title: In vitro and in vivo antibacterial efficacies of CFC-222, a new fluoroquinolone.
abstract: 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.
authors.affiliation: Department of Microbial Chemistry, College of Pharmacy, Seoul National University, Korea.
authors.forename: J H
authors.initials: JH
authors.lastname: Kim
authors.forename: J A
authors.initials: JA
authors.lastname: Kang
authors.forename: Y G
authors.initials: YG
authors.lastname: Kim
authors.forename: J W
authors.initials: JW
authors.lastname: Kim
authors.forename: J H
authors.initials: JH
authors.lastname: Lee
authors.forename: E C
authors.initials: EC
authors.lastname: Choi
authors.forename: B K
authors.initials: BK
authors.lastname: Kim
mesh_terms: D000818:Animals; D000890:Anti-Infective Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy* / Q000382:microbiology; D002939:Ciprofloxacin / Q000494:pharmacology; D003470:Culture Media; D024841:Fluoroquinolones; D051379:Mice; D008826:Microbial Sensitivity Tests; D015242:Ofloxacin / Q000494:pharmacology; D015363:Quinolones / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; C097672:CFC 222; D003470:Culture Media; D024841:Fluoroquinolones; D015363:Quinolones; D002939:Ciprofloxacin; D015242:Ofloxacin; C053091:lomefloxacin