A new series of macrolide derivatives with 4''-O-saccharide substituents.
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.
Xu
Peng
P
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.
Chen
Xiao-zhuo
XZ
Liu
Lu
L
Jin
Zhi-ping
ZP
Lei
Ping-sheng
PS
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D024881:Drug Resistance, Bacterial; D006031:Glycosylation; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D016908:Gram-Positive Bacterial Infections / Q000188:drug therapy; D006801:Humans; D018942:Macrolides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects; D013291:Streptococcus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D018942:Macrolides