一种新头孢类化合物的合成与生物活性  

Synthesis and Bioactivity of a New Cephalosporins Compound

作　　者：林辉 傅海燕 关晴 刁富城 Lin Hui;Fu Haiyan;Guan Qing;Diao Fucheng(Guangzhou Baiyunshan Pharmaceutical Holdings Co.,Ltd.,Baiyunshan Chemical Pharmaceutical Factory,Guangzhou 510515,China)

机构地区：[1]广州白云山医药集团股份有限公司白云山化学制药厂,广东广州510515

出　　处：《广东化工》2023年第21期26-29,共4页Guangdong Chemical Industry

基　　金：广东省重点领域研发计划项目(2022B1111070004)。

摘　　要：头孢类抗生素是一类广谱半合成抗生素,具有抗菌作用强、临床疗效高、耐青霉素酶、毒性低、过敏反应较青霉素少等特点,目前已有近70个品种在临床广泛应用。本文介绍了一种以7-氨基-3-乙烯基头孢烷酸和AE-活性酯为起始物料,经缩合、脱色、成盐、精制步骤,得到新头孢类化合物[6R-[6a,7ß(Z)]]-3-乙烯基-7-[[(2-氨基-4-噻唑基)(甲氧亚氨基)乙酰基]氨基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸,初步抗菌活性测试显示了良好的抑菌活性。Cephalosporin antibiotics are a kind of broad-spectrum semi-synthetic antibiotics,which have the characteristics of strong antibacterial effect,high clinical efficacy,penicillinase resistance,low toxicity and less allergic reaction than penicillin.At present,nearly 70 varieties have been widely used in clinical practice.In this paper,a new cephalosporin compound(Z)-7-(2-(2-aminothiazol-4-yl)-2-(methoxyimino)acetamido)-8-oxo-3-vinyl-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid was obtained by condensation reaction,decolorization,salify and refining steps by using 7-amino-3-vinylcephalosporanic acid and thiobenzothiazole ester as starting materials.The preliminary antibacterial activity test showed good antibacterial activity.

关 键 词：头孢菌素 7-氨基-3-乙烯基头孢烷酸 生物活性 合成 AE-活性酯 

分 类 号：O65[理学—分析化学]