Synthesis and anti-HIV activity of Triazolo-fused 3′,4′-cyclic and 4′-spiro nucleoside analogues

Abstract

Triazolo-fused 3′,4′-cyclic nucleoside 4′-spiro nucleoside analogues were synthesized by an intramolecular 1,3-dipolar cycloaddition of 4′-azido nucleoside derived azido-alkynes in a regio- and stereo-specific manner. The thymine nucleoside base in these target compounds was transformed into the corresponding 5-methyl cytosine component. The synthesized compounds were examined in an MAGI(multinuclear-activation galactosidase indicator) assay for exploring the anti-HIV activity and in a H9 T(human T lymphocytes H9) assay for measuring the cell toxicity.

Keywords

4′-Spiro nucleoside / 3′,4′-fused nucleoside / Biological activity / 1, 3-Dipolar cycloaddition

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