Synthesis and broad-spectrum antiviral activity of some novel benzo-heterocyclic amine compounds

Molecules. 2014 Jan 15;19(1):925-39. doi: 10.3390/molecules19010925.

Abstract

A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC50=3.21-5.06 μM) and 3g (IC50=0.71-34.87 μM) showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus) and a DNA virus (HBV) at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / pharmacology*
  • Benzimidazoles / chemical synthesis
  • Benzimidazoles / pharmacology*
  • Benzothiazoles / chemical synthesis
  • Benzothiazoles / pharmacology*
  • Hepacivirus / drug effects
  • Hepatitis B virus / drug effects
  • Influenza A virus / drug effects
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • Benzimidazoles
  • Benzothiazoles