CFC-222 is a novel
fluoroquinolone with potent and broad-spectrum antibacterial activity. The in-vitro and in-vivo activities of
CFC-222 were compared with those of
ciprofloxacin,
ofloxacin,
lomefloxacin and
sparfloxacin. Against gram-positive bacteria such as Staphylococcus aureus (
quinolone-susceptible and
quinolone-resistant), Staphylococcus epidermidis, Streptococcus pneumoniae and Enterococcus faecalis,
CFC-222 was more active than
ciprofloxacin and similar to
sparfloxacin. Against gram-negative bacteria, including Enterobacteriaceae, the in-vitro activity of
CFC-222 was similar to that of
sparfloxacin, but less than that of
ciprofloxacin. However, it was less active than
ciprofloxacin and
sparfloxacin against Pseudomonas aeruginosa. In mouse systemic
infection caused by S. aureus Smith or S. aureus TMS 33,
CFC-222 demonstrated an activity similar to that of
ciprofloxacin and
sparfloxacin, but better than that of
ofloxacin. The compound was more effective than
ciprofloxacin and
sparfloxacin in murine
infection caused by Streptococcus pyogenes ATCC 8668. Against Escherichia coli, Klebsiella pneumoniae and Enterobacter cloacae
infections, the efficacy of
CFC-222 was similar to those of
ciprofloxacin,
ofloxacin and
sparfloxacin. The activity of
CFC-222 was similar to those of
ciprofloxacin and
sparfloxacin against P. aeruginosa MB4-16 in the same
infection model. These results suggest that
CFC-222 may be a promising therapeutic agent for the treatment of various
bacterial infections.