White A R, Cooper C E, Griffin K E, Slocombe B
J Antimicrob Chemother. 1986 Sep;18(3):335-43. doi: 10.1093/jac/18.3.335.
The antibacterial activity of pure resolved R and S epimers of temocillin was determined in a variety of in-vitro test systems, including those that allowed measurement of activity during the early period following exposure to the agents, thus minimising the effect of epimerization. In conventional agar- and broth-dilution susceptibility tests involving incubation at 37 degrees C for 18 h, little difference was evident between the activities of the individual epimers. In contrast, in other tests of antibacterial activity, such as time-kill and turbidimetric studies, the R epimer and temocillin (R/S mixture 1.8:1.0) were shown to be more rapidly bactericidal than the S epimer. Overall, the R epimer and temocillin (R/S) exhibited a similar degree of bactericidal activity in vitro.
在多种体外测试系统中测定了替莫西林纯拆分的R和S差向异构体的抗菌活性,包括那些能够在接触药物后的早期阶段测量活性的系统,从而将差向异构化的影响降至最低。在常规的琼脂稀释和肉汤稀释药敏试验中,于37℃孵育18小时,各差向异构体的活性之间几乎没有明显差异。相比之下,在其他抗菌活性测试中,如时间杀菌和比浊法研究,R差向异构体和替莫西林(R/S混合物1.8:1.0)显示出比S差向异构体更快速的杀菌作用。总体而言,R差向异构体和替莫西林(R/S)在体外表现出相似程度的杀菌活性。