Kesado T, Watanabe K, Asahi Y, Isono M, Ueno K
Antimicrob Agents Chemother. 1984 Jan;25(1):131-3. doi: 10.1128/AAC.25.1.131.
The in vitro antibacterial activities of the newly developed 7 alpha-methoxy cephalosporins and 7 beta-methoxyiminoacetamido cephalosporins against 67 clinical isolates of Bacteroides fragilis and their resistance to the hydrolytic action of a beta-lactamase produced by B. fragilis were simultaneously compared. The minimal inhibitory concentrations that inhibited 90% of the 7 alpha-methoxy cephalosporins, cefoxitin, cefmetazole, moxalactam, and cefotetan, against the isolates were 4, 8, 8, and 16 micrograms/ml, respectively, and these antibiotics were entirely resistant to hydrolysis by beta-lactamases (0.10 mumol/h per mg of protein) of the isolates. By contrast, 7 beta-methoxyiminoacetamido cephalosporins represented by cefotaxime, ceftizoxime, and cefmenoxime were not effective, as indicated by the minimal inhibitory concentrations that inhibited 90%, 64, 32, and 128 micrograms/ml, respectively. Their antibacterial activities clearly corresponded to their resistance to the hydrolytic action of the beta-lactamase: namely, the correlation coefficients in regression curves of cefotaxime, ceftizoxime, and cefmenoxime, which were expressed by the antibacterial activity (x axis) and the beta-lactamase activity (y axis) were 0.098, 0.034, and 0.163, respectively.
同时比较了新开发的7α-甲氧基头孢菌素和7β-甲氧基亚氨基乙酰氨基头孢菌素对67株脆弱拟杆菌临床分离株的体外抗菌活性及其对脆弱拟杆菌产生的β-内酰胺酶水解作用的抗性。7α-甲氧基头孢菌素、头孢西丁、头孢美唑、拉氧头孢和头孢替坦对这些分离株的最低抑菌浓度(抑制90%菌株生长的浓度)分别为4、8、8和16微克/毫升,并且这些抗生素对分离株的β-内酰胺酶(0.10微摩尔/小时·毫克蛋白)完全耐药。相比之下,以头孢噻肟、头孢唑肟和头孢甲肟为代表的7β-甲氧基亚氨基乙酰氨基头孢菌素无效,其抑制90%菌株生长的最低抑菌浓度分别为64、32和128微克/毫升。它们的抗菌活性与其对β-内酰胺酶水解作用的抗性明显相关:即,以抗菌活性(x轴)和β-内酰胺酶活性(y轴)表示的头孢噻肟、头孢唑肟和头孢甲肟回归曲线的相关系数分别为0.098、0.034和0.163。