Synthesis of the 5-phosphono-pent-2-en-1-yl nucleosides: a new class of antiviral acyclic nucleoside phosphonates

Bioorg Med Chem. 2007 Feb 15;15(4):1771-9. doi: 10.1016/j.bmc.2006.11.038. Epub 2006 Nov 30.

Abstract

A new class of acyclic nucleoside phosphonates, the 5-phosphono-pent-2-en-1-yl nucleosides and their hexadecyloxypropyl esters, were synthesized from butyn-1-ol. Only the hexadecyloxypropyl esters showed antiviral activity against herpes simplex virus type 1, in vitro. Hexadecyloxypropyl 1-(5-phosphono-pent-2-en-1-yl)-thymine was the most active and selective compound among the synthesized nucleotides with an EC50 value of 0.90 microM.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology
  • Herpesvirus 1, Human / drug effects
  • Humans
  • Inhibitory Concentration 50
  • Nucleosides / chemical synthesis*
  • Nucleosides / pharmacology*
  • Organophosphonates
  • Thymine

Substances

  • Antiviral Agents
  • Nucleosides
  • Organophosphonates
  • Thymine