Aryl furano pyrimidines: the most potent and selective anti-VZV agents reported to date.
Bicyclic aryl furano pyrimidines represent the most potent anti-VZV agents reported to date. Lead compounds have EC50 values in vitro as low as 0.1 nM and selectivity index values exceeding one million. They have an absolute requirement for VZV thymidine kinase (TK) and most likely act as their phosphate forms. Some structural modification, such as aryl substitution, is tolerated, while little sugar modification is acceptable. We herein summarise their biological profiles and structure activity relationships as discovered to date.
McGuigan
Christopher
C
Welsh School of Pharmacy, University of Wales Cardiff, Redwood Building, King Edward Vll Avenue, Cardiff CF1 3XF, UK. mcguigan@cardiff.ac.uk
Balzarini
Jan
J
D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D005663:Furans / Q000737:chemistry; D014645:Herpesvirus 3, Human / Q000187:drug effects*; D006801:Humans; D008826:Microbial Sensitivity Tests; D011741:Pyrimidine Nucleosides / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000998:Antiviral Agents; D005663:Furans; D011741:Pyrimidine Nucleosides