Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors.
J Enzyme Inhib Med Chem
; 36(1): 462-468, 2021 Dec.
Article
in En
| MEDLINE
| ID: mdl-33455472
ABSTRACT
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 (EC50 < 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.
Key words
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Thiophenes
/
Urea
/
Hepacivirus
Language:
En
Journal:
J Enzyme Inhib Med Chem
Year:
2021
Document type:
Article