【摘要】 制备5种氯霉素糖基化衍生物,并对这些衍生物的抑菌活性和安全性进行初步测试。实验结果表明:1)氯霉素被糖基化后水溶性得到了明显提高;2)氯霉素糖基化衍生物时未产生抗菌活性,但经相关糖苷酶水解后,可重新表现出抗菌活性;3)小鼠急毒试验证明,氯霉素糖基化衍生物的毒副作用与原药相比显著降低。该项研究对于设计和合成类氯霉素前药开辟了新领域。更多还原

【Abstract】 Five glycosylated chloramphenicol derivatives were synthesized in this study.Their antibacterial activities and safety were investigated.The results showed that: 1) The water-solubility of the glycosylated analogues were remarkably improved compared to the original chloramphenicol;2) Though the glycosylated derivatives showed no antibacterial activity,the antibacterial activity was observed when hydrolyzed by some corresponding specific glycosidase;3) The mouse acute toxicity test showed that the toxicity and the side effects were deeply reduced compared to the original chloramphenicol.This investigation may open a new field in the design and sythesis of shloramphenicol-like prodrugs.更多还原