The discovery of pyrano[3,4-b]indole-based allosteric inhibitors of HCV NS5B polymerase with in vivo activity.
Matthew G Laporte, Randy W Jackson, Tandy L Draper, Janet A Gaboury, Kristin Galie, Torsten Herbertz, Alison R Hussey, Susan R Rippin, Christopher A Benetatos, Srinivas K Chunduru, Joel S Christensen, Glen A Coburn, Christopher J Rizzo, Gerry Rhodes, John O'Connell, Anita YM Howe, Tarek S Mansour, Marc S Collett, Daniel C Pevear, Dorothy C Young Show all
ChemMedChem | Published : 2008
(Chemical Equation Presented) Antiviral agents against hepatitis C: The discovery and synthesis of pyrano-[3,4-b]indole based inhibitors of HCV NS5B polymerase is described. These compounds effectively inhibit HCV NS5B polymerase and display potent activities in a subgenomic HCV replicon assay. In particular, a sec-butylanalogue of HCV-371 demonstrates in vivo antiviral activityin the chimeric mouse model of HCV infection. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.