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  • Title: Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole.
    Author: Ishida T, Suzuki T, Hirashima S, Mizutani K, Yoshida A, Ando I, Ikeda S, Adachi T, Hashimoto H.
    Journal: Bioorg Med Chem Lett; 2006 Apr 01; 16(7):1859-63. PubMed ID: 16455252.
    Abstract:
    A series of 1-cycloalkyl-2-phenyl-1H-benzimidazole-5-carboxylic acid derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase (RdRp). A SAR study was performed and led to identify the 2-[(4-diarylmethoxy)phenyl]-benzimidazoles as potent inhibitors. They inhibit subgenomic HCV RNA replication in the replicon cells at low micromolar concentrations (EC(50) as low as 1.1microM). They are selective against DNA polymerases (IC(50)>10microM) and exhibit low cytotoxicity.
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