Biedenbach D J, Sutton L D, Jones R N
Department of Pathology, University of Iowa College of Medicine, Iowa City 52242, USA.
Antimicrob Agents Chemother. 1995 Oct;39(10):2325-30. doi: 10.1128/AAC.39.10.2325.
The antimicrobial activity of CS-940, a new trifluorinated quinolone drug, was tested against 761 clinical isolates. CS-940 activity against members of the family Enterobacteriaceae was most similar to that of ciprofloxacin and ofloxacin, with a large range of MICs inhibiting 90% of isolates tested (MIC90S) of 0.015 to 16 micrograms/ml (median MIC90, 0.06 micrograms/ml). CS-940 had greater activity than ciprofloxacin or ofloxacin when they were tested against Acinetobacter spp. (MIC90S, 0.03 micrograms/ml) and Stenotrophomonas (Xanthomonas) maltophilia (MIC90S, 2 micrograms/ml). CS-940 demonstrated a high degree of potency against Haemophilus influenzae, Moraxella catarrhalis, and Neisseria spp. (MIC90S, < or = 0.06 micrograms/ml). CS-940 was two- to eightfold more active than ciprofloxacin or ofloxacin against oxacillin-susceptible Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, and coagulase-negative Staphylococcus spp. CS-940 was also very active against Streptococcus spp. and enterococci, for which MIC90S were < or = 2 micrograms/ml; for Enterococcus faecium, however, the MIC90 was 4 micrograms/ml. CS-940 was generally less active than a comparison investigational fluoroquinolone, clinafloxacin. This compound appears promising by in vitro test analysis and warrants further in vivo trials.
新型三氟喹诺酮药物CS - 940的抗菌活性针对761株临床分离菌进行了测试。CS - 940对肠杆菌科成员的活性与环丙沙星和氧氟沙星最为相似，抑制90%测试分离菌的最低抑菌浓度（MIC90）范围很大，为0.015至16微克/毫升（MIC90中位数为0.06微克/毫升）。当针对不动杆菌属（MIC90为0.03微克/毫升）和嗜麦芽窄食单胞菌（以前称嗜麦芽黄单胞菌，MIC90为2微克/毫升）进行测试时，CS - 940的活性高于环丙沙星或氧氟沙星。CS - 940对流感嗜血杆菌、卡他莫拉菌和奈瑟菌属显示出高度效力（MIC90≤0.06微克/毫升）。CS - 940对苯唑西林敏感的金黄色葡萄球菌、表皮葡萄球菌、溶血葡萄球菌和凝固酶阴性葡萄球菌的活性比环丙沙星或氧氟沙星高两至八倍。CS - 940对链球菌属和肠球菌也非常活跃，其MIC90≤2微克/毫升；然而，对于粪肠球菌，MIC90为4微克/毫升。总体而言，CS - 940的活性低于对照研究性氟喹诺酮类药物克林沙星。通过体外试验分析，该化合物似乎很有前景，值得进一步进行体内试验。
