Article
Design, synthesis and evaluation of novel anti-HCV molecules that deliver intracellularly three highly potent NS5A inhibitors.
Bioorganic & medicinal chemistry letters - 1 Sept 2015
Boucle Sebastien, Tao Sijia, Amblard Franck, Stanton Richard A, Nettles James H, Li Chengwei, McBrayer Tamara R, Whitaker Tony, Coats Steven J, Schinazi Raymond F
Abstract excerpt
The design and synthesis of new non-symmetrical NS5A inhibitors with sulfur containing amino acids is reported along with their ability to block HCV replication in an HCV 1b replicon system. These compounds display EC50 values in the picomolar range with a large therapeutic index (>10(6)). Moreover, cellular pharmacology studies show that our preferred compounds intracellularly deliver three potent NS5A inhibitors.
Read the complete abstract on PubMedTopics
Share this publication in a Topic to start or enrich a Post.