development of ciprofloxacin resistance in methicillin-susceptible and -resistantStaphylococcus aureus, J. Infect. Dis., 163, 1279–1285 (1991).

  2. Chin, N. X., Chu, D., Huang, H. B., and Neu, H. C., A-86719.1, a new class DNA gyrase inhibitor, its time-killing activity, postantibiotic effect and assay condition effect. InAbstracts of the 34th Interscience Conference on Antimicrobial agents and Chemotherapy, Orlando, FL, 1994. Abstract F51, p. 109. American Society for Microbiology, Washington, D.C. (1994).

  3. Kaatz, G. W., Seo, S. M. and Ruble, C. A., Mechanisms of fluoroquinolone resistance inStaphylococcus aureus, J. Infect. Dis. 163, 1080–1086 (1991).

  4. Kim, Y. K., Choi, H., Kim, S. H., Chang, J. H., Nam, D. H., Kim, Y. Z., Kwak, J. H. and Hong, C. Y., Synthesis and antibacterial activities of LB20304: a new fluoronaphthyridone antibiotic containing novel oxime functionalized pyrrolidine. InAbstracts of the 35th Interscience Conference on Antimicrobial agents and Chemotherapy, San Francisco, CA, 1995. Abstract F204, p. 148. American Society for Microbiology, Washington, D.C. (1995).

  5. Marshall, A. S., and Jones, R. N.,In vitro activity of DU-6859a, a new fluorocyclopropyl quinolone.Antimicrob. Agents Chemother., 37, 2747–2753 (1993).

  6. Marshall, A. J. H., and Piddock, L. J. V., Interaction of divalent cations, quinolones and bacteria.J. Antimicrob. Chemother., 34, 465–483 (1994).

  7. National Committee for Clinical Laboratory Standards. Methods for determining bactericidal activity of antimicrobial agents. M26-T. NCCLS, Villanova, Pa. (1992).

  8. National Committee for Clinical Laboratory Standards. Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically, Third edition; Approved standard M7-A3. NCCLS, Villanova, Pa. (1993).

  9. Neu, H. C., Quinolone antimicrobial agents.Ann. Rev. Med., 43, 465–486 (1992).

  10. Oh, J. I., Paek, K. S., Kim, M. Y., Seo, S. M., Lee, Y. H., Hong, C.-Y., Nam, D. H., Kim, Y. Z., Kim, I. C. and Kwak, J. H.,In vitro andin vivo antibacterial activities of LB20304, a new fluoronaphthyridone. InAbstracts of the 35th Interscience Conference on Antimicrobial agents and Chemotherapy, San Francisco, CA, 1995. Abstract F205, p. 148. American Society for Microbiology, Washington, D.C. (1995).

  11. Raviglione, M. C., Boyle, J. F., Mariuz, P., Pablos-Mendez, A., Cotes, H. and Merlo, A., Ciprofloxacin-resistant methicillin-resistantStaphylococcus aureus in an acute-care hospital,Antimicrobial Agents and Chemotheraphy, 34, 2050–2054 (1990).

  12. Thys, J. P., Jacobs, F. and Motte, S., Quinolones in the treatment of lower respiratory tract infections,Rev. Infect. Dis., 11(Suppl. 5), S1212-S1219 (1989).

  13. Wolfson, J. S., and Hooper, D. C., Fluoroquinolone antimicrobial agents.Clin. Microbiol. Rev., 2, 378–424 (1989).

Download references

Author information

Correspondence to Jin-Hwan Kwak.

Rights and permissions

Reprints and Permissions

About this article

Cite this article

Paek, K., Ahn, M., Kim, M. et al. Factors affectingin vitro activity of LB20304, a new fluoroquinolone. Arch. Pharm. Res. 19, 143–147 (1996). https://doi.org/10.1007/BF02976850

Download citation

Key words

  • LB20304
  • Quinolone
  • MIC
  • MBC
  • Resistance