Synthesis and evaluation of 3′-azido-2′,3′-dideoxypurine nucleosides as inhibitors of human immunodeficiency virus

Based on the promising drug resistance profile and potent anti-HIV activity of β-d-3′-azido-2′,3′-dideoxyguanosine, a series of purine modified nucleosides were synthesized by a chemical transglycosylation reaction and evaluated for their antiviral activity, cytotoxicity, and intracellular metabolism. Among the synthesized compounds, several show potent and selective anti-HIV activity in primary lymphocytes.

Graphical abstractA series of purine modified 3′-azido nucleosides were synthesized by a chemical transglycosylation reaction and evaluated for their anti-HIV-1 activity, cytotoxicity and intracellular metabolism.Figure optionsDownload full-size imageDownload as PowerPoint slide