7β-杂环酰胺基-3-杂环硫亚甲基头孢菌素衍生物的半合成及抗菌活性研究  

Studies on Semisynthesis and Antibacterial Activity of 7β-Heterocyclocamido-3-heterothiomethyl Cephalosporins

作　　者：惠新平[1] 郝兰[1] 张自义[1] 王勤[2] 王芳 管作武[3] 

机构地区：[1]兰州大学化学化工学院 [2]兰州大学生物系,兰州730000 [3]北京医科大学应用药物研究所,北京100083

出　　处：《高等学校化学学报》2000年第12期1844-1847,共4页Chemical Journal of Chinese Universities

摘　　要：通过 2 -取代 1 ,3 ,4 -二唑 -5-硫醇 1 a-1 f和头孢菌素母体 7-ACA反应 ,制得头孢菌素中间体 2 a_ 2 f,用氨噻唑肟活性酯 3和 1 -芳基 -5-甲基 -1 H-1 ,2 ,3 -三唑 -4 -甲酰氯 4 a_ 4 e分别和头孢菌素中间体缩合 ,制得头孢菌素新衍生物 5a_ 5b和 6a_ 6h.新化合物的结构经 1H NMR,IR及 MS确认 .初步体外抗菌结果表明 ,头孢菌素 5a_ 5b对革兰氏阳性和阴性菌有显著抑制活性 ,而 6a_New cephalosporin derivatives 5a_5b and 6a_6h were prepared by condensation of 2a_2f with aminothiazoleoxime active ester 3 and 1 aryl 5 methyl 1H 1,2,3 triazol 3 formyl chloride 4a_4e, respectively. The intermediate 2a_2f were synthesized by reaction of 2 substituted 1,3,4 oxadiazol 5 thiols 1a—1f with 7 ACA. The structures of the compounds synthesized were confirmed by IR, 1H NMR and MS spectra. The preliminary results of antibacterial activities revealed that 5a_5b showed significant antibacterial activities against both Gram positive and Gram negative bacteria, and 6a_6h had moderate antibacterial activities against these bacteria. [WT5HZ]

关 键 词：头孢菌素衍生物 半合成 抗菌活性 离心薄层层析 

分 类 号：TQ465.1[化学工程—制药化工] R978.11[医药卫生—药品]