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大约50年前,Brotzu在沿撒丁海岸线的污水、污物中,首次发现了一种可产生头孢菌素的微生物Cephalosporinum acinonium,其可产生含头孢菌素C等抗生素的混合物.从那时起,通过对天然头孢菌素C的化学修饰(半合成)或利用全合成方法,相继合成了许多新型的头孢菌素.由于头孢菌素不易依照其结构一活性的关系进行分类,故通常按其在市场上出现的日期和抗菌特性以“世代”进行分类.部分不同世代的头孢菌素类抗生素及其体外抗菌活性如表1、2所示.
About 50 years ago, Brotzu first discovered Cephalosporinum acinonium, a cephalosporin-producing microorganism, that produces a mixture of antibiotics, including cephalosporin C, in sewage and soil along the Sardinian coastline. , Many new types of cephalosporins have been synthesized by chemical modification (semi-synthesis) of natural cephalosporins C or by total synthesis methods. Since cephalosporins are not easily classified according to their structure-activity relationship, The dates and antibacterial properties that appear on the market are categorized as “generations.” Some of the different generations of cephalosporins and their in vitro antibacterial activity are shown in Tables 1 and 2.