Rethinking the old antiviral drug moroxydine: Discovery of novel analogues as anti-hepatitis C virus (HCV) agents

Bioorg Med Chem Lett. 2015 Nov 15;25(22):5372-6. doi: 10.1016/j.bmcl.2015.09.029. Epub 2015 Sep 12.

Abstract

The discovery of a novel class of HCV inhibitors is described. The new amidinourea compounds were designed as isosteric analogues of the antiviral drug moroxydine. The two derivatives 11g and 11h showed excellent HCV inhibition activity and viability and proved to inhibit a step(s) of the RNA replication. The new compounds have been synthesized in only three synthetic steps from cheap building blocks and in high yields, thus turning to be promising drug candidates in the development of cheaper HCV treatments.

Keywords: Amidinourea; Guanidine; HCV; Hepatitis C life cycle; RNA replication.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / economics*
  • Antiviral Agents / pharmacology*
  • Biguanides
  • Biological Assay
  • Dose-Response Relationship, Drug
  • Drug Discovery* / trends
  • Hepacivirus / drug effects*
  • Humans
  • Microbial Viability / drug effects
  • Molecular Structure
  • Morpholines / chemical synthesis
  • Morpholines / chemistry*
  • Morpholines / pharmacology*

Substances

  • Antiviral Agents
  • Biguanides
  • Morpholines
  • moroxydine