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Synthesis and antibacterial activities of heterocyclic ring-fused 20 (S)-protopanaxadiol derivatives

文献类型：期刊论文

作者Zhang, De-Jie5; Yuan, Zi-Qi4,6; Yue, Yan-Xin5; Zhang, Min3; Wu, Wen-Juan3; Yang, Cai-Guang1,2,4,6; Qiu, Wen-Wei5
刊名BIOORGANIC & MEDICINAL CHEMISTRY
出版日期2024-10-01
卷号112页码:17
关键词PPD Heterocycle Multidrug-resistant S. aureus Antibacterial agent
ISSN号0968-0896
DOI10.1016/j.bmc.2024.117901
通讯作者Yang, Cai-Guang(yangcg@simm.ac.cn) ; Qiu, Wen-Wei(wwqiu@chem.ecnu.edu.cn)
英文摘要Multidrug-resistant (MDR) bacterial infections are becoming a life-threatening issue in public health; therefore, it is urgent to develop novel antibacterial agents for treating infections caused by MDR bacteria. The 20(S)-protopanaxadiol (PPD) derivative 9 was identified as a novel antibacterial hit compound in screening of our small synthetic natural product-like (NPL) library. A series of novel PPD derivatives with heterocyclic rings fused at the C-2 and C-3 positions of the A-ring were synthesized and their antibacterial activities against Staphylococcus aureus (S. aureus) Newman strain and MDR S. aureus strains (USA300, NRS-1, NRS-70, NRS-100, NRS-108, NRS271, XJ017, and XJ036) were evaluated. Among these compounds, quinoxaline derivative 56 (SH617) exhibited the highest activity with MICs of 0.5-4 mu g/mL against the S. aureus Newman strain and the eight MDR S. aureus strains. Its antibacterial activity was comparable to that of the positive control, vancomycin. In the zebrafish, 56 revealed no obvious toxicity even at a high administered dose. In vivo, following a lethal infection induced by USA300 strains in zebrafish, 56 exhibited significantly increased survival rates in a dose-dependent manner.
WOS关键词STAPHYLOCOCCUS-AUREUS ; BIOLOGICAL EVALUATION ; 20(S)-PROTOPANAXADIOL ; INHIBITORS ; ANALOGS
资助项目National Natural Science Foundation of China[22077035] ; National Natural Science Foundation of China[22037007] ; National Natural Science Foundation of China[81861138046]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry
语种英语
WOS记录号WOS:001306427700001
出版者PERGAMON-ELSEVIER SCIENCE LTD
源URL[http://119.78.100.183/handle/2S10ELR8/313095]  
专题新药研究国家重点实验室
通讯作者Yang, Cai-Guang; Qiu, Wen-Wei
作者单位1.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Peoples R China
2.Univ Chinese Acad Sci, Hangzhou Inst Adv Study, Sch Pharmaceut Sci & Technol, Hangzhou 310024, Peoples R China
3.Tongji Univ, Sch Med, Shanghai East Hosp, Dept Lab Med, Shanghai 200123, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Chem Biol, Shanghai 201203, Peoples R China
5.East China Normal Univ, Shanghai Engn Res Ctr Mol Therapeut & New Drug Dev, Sch Chem & Mol Engn, Shanghai 200062, Peoples R China
6.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Zhang, De-Jie,Yuan, Zi-Qi,Yue, Yan-Xin,et al. Synthesis and antibacterial activities of heterocyclic ring-fused 20 (S)-protopanaxadiol derivatives[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2024,112:17.
APA Zhang, De-Jie.,Yuan, Zi-Qi.,Yue, Yan-Xin.,Zhang, Min.,Wu, Wen-Juan.,...&Qiu, Wen-Wei.(2024).Synthesis and antibacterial activities of heterocyclic ring-fused 20 (S)-protopanaxadiol derivatives.BIOORGANIC & MEDICINAL CHEMISTRY,112,17.
MLA Zhang, De-Jie,et al."Synthesis and antibacterial activities of heterocyclic ring-fused 20 (S)-protopanaxadiol derivatives".BIOORGANIC & MEDICINAL CHEMISTRY 112(2024):17.

入库方式： OAI收割

来源：上海药物研究所

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