| 新型头孢菌素的合成和抑菌试验 |
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| 引用本文： | 孙快麟,李润荪.新型头孢菌素的合成和抑菌试验[J].药学学报,1988,23(11):825-829. |
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| 作者姓名： | 孙快麟 李润荪 |
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| 作者单位： | 上海医药工业研究院
(孙快麟)，上海医药工业研究院(李润荪) |
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| 摘 要： | 从7-氨基头孢烷酸(7 ACA)和7-氨基-3-去乙酰氧基头孢烷酸(7 ADCA)合成了六个7-取代连氮基头孢菌素和六个7α-甲氧基-7β-取代腙基头孢菌素,体外抑菌试验表明大部分化合物的抑菌活性较弱。
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| 关 键 词： | 7-取代连氮基头孢菌素 7α-甲氧基-7β-取代腙基头孢菌素 |
| 收稿时间： | 1987-10-22 |
SYNTHESIS AND ANTIMICROBIAL TEST OF SOME NEW CEPHALOSPORINS |
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| KL Sun and RS Li.SYNTHESIS AND ANTIMICROBIAL TEST OF SOME NEW CEPHALOSPORINS[J].Acta Pharmaceutica Sinica,1988,23(11):825-829. |
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| Authors: | KL Sun and RS Li |
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| Abstract: | Six new 7-substituted-azino-cephalosporins and six new 7α-methoxy-Tβ-substituted-hydrazono-cephalosporins were synthesized from 7ACA and 7ADCA. A new method of introducing 7α-methoxy in this type of cephalosporin was developed. While an electrophilic centre was formed at C7 position of 7-substituted-azino-cephalosporins with the help of nitro and conjugated chain, in the presence of p-TsOH in MeOH, methoxy was introduced into C-7α position easily due to steric effect. All compounds were subjected to antimicrobial test in vitro, Ⅱa～Ⅵa and Ⅱb～Ⅵb showed weak activity against Gram positive bacteria. The MIC of cephalosporins with a 7α-methoxy group is lower than cephalosporins without the 7α-methoxy group. |
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| Keywords: | 7α-Methoxy-7β-substituted-hydrazono-cephalosporins 7-Substituted-azino-cephalosporins |
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