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Bioorg Med Chem Lett. 2006 Apr 1;16(7):1859-63. Epub 2006 Feb 7.

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

Author information

1
Chemical Research Laboratories, Central Pharmaceutical Research Institute, Japan Tobacco Inc, 1-1 Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.

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.

PMID:
16455252
DOI:
10.1016/j.bmcl.2006.01.032
[Indexed for MEDLINE]

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