Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
Bioorg Med Chem Lett. 2013 Sep 15;23(18):5057-60. doi: 10.1016/j.bmcl.2013.07.042. Epub 2013 Jul 25.
A series of 11,12-cyclic carbonate azithromycin-4″-O-carbamoyl glycosyl derivatives were designed, synthesized, and evaluated as antibacterial agents to search for target compounds with excellent activity. The results of preliminary antibacterial tests against eight strains in vitro revealed that all of the title compounds exhibited improved activities with broad spectrum compared with the parent compound. The glycosylated side chains may be the pharmacophores responsible for the improved activity.
设计、合成并评价了一系列 11,12-环碳酸酯阿奇霉素-4″-O-氨甲酰基糖苷衍生物，作为抗菌剂来寻找具有优异活性的目标化合物。体外对 8 株菌的初步抗菌试验结果表明，与母体化合物相比，所有标题化合物均表现出广谱活性提高。糖基化侧链可能是提高活性的药效团。
