Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: identification of 2-[(4-diarylmethoxy) phenyl]-benzimidazole

…, T Suzuki, S Hirashima, K Mizutani, A Yoshida…

Index: Ishida, Tomio; Suzuki, Takayoshi; Hirashima, Shintaro; Mizutani, Kenji; Yoshida, Atsuhito; Ando, Izuru; Ikeda, Satoru; Adachi, Tsuyoshi; Hashimoto, Hiromasa Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 7 p. 1859 - 1863

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Citation Number: 111

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 (EC50 as low as 1.1 μM). They are ...