State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Department of Medicinal Chemistry, Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Sciences, Beijing 100050, PR China.
Eur J Med Chem. 2013 Nov;69:174-81. doi: 10.1016/j.ejmech.2013.08.023. Epub 2013 Aug 23.
A practicable method of introducing a side chain to the C-4' position of 5-O-desosamine in the 14-membered ketolides was developed. And using this method, a series of novel modified 5-O-mycaminose ketolides were synthesized. These ketolides containing 5-O-4'-carbamate mycaminose were evaluated for their in vitro antibacterial activities against some respiratory pathogens. 15b and 18e showed comparable activity to telithromycin and clarithromycin.
开发了一种在 14 元酮内酯的 5-O-去氧氨基糖的 C-4'位引入侧链的可行方法。并且使用这种方法，合成了一系列新型的修饰的 5-O-胞嘧啶酮内酯。这些含有 5-O-4'-氨基甲酸酯胞嘧啶的酮内酯被评估了对一些呼吸道病原体的体外抗菌活性。15b 和 18e 与泰利霉素和克拉霉素具有相当的活性。
