Synthesis and antibacterial activity of novel 3-O-descladinosylazithromycin derivatives.

摘要: Abstract Novel series of novel 3- O -arylalkylcarbamoyl descladinosylazithromycin derivatives with the 2′- -acetyl and 11,12-cyclic carbonate groups, group 11- side chain, were designed, synthesized evaluated for their antibacterial activity using broth microdilution method. The results showed that majority target compounds moderate to favorable against six kinds susceptible strains almost all them displayed significantly improved compared references three erythromycin-resistant S. pneumoniae B1 expressing erm B gene, AB11 mef A genes, S. pyogenes R1. In particular, compound 6h exhibited most potent B. subtilis ATCC9372 (0.5 μg/mL), penicillin-resistant S. epidermidis (0.125 μg/mL), (1 μg/mL) (1 μg/mL), which 2-, 256-, 256-fold better than azithromycin, respectively. Additionally, 6f (0.5 μg/mL) 6g (0.25 μg/mL) active A22072, 8- 16-fold azithromycin (4 μg/mL). As R1, 5a presented excellent (8 μg/mL), showing 32- 32-fold higher (256 μg/mL) clarithromycin (256 μg/mL).