HOMEPRODUCTSSERVICESCOMPANYCONTACTFAQResearchDictionaryPharmaMobileSign Up FREE or Login

In vitro and in vivo antibacterial activities of KB-5246, a new tetracyclic quinolone.

Abstract
The in vitro and in vivo antibacterial activities of KB-5246, a tetracyclic quinolone, were compared with those of ciprofloxacin, ofloxacin, and norfloxacin. KB-5246 demonstrated a broad antibacterial spectrum. The in vitro activity of KB-5246 against gram-negative bacteria was higher than that of ofloxacin or norfloxacin and was comparable to that of ciprofloxacin. KB-5246 demonstrated the greatest activity against gram-positive bacteria of the four agents tested. Among Streptococcus pyogenes strains resistant to 1.56 micrograms of norfloxacin per ml, there were 26 strains susceptible to 0.2 micrograms of KB-5246 per ml. Similarly, among the Staphylococcus aureus and Staphylococcus epidermidis strains resistant to 3.13 micrograms of norfloxacin per ml, there were 23 S. aureus and 11 S. epidermidis strains susceptible to 0.39 micrograms of KB-5246 per ml. Among the Streptococcus pneumoniae and Enterococcus faecalis strains resistant to 12.5 micrograms of norfloxacin per ml, there were 5 S. pneumoniae and 10 E. faecalis strains susceptible to 0.39 micrograms of KB-5246 per ml. KB-5246 had bactericidal activity at the MIC. KB-5246 demonstrated excellent antibacterial activity against various systemic infections in mice. After oral administration, KB-5246 was as active as ofloxacin and about two times more active than norfloxacin.
AuthorsY Kotera, S Mitsuhashi
JournalAntimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 33 Issue 11 Pg. 1896-900 (Nov 1989) ISSN: 0066-4804 [Print] UNITED STATES
PMID2610501 (Publication Type: Journal Article)
Chemical References
  • Anti-Infective Agents
  • Fluoroquinolones
  • Phenalenes
  • Quinolones
  • KB 5246
  • Ciprofloxacin
  • Ofloxacin
  • Norfloxacin
Topics
  • Animals
  • Anti-Infective Agents (pharmacology, therapeutic use)
  • Bacterial Infections (drug therapy)
  • Ciprofloxacin (pharmacology, therapeutic use)
  • Fluoroquinolones
  • Male
  • Mice
  • Microbial Sensitivity Tests
  • Norfloxacin (pharmacology, therapeutic use)
  • Ofloxacin (pharmacology, therapeutic use)
  • Phenalenes
  • Quinolones

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research network!


Choose Username:
Email:
Password:
Verify Password: