Wise R, Cross C, Andrews J M
Antimicrob Agents Chemother. 1984 Dec;26(6):876-80. doi: 10.1128/AAC.26.6.876.
The in vitro activity of CGP 31523A, a new aminothiazolyl cephalosporin, was compared with those of cefoxitin, cefuroxime, moxalactam, piperacillin, ciprofloxacin, and other beta-lactams, when appropriate, against 533 recent clinical isolates and known resistant strains of bacteria. The MICs of CGP 31523A required to inhibit 90% (MIC90S) of the members of the family Enterobacteriaceae, Neisseria gonorrhoeae, and Streptococcus pneumoniae were less than or equal to 0.25 micrograms/ml. Of Staphylococcus aureus (excluding methicillin-resistant strains) and Haemophilus influenzae, 90% were susceptible to 0.5 micrograms/ml. Pseudomonas aeruginosa and Lancefield group D streptococci were resistant to CGP 31523A (MIC90, greater than or equal to 128 micrograms/ml). The activity against Bacteroides fragilis was modest (MIC90, 32 micrograms/ml). The susceptibility of known beta-lactamase-producing strains suggested that CGP 31523A was resistant to many beta-lactamases (but not those of Bacteroides fragilis). The serum protein binding of CGP 31523A was about 73%. The primary target site of CGP 31523A in Escherichia coli appeared to be penicillin-binding protein 3.
将新型氨噻唑基头孢菌素CGP 31523A的体外活性与头孢西丁、头孢呋辛、拉氧头孢、哌拉西林、环丙沙星及其他β-内酰胺类药物(如适用)针对533株近期临床分离菌和已知耐药菌株的活性进行了比较。抑制肠杆菌科、淋病奈瑟菌和肺炎链球菌90%菌株(MIC90)所需的CGP 31523A的最低抑菌浓度小于或等于0.25微克/毫升。金黄色葡萄球菌(不包括耐甲氧西林菌株)和流感嗜血杆菌中,90%对0.5微克/毫升的CGP 31523A敏感。铜绿假单胞菌和D组链球菌对CGP 31523A耐药(MIC90大于或等于128微克/毫升)。对脆弱拟杆菌的活性中等(MIC90为32微克/毫升)。对已知产β-内酰胺酶菌株的敏感性表明,CGP 31523A对多种β-内酰胺酶耐药(但对脆弱拟杆菌的β-内酰胺酶不耐药)。CGP 31523A的血清蛋白结合率约为73%。CGP 31523A在大肠杆菌中的主要靶点似乎是青霉素结合蛋白3。