标题：Synthesis and antibacterial activity of novel 11,12-cyclic carbonate azithromycin 4\'\'-O-carbamate derivatives.
作者：Ma C;Liu Z;Song H;Jiang R;He F;Ma S
作者机构：[Ma, C] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, China;[ Liu, Z 更多
通讯作者地址：[Ma, ST]Shandong Univ, Dept Med Chem, Sch Pharmaceut Sci, 44 W Culture Rd, Jinan 250012, Peoples R China.
来源：The Journal of Antibiotics: An International Journal
关键词：antibacterial activity; 4 ''-O-carbamate derivatives; macrolides;; resistance; synthesis
摘要：A series of novel 11,12-cyclic carbonate azithromycin 4\'\'-O-carbamate derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. Compounds 7b and 7d were the most effective (0.5 and 0.5 microg ml(-1)) against two strains of erythromycin-resistant Streptococcus pneumoniae whose resistance was encoded by the erm gene and the erm and mef genes, respectively. Compounds 7a, 7e and 7g showed significantly potent activity against erythromycin-susceptible strains such as Staphylococcus aureus and S. pyogenes. These results suggest that the introduction of the prolonged arylalkylcarbamoyl group to the C-4\'\' position can dramatically enhance the activity against erythromycin-resistant bacteria encoded by the erm gene or the erm and mef genes.