Cargando…

RETRACTED ARTICLE: Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors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(50) < 30 nM) and subsequently,...

Descripción completa

Detalles Bibliográficos
Autores principales: Ryu, Hyung Chul, Windisch, Marc, Lim, Jee Woong, Choi, Inhee, Lee, Eun Kyu, Yoo, Hye Hyun, Kim, Tae Kon
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7822064/
https://www.ncbi.nlm.nih.gov/pubmed/33455472
http://dx.doi.org/10.1080/14756366.2020.1870456
Descripción
Sumario: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(50) < 30 nM) and subsequently, they were further investigated; based on the pharmacological, metabolic, pharmacokinetic, and safety profiles, J2H-1701 was selected as the optimised lead compound as an HCV entry inhibitor. J2H-1701 possesses effective multi-genotypic antiviral activity. The docking results suggested the potential interaction of J2H-1701 with the HCV E2 glycoprotein. These results suggest that J2H-1701 can be a potential candidate drug for the development of HCV entry inhibitors.