Structure-based Design, Synthesis and Anti-influenza A Virus Activities of Substituted Phenyl-coupled Heterocyclic Ethylamide Derivatives  

作　　者：WANG Yang LEI Fan LI Xiaolong HE Yi LI Jue QIU Rui WU Xueying HAI Li WU Yong 

机构地区：[1]Department of Pathology, The First Affiliate Hospital, College of Medicine, Zhejiang University, Hangzhou 310003, P. R. China [2]Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Siehuan University, Chengdu 610041, P. R. China [3]School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

出　　处：《Chemical Research in Chinese Universities》2015年第6期942-951,共10页高等学校化学研究（英文版）

摘　　要：A series of new substituted phenyl-coupled heterocyclic ethylamide derivatives was designed and synthe- sized as anti-influenza agents. In vitro anti-influenza A（A/PR/8/34 H1N1 strain） activities of these compounds were investigated and compared to those of the commercial antiviral drugs（Arbidol and Ribavirin） against the influenza. Specifically, among these twelve compounds exhibiting moderate levels of antiviral activity against influenza A, compounds 30c and 30d are the most effective ones, and as efficacious as the positive control Ribavirin and much more effective than Ingavirin and Arbidol, indicating that they are prospective candidates for further exploration. These results are also consistent with the docking study results in terms of the design of compounds targeting in- fluenza A via viral nucleoprotein.A series of new substituted phenyl-coupled heterocyclic ethylamide derivatives was designed and synthe- sized as anti-influenza agents. In vitro anti-influenza A（A/PR/8/34 H1N1 strain） activities of these compounds were investigated and compared to those of the commercial antiviral drugs（Arbidol and Ribavirin） against the influenza. Specifically, among these twelve compounds exhibiting moderate levels of antiviral activity against influenza A, compounds 30c and 30d are the most effective ones, and as efficacious as the positive control Ribavirin and much more effective than Ingavirin and Arbidol, indicating that they are prospective candidates for further exploration. These results are also consistent with the docking study results in terms of the design of compounds targeting in- fluenza A via viral nucleoprotein.

关 键 词：Influenza virus A Nucleoprotein inhibitor Ingavirin Nucleozin Biological evaluation 

分 类 号：S855.3[农业科学—临床兽医学] TQ463.6[农业科学—兽医学]