Synthesis and in vitro evaluation of novel anti-varicella-zoster virus (VZV) nucleosides.
A series of alkyl-aryl, -phenoxy, and -thiophenoxy bicyclic furo pyrimidine nucleosides have been successfully synthesised by Pd-coupling of 5-iodo-2'-deoxyuridine (IDU) with terminal alkynes, followed by in situ copper-cyclisation. Synthesised compounds (4a-i) showed an anti-VZV activity at low microM concentration, comparable to that of current treatment acyclovir.
Carangio
A
A
Welsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff, CF10 3XF, United Kingdom.
McGuigan
C
C
Cahard
D
D
Andrei
G
G
Snoeck
R
R
De Clercq
E
E
Balzarini
J
J
D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014645:Herpesvirus 3, Human / Q000187:drug effects*; D006801:Humans; D011741:Pyrimidine Nucleosides / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D011741:Pyrimidine Nucleosides