Chemical Synthesis and Biological Activities of Novel Pleuromutilin Derivatives with Substituted Amino Moiety

文献类型: 外文期刊

第一作者: Shang, Ruofeng

作者: Shang, Ruofeng;Yi, Yunpeng;Guo, Wenzhu;YuLiu;Liang, Jianping;Wang, Shengyu;Xu, Ximing

作者机构:

期刊名称:PLOS ONE ( 影响因子:3.24; 五年影响因子:3.788 )

ISSN: 1932-6203

年卷期: 2013 年 8 卷 12 期

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收录情况: SCI

摘要: Novel pleuromutilin derivatives designed based on the structure of valnemulin were synthesized and evaluated for their in vitro antibacterial activities. These pleuromutilin derivatives with substituted amino moiety exhibited excellent activities against methicillin-resistant Staphylococcus aureus, methicillin-resistant Staphylococcus epidermidis, Escherichia coli, and Streptococcus agalactiae. Compound 5b showed the highest antibacterial activities and even exceeded tiamulin. Moreover, the docking experiments provided information about the binding model between the synthesized compounds and peptidyl transferase center (PTC) of 23S rRNA.

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