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： Luo, Xinyu 1 ; Wu, Guangxu 2 ; Feng, Jing 1 ; Zhang, Jie 1 ; Fu, Hengjian 2 ; Yu, Hang 1 ; Han, Zunsheng 1 ; Nie, Wansen 3 ; Zhu, Zihao 1 ; Liu, Bo 1 ; Pan, Weidong 2 ; Li, Beibei 3 ; Wang, Yan 1 ; Zhang, Chi 1 ; Li, Tianlei 1 ; Zhang, Wenxuan 1 ; Wu, Song 1 ;
作者机构： 1.Chinese Acad Med Sci & Peking Union Med Coll, Inst Mat Med, Dept New Drug Res & Dev, State Key Lab Bioact Subst & Funct Nat Med, Beijing 100050, Peoples R China
2.Guizhou Med Univ, State Key Lab Funct & Applicat Med Plants, Guiyang 550014, Peoples R China
3.Chinese Acad Agr Sci, Shanghai Vet Res Inst, Shanghai 200241, Peoples R China
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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