【摘要】 通过将新霉胺、卡那霉素A、核糖霉素氨基选择性环氨基甲酸酯保护、羟基胺亲核开环,合成了一系列脲连接的新霉胺、卡那霉素A、核糖霉素羟基胺衍生物,并对它们的抗菌活性进行了体外活性筛选,结果表明衍生物没有明显的抗菌活性,因此脲连接的氨基糖苷-羟基胺结构不能增加氨基糖苷的抗菌活性。更多还原

【Abstract】 A series of urea-linked hydroxyl-alkylamine derivatives of aminoglycosides have been obtained by modification of neamine(1),kanamycin(2) and ribostamycin(3) at 1,6’ and 3" N-sites,respectively,through selective cyclization and nucleophilic ring-opening of cyclic carbamates.All the products showed no noticeable activity in the antibiotic test in vitro.The result suggests that the urea-linked hydroxyl-alkylamine derivatives of aminoglycosides may not be suitable structures for the enhancement of antibiotic activity.更多还原