Discovery of 4′-azido-2′-deoxy-2′-C-methyl cytidine and prodrugs thereof: A potent inhibitor of Hepatitis C virus replication

Abstract 4′-Azido-2′-deoxy-2′-methylcytidine ( 14 ) is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC 50 value of 1.2 μM and showing moderate in vivo bioavailability in rat ( F  = 14%). Here we describe the synthesis and biological evaluation of 4′-azido-2′-deoxy-2′-methylcytidine and prodrug derivatives thereof.