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六十年代中期,随着各种青霉素和头孢菌素的广泛使用,部分细菌因产生一系列β-内酰胺酶而产生耐药性,包括对青霉素酶较稳定的甲氧苯青霉素、异(口恶)唑青霉素类药物。这一问题引起了广泛重视。目前,研究对β-内酰胺酶有高度稳定性的青霉素、头孢菌素类药物仍是一项重大的课题,在这方面取得较大进展的是1970年头霉素的发现。头霉素族是7α-甲氧基头孢菌素化合物。7α-甲氧基的引入增加了头孢菌素类化合物对β-内酰胺酶的稳定性,为化学合成耐β-内酰胺酶药物指出了方向,临床使用的头孢西丁(cefoxitin,1)就是个成功的例子。
In the mid-1960s, with the widespread use of various penicillins and cephalosporins, some bacteria became resistant to a series of β-lactamase enzymes, including methicillin, which is more stable against penicillinase, Evil) carbapenem drugs. This issue has drawn wide attention. At present, the study of penicillins and cephalosporins with high stability to β-lactamase remains a major issue. The great progress made in this regard is the discovery of the 1970 cephamycin. The family of cephamycins is a 7α-methoxycephalosporin compound. The introduction of 7α-methoxy increased the stability of β-lactamases by cephalosporins and pointed out the direction for the chemical synthesis of β-lactamase-resistant drugs. Cefoxitin (1) in clinical use is A successful example.