Cavalleri B, Malabarba A, Berti M, Arioli V
Farmaco Sci. 1978 Jul;33(7):496-509. doi: 10.1002/chin.197849355.
The synthesis and the physicochemical properties of some cephalosporin derivatives with a carbonylamino- or acetylaminoimidazole moiety in position 7 are described. The effects on biological activity of the presence of some groups (methyl or ethyl, 2-nitro or 5-nitro, 2-amino) on the imidazole nucleus are examined. Selected heterocyclicthiomethyl substituents were also introduced in the 3 position of the cephalosporin nucleus. The in vitro antimicrobial activities of the compounds and their effectiveness in protecting against bacterial (S. aureus) infections in mice were evaluated. Two of the compounds (V b) and (V d) are as active as cephalexin and more active than cephalothin when administered subcutaneously, while they appear to be less effective when administered orally.
描述了一些在7位带有羰基氨基或乙酰氨基咪唑部分的头孢菌素衍生物的合成及其物理化学性质。研究了咪唑核上某些基团（甲基或乙基、2-硝基或5-硝基、2-氨基）的存在对生物活性的影响。还在头孢菌素核的3位引入了选定的杂环硫甲基取代基。评估了这些化合物的体外抗菌活性及其在小鼠中预防细菌（金黄色葡萄球菌）感染的有效性。其中两种化合物（V b）和（V d）皮下给药时与头孢氨苄活性相当，且比头孢噻吩活性更强，而口服给药时似乎效果较差。
