Article ID Journal Published Year Pages File Type
1370755 Bioorganic & Medicinal Chemistry Letters 2011 7 Pages PDF
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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Physical Sciences and Engineering Chemistry Organic Chemistry
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