In vitro and in vivo antibacterial efficacies of CFC-222, a new fluoroquinolone.

CFC-222 is a novel fluoroquinolone containing a C-7 bicyclic amine moiety with potent antibacterial activities against gram-positive, gram-negative, and anaerobic organisms. We compared the in vitro and in vivo activities of CFC-222 with those of ciprofloxacin, ofloxacin, and lomefloxacin. CFC-222 was more active than the other fluoroquinolones tested against gram-positive bacteria. CFC-222 was particularly active against Streptococcus pneumoniae (MIC at which 90% of isolates are inhibited [MIC90], 0.2 microg/ml), Staphylococcus aureus (MIC90, 0.2 microg/ml for ciprofloxacin-susceptible strains), and Enterococcus faecalis (MIC90, 0.39 microg/ml). Against Escherichia coli and other members of the family Enterobacteriaceae, CFC-222 was slightly less active than ciprofloxacin (MIC90s for E. coli, 0.1 and 0.025 microg/ml, respectively). The in vitro activity of CFC-222 was not influenced by inoculum size, medium composition, or the presence of horse serum. However, its activity was decreased significantly by a change in the pH of the medium from 7.0 to 6.0, as was the case for the other quinolones tested. The in vivo protective efficacy of CFC-222 by oral administration was greater than those of the other quinolones tested in a mouse model of intraperitoneally inoculated systemic infection caused by S. aureus. CFC-222 exhibited efficacy comparable to that of ciprofloxacin in the same model of infection caused by gram-negative organisms, such as E. coli and Klebsiella pneumoniae. In this infection model, CFC-222 was slightly less active than ciprofloxacin against Pseudomonas aeruginosa. These results suggest that CFC-222 may be a promising therapeutic agent in various bacterial infections.
AuthorsJ H Kim, J A Kang, Y G Kim, J W Kim, J H Lee, E C Choi, B K Kim
JournalAntimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 41 Issue 10 Pg. 2209-13 (Oct 1997) ISSN: 0066-4804 [Print] UNITED STATES
PMID9333049 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Anti-Infective Agents
  • CFC 222
  • Culture Media
  • Fluoroquinolones
  • Quinolones
  • Ciprofloxacin
  • Ofloxacin
  • lomefloxacin
  • Animals
  • Anti-Infective Agents (pharmacology, therapeutic use)
  • Bacteria (drug effects)
  • Bacterial Infections (drug therapy, microbiology)
  • Ciprofloxacin (pharmacology)
  • Culture Media
  • Fluoroquinolones
  • Mice
  • Microbial Sensitivity Tests
  • Ofloxacin (pharmacology)
  • Quinolones (pharmacology)

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