一类具有 4''-O-糖基取代基的新型大环内酯衍生物。
A new series of macrolide derivatives with 4''-O-saccharide substituents.
机构信息
Key Laboratory of Bioactivity Substance and Resources Utilization of Chinese Herbal Medicine, Ministry of Education Institute of Materia Medica, Peking Union Medica College & Chinese Academy of Medical Sciences, Beijing 100050, PR China.
出版信息
Bioorg Med Chem Lett. 2010 Sep 15;20(18):5527-31. doi: 10.1016/j.bmcl.2010.07.072. Epub 2010 Jul 21.
A series of novel derivatives of macrolide with 4''-O-mono- or disaccharides were synthesized. The corresponding glycosyl trichloroacetimidates were used as the donors in the glycosylations. The in vitro antibacterial activities of 7a-f and 13-16 against a panel of susceptible and resistant pathogens were tested. The modification of 4''-O-mono- or disaccharides may lead to the understanding of interaction of the macrolide and the bacterial ribosome.
合成了一系列新型的 4''-O-单糖或二糖的大环内酯衍生物。相应的糖基三氯乙酰亚胺酯被用作糖苷化反应的供体。对 7a-f 和 13-16 对一系列敏感和耐药病原体的体外抗菌活性进行了测试。4''-O-单糖或二糖的修饰可能有助于理解大环内酯与细菌核糖体的相互作用。
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