SAR studies of 9-norbornylpurines as Coxsackievirus B3 inhibitors

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4271-5. doi: 10.1016/j.bmcl.2011.05.070. Epub 2011 May 27.

Abstract

Coxsackievirus and related enteroviruses are important human pathogens that cause various diseases with clinical manifestations ranging from trivial flu-like syndromes to dangerous or even fatal diseases such as myocarditis, meningitis and encephalitis. Here, we report on our continuous SAR study focused on 9-(bicyclo[2.2.1]hept-2-yl)-9H-purines as anti-enteroviral inhibitors. The purine moiety was modified at positions 2, 6 and 8. Several analogues inhibited Coxsackievirus B3 as well as other enteroviruses at low-micromolar concentrations. The 6-chloropurine derivative was confirmed as the most active compound in this series.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry*
  • Antiviral Agents / pharmacology
  • Chlorocebus aethiops
  • Enterovirus / drug effects*
  • Purines / chemical synthesis
  • Purines / chemistry*
  • Purines / pharmacology
  • Structure-Activity Relationship
  • Vero Cells

Substances

  • Antiviral Agents
  • Purines