Kim J H, Choi K H, Kim J W, Lee J H, Choi E C, Kim B K
Department of Microbial Chemistry, College of Pharmacy, Seoul National University, South Korea.
J Antimicrob Chemother. 1998 Feb;41(2):223-9. doi: 10.1093/jac/41.2.223.
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.
CFC - 222是一种新型氟喹诺酮类药物，具有强大的广谱抗菌活性。将CFC - 222的体外和体内活性与环丙沙星、氧氟沙星、洛美沙星和司帕沙星进行了比较。对于革兰氏阳性菌，如金黄色葡萄球菌（对喹诺酮敏感和耐药）、表皮葡萄球菌、肺炎链球菌和粪肠球菌，CFC - 222比环丙沙星更具活性，与司帕沙星相似。对于革兰氏阴性菌，包括肠杆菌科细菌，CFC - 222的体外活性与司帕沙星相似，但低于环丙沙星。然而，它对铜绿假单胞菌的活性低于环丙沙星和司帕沙星。在由金黄色葡萄球菌史密斯株或金黄色葡萄球菌TMS 33株引起的小鼠全身感染中，CFC - 222表现出与环丙沙星和司帕沙星相似的活性，但优于氧氟沙星。在由化脓性链球菌ATCC 8668株引起的小鼠感染中，该化合物比环丙沙星和司帕沙星更有效。对于大肠杆菌、肺炎克雷伯菌和阴沟肠杆菌感染，CFC - 222的疗效与环丙沙星、氧氟沙星和司帕沙星相似。在相同感染模型中，CFC - 222对铜绿假单胞菌MB4 - 16的活性与环丙沙星和司帕沙星相似。这些结果表明，CFC - 222可能是治疗各种细菌感染的一种有前景的治疗药物。
