Antibacterial activity of NM394, the active form of prodrug NM441, a new quinolone
Antibacterial activity of NM394, the active form of prodrug NM441, a new quinolone
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NM394 的抗菌活性，NM394 是一种新型喹诺酮前药 NM441 的活性形式
DOI：
10.1128/aac.37.4.793
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发表时间：
1993
影响因子：
4.9
通讯作者：
S. Mitsuhashi
中科院分区：
文献类型：
--
作者：
T. Yoshida;S. Mitsuhashi
并与其他新喹诺酮类药物进行了体外抗菌活性比较。NM 394对2，606个最近的临床分离株显示出有效和广谱的抗菌活性。NM 394对革兰氏阳性菌的活性比妥磺沙星和司帕沙星低2- 16倍，但与氧氟沙星相当。只有对化脓性链球菌的抗菌活性与司帕沙星相当。对革兰氏阴性菌，NM 394表现出与环丙沙星相当的抗菌活性。针对喹诺酮类耐药铜绿假单胞菌（诺氟沙星MIC，> 6.25微克/ml），NM 394的活性大于所测试的其他试剂的活性。NM 394在接近MIC的浓度下快速杀菌。NM 394抑制从金黄色葡萄球菌、大肠杆菌和铜绿假单胞菌中纯化的DNA旋转酶的超螺旋活性; 50%抑制浓度分别为18.0、0.41和2.05 μ g/ml。
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.
新型噻氮喹啉衍生物 NM441 的体内评价
影响因子：
4.9
作者：
M. Ozaki;M. Matsuda;Y. Tomii;K. Kimura;J. Segawa;M. Kitano;M. Kise;K. Shibata;M. Otsuki;Takeshi Nishino
通讯作者：
Takeshi Nishino