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:Ma, ST
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
出版年:2011
卷:46
期:7
页码:3105-3111
DOI:10.1016/j.ejmech.2011.04.004
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.
收录类别:SCOPUS;SCIE
WOS核心被引频次:12
Scopus被引频次:10
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-79957449856&doi=10.1016%2fj.ejmech.2011.04.004&partnerID=40&md5=174e70cf102422356c82c8b7d413e82b
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