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The Discovery of Pyrano[3,4‐ b ]indole‐Based Allosteric Inhibitors of HCV NS5B Polymerase with In Vivo Activity
Author(s) -
LaPorte Matthew G.,
Jackson Randy W.,
Draper Tandy L.,
Gaboury Janet A.,
Galie Kristin,
Herbertz Torsten,
Hussey Alison R.,
Rippin Susan R.,
Benetatos Christopher A.,
Chunduru Srinivas K.,
Christensen Joel S.,
Coburn Glen A.,
Rizzo Christopher J.,
Rhodes Gerry,
O'Connell John,
Howe Anita Y. M.,
Mansour Tarek S.,
Collett Marc S.,
Pevear Daniel C.,
Young Dorothy C.,
Gao Tiejun,
Tyrrell D. Lorne J.,
Kneteman Norman M.,
Burns Christopher J.,
Condon Stephen M.
Publication year - 2008
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800168
Subject(s) - ns5b , subgenomic mrna , indole test , in vivo , virology , hepatitis c virus , polymerase , replicon , sofosbuvir , biology , chemistry , stereochemistry , enzyme , hepacivirus , biochemistry , gene , virus , genetics , crispr , plasmid , ribavirin
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 ‐butyl‐analogue of HCV‐371 demonstrates in vivo antiviral activity in the chimeric mouse model of HCV infection.