Yoshida T, Mitsuhashi S
Episome Institute, Gunma, Japan.
Antimicrob Agents Chemother. 1993 Apr;37(4):793-800. doi: 10.1128/AAC.37.4.793.
The in vitro antibacterial activity of NM394 was compared with those of other new quinolones. NM394 showed potent and broad-spectrum antibacterial activity against 2,606 recent clinical isolates. The activity of NM394 against gram-positive bacteria was 2- to 16-fold less than that of tosulfoxacin and sparfloxacin but was comparable to that of ofloxacin. Only against Streptococcus pyogenes was the activity of NM394 equal to that of sparfloxacin. Against gram-negative bacteria, NM394 showed antibacterial activity equal to that of ciprofloxacin. Against quinolone-resistant Pseudomonas aeruginosa (norfloxacin MIC, > 6.25 micrograms/ml), the activity of NM394 was greater than those of the other agents tested. NM394 was rapidly bactericidal at concentrations near the MIC. NM394 inhibited supercoiling activities of DNA gyrase purified from Staphylococcus aureus, Escherichia coli, and P. aeruginosa; the 50% inhibitory concentrations were 18.0, 0.41, and 2.05 micrograms/ml, respectively.
将NM394的体外抗菌活性与其他新型喹诺酮类药物进行了比较。NM394对2606株近期临床分离株显示出强效和广谱抗菌活性。NM394对革兰氏阳性菌的活性比对磺氟沙星和司帕沙星低2至16倍，但与氧氟沙星相当。仅对化脓性链球菌，NM394的活性与司帕沙星相当。对革兰氏阴性菌，NM394显示出与环丙沙星相当的抗菌活性。对喹诺酮耐药的铜绿假单胞菌（诺氟沙星MIC，>6.25微克/毫升），NM394的活性高于其他受试药物。NM394在接近MIC的浓度下具有快速杀菌作用。NM394抑制了从金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌中纯化的DNA促旋酶的超螺旋活性；50%抑制浓度分别为18.0、0.41和2.05微克/毫升。
