头孢菌素药物发展和头孢洛扎工艺开发历程

Development of cephalosporin drugs and process of ceftolozane

在过去的50年里,全球批准上市50多种头孢菌素药物,几乎占所有批准的抗菌药物的一半。主要阐述了抗菌药物研发面临的问题和抗菌药物研发进展,并回顾了头孢菌素合成路线变更历程和头孢菌素药物历史发展过程。头孢洛扎是一种头孢菌素类肠外抗生素。其硫酸盐分子式为C_(23)H_(31)N_(12)O_(8)S_(2)^(+)·HSO_(4)^(–)。与头孢菌素类的其他成员一样,头孢洛扎是通过抑制青霉素结合蛋白(PBPs)发挥杀菌作用,从而抑制细胞壁合成,随后细胞死亡。

In the past 50 years,more than fifty cephalosporin drugs have been approved worldwide,accounting for almost half of all approved antimicrobial drugs.This paper mainly expounded the problems and progress of antibacterial drug research and development,reviewed the change process of cephalosporin synthesis route and the historical development process of cephalosporin drug.Cefolozane is a parenteral antibiotic of the cephalosporin class.Ceftolozane sulfate molecular formula is C_(23)H_(31)N_(12)O_(8)S_(2)^(+)·HSO_(4)^(-).Like other members of cephalosporins,it plays a bactericidal role by inhibiting penicillin binding protein(PBPs),thereby inhibiting cell wall synthesis,and then cell death.