Nucleosides with anti-hepatitis B virus activity

Abstract

Hepatitis B virus (HBV) infection represents a serious medical problem. Introduction of antiviral nucleosides such as lamivudine into the clinic has been the most successful approach. By using this and the structurally related agent zidovudine (AZT) as lead molecules, CNRS and UAB Research Foundation report β-L-2′- or β-L-3′-azido-2′,3′- dideoxy-fluorocytosine derivatives, possessing potent in vitro anti-HBV activity. An entire series of such isomeric azido-nucleosides has been obtained by classical procedures of nucleoside chemistry and greatest activity has been evidenced for the unsubstituted (at the pyrimidine amino moiety) azido-fluorocytosines. These two last nucleosides have the same anti-HBV activity as the clinically used drug lamivudine.

• antiviral agents
• azido-nucleosides
• fluoro-nucleosides
• hepatitis B virus
• lamivudine
• nucleosides