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Title: Halophenyl furanopyrimidines as potent and selective anti-VZV agents
Authors: McGuigan, Christopher ×
Jukes, Alison
Blewett, Sally
Barucki, Hubert
Erichsen, Jonathan T
Andrei, Graciela
Snoeck, Robert
De Clercq, Erik
Balzarini, Jan #
Issue Date: May-2003
Series Title: Antiviral chemistry & chemotherapy vol:14 issue:3 pages:165-70
Abstract: Bicyclic furano pyrimidines have been previously reported by us to be highly potent and selective inhibitors of varicella zoster virus (VZV). p-Alkyl phenyl analogues are particularly potent with EC50 values below 1 nM. In this article we report the synthesis and anti-VZV activity of a series of halophenyl analogues, with variation in the nature (F, Cl, Br) and location (o, m, p) of the halogen substituent. The compounds show a range of activities from ca. 10 nM to > 50 microM. In most cases, ortho substitution leads to greatest activity, meta substitution is in general poor, and the effect of p-substitution shows a marked dependence on the halogen atom. The p-fluorophenyl compound is unique amongst compounds of this class in being inactive as an antiviral. The possible origins of these marked SARs are discussed.
ISSN: 0956-3202
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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