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
Hauptverfasser: Ryu, Hyung Chul, Windisch, Marc, Lim, Jee Woong, Choi, Inhee, Lee, Eun Kyu, Yoo, Hye Hyun, Kim, Tae Kon
Format: Artikel
Sprache:eng
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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.
ISSN:1475-6374
DOI:10.1080/14756366.2020.1870456