反式头孢丙烯；_酶法合成；(分离纯化与化学合成)

反式头孢丙烯的酶法合成及其体外抗菌活性

http://www.100md.com 《中国抗生素杂志》 2007年第1期

反式头孢丙烯；,酶法合成；,7苯乙酰氨基3E丙烯基3头孢菌素4羧酸(反式GPRA)；,7氨基3E丙烯基3头孢菌素4羧酸(反式APRA)；,青霉素酰化酶(IPA750)；,抗菌活性,,反式头孢丙烯；,酶法合成；,7苯乙酰氨基3E丙烯基3头孢菌素4

     摘要：以7苯乙酰氨基3E丙烯基3头孢菌素4羧酸(反式GPRA)为原料，在青霉素酰化酶作用下，首先酶法水解得到3E丙烯基3头孢菌素4羧酸(反式APRA)，过滤固相酶，滤液调pH分离得到反式APRA固体；在青霉素酰化酶作用下，反式APRA再与对羟基苯甘氨酸乙二醇酯缩合，得到反式头孢丙烯；酶法合成所得的产品与进口反式头孢丙烯对照品一致。初步体外抗菌试验表明，反式头孢丙烯对金葡菌和大肠埃希菌的体外抗菌活性比临床用头孢丙烯(顺式900%，反式9%)弱。

    关键词：反式头孢丙烯；酶法合成； 7苯乙酰氨基3E丙烯基3头孢菌素4羧酸(反式GPRA)； 7氨基3E丙烯基3头孢菌素4羧酸(反式APRA)；青霉素酰化酶(IPA750)；抗菌活性

    Enzymatic synthesis and in vitro antibacterial activity of transcefprozil

    Feng Shengxi, Liang Shizhong and Yutaka Kameyama

    (School of Biological Science & Biotechnology, South China University of Technology, Guangzhou 510641;Guangzhou Baiyunshan Pharmaceutical Co., Ltd., Guangzhou Baiyunshan Chemical Pharmaceutical Factory, Guangzhou 510515;Otsuka Chemical Co., Ltd., Osaka 5400021)

    ABSTRACT Immobilized penicillin acylase (from E.coli) was used to catalyze 7phenylacetamido3Epropenylcephalosporanic acid (transGPRA) hydrolyzation into 7amino3Epropenylcephalosporanic acid (transAPRA). Then, transAPRA was acylated with hydroxyethyl ester of 4hydroxyDphenylglycine (HPGHE) to obtain transcefprozil. The activities of transcefprozil and cefprozil (cis 90%, trans 9%) against Staphylococcus aureus and Escherichia coli were tested. Transcefprozil showed less activity than cefprozil. ......

百拇医药网 http://www.100md.com/html/DirDu/2007/04/28/42/82/83.htm

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