标题：Synthesis and antibacterial activity of novel 4\'\'-O-benzimidazolyl clarithromycin derivatives.
作者：Cong C;Wang H;Hu Y;Liu C;Li X;Cao J;Ma S
作者机构：[Cong, C] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, China;[ Wang 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：European Journal of Medicinal Chemistry: Chimie Therapeutique
关键词：Benzimidazolyl derivatives; Clarithromycin; Synthesis; Antibacterial; activity
摘要：Novel 4\'\'-O-benzimidazolyl clarithromycin derivatives were designed, synthesized and evaluated for their in vitro antibacterial activities. These benzimidazolyl derivatives exhibited excellent activity against erythromycin-susceptible strains better than the references, and some of them showed greatly improved activity against erythromycin-resistant strains. Compounds 16 and 17, which have the terminal 2-(4-methylphenyl)benzimidazolyl and 2-(2-methoxyphenyl)benzimidazolyl groups on the C-4\'\' bishydrazide side chains, were the most active against erythromycin-resistant Staphylococcus pneumoniae expressing the erm gene and the mef gene. In addition, compound 17 exhibited the highest activity against erythromycin-susceptible S. pneumoniae ATCC49619 and Staphylococcus aureus ATCC25923 as well. It is worth noting that the 4\'\'-O-(2-aryl)benzimidazolyl derivatives show higher activity against erythromycin-susceptible and erythromycin-resistant strains than the 4\'\'-O-(2-alkyl)benzimidazolyl derivatives.