Synthesis and evaluation of novel pleuromutilin derivatives targeting the 50S ribosomal subunit for antibacterial ability
文献类型： 外文期刊
作者： Liu, Qinqin 1 ; Zhang, Hongjuan 1 ; Yi, YunPeng 2 ; Wang, Panpan 1 ; Pu, Wanxia 1 ; Wang, Shengyi 1 ; Shang, Ruofeng 1 ;
作者机构： 1.CAAS, Minist Agr & Rural Affairs, Key Lab New Anim Drug Project, Gansu Prov Key Lab Vet Pharmaceut Dev,Lanzhou Inst, Lanzhou 730050, Peoples R China
2.Shandong Acad Agr Sci, Inst Poultry Sci, Shandong Prov Anim & Poultry Green Hlth Prod Creat, 202 Gongyebeilu, Jinan 250023, Shandong, Peoples R China
关键词： Pleuromutilin derivatives; Synthesis; Antibacterial activity; Toxicity
期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：6.7； 五年影响因子：6.5 ）
ISSN： 0223-5234
年卷期： 2023 年 262 卷
页码：
收录情况： SCI
摘要： Multidrug-resistant bacteria, particularly methicillin-resistant Staphylococcus aureus, have become a major global public health concern. Therefore, developing new antibiotics that do not possess cross-resistance for the currently available antibiotics is critical. Herein, we synthesized a novel class of pleuromutilin derivatives containing substituted triazine with improved antibacterial activity. Among these derivatives, 6d, which contains 4-dimethylamino-1,3,5-triazine in the side chain of pleuromutilin, exhibited highly promising antimicrobial activity and mitigated antibiotic resistance. The high antibacterial potency of 6d was further supported by docking model analysis and green fluorescent protein inhibition assay. Additionally, cytotoxicity and acute oral toxicity evaluation and in vivo mouse systemic infection experiments revealed that 6d possessed tolerable toxicity and promising therapeutic efficacy.
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