Design, synthesis and antibacterial activity evaluation of pleuromutilin derivatives according to twin drug theory

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; twin drugs theory

期刊名称：JOURNAL OF ASIAN NATURAL PRODUCTS RESEARCH （ 影响因子：1.345； 五年影响因子：1.237 ）

ISSN： 1028-6020

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收录情况： SCI

摘要： A series of novel pleuromutilin derivatives were designed and synthesized based on the twin drugs theory. Piperazinyl and thioether were used as the linkage to connect the pleuromutilin nuclear and sulfonamide to improve the biological activity and water solubility of derivatives. The in vitro antibacterial activities against drug-sensitive and drug-resistance bacteria were evaluated by agar dilution method. Most of the 25 compounds displayed excellent antibacterial activities against drug-sensitive bacteria, particularly, five compounds (9, 10, 11, 14a and 14b) exerted the excellent antibacterial activities against drug-resistance bacteria.

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