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

Basic Information

ID: ALA1146135

Journal: Bioorg Med Chem Lett

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

Authors: Ishida T, Suzuki T, Hirashima S, Mizutani K, Yoshida A, Ando I, Ikeda S, Adachi T, Hashimoto H.

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.

CiteXplore: 16455252

DOI: 10.1016/j.bmcl.2006.01.032

Patent ID: