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

Structure-based Design, Synthesis and Anti-influenza A Virus Activities of Substituted Phenyl-coupled Heterocyclic Ethylamide Derivatives
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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.
出处 《Chemical Research in Chinese Universities》 SCIE CAS CSCD 2015年第6期942-951,共10页 高等学校化学研究(英文版)
关键词 Influenza virus A Nucleoprotein inhibitor Ingavirin Nucleozin Biological evaluation Influenza virus A Nucleoprotein inhibitor Ingavirin Nucleozin Biological evaluation
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