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Thiophen urea derivatives as a new class of hepatitis C virus entry inhibitorsopen access
- Authors
- Ryu, Hyung Chul; Windisch, Marc; Lim, Jee Woong; Choi, Inhee; Lee, Eun Kyu; Yoo, Hye Hyun; Kim, Tae Kon
- Issue Date
- Jan-2021
- Publisher
- Taylor & Francis
- Keywords
- Entry inhibitor; hepatitis C virus; small molecule; thiophen urea
- Citation
- Journal of Enzyme Inhibition and Medicinal Chemistry, v.36, no.1, pp 462 - 468
- Pages
- 7
- Indexed
- SCIE
SCOPUS
- Journal Title
- Journal of Enzyme Inhibition and Medicinal Chemistry
- Volume
- 36
- Number
- 1
- Start Page
- 462
- End Page
- 468
- ISSN
- 1475-6366
1475-6374
- 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 < 30nM) 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.
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Related Researcher
- Yoo, Hye Hyun
- COLLEGE OF PHARMACY (DEPARTMENT OF PHARMACY)