Non-nucleoside inhibitors of the hepatitis C virus NS5B RNA-dependant RNA polymerase: 2-Aryl-3-heteroaryl-1,3-thiazolidin-4-one derivatives

Hepatitis C virus (HCV) NS5B RNA polymerase is crucial for replicating the HCV RNA genome and is an attractive target for developing anti-HCV drugs. A novel series of 2,3-diaryl-1,3-thiazolidin-4-one derivatives were evaluated for their ability to inhibit HCV NS5B. Of this series, compounds 4c, 5b, 5c and 6 emerged as more potent, displaying over 95% inhibition of NS5B RNA polymerase activity in vitro. The two most active compounds 4c and 5c exhibited an IC50 of 31.9 μM and 32.2 μM, respectively, against HCV NS5B.

A library of 4-thiazolidinones was evaluated for their ability to inhibit HCV NS5B. The two most active compounds 4c and 5c exhibited an IC50 of 31.9 μM and 32.2 μM, respectively, against HCV NS5B.Figure optionsDownload as PowerPoint slide