Pyridine Carboxamides: Potent Palm Site Inhibitors of HCV NS5B Polymerase.

ABSTRACT: Pyridine carboxamide-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified and optimized to a variety of topologically related scaffolds. In particular, the 2-methyl nicotinic acid scaffold was developed into inhibitors with improved biochemical (IC50-GT1b = 0.014 μM) and cell-based HCV replicon potency (EC50-GT1b = 0.7 μM). Biophysical and biochemical characterization identified this novel series of compounds as palm site binders to HCV polymerase.

SUBMITTER: Cheng CC 

PROVIDER: S-EPMC4007899 | biostudies-literature | 2010 Dec

REPOSITORIES: biostudies-literature