Abstract: Aim To synthesize 4''-carbamate derivatives of erythromycin and test their antibacterial activities in vitro. Methods New erythromycin antibacterial agents containing 4''-carbamate group were designed and synthesized from azithromycin via protection, aminoformylation, amination and deprotection. Their antibacterial activities against Staphylococcus aureus strains were tested. Results Nine compounds were synthesized. Their structures were confirmed by MS, IR, ¹H NMR and ¹³C NMR, and the synthetic condition (reagent ratios) was exploited. Among them, compounds F-3 and F-4 showed strong antibacterial activities against Staphylococcus aureus. But, all compounds did not show bactericidal activity. Discussion The test results showed that piperidinyl or pyrrolidinyl group may be of benefit to enhancing antibacterial activities.

Key words: Erythromycin derivatives, Erythromycin derivatives, synthesis, synthesis, antibacterial activities, antibacterial activities