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.

Graphical abstractA novel series of macrolide derivatives with mono- or disaccharides substituted at the 4′′-O- position has been synthesized, and their in vitro antibacterial activities were tested.Figure optionsDownload full-size imageDownload as PowerPoint slide