Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides

…, A Siddiqui, CG Yannopoulos, N Nguyen-Ba…

文献索引：Chan, Laval; Pereira, Oswy; Reddy, T. Jagadeeswar; Das, Sanjoy K.; Poisson, Carl; Courchesne, Marc; Proulx, Melanie; 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, Stephanie; Bilimoria, Darius; Bedard, Jean Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 3 p. 797 - 800

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被引用次数: 107

摘要

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.