- Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.
Bioorganic & medicinal chemistry letters (2004-01-27)
Laval Chan, Oswy Pereira, T Jagadeeswar Reddy, Sanjoy K Das, Carl Poisson, Marc Courchesne, Mélanie Proulx, Arshad Siddiqui, Constantin G Yannopoulos, Nghe Nguyen-Ba, Caroline Roy, Daniel Nasturica, Christophe Moinet, Richard Bethell, Martine Hamel, Lucille L'Heureux, Maud David, Olivier Nicolas, Philippe Courtemanche-Asselin, Stéphanie Brunette, Darius Bilimoria, Jean Bédard
PMID14741292
RÉSUMÉ
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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