标题：Synthesis and antibacterial activity of novel 4\'\'-O-arylalkylcarbamoyl and 4\'\'-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives.
作者：Ju Y;Xian R;Zhang L;Ma R;Cao J;Ma S
作者机构：[Ju, Y] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan, 250012, China;[ Xian, 更多
通讯作者地址：[Ma, ST]Shandong Univ, Sch Pharmaceut Sci, Dept Med Chem, 44 W Culture Rd, Jinan 250012, Peoples R China.
来源：Bioorganic and Medicinal Chemistry Letters
关键词：Clarithromycin derivatives; Synthesis; Antibacterial activity; Bacterial; resistance
摘要：Novel series of novel 4\'\'-O-arylalkylcarbamoyl and 4\'\'-O-((arylalkylamino)-4-oxo-butyl)carbamoyl clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. These derivatives retained excellent activity against the erythromycin-susceptible strains and showed significantly improved activity against all of the tested erythromycin-resistant strains. Among them, compound 4c was the most effective (0.06 microg/mL) against Streptococcus pneumonia encoded by the erm gene and compound 4a was had the most potent activity (0.25 microg/mL) against S. pneumonia encoded by the erm and mef genes.