A new series of NS3/4A protease boronic acid inhibitors is described. The compounds show good biochemical potency and cellular activity. The peptidomimetic inhibitors were evaluated against proteases from different HCV genotypes and clinically relevant NS3/4A mutants. Compound 28 displayed subnanomolar to single digit nanomolar potencies in the enzymatic assays and an EC50 of 25 nM in the replicon cell-based assay.
Bioorganic & medicinal chemistry letters 09/2009; 19(19):5708-11. DOI:10.1016/j.bmcl.2009.08.017 · 2.33 Impact Factor