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一、抗菌活性第一个四环素类抗生素(金霉素)是1944年分离得到。以后又发现了几个四环素同类物:土霉素(1950年)、盐酸四环素(1953年)及去甲金霉素。五十年代后期,在四环素结构上去掉6-羟基,得到了6-脱氧四环素,其细菌学及药代动力学性质有明显的改变。六十年代又出现了“第二代”或长效四环素。强力霉素是1962年得到,二甲胺四环素是1967年引入。所有的四环素均抑制细菌蛋白质合成,但短效和长效四环素的固有抗菌活性,有明显的差别。
First, antibacterial activity The first tetracycline antibiotic (chlortetracycline) was isolated in 1944. Later found several similar tetracycline substances: oxytetracycline (1950), tetracycline hydrochloride (1953) and naringin. In the late fifties, the 6-hydroxy group was removed from the tetracycline structure and the 6-deoxytetracycline was obtained. The bacteriological and pharmacokinetic properties were significantly changed. Sixty time there have been “second generation” or long-acting tetracycline. Doxycycline was obtained in 1962 and minocycline was introduced in 1967. All tetracyclines inhibit bacterial protein synthesis, but the short-acting and long-acting tetracycline inherent antibacterial activity, there are significant differences.