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

doi:10.1007/s40242-015-5197-9

Chemical Research in Chinese Universities ›› 2015, Vol. 31 ›› Issue (6): 942-951.doi: 10.1007/s40242-015-5197-9

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

WANG Yang¹, LEI Fan², LI Xiaolong², HE Yi², LI Jue², QIU Rui², WU Xueying³, HAI Li², WU Yong²

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, Sichuan University, Chengdu 610041, P. R. China;
3. School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, P. R. China

Received:2015-05-15 Revised:2015-08-05 Online:2015-11-01 Published:2015-11-24
Contact: HAI Li, WU Yong E-mail:smile@scu.edu.cn;wyong@scu.edu.cn

Abstract

Abstract:

A series of new substituted phenyl-coupled heterocyclic ethylamide derivatives was designed and synthesized 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 influenza A via viral nucleoprotein.

Key words: Influenza virus A, Nucleoprotein inhibitor, Ingavirin, Nucleozin, Biological evaluation

WANG Yang, LEI Fan, LI Xiaolong, HE Yi, LI Jue, QIU Rui, WU Xueying, HAI Li, WU Yong. Structure-based Design, Synthesis and Anti-influenza A Virus Activities of Substituted Phenyl-coupled Heterocyclic Ethylamide Derivatives[J]. Chemical Research in Chinese Universities, 2015, 31(6): 942-951.

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

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