Design, Synthesis and Anti-HIV Activity of Homologous PMEA Derivatives

Abstract

This article describes an efficient route for synthesizing novel cyclopropyl homologous PMEA analogues. The condensation of the bromide 8 with nucleosidic bases (A, U, T, C, 5-FU, G) under standard nucleophilic substitution and deprotection conditions, afforded the target phosphonic acid analogues 14∼18 and 21. These compounds were evaluated for their potential antiviral properties against various viruses. Guanine derivative 21 showed significant antiviral activity.

Keywords:

• Homologous PMEA
• acyclic nucleoside
• antiviral agent

Acknowledgments

This work was supported by Seoul Research and Business Development Program (grant number 10574).