摘要
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.
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。
基金
National Basic Research Program(973 Program Grant No.2004CB518904)
