Cohen M A, Huband M D, Yoder S L, Gage J W, Roland G E
Parke-Davis Pharmaceutical Research, Ann Arbor, MI 48105, USA.
J Antimicrob Chemother. 1998 Jun;41(6):605-14. doi: 10.1093/jac/41.6.605.
Bactericidal activities of clinafloxacin, CI-990 and ciprofloxacin were examined and compared for a small collection of gram-positive and gram-negative pathogens. In-vitro antimicrobial activities were measured by MIC, MBC and time-kill studies; in-vivo efficacy of each drug was assessed in an acute lethal mouse infection model that monitored median protective dose, eradicative dose and time-kill in blood. In general, for all test methods, activity of clinafloxacin exceeded that of CI-990, which in turn exceeded that of ciprofloxacin. Improvement in clinafloxacin and CI-990 activity over ciprofloxacin was more apparent against gram-positive cocci; differences were less noticeable against Escherichia coli and Pseudomonas aeruginosa. Clinafloxacin activity was notably high against Staphylococcus aureus and, against ciprofloxacin-resistant strains, this high activity was maintained in vitro and measurable activity was demonstrated in vivo.
对一小批革兰氏阳性和革兰氏阴性病原体检测并比较了克林沙星、CI-990和环丙沙星的杀菌活性。通过最低抑菌浓度（MIC）、最低杀菌浓度（MBC）和时间杀菌研究测定体外抗菌活性；在急性致死性小鼠感染模型中评估每种药物的体内疗效，该模型监测半数保护剂量、根除剂量和血液中的时间杀菌情况。总体而言，对于所有测试方法，克林沙星的活性均超过CI-990，而CI-990又超过环丙沙星。克林沙星和CI-990相对于环丙沙星的活性改善在革兰氏阳性球菌中更为明显；对大肠杆菌和铜绿假单胞菌的差异则不太明显。克林沙星对金黄色葡萄球菌的活性显著较高，并且对于耐环丙沙星菌株，这种高活性在体外得以维持，在体内也表现出可测量的活性。
