Synthesis and Anti-HSV Activity of new N₁-Acyclic C₄ and C₆-Disubstituted Pyrazolo[3,4-D]Pyrimidine Nucleosides

Abstract

Several N ₁ -(2-hydroxyethoxy)methyl, (4-hydroxybutyl) and (2,3-dihydroxy-1-propoxy)methyl-C ₄ ,C ₆ -disubstituted-1H-pyrozolo[3,4-d]pyrimidines were synthesized. Some of them were evaluated against herpes simplex virus 1 and 2 replications in E ₆ SM cells.

Keywords:

• Pyrazolo[3,4-d]pyrimidines
• acyclonucleoside analogues

Acknowledgments

This investigation was supported by Ibn Zoher University, Faculty of Sciences, Agadir Morocco. We thank Dr. E. De Clercq (Katholieke Universiteit Leuven, Leuven, Belgium) for the antiviral assays. J. J. Vasseur (Lab. de Chimie Organique Biomoleculaire de Synthese, U.S.T. Montpellier II, France) is gratefully acknowledged for help with some spectral and elemental analysis.

Notes

^a Inhibitory concentration required to reduce virus plaque formation by 50%. Virus input was 100 plaque forming units (PFU).

^b Minimum cytotoxic concentration required to cause a microscopically detectable alteration of normal cell morphology.