Synthesis and antibacterial activity of novel modified 5-O-mycaminose 14-membered ketolides.

Abstract 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.