Synthesis and Antibacterial Activity of Novel Pleuromutilin Derivatives

文献类型： 外文期刊

第一作者： Liu, Huixian

作者： Liu, Huixian;Xiao, Sui;Zhang, Lifang;Wang, Xiaoyang;Xue, Feiqun;Zhang, Depeng;Mu, Shuhua

作者机构：

关键词： pleuromutilin;antibacterial activity;design;synthesis;Gram positive

期刊名称：BIOLOGICAL & PHARMACEUTICAL BULLETIN （ 影响因子：2.233； 五年影响因子：2.309 ）

ISSN：

年卷期：

页码：

收录情况： SCI

摘要： In this study we describe the design, synthesis, and antibacterial activity of novel pleuromutilin analogs. A series of new compounds containing piperazine and alkylamino or arylamino groups was synthesized. The new compounds were characterized via H-1-NMR, C-13-NMR, Fourier transform (FT)-IR and MS, and were further evaluated for their in vitro activity against seven Gram-positive, and one Gram-negative, pathogens. Antibacterial data revealed that all compounds exhibited moderate to good antibacterial activities against sensitive Gram-positive pathogens. Specifically, 9d displayed the best activity: its activity to Staphylococcus aureus (ATCC25923) is 0.125 mu g/mL, which is equal to the control compound tiamulin. The antibacterial activities of 9d to Streptococcus sins (minimum inhibitory concentration (MIC) of 2 mu g/mL), Streptococcus agalactiae (MIC of 0.5 mu g/mL), and Streptococcus dysgalactiae (MIC of 0.5 mu g/mL) were also excellent compared with the control drug erythromycin (MIC of >128 mu g/mL). The binding modes of these compounds with active sites were calculated using the programs of Molecular Operating Environment (MOE) and Pymol.

分类号： R9

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