Structure-based design, synthesis and anti-influenza A virus activities of substituted phenyl-coupled heterocyclic ethylamide derivatives

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.

Keywords

Influenza virus A / Nucleoprotein inhibitor / Ingavirin / Nucleozin / Biological evaluation

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RIGHTS & PERMISSIONS

Jilin University, The Editorial Department of Chemical Research in Chinese Universities and Springer-Verlag GmbH