Activity of the cefotaxime (HR756) desacetyl metabolite compared with those of cefotaxime and other cephalosporins
Activity of the cefotaxime (HR756) desacetyl metabolite compared with those of cefotaxime and other cephalosporins
复制标题
头孢噻肟 (HR756) 去乙酰代谢物的活性与头孢噻肟和其他头孢菌素的活性相比
DOI：
10.1128/aac.17.1.84
复制
发表时间：
1980
影响因子：
4.9
通讯作者：
K. Bedford
中科院分区：
文献类型：
--
作者：
R. Wise;P. J. Wills;J. Andrews;K. Bedford
头孢噻肟（HR 756）的脱乙酰代谢物（DES）在体内形成的程度很大。DES，母体化合物，头孢唑啉，头孢西丁，头孢呋辛的体外活性进行了比较，对70个细菌分离株。发现DES对常见肠杆菌科的活性约为母体化合物的1/10，但比其他三种测试化合物的活性略高。DES对铜绿假单胞菌没有有效的活性，对金黄色葡萄球菌或脆弱拟杆菌的活性低于头孢噻肟或头孢西丁。由于DES可在肾衰竭中蓄积或在胆道中浓缩，因此其抗菌活性可能具有相当大的临床意义。
The desacetyl metabolite (DES) of cefotaxime (HR756) is formed in vivo to a significant extent. The in vitro activities of DES, the parent compound, and cefazolin, cefoxitin, and cefuroxime were compared against 70 bacterial isolates. DES was found to possess approximately 1/10th the activity of the parent compound against the common Enterobacteriaceae, but was somewhat more active than the other three compounds tested. DES had no useful activity against Pseudomonas aeruginosa and was less active than cefotaxime or cefoxitin against Staphylococcus aureus or Bacteroides fragilis. Because DES may accumulate in renal failure or be concentrated in the biliary tract, its antimicrobial activity may have considerable clinical significance.