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  • Title: Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 2: tertiary amides.
    Author: Chan L, Pereira O, Reddy TJ, Das SK, Poisson C, Courchesne M, Proulx M, Siddiqui A, Yannopoulos CG, Nguyen-Ba N, Roy C, Nasturica D, Moinet C, Bethell R, Hamel M, L'Heureux L, David M, Nicolas O, Courtemanche-Asselin P, Brunette S, Bilimoria D, Bédard J.
    Journal: Bioorg Med Chem Lett; 2004 Feb 09; 14(3):797-800. PubMed ID: 14741292.
    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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