摘要
(6S)或(7S)-甲氧基-β-内酰胺类抗生素具有良好的耐酶作用。目前已有多个品种上市,例如:头孢西丁、头孢美唑、拉氧头孢和替莫西林。其(6S)或(7S)-甲氧基造成的空间位阻是该类药物耐酶的关键所在。这种空间位阻作用使得其自身的结构对β-内酰胺酶稳定,从而解决或减少了大量使用β-内酰胺类抗生素而引起的细菌耐药性问题。化学合成这类药物可根据甲氧基取代C-6位氢原子的方法不同分为直接法和间接法。
（6S）- or （7S）-methoxyl- β -lactams are a group of compounds with a strong 3 -lactamase-resistant action. A number of them have been in clinical use, such as cefoxitin, cefmetazole, latamoxef, flomoxef and temocillin. The steric hinderance effect that is enhanced by introducing （6S）- or （7S）-methoxy into the β -lactam ring significantly increases the stability of β -lactam antibiotics against β -lactomase, and to some extent reduces the problems of bacterial drugresistance. The synthetic routes of such antibiotics, according to the ways employed to replace C6-hydragen with methoxy, mainly includes direct method and indirect method.
出处
《国外医药（抗生素分册）》
CAS
2007年第6期252-258,276,共8页
World Notes on Antibiotics
