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Discovery of pyridine formyl hydrazide derivatives as potent non-nucleoside RSV polymerase inhibitors. 期刊论文

编号：

E881EBAF2CADD8D068A939B6426C1757
作者：

Li Xin^[0] Wu Jinyuan^[0] Zheng Lin^[0] Tao Sining^[0] Jin Wenjing^[0] Zhao Xiaolei^[3] De Jonghe Steven^[4] Persoons Leentje^[4] Daelemans Dirk^[4] Liu Xinyong^[0] Fu Yuanhui^[3] Kang Dongwei^[0] Gao Ni^[0,7]
地址：

(Li Xin)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China.,(Wu Jinyuan)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China.,(Zheng Lin)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China.,(Tao Sining)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China.,(Jin Wenjing)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China.,(Zhao Xiaolei)College of Life Sciences and Bioengineering, Beijing Jiaotong University, Beijing, PR China.,(De Jonghe Steven)KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Molecular Genetics and Therapeutics in Virology and Oncology Research Group, Herestraat 49, box 1048, Leuven, 3000, Belgium.,(Persoons Leentje)KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Molecular Genetics and Therapeutics in Virology and Oncology Research Group, Herestraat 49, box 1048, Leuven, 3000, Belgium.,(Daelemans Dirk)KU Leuven, Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, Molecular Genetics and Therapeutics in Virology and Oncology Research Group, Herestraat 49, box 1048, Leuven, 3000, Belgium.,(Liu Xinyong)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China.,(Fu Yuanhui)College of Life Sciences and Bioengineering, Beijing Jiaotong University, Beijing, PR China.,(Kang Dongwei)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China. Electronic address: kangdongwei@126.com.,(Gao Ni)Department of Medicinal Chemistry, Shandong Key Laboratory of Druggability Optimization and Evaluation for Lead Compounds, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 Culture Road, Jinan, Shandong, 250012, PR China; Department of Pediatrics, Qilu Hospital, Cheeloo College of Medicine, Shandong University, Jinan, Shandong Province, 250012, PR China.
语种：

英文
期刊：

European journal of medicinal chemistry ISSN：1768-3254 2026 年 319 卷 (119256 - ) ; 2026-Aug-21
收录：
摘要：

Respiratory syncytial virus (RSV) is an RNA virus that infects both the upper and lower respiratory tract and is recognized as a major respiratory health threat. In this study, guided by the cryo-EM structure of the MRK-1-RSV polymerase complex, the substituent region at the C4 position of the shared pyridine core was redesigned. A series of 32 pyridine carbohydrazide derivatives bearing structurally diverse N-substituted amino groups was synthesized to explore the structure-activity relationship and substituent tolerance of the adjacent pocket region. LX1 was selected as a representative compound for further investigation and exhibited potent activity against RSV-A Long strain, with an EC50 value of 37 nM. Minigenome assays showed that LX1 reduces polymerase-dependent reporter activity, consistent with inhibiting RSV RNA synthesis. Furthermore, molecular dynamics simulations revealed that LX1 forms stable hydrogen bonds and π-π stacking interactions with key amino acids in the PRNTase domain. Collectively, LX1 represents a promising lead compound for the further development of novel RSV inhibitors.;
推荐引用方式
GB/T 7714：

Li Xin,Wu Jinyuan,Zheng Lin, et al. Discovery of pyridine formyl hydrazide derivatives as potent non-nucleoside RSV polymerase inhibitors. [J].European journal of medicinal chemistry,2026,319:119256-.
APA：

Li Xin,Wu Jinyuan,Zheng Lin,Tao Sining,&Gao Ni.(2026).Discovery of pyridine formyl hydrazide derivatives as potent non-nucleoside RSV polymerase inhibitors. .European journal of medicinal chemistry,319:119256-.
MLA：

Li Xin, et al. "Discovery of pyridine formyl hydrazide derivatives as potent non-nucleoside RSV polymerase inhibitors." .European journal of medicinal chemistry 319(2026):119256-.
入库时间：

8/31/2026 10:35:32 AM
更新时间：

8/31/2026 10:35:32 AM

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