【摘要】 本文根据构效关系,设计并合成了17个7-(4,7-二取代香豆素-3-乙酰氨基)头孢菌素衍生物。其缩合方法采用酰氯法、Vilsmeier试剂法及混合酐法。初步体外抑菌试验表明,化合物对革兰氏阳性菌和少数革兰氏阴性菌有较强的抗菌作用。进一步药理试验尚在进行。更多还原

【Abstract】 Seventeen derivatives of 7-(4,7-di-substituted conmarin-3-acetamido)cephalosporins were synthesized with acid chloride method, Vilsmeier reagent method and mixed anhydride method. Isolation and purification were fulfilled with Sephadex LH-20 column chromatography and centrifugal-TLC technique. Their chemical structures were identified by elemental analysis, IR and ~1HNMR spectrum. The preliminary antibacterial activity tests showed that these cephalosporin derivatiyes exhibited good activity against Gram-positive bacteria and individual Gramnegative bacteria. Further experiments in pharmacology will be made.更多还原