Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1370755 | Bioorganic & Medicinal Chemistry Letters | 2011 | 7 Pages |
Abstract
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.
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Related Topics
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Organic Chemistry
Authors
Xianfeng Li, Suoming Zhang, Yong-Kang Zhang, Yang Liu, Charles Z. Ding, Yasheen Zhou, Jacob J. Plattner, Stephen J. Baker, Wei Bu, Liang Liu, Wieslaw M. Kazmierski, Maosheng Duan, Richard M. Grimes, Lois L. Wright, Gary K. Smith, Richard L. Jarvest,