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作者试验了600余个头孢菌素C类化合物的体外抗结核菌H_(37)Rv的作用,并详细列表探讨其中作用较好化合物的结构与抗菌作用关系。在7-位上具有吡啶硫基或吡啶氨基取代的乙酰氨基侧链者都具有良好作用。吡啶环氮的位置在4-位上效果最好,cephapirin(Ⅰ)比3-位及2-位同系物强4~6倍。吡啶环经N-甲基化后效果增强,BL-S217和226(Ⅱ,Ⅲ)的最低抑菌浓度(MIC)比未甲基化者强2~10
The author tested more than 600 cephalosporin C compounds in vitro anti-tuberculosis H_ (37) Rv role, and a detailed list to explore where the role of better compounds structure and antibacterial effect relationship. Acetylamino side-chains with pyridylthio or pyridylamino groups in the 7-position all have a good effect. The position of the pyridine ring nitrogen is most effective at the 4-position, and cephapirin (I) is 4 to 6-fold stronger than the 3- and 2-position homologues. The effect of N-methylation of pyridine ring was enhanced. The minimum inhibitory concentration (MIC) of BL-S217 and 226 (Ⅱ, Ⅲ) was 2 to 10 stronger than that of unmethylated