文献类型： 外文期刊
作者： Zhou, Yuhang 1 ; Yi, Yunpeng 2 ; Wang, Jiangkun 3 ; Yang, Zheng 1 ; Liu, Qinqin 1 ; Pu, Wanxia 1 ; Shang, Ruofeng 1 ;
作者机构： 1.CAAS, Lanzhou Inst Husb & Pharmaceut Sci, Minist Agr & Rural Affairs, Key Lab New Anim Drug Project Gansu Prov,Key Lab, Lanzhou 730050, Peoples R China
2.Shandong Acad Agr Sci, Shandong Prov Anim & Poultry Green Hlth Prod Crea, Inst Poultry Sci, 202 Gongyebeilu, Jinan 250023, Shandong, Peoples R China
3.Lanzhou Univ, Sch Basic Med Sci, Lanzhou 730000, Peoples R China
关键词： Pleuromutilin derivatives; Synthesis; Antibacterial activity; In vivo efficacy; Molecular docking
期刊名称：EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：7.088； 五年影响因子：6.427 ）
ISSN： 0223-5234
年卷期： 2022 年 237 卷
页码：
收录情况： SCI
摘要： Novel pleuromutilin derivatives with 3,4-dihydropyrimidin and pyrimidine moieties were designed, synthesized, and evaluated for their antibacterial activities. Most of the synthesized derivatives, especially the compounds bearing the pyrimidine moieties, exhibited potent antibacterial activities against methicillin-resistant Staphylococcus aureus BNCC 337371 (MRSA-337371), Staphylococcus aureus ATCC 25923 (S. aureus-25923) and methicillin-resistant Staphylococcus epidermidis ATCC 51625 (MRSE-51625). Compounds 5a, 5g and 5h exerted the excellent antibacterial activities and selected to evaluate their bacterial killing kinetics. Compound 5h displayed the highest antibacterial activities with bacteriostatic activities against MRSA and further evaluated its efficacy in mouse systemic infection. The results showed that compound 5h exhibited potent in vivo antibacterial effects to significantly improve the survival rate of mice (ED50 = 16.14 mg/kg), reduce the bacterial load and alleviate the pathological changes in the lungs of the affected mice. Furthermore, molecular docking studies revealed that the selected compounds successfully localized in the pocket of 50S ribosomal subunit and the formed hydrogen bonds were the main interaction.
- 相关文献
作者其他论文 更多>>
-
Comparison of gut microbiota immunity and pathology in specific-pathogen-free chickens with glandular and muscular gastritis using different methods
作者：Yan, Zunxiang;Yang, Shifa;Lin, Shuqian;Zhao, Zengcheng;Liu, Yueyue;Yin, Bin;Yi, Yunpeng;Song, Shikai;Zhang, Rongling;Huang, Zhongli
关键词：glandular and muscular gastritis; SPF chicken; animal model; 16S rDNA; gut microbiome
-
GLORI for absolute quantification of transcriptome-wide m6A at single-base resolution
作者：Shen, Weiguo;Yi, Yunpeng;Hou, Yongkang;Hu, Yufei;Wang, Jing;Sun, Hanxiao;Liu, Cong;Lu, Bo;Peng, Jinying;Yi, Chengqi;Yi, Yunpeng;Xiao, Ye;Yi, Chengqi;Yi, Chengqi;Yi, Chengqi
关键词：
-
A rapid simultaneous detection of duck hepatitis A virus 3 and novel duck reovirus based on RPA CRISPR Cas12a/Cas13a
作者：Zhang, Qiaoli;Yu, Guanliu;Zhang, Kaini;Chen, Lei;Ding, Xinli;Sun, Wenbo;Li, Qingmei;Yi, Yunpeng;Wang, Jianhua;Pang, Xuehui
关键词：RPA-CRISPR Cas12a/Cas13a; Duck hepatitis a virus 3; Novel duck reovirus; Lateral flow assay
-
Safety and efficacy evaluation of halicin as an effective drug for inhibiting intestinal infections
作者：Zhang, Maolu;Han, Lianquan;Wang, Ruiming;Yang, Xiaohui;Zhang, Maolu;Lin, Shuqian;Zhang, Jiaming;Yi, Yunpeng;Liu, Shaoning;Yang, Xiuzhen
关键词：halicin; antimicrobial activities; ames test; safety evaluation; Clostridium perfringens
-
Design and Synthesis of Pleuromutilin Derivatives as Antibacterial Agents Using Quantitative Structure-Activity Relationship Model
作者：Zhang, Jiaming;Liu, Qinqin;Zhao, Haoxia;Li, Guiyu;Shang, Ruofeng;Zhang, Jiaming;Yi, Yunpeng
关键词：pleuromutilin; QSAR; synthesis; antimicrobial activity; molecular docking
-
The Effect of Polymer Blends on the In Vitro Release/Degradation and Pharmacokinetics of Moxidectin-Loaded PLGA Microspheres
作者：Zhang, Hongjuan;Yang, Zhen;Wu, Di;Hao, Baocheng;Liu, Yu;Wang, Xuehong;Pu, Wanxia;Yi, Yunpeng;Shang, Ruofeng;Wang, Shengyi;Yi, Yunpeng
关键词：PLGA microspheres; moxidectin; polymer blends; in vitro release; pharmacokinetics
-
Synthesis and evaluation of novel pleuromutilin derivatives targeting the 50S ribosomal subunit for antibacterial ability
作者：Liu, Qinqin;Zhang, Hongjuan;Wang, Panpan;Pu, Wanxia;Wang, Shengyi;Shang, Ruofeng;Yi, YunPeng
关键词：Pleuromutilin derivatives; Synthesis; Antibacterial activity; Toxicity
