Novel pleuromutilin derivatives conjugated with phenyl-sulfide and boron-containing moieties as potent antibacterial agents against antibiotic-resistant bacteria

文献类型： 外文期刊

第一作者： Luo, Xinyu

作者： Luo, Xinyu;Feng, Jing;Zhang, Jie;Yu, Hang;Han, Zunsheng;Zhu, Zihao;Liu, Bo;Wang, Yan;Zhang, Chi;Li, Tianlei;Zhang, Wenxuan;Wu, Song;Wu, Guangxu;Fu, Hengjian;Pan, Weidong;Nie, Wansen;Li, Beibei

作者机构：

关键词： Antimicrobial resistance; Pleuromutilin derivatives; Conjugated compounds; MRSA; Pleuromutilin-resistant strain

期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.0； 五年影响因子：6.1 ）

ISSN： 0223-5234

年卷期： 2024 年 277 卷

页码：

收录情况： SCI

摘要： In response to the escalating threat of microbial resistance, a series of novel pleuromutilin derivatives, conjugated with phenyl-sulfide and boron-containing moieties, were designed and synthesized. Most derivatives, especially 14b and 16b, demonstrated significant efficacy against Gram-positive bacteria, including multidrugresistant strains, as well as pleuromutilin-resistant strains. Compound 16b showed high stability in the liver microsomes of rats and humans, along with acceptable tolerance in vitro and in vivo. Additionally, compound 16b exhibited promising efficacy in MRSA-infected mouse models. Our data highlight the potential of conjugated pleuromutilin derivatives as valuable agents against drug-resistant bacteria.

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