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7-(4,7-二取代香豆素-3-乙酰氨基)头孢菌素的合成
引用本文:范华娟,段廷汉,李明华,.7-(4,7-二取代香豆素-3-乙酰氨基)头孢菌素的合成[J].药学学报,1989,24(3):175-181.
作者姓名:范华娟  段廷汉  李明华  
作者单位:中国药科大学制药化学教研室,中国药科大学制药化学教研室,中国药科大学制药化学教研室 南京 210009 南京医学院化学教研室,南京 210009,南京 210009
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。

关 键 词:7-(4  7-二取代香豆素-3-乙酰氨基)头孢菌素  酰氯  Vilsmeier试剂  混合酐  抗菌活性
收稿时间:1988-02-21

Synthesis of 7-(4,7-di-substituted coumarin-3-acetamido)cephalosporins
HJ Fan,TH Duan and MH Li.Synthesis of 7-(4,7-di-substituted coumarin-3-acetamido)cephalosporins[J].Acta Pharmaceutica Sinica,1989,24(3):175-181.
Authors:HJ Fan  TH Duan and MH Li
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.
Keywords:7-(4  7-Di-substituted coumarin-3-acetamido)cephalosporins  Acid chloride  Vilsmeier reagent  Mixed anhydride  Antibiotic activity
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