1887

Abstract

Summary

A new 1,8-naphthyridine quinolone antimicrobial, PD131628, was found to be as, or more active than ciprofloxacin or ofloxacin against and considerably more active than the two 4-quinolone agents against staphylococci in terms of both MIC and OBC (the optimum bactericidal concentration, at which the rate of kill is greatest). In common with ciprofloxacin and ofloxacin, the rate of kill of PD131628 against was considerably slower than against the other three species tested. Bacterial protein synthesis, RNA synthesis and cell division were not required for the bactericidal activity of PD131628 against or the staphylococci, although the lethality of PD131628 in the absence of these activities was reduced.

Loading

Article metrics loading...

/content/journal/jmm/10.1099/00222615-36-5-353
1992-05-01
2022-08-16
Loading full text...

Full text loading...

/deliver/fulltext/jmm/36/5/medmicro-36-5-353.html?itemId=/content/journal/jmm/10.1099/00222615-36-5-353&mimeType=html&fmt=ahah

References

  1. Smith J. T. Awakening the slumbering potential of the 4-quinolone antibacterials. Pharmaceut J 1984; 233:299–305
    [Google Scholar]
  2. Smith J. T., Lewin C. S. Chemistry and mechanisms of action of the quinolone antibacterials. In Andriole V. T. (ed) The quinolones London: Academic Press; 198823–82
    [Google Scholar]
  3. Lewin C. S., Morrissey I., Smith J. T. The mode of action of quinolones–the paradox in activity of low and high concentrations and activity in the anaerobic environment. Eur J Clin Microbiol Infect Dis 1991; 10:240–248
    [Google Scholar]
  4. Sanchez J. P., Domagala J. M., Hagen S. E. Quinolone antibacterial agents. Synthesis and structure-activity relationships of 8-substituted quinolone-3-carboxylic acids and 1, 8 naphthyridine-3-carboxylic acids. J Med Chem 1988; 31:983–991
    [Google Scholar]
  5. Cohen M. A., Huband M. D., Mailloux G. B. In vitro antibacterial activities of PD 131628, a new 1-8-naphthyr-idine anti-infective agent. Antimicrob Agents Chemother 1991; 35:141–146
    [Google Scholar]
  6. Fuchs P. C., Barry A. L., Pfaller M. A., Allen S. D., Gerlach E. H. Multicentre evaluation of the in-vitro activities of three new quinolones, sparfloxacin, CI-960 and PD 131, 628, compared with the activity of ciprofloxacin against 5252 clinical bacterial isolates. Antimicrob Agents Chemother 1991; 35:764–766
    [Google Scholar]
  7. Piddock L. J. V., Walters R. N., Diver J. M. Correlation of quinolone MIC and inhibition of DNA, RNA, and protein synthesis and induction of the SOS response in Escherichia coli. Antimicrob Agents Chemother 1990; 34:2331–2336
    [Google Scholar]
  8. Huisman O., D’Ari R. An inducible DNA replication-cell division coupling mechanism in E. coli. Nature 1981; 290:797–799
    [Google Scholar]
  9. Lewin C. S., Amyes S. G. B. Bactericidal activity of DR-3355, an optically active isomer of ofloxacin. J Med Microbiol 1989; 30:227–231
    [Google Scholar]
  10. Lewin C. S., Howard B. M. A., Ratclifle N. T., Smith J. T. 4-quinolones and the SOS response. J Med Microbiol 1989; 29:139–144
    [Google Scholar]
  11. Miller J. H. Experiments in molecular genetics. Cold Spring Harbor, NY, Cold Spring Harbor Laboratory 1972
    [Google Scholar]
  12. Morrissey I., Lewin C. S., Smith J. T. Ciprofloxacin’s slow rate of kill against Enterococcus faecalis. J Med Microbiol 1991; 34:vi
    [Google Scholar]
  13. Lewin C. S., Morrissey I., Smith J. T. Fluoroquinolones exert a reduced rate of kill against Enterococcus faecalis. J Pharm Pharmacol 1991; 43:492–494
    [Google Scholar]
  14. Lewin C. S., Smith J. T. Bactericidal mechanism of ofloxacin. J Antimicrob Chemother 1988; 22: Suppl C 1–8
    [Google Scholar]
  15. Lewin C. S., Amyes S. G. B. The role of the SOS response in bacteria exposed to zidovudine or trimethoprim. J Med Microbiol 1991; 34:329–332
    [Google Scholar]
  16. Smith S. M., Eng R. H. K., Bais P., Fan-Havard P. Tecson-Tumang,. F., Epidemiology of ciprofloxacin resistance among patients with methicillin-resistant Staphylococcus aureus. J Antimicrob Chemother 1990; 26:567–572
    [Google Scholar]
http://instance.metastore.ingenta.com/content/journal/jmm/10.1099/00222615-36-5-353
Loading
/content/journal/jmm/10.1099/00222615-36-5-353
Loading

Data & Media loading...

Most cited this month Most Cited RSS feed

This is a required field
Please enter a valid email address
Approval was a Success
Invalid data
An Error Occurred
Approval was partially successful, following selected items could not be processed due to error