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一、前言众所周知,所谓半合成青霉素和头孢菌素指的是相应于天然β-内酰胺,如青霉素G和头孢菌素C的化学衍生物,因为它们颇为有效,副作用又少,在感染疾病的治疗上起着重要作用。最近由于发现了所谓非典型的β-内酰胺抗生素,诸如克拉维酸、Thienamycin和单环菌素,它们有着很特殊的生物学性质,β-内酰胺类抗生素的研究又掀起了一个新高潮。直至20世纪70年代初,为了得到生物学性能更好的β-内酰胺抗生素,大多数是在青霉素或头孢菌素母体化合物的侧链上进行化学修饰。当1974年我们开始研究β-内酰胺时,核的类型甚少。我们认为侧链的修饰已快要过时,应当去探索核修饰的可能性。因为关于β-内酰胺抗生素作用机理和构效关系的研究
I. Preface As we all know, the so-called semisynthetic penicillins and cephalosporins refer to chemical derivatives corresponding to natural beta-lactams such as penicillin G and cephalosporin C because they are quite effective and have few side effects. In infectious diseases The treatment plays an important role. Recently, the discovery of so-called atypical beta-lactam antibiotics, such as clavulanic acid, Thienamycin and monocyclostin, have very special biological properties and a new upsurge of research on beta-lactam antibiotics has started. Until the early 1970s, chemical modifications were mostly performed on the side chains of penicillins or cephalosporin compounds in order to obtain better biologically-active beta-lactam antibiotics. When we started the study of beta-lactam in 1974, there were very few types of nuclei. We think the modification of the side chain is almost out of date and the possibility of nuclear modification should be explored. Because of β-lactam antibiotics on the mechanism of action and structure-activity relationship studies