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Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides |
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| Authors: | Chan Laval Pereira Oswy Reddy T Jagadeeswar Das Sanjoy K Poisson Carl Courchesne Marc Proulx Mélanie Siddiqui Arshad Yannopoulos Constantin G Nguyen-Ba Nghe Roy Caroline Nasturica Daniel Moinet Christophe Bethell Richard Hamel Martine L'Heureux Lucille David Maud Nicolas Olivier Courtemanche-Asselin Philippe Brunette Stéphanie Bilimoria Darius Bédard Jean |
| Affiliation: | Shire BioChem Inc, 275 Armand-Frappier, Laval, Quebec, Canada H7V 4A7. lchan@ca.shire.com |
| Abstract: | Further SAR studies on the thiophene-2-carboxylic acids are reported. These studies led to the identification of a series of tertiary amides that show inhibition of both HCV NS5B polymerase in vitro and HCV subgenomic RNA replication in Huh-7 cells. Structural insights about the bioactive conformation of this class of molecules were deduced from a combination of modeling and transferred NOE (trNOE) studies. |
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