反式头孢丙烯的酶法合成及其体外抗菌活性
反式头孢丙烯;,酶法合成;,7苯乙酰氨基3E丙烯基3头孢菌素4羧酸(反式GPRA);,7氨基3E丙烯基3头孢菌素4羧酸(反式APRA);,青霉素酰化酶(IPA750);,抗菌活性,,反式头孢丙烯;,酶法合成;,7苯乙酰氨基3E丙烯基3头孢菌素4
摘要: 以7苯乙酰氨基3E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3E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900%,反式9%)弱。关键词: 反式头孢丙烯; 酶法合成; 7苯乙酰氨基3E丙烯基3头孢菌素4羧酸(反式GPRA); 7氨基3E丙烯基3头孢菌素4羧酸(反式APRA); 青霉素酰化酶(IPA750); 抗菌活性
Enzymatic synthesis and in vitro antibacterial activity of transcefprozil
Feng Shengxi, Liang Shizhong 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 5400021)
ABSTRACT Immobilized penicillin acylase (from E.coli) was used to catalyze 7phenylacetamido3Epropenylcephalosporanic acid (transGPRA) hydrolyzation into 7amino3Epropenylcephalosporanic acid (transAPRA). Then, transAPRA was acylated with hydroxyethyl ester of 4hydroxyDphenylglycine (HPGHE) to obtain transcefprozil. The activities of transcefprozil and cefprozil (cis 90%, trans 9%) against Staphylococcus aureus and Escherichia coli were tested. Transcefprozil showed less activity than cefprozil. ......
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