R&D Center, J2H Biotech, Suwon, Gyeonggi-do, Republic of Korea.
Medicinal Chemistry, Institut Pasteur Korea, Seongnam, Gyeonggi-do, Republic of Korea.
J Enzyme Inhib Med Chem. 2021 Dec;36(1):462-468. doi: 10.1080/14756366.2020.1870456.
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.
为了开发丙型肝炎病毒（HCV）的独特小分子抑制剂，我们合成了噻吩脲（TU）衍生物，并对其抑制 HCV 进入的活性进行了筛选。其中，有七种 TU 化合物对基因型 1/2（EC<30nM）表现出良好的抗病毒活性，随后对它们进行了进一步研究；基于药理、代谢、药代动力学和安全性特征，选择 作为优化的先导化合物，作为 HCV 进入抑制剂。 具有有效的多基因型抗病毒活性。对接结果表明， 与 HCV E2 糖蛋白可能存在相互作用。这些结果表明， 可能成为开发 HCV 进入抑制剂的潜在候选药物。
