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Bioorg Med Chem Lett. 2011 Apr 1;21(7):2048-54. doi: 10.1016/j.bmcl.2011.02.006. Epub 2011 Feb 23.

Synthesis and SAR of acyclic HCV NS3 protease inhibitors with novel P4-benzoxaborole moieties.

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  • 1Anacor Pharmaceuticals, Inc, 1020 E Meadow Circle, Palo Alto, CA 94303, USA.


We have synthesized and evaluated a new series of acyclic P4-benzoxaborole-based HCV NS3 protease inhibitors. Structure-activity relationships were investigated, leading to the identification of compounds 5g and 17 with low nanomolar potency in the enzymatic and cell-based replicon assay. The linker-truncated compound 5j was found to exhibit improved absorption and oral bioavailability in rats, suggesting that further reduction of molecular weight and polar surface area could result in improved drug-like properties of this novel series.

Copyright © 2011 Elsevier Ltd. All rights reserved.

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