It's estimated that more than 170 million people are chronically infected with HCV worldwide. While the infection is often asymptomatic, chronic infection can lead to liver cirrhosis and cancer. The current standard of care is associated with significant tolerability issues and a lack of efficacy in some patient groups. As a result, current efforts are aimed at developing combinations of direct acting antiviral agents. Along with HCV polymerase and protease inhibiting agents, inhibitors of NS5A have demonstrated clinical efficacy. This work describes a novel series of HCV NS5A inhibitors and selection of a compound suitable for administration in an HCV-infected chimpanzee. Observation of a robust viral load decline provided positive proof of concept for this new series of compounds as inhibitors of HCV infection. The design, synthesis, and structure activity relationships of these compounds will be reported.

Discovery of novel inhibitors of HCV NS5A and proof of concept study in an HCV-infected chimpanzee

243rd National Meeting (2012)

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