McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Jukes, Alison, Blewett, Sally Ann, Barucki, H., Erichsen, Jonathan Thor ORCID: https://orcid.org/0000-0003-1545-9853, Andrei, G., Snoeck, R., De Clercq, E. and Balzarini, J. 2003. Halophenyl furanopyrimidines as potent and selective anti-VZV agents. Antiviral Chemistry & Chemotherapy 14 (3) , pp. 165-170. |
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 1nM. 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 μM. In most cases, ortho substitution leads to greatest activity, meta substitution is in general poor, and the effect of psubstitution 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.
Item Type: | Article |
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Date Type: | Publication |
Status: | Published |
Schools: | Pharmacy Optometry and Vision Sciences Systems Immunity Research Institute (SIURI) |
Subjects: | R Medicine > RM Therapeutics. Pharmacology |
Uncontrolled Keywords: | VZV, bicyclic furano pyrimidines, SARs |
Publisher: | International Medical Press |
ISSN: | 0956-3202 |
Last Modified: | 19 Oct 2022 08:39 |
URI: | https://orca.cardiff.ac.uk/id/eprint/18552 |
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