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

[ Vol. 8 , Issue. 4 ]

Author(s):

Vaishali M. Patil, Gurukumar K. R., Maksim Chudayeu, Satya Prakash Gupta, Subeer Samanta, Neeraj Masand and Neerja Kaushik-Basu   Pages 629 - 635 ( 7 )

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.

Keywords:

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

Affiliation:

Medicinal Chemistry Research Lab, School of Pharmacy, Bharat Institute of Technology, Partapur, Meerut-250 103 (UP) India.



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