Synthesis and antibacterial activity of 11,12-cyclic carbonate 4″-O-aralkylacetylhydrazineacyl azithromycin derivatives

Abstract Two series of novel 4″-O-aralkylacetylhydrazineacyl azithromycin derivatives were synthesized and evaluated for their in vitro antibacterial activities. Among them, compound B4, B5, B13 and B18 were found to display significantly improved activity than control drugs (MIC > 128 μg/mL) against methicillin-resistant strain S. aureus ATCC 43,300 with an MIC value 2–4 μg/mL. Remarkably, compound B5 and B13 showed potent activity against penicillin-resistant S. aureus ATCC31007 (MIC = 4 μg/mL) and methicillin-resistant S. aureus ATCC 43,300 (MIC = 2 μg/mL).