Synthesis and antibacterial activity of novel C12 vinyl ketolides.

摘要: A novel series of C12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and vivo potency against key respiratory pathogens. The modification involves replacing the natural methyl group core with a via chemical synthesis. From macrolide core, ketolides was prepared. Several compounds were found to be potent macrolide-sensitive -resistant bacteria. 6j 6k showed similar antimicrobial spectrum comparable activity commercial ketolide telithromycin. However, pharmacokinetic profiles rats differ from that telithromycin by having higher lung-to-plasma ratios, larger volumes distribution, longer half-lives. These differences pharmacodynamic effect as both exhibited better efficacy than rat lung infection models Streptococcus pneumoniae Haemop...