Synthesis and antiviral activity of N-phenylbenzamide derivatives, a novel class of enterovirus 71 inhibitors

Molecules. 2013 Mar 21;18(3):3630-40. doi: 10.3390/molecules18033630.

Abstract

A series of novel N-phenylbenzamide derivatives were synthesized and their anti-EV 71 activities were assayed in vitro. Among the compounds tested, 3-amino-N-(4-bromophenyl)-4-methoxybenzamide (1e) was active against the EV 71 strains tested at low micromolar concentrations, with IC50 values ranging from 5.7 ± 0.8-12 ± 1.2 μM, and its cytotoxicity to Vero cells (TC50 = 620 ± 0.0 μM) was far lower than that of pirodavir (TC50 = 31 ± 2.2 μM). Based on these results, compound 1e is a promising lead compound for the development of anti-EV 71 drugs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Antiviral Agents / toxicity
  • Benzamides / chemical synthesis*
  • Benzamides / pharmacology
  • Benzamides / toxicity
  • Chlorocebus aethiops
  • Drug Evaluation, Preclinical
  • Enterovirus / drug effects
  • Inhibitory Concentration 50
  • Piperidines / pharmacology
  • Piperidines / toxicity
  • Pyridazines / pharmacology
  • Pyridazines / toxicity
  • Structure-Activity Relationship
  • Vero Cells

Substances

  • Antiviral Agents
  • Benzamides
  • Piperidines
  • Pyridazines
  • pirodavir