Inhibitory properties of 2-substituent-1H-benzimidazole-4-carboxamide derivatives against enteroviruses

Bioorg Med Chem. 2011 Apr 15;19(8):2641-9. doi: 10.1016/j.bmc.2011.03.007. Epub 2011 Mar 10.

Abstract

A series of novel benzimidazole derivatives were designed, synthesized, and evaluated for their activities against four kinds of enteroviruses, that is, Coxsackie virus A16, B3, B6 and Enterovirus 71 in VERO cells. Strong activities against enterovirus replication and low cytotoxicities were observed in these benzimidazoles generally. The most promising compound was (l)-2-(pyridin-2-yl)-N-(2-(4-nitrophenyl)pentan-3-yl)-1H-benzimidazole-4-carboxamide (16), with a high antiviral potency (IC(50)=1.76 μg/mL) and a remarkable selectivity index (328). These compounds were selected for further evaluation as novel enterovirus inhibitors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / pharmacology*
  • Chlorocebus aethiops
  • Drug Design
  • Enterovirus / drug effects
  • Inhibitory Concentration 50
  • Microbial Sensitivity Tests
  • Structure-Activity Relationship
  • Vero Cells / drug effects*

Substances

  • Antiviral Agents
  • Benzimidazoles