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Synthesis and antiviral activity of HCV NS3/4A peptidomimetic boronic acid inhibitors. 2009
Amogh Boloor, and
Denise Hanway, and
Maria Joshi, and
David T Winn, and
Gabriel Mendez, and
Marlena Walls, and
Ping Wei, and
Fuxin Qian, and
Xiaoli Zhang, and
Yuliang Zhang, and
Michael E Hepperle, and
Xinqiang Li, and
David A Campbell, and
Juan M Betancort
Phenomix Corporation, 5930 Cornerstone Court West, Suite 230, San Diego, CA 92121, USA.
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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