Synthesis and Antiviral Activity of C-5 Substituted β-D- and β-L-D4T Analogues

Abstract

A series of β-D-2′,3′-didehydro-2′,3′-dideoxy-nucleosides bearing a tether attached at the C-5 position and their β-L-counterparts was synthesized. Their inhibitory activities against human immunodeficiency virus (HIV) were investigated and compared to establish relationship(s) between compound structure and their antiviral activity. No significant activity was observed for β-D- and β-L-modified nucleosides respectively 7a-c and 14a-c, but 7d and 14d exhibited a weak activity against HIV-1.