Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 218, Issue -, Pages -Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2021.113395
Keywords
Flavonoid-triazolyl hybrids; Anti-HCV activity; HCV entry Inhibitors
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Funding
- China Natural Science Foundation [81872766]
- Key R&D projects of Liaoning Province, China [2020JH2/10300058]
- Young and Middle-aged Science and Technology Innovative Talent Support Program of Shenyang City [RC180250]
- Research Program on Hepatitis from the Japan Agency for Medical Research and Development [20fk0210053j0002]
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A series of flavonoid-triazolyl hybrids were synthesized and evaluated as novel inhibitors of hepatitis C virus (HCV). Among these compounds, 10m and 10r showed the most potent anti-HCV activity by significantly inhibiting viral entry. These results suggest further effective application of 10m and 10r as potential HCV preventive agents.
A series of flavonoid-triazolyl hybrids were synthesized and evaluated as novel inhibitors of hepatitis C virus (HCV). The results of anti-HCV activity assays showed that most of the synthesized derivatives at a concentration of 100 mu g/mL inhibited the generation of progeny virus. Among these derivatives, 10m and 10r exhibited the most potent anti-HCV activity and inhibited the production of HCV in a dose-dependent manner. Interestingly, 10m and 10r had no significant inhibitory effect on viral translation or replication. Additional action mechanism studies revealed that the most potent compounds, 10m and 10r, significantly inhibited viral entry to 34.0% and 52.0%, respectively, at 10 mu M. These results suggest further effective application of 10m and 10r as potential HCV preventive agents. (c) 2021 Elsevier Masson SAS. All rights reserved.
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