Article ID Journal Published Year Pages File Type
10594407 Bioorganic & Medicinal Chemistry Letters 2012 7 Pages PDF
Abstract
A series of macrocyclic compounds containing a cyclic constraint in the P2-P4 linker region have been discovered and shown to exhibit excellent HCV NS3/4a genotype 3a and genotype 1b R155 K, A156T, A156 V, and D168 V mutant activity while maintaining high rat liver exposure. The effect of the constraint is most dramatic against gt 1b A156 mutants where ∼20-fold improvements in potency are achieved by introduction of a variety of ring systems into the P2-P4 linker.
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
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