Article
Synthesis and antiviral activity of HCV NS3/4A peptidomimetic boronic acid inhibitors.
Bioorganic & medicinal chemistry letters - 1 Oct 2009
Boloor Amogh, Hanway Denise, Joshi Maria, Winn David T, Mendez Gabriel, Walls Marlena, Wei Ping, Qian Fuxin, Zhang Xiaoli, Zhang Yuliang, Hepperle Michael E, Li Xinqiang, Campbell David A, Betancort Juan M
Abstract excerpt
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.
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