Synthesis, In Vitro and In Silico NS5B Polymerase Inhibitory Activity of Benzimidazole Derivatives

Title:Synthesis, In Vitro and In Silico NS5B Polymerase Inhibitory Activity of Benzimidazole Derivatives

Volume: 8 Issue: 4

Author(s): Vaishali M. Patil, Gurukumar K. R., Maksim Chudayeu, Satya Prakash Gupta, Subeer Samanta, Neeraj Masand and Neerja Kaushik-Basu

Affiliation:

Keywords: HCV, NS5B polymerase, Benzimidazole derivatives, RNA-dependent RNA polymerase, methylbenzyloxy, hepatocellular carcinoma, orthotopic liver transplants, CMV, RdRp, QSAR

Abstract: Hepatitis C virus (HCV) NS5B polymerase is the key replicating protein of the virus and thus an attractive target for drug development. Here we report on the synthesis and biological evaluation of a new series of benzimidazole derivatives as HCV NS5B inhibitors. This yielded compound 6b and 6d bearing 2-(2-benzyloxy)phenyl and 2-(4- methylbenzyloxy)phenyl moieties, respectively, as promising leads. Binding mode of compound 6d in allosteric pocket (AP)-1 of NS5B will form the basis for future structure-activity relationship optimization.

Cite this article as:

M. Patil Vaishali, K. R. Gurukumar, Chudayeu Maksim, Prakash Gupta Satya, Samanta Subeer, Masand Neeraj and Kaushik-Basu Neerja, Synthesis, In Vitro and In Silico NS5B Polymerase Inhibitory Activity of Benzimidazole Derivatives, Medicinal Chemistry 2012; 8 (4) . https://dx.doi.org/10.2174/157340612801216120