Synthesis and antibacterial evaluation of novel pleuromutilin derivatives

文献类型: 外文期刊

第一作者: Shang, Ruofeng

作者: Shang, Ruofeng;Liu, Yu;Guo, Wenzhu;Guo, Zhiting;Hao, Baocheng;Liang Jianping;Xin, Zhijun

作者机构:

关键词: Acylation reaction;Antibacterial activity;Antibiotics;Pleuromutilin derivative;Synthesis

期刊名称:EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY ( 影响因子:6.514; 五年影响因子:6.099 )

ISSN:

年卷期:

页码:

收录情况: SCI

摘要: A series of novel pleuromutilin derivatives possessing thioether moiety has been synthesized via acylation reaction under mild conditions. Their in vitro antibacterial activity against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae were tested by agar dilution method and Oxford cup assay. Among the 17 compounds screened, 14-O-[(4-methoxybenzamide-2- methylpropane-2-yl) thioacetate] mutilin 4i, 14-O-[(2-aminobenzamide-2- methylpropane-2-yl) thioacetate] mutilin 5a and 14-O-[(4-aminobenzamide-2- methylpropane-2-yl) thioacetate] mutilin 5c were resulted as most active antibacterial agents.

分类号: R9

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