Parallel synthesis of 5-cyano-6-aryl-2-thiouracil derivatives as inhibitors for hepatitis C viral NS5B RNA-dependent RNA polymerase

From random screening of our compound libraries, we identified a hit compound with an IC50 of 27 μM against hepatitis C viral NS5B RNA-dependent RNA polymerase. By using a parallel synthetic strategy, a series of its derivatives were synthesized. From their anti-HCV activity screening, compounds with single digital 3.8 micromolar activity were obtained.

Graphical abstractThrough the parallel synthetic strategy, 5-cyano-6-aryl-2-thiouracilderivatives with single digital micromolar inhibitory activity for the hepatitis C viral NS5B RNA-dependent RNA polymerase were obtained.Figure optionsDownload full-size imageDownload as PowerPoint slide