Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors
To develop unique small-molecule inhibitors of hepatitis C virus (HCV), thiophen urea (TU) derivatives were synthesised and screened for HCV entry inhibitory activities. Among them, seven TU compounds exhibited portent anti-viral activities against genotypes 1/2 (EC < 30 nM) and subsequently, the...
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Veröffentlicht in: | Journal of enzyme inhibition and medicinal chemistry 2021-12, Vol.36 (1), p.462-468 |
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Hauptverfasser: | , , , , , , |
Format: | Artikel |
Sprache: | eng |
Online-Zugang: | Volltext |
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Zusammenfassung: | To develop unique small-molecule inhibitors of hepatitis C virus (HCV), thiophen urea (TU) derivatives were synthesised and screened for HCV entry inhibitory activities. Among them, seven TU compounds exhibited portent anti-viral activities against genotypes 1/2 (EC
< 30 nM) and subsequently, they were further investigated; based on the pharmacological, metabolic, pharmacokinetic, and safety profiles,
was selected as the optimised lead compound as an HCV entry inhibitor.
possesses effective multi-genotypic antiviral activity. The docking results suggested the potential interaction of
with the HCV E2 glycoprotein. These results suggest that
can be a potential candidate drug for the development of HCV entry inhibitors. |
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ISSN: | 1475-6374 |
DOI: | 10.1080/14756366.2020.1870456 |