Design, Synthesis, Molecular Docking Analysis and Biological Evaluations of 4-[(Quinolin-4-yl)amino]benzamide Derivatives as Novel Anti-Influenza Virus Agents

In this study, a series of 4-[(quinolin-4-yl)amino]benzamide derivatives as the novel anti-influenza agents were designed and synthesized. Cytotoxicity assay, cytopathic effect assay and plaque inhibition assay were performed to evaluate the anti-influenza virus A/WSN/33 (H1N1) activity of the targe...

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Bibliographic Details
Published in:International journal of molecular sciences 2022-06, Vol.23 (11), p.6307
Main Authors: Zhang, Chao, Tang, Yun-Sang, Meng, Chu-Ren, Xu, Jing, Zhang, De-Liang, Wang, Jian, Huang, Er-Fang, Shaw, Pang-Chui, Hu, Chun
Format: Article
Language:English
Subjects:
Acids
Antiviral Agents - pharmacology
Assaying
Avian flu
Benzamide
Benzamides - pharmacology
Cytotoxicity
DNA Viruses
DNA-directed RNA polymerase
Drug resistance
Genomes
Hydrocarbons
Influenza A Virus, H1N1 Subtype
Influenza A Virus, H3N2 Subtype
Influenza B
Molecular docking
Molecular Docking Simulation
Pharmaceutical industry
Proteins
Ribonucleoproteins
RNA polymerase
Viral infections
Virus Replication
Viruses
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Summary:In this study, a series of 4-[(quinolin-4-yl)amino]benzamide derivatives as the novel anti-influenza agents were designed and synthesized. Cytotoxicity assay, cytopathic effect assay and plaque inhibition assay were performed to evaluate the anti-influenza virus A/WSN/33 (H1N1) activity of the target compounds. The target compound demonstrated significant anti-influenza virus A/WSN/33 (H1N1) activity both in cytopathic effect assay (EC = 11.38 ± 1.89 µM) and plaque inhibition assay (IC = 0.23 ± 0.15 µM). also exhibited significant anti-influenza virus activities against other three different influenza virus strains A/PR/8 (H1N1), A/HK/68 (H3N2) and influenza B virus. According to the result of ribonucleoprotein reconstitution assay, could interact well with ribonucleoprotein with an inhibition rate of 80.65% at 100 µM. Furthermore, exhibited significant activity target PA-PB1 subunit of RNA polymerase according to the PA-PB1 inhibitory activity prediction by the best pharmacophore Hypo1. In addition, was well drug-likeness based on the results of Lipinski's rule and ADMET prediction. All the results proved that 4-[(quinolin-4-yl)amino]benzamide derivatives could generate potential candidates in discovery of anti-influenza virus agents.
ISSN:1422-0067
1661-6596
1422-0067
DOI:10.3390/ijms23116307