Article
Pan-NS3 protease inhibitors of hepatitis C virus based on an R3-elongated pyrazinone scaffold.
European journal of medicinal chemistry - 25 Mar 2018
Belfrage Anna Karin, Abdurakhmanov Eldar, Åkerblom Eva, Brandt Peter, Alogheli Hiba, Neyts Johan, Danielson U Helena, Sandström Anja
Abstract excerpt
Herein, we present the design and synthesis of 2(1H)-pyrazinone based HCV NS3 protease inhibitors and show that elongated R3 urea substituents were associated with increased inhibitory potencies over several NS3 protein variants. The inhibitors are believed to rely on β-sheet mimicking hydrogen bonds which are similar over different genotypes and current drug resistant variants and correspond to the β-sheet...
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