Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors
- Title
- Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitors
- Author
- 유혜현
- Keywords
- Entry inhibitor; hepatitis C virus; small molecule; thiophen urea
- Issue Date
- 2021-01
- Publisher
- TAYLOR & FRANCIS LTD
- Citation
- JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v. 36, Issue. 1, Page. 462-468
- 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.
- URI
- https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7822064/https://repository.hanyang.ac.kr/handle/20.500.11754/167034
- DOI
- 10.1080/14756366.2020.1870456
- Appears in Collections:
- COLLEGE OF PHARMACY[E](약학대학) > PHARMACY(약학과) > Articles
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