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Evaluation of novel phosphoramidate ProTides of the 2′-fluoro derivatives of a potent anti-varicella zoster virus bicyclic nucleoside analogue

Derudas, Marco, Quintiliani, Maurizio, Brancale, Andrea, Andrei, Graciela, Snoeck, Robert, Balzarini, Jan and McGuigan, Christopher 2010. Evaluation of novel phosphoramidate ProTides of the 2′-fluoro derivatives of a potent anti-varicella zoster virus bicyclic nucleoside analogue. Antiviral Chemistry and Chemotherapy 21 (1) , pp. 15-31. 10.3851/IMP1661

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Abstract

Background: Recently, the synthesis and antiviral activity of a series of 2′-fluoro derivatives of the most potent anti-varicella zoster virus (VZV) agent reported to date, the bicyclic nucleoside analogue Cf1743, have been reported. Methods: Here, we present molecular modelling studies for the interaction of these compounds with VZV-encoded thymidine kinase (TK) and we report the synthesis of a series of phosphoramidate ProTides of these compounds designed to bypass the nucleoside kinase dependence of the parent nucleoside analogues. Results: The phosphoramidate prodrugs were equally effective as their parent compounds against VZV in cell culture, but lost antiviral potency against TK-deficient VZV strains. Conclusions: ProTide-based kinase bypass is not successful in this case.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Pharmacy
Systems Immunity Research Institute (SIURI)
Subjects: R Medicine > RS Pharmacy and materia medica
Publisher: International Medical Press
ISSN: 0956-3202
Last Modified: 18 Oct 2017 13:42
URI: http://orca-mwe.cf.ac.uk/id/eprint/7430

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