Synthesis of C-6 substituted pyrazolo[1,5-a]pyridines with potent activity against herpesviruses

Bioorg Med Chem. 2006 Feb 15;14(4):944-54. doi: 10.1016/j.bmc.2005.09.015. Epub 2005 Oct 4.

Abstract

A novel series of potent C-6 substituted pyrazolo[1,5-a]pyridine inhibitors of herpes simplex viruses has been identified. A synthetic methodology was developed involving functionalization of a C-6 trifluoromethyl pyrazolo[1,5-a]pyridine to allow facile access to a diverse set of analogues from common late stage intermediates. The expansion of the SAR of this series at the 6 position allows for modifications to developability parameters such as clogP, while maintaining potency comparable to acyclovir.

MeSH terms

  • Animals
  • Cell Line
  • Chlorocebus aethiops
  • Herpesviridae / drug effects*
  • Molecular Structure
  • Pyrazoles / chemical synthesis
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology*
  • Pyrazoles / toxicity
  • Pyridines / chemical synthesis
  • Pyridines / chemistry*
  • Pyridines / pharmacology*
  • Pyridines / toxicity
  • Structure-Activity Relationship

Substances

  • Pyrazoles
  • Pyridines
  • pyrazolopyridine