2′-Fluorosugar analogues of the highly potent anti-varicella-zoster virus bicyclic nucleoside analogue (BCNA) Cf 1743 |
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| Authors: | Christopher McGuigan Marco Derudas Maurizio Quintiliani Graciela Andrei Robert Snoeck Geoffrey Henson Jan Balzarini |
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| Institution: | aWelsh School of Pharmacy, Cardiff University, King Edward VII Avenue, Cardiff CF10 3XF, UK;bRega Institute for Medical Research, Minderbroedersstraat 10, Leuven B-3000, Belgium;cInhibitex, 9005 Westside Parkway, Alpharetta, GA 30004, USA |
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| Abstract: | We report the preparation of 2′-α-F, 2′-β-F and 2′,2′-difluoro analogues of the leading anti-varicella zoster virus (VZV) pentylphenyl BCNA Cf 1743. VZV thymidine kinase showed the highest phosphorylating capacity for the β-fluoro derivative, that retained equal antiviral potency as the parent compound. In contrast, the α-fluoro- and 2′,2′-difluoro BCNA derivatives were markedly less ( 100-fold) antivirally active. |
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| Keywords: | VZV BCNAs Cf 1743 Thymidine kinase Zoster Shingles Nucleosides Herpes Fluorosugars |
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