标题:Synthesis and antibacterial evaluation of novel 11,4″-disubstituted azithromycin analogs with greatly improved activity against erythromycin- resistant bacteria
作者:Li X.; Ma S.; Yan M.; Wang Y.; Ma S.
作者机构:[Li, X] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, China;[ Ma, S] 更多
通讯作者:Ma, S(mashutao@sdu.edu.cn)
通讯作者地址:[Ma, S] Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44, West Culture Road, Jinan 250012, China;
来源:European Journal of Medicinal Chemistry
出版年:2013
卷:59
页码:209-217
DOI:10.1016/j.ejmech.2012.11.028
关键词:11,4″-disubstituted azithromycin analogs; Antibacterial activity; Erythromycin-resistant bacteria; Synthesis
摘要:A series of novel 11,4″-disubstituted azithromycin analogs were synthesized and evaluated for their antibacterial activity. All the 11,4″-disubstituted analogs exhibited excellent activity (0.03-0.12 μg/ml) against erythromycin-susceptible Streptococcus pneumoniae, and significantly improved activity against three phenotypes of erythromycin- resistant S. pneumoniae compared with erythromycin A, clarithromycin or azithromycin. Among them, compounds 26-28 showed the most potent activity (0.25, 0.03 and 2 μg/ml) against S. pneumoniae expressing the erm gene, the mef gene and the erm and mef genes, respectively. In addition, compound 28 was the most effective (0.03 and 0.12 μg/ml) against erythromycin-susceptible S. pneumoniae and Staphylococcus aureus as well. It is noteworthy that the most active compounds described above possess the same terminal 3,5-dinitrophenyl groups on their C-4″ bisamide side chains.© 2012 Elsevier Masson SAS. All rights reserved.
收录类别:SCOPUS
Scopus被引频次:11
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84870698464&doi=10.1016%2fj.ejmech.2012.11.028&partnerID=40&md5=ad6c379cf6fbd83f0dcde0565dfce014
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