Novel pyridinium cationic pleuromutilin analogues overcoming bacterial multidrug resistance
文献类型： 外文期刊
作者： Yi, Yunpeng 1 ; Zhang, Jiaming 1 ; Zuo, Jiakun 2 ; Zhang, Maolu 1 ; Yang, Shifa 1 ; Huang, Zhongli 1 ; Li, Guiyu 3 ; Shang, Ruofeng 4 ; Lin, Shuqian 1 ;
作者机构： 1.Shandong Acad Agr Sci, Inst Poultry Sci, Shandong Prov Anim & Poultry Green Hlth Prod Creat, Jinan 250100, Shandong, Peoples R China
2.Chinese Acad Agr Sci, Shanghai Vet Res Inst, Shanghai 200241, Peoples R China
3.Gansu Agr Univ, Coll Vet Med, Lanzhou 730070, Gansu, Peoples R China
4.CAAS, Minist Agr & Rural Affairs, Key Lab New Anim Drug Project, Gansu Prov Key Lab Vet Pharmaceut Dev,Lanzhou Inst, Lanzhou 730050, Gansu, Peoples R China
5.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; Antibacterial activity; Multi-drug resistant bacteria; Molecular docking
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 251 卷
页码：
收录情况： SCI
摘要： A series of pyridinium cation-substituted pleuromutilin analogues were designed, synthesized and evaluated for their antibacterial activities in vitro and in vivo. Most derivatives showed potent antibacterial activities, especially e4 that displayed the highest antibacterial activity against multi-drug resistant bacteria and was subjected to time-kill kinetics, resistance studies, cytotoxicity and molecular docking assays. Molecular docking results, scanning electron microscopy and o-nitrophenyl-beta-galactopyranoside tests showed that e4 not only inhibited bacterial protein synthesis but also disrupted bacterial cell walls. Compound e4 showed an ED50 of 5.68 mg/kg against multi-drug resistant Staphylococcus aureus in infected mice model. In in vivo and in vitro toxicity tests, e4 showed low toxic effects with an LD50 of 879 mg/kg to mice. These results suggest that compound e4 may be considered as a new therapeutic candidate for bacterial infections.
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