Author/Authors :
Tomio Ishida، نويسنده , , Takayoshi Suzuki، نويسنده , , Shintaro Hirashima، نويسنده , , Kenji Mizutani، نويسنده , , Atsuhito Yoshida، نويسنده , , Izuru Ando، نويسنده , , Satoru Ikeda، نويسنده , , Tsuyoshi Adachi، نويسنده , , Hiromasa Hashimoto، نويسنده ,
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 selective against DNA polymerases (IC50 > 10 μM) and exhibit low cytotoxicity.
Keywords :
HCV , NS5B polymerase , inhibitor , Benzimidazole
