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

作者：Rawal Ravindra K; Katti S B^*; Kaushik Basu Neerja; Arora Payal; Pan Zhenhua

来源：Bioorganic & Medicinal Chemistry Letters, 2008, 18(23): 6110-6114.

DOI：10.1016/j.bmcl.2008.10.023

• HCV
• NS5B
• RdRp
• 4-Thiazolidinones

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 IC(50) of 31.9 mu M and 32.2 mu M, respectively, against HCV NS5B.

• 出版日期2008-12-1