数字农科院2.0

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

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

作者机构:

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

期刊名称: European Journal of Medicinal Chemistry

ISSN: 0223-5234

年卷期: 2024 年 277 卷

页码:

收录情况: SCIE(2024版)

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 multidrug-resistant 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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