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自1929年Fleming发现青霉素至今已有五十年了。众所周知,用发酵法首先得到青霉素类(1),其次是头孢菌素类(2)和甲氧头孢菌素类(3)。由R,X取代基的改造,已制得很多良好的抗生素。此外,还有一类由合成得到的具全新骨架的β-内酰胺抗菌药物,最近已发现了一些有价值的化合物,即类似于1的青霉烷衍生物(4),类似于2的头孢烯衍生物(5),还有具4与5混合形式的青霉烯衍生物(6)。其中A、B是表示改变环内原子和原子团所进行的改造,如图1。
It has been 50 years since Fleming discovered penicillin in 1929. It is well known that penicillins (1) are first obtained by fermentation, followed by cephalosporins (2) and cephalosporins (3). By R, X substituent transformation, has made a lot of good antibiotics. In addition, there is a class of newly synthesized β-lactam antibiotics with novel backbones. Some valuable compounds have recently been identified, namely the penicillamine derivative (4) analogous to 1, a cephem like 2 Derivative (5), and penem derivative (4) in a mixed form of 4 and 5 (6). Where A, B is said to change the ring atoms and atomic groups carried out by the transformation, as shown in Figure 1.