论文部分内容阅读
如同β-内酰胺类抗生素结构改造的一般程序一样,本文作者从6-APA出发把6-APAC-3位上的羧基由醋酸基取代;C-6侧链由溴或氢取代,合成了几种简单的青霉素化合物。有些有一定的抗枯草杆菌作用。结构改造实验表明:青霉素C-3位和头孢菌素C-4位有一个酸性基团对保持生物学活性是必不可少的。青霉素酸和它的6-溴代衍生物的砜类衍生物有β-内酰胺酶抑制剂的性质的报道引
Like the general procedure for the structural transformation of the beta-lactam antibiotics, the authors de- tailed to replace the carboxyl group at the 6-APAC-3 position with acetate by 6-APA; the C-6 side chain was replaced by bromine or hydrogen to synthesize several A simple penicillin compound. Some have a certain anti-Bacillus role. Structural modification experiments show that: penicillin C-3 position and cephalosporin C-4 has an acidic group to maintain the biological activity is essential. The properties of β-lactamase inhibitors for penicillinic acid and its sulfone derivatives of 6-bromo derivatives have been reported