Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives

Karine Barral (1) , Robert Hider (2) , Jan Balzarini (3) , Johan Neyts (3) , Erik de Clercq (3) , Michel Camplo (1)

1 GCOMM - Groupe de chimie organique et matériaux moléculaires
2 King‘s College London
3 KU Leuven - Catholic University of Leuven - Katholieke Universiteit Leuven

We describe the synthesis and the antiviral evaluation of novel alpha and beta dideoxynucleoside derivatives in which the base has been replaced by a 3-hydroxy-2-methylpyridin-4-one. The syntheses were successfully achieved by the use of the standard Vorbrüggen coupling conditions. Moderate activity of these compounds were found on herpes simplex virus (HSV) type 1 and type 2.

Domains: Chemical Sciences; Chemical Sciences; Medicinal Chemistry

Karine Barral, Robert Hider, Jan Balzarini, Johan Neyts, Erik de Clercq, et al.. Synthesis and antiviral evaluation of 3-hydroxy-2-methylpyridin-4-one dideoxynucleoside derivatives. Bioorganic and Medicinal Chemistry Letters, 2003, 13 (24), pp.4371-4374. ⟨10.1016/j.bmcl.2003.09.033⟩. ⟨hal-02061650⟩