Design, synthesis and antibacterial activities of pleuromutilin derivatives

文献类型： 外文期刊

第一作者： Liu, Hui-Xian

作者： Liu, Hui-Xian;Ma, Dong-Lai;Cui, Ge;Zhang, Yue;Xue, Fei-Qun

作者机构：

关键词： Pleuromutilin derivatives; antibacterial activity; design; synthesis; Gram-positive bacteria

期刊名称：JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH （ 影响因子：1.569； 五年影响因子：1.598 ）

ISSN： 1028-6020

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页码：

收录情况： SCI

摘要： We described the design, synthesis and antimicrobial activities of novel pleuromutilin derivatives with substituted piperazine substrate. Minimum inhibitory concentration (MIC) was used to evaluate the activity of the derivatives against six bacteria in vitro, and compound 8 was potent against Staphylococcus aureus and Staphylococcus epidermidis with the MIC value of 0.0625 mu g/ml. 10a and 10 b showed similar activity to positive control drugs (tiamulin, erythromycin) against S. aureus with the MIC value of 0.125 mu g/ml. The binding mode of compound 8 and tiamulin to the ribosome pocket showed the correlation between binding parameters and the antibacterial activity, and more bonds and stronger combination could effectively enhance the activity of compounds.

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