Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin

Derudas, Marco, Brancale, Andrea, Naesens, Lieve, Neyts, Johan, Balzarini, Jan and McGuigan, Christopher (2010) Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin. Bioorganic & Medicinal Chemistry, 18 (7). pp. 2748-2755. ISSN 0968-0896

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Abstract

Ribavirin is a nucleoside analogue with broad antiviral activity. Here we report the synthesis and biological evaluation of novel ribavirin ProTides designed to deliver the bioactive ribavirin monophosphate into cells. Some of the compounds display activity similar to the parent nucleoside against a range of viruses. Enzymatic, cell lysate and preliminary modeling studies have been performed to investigate the lack of enhancement of potency by the ProTides, and these indicate a failure at the final, amino acid cleavage step in the ProTide activation process, leading to inefficient release of the nucleoside monophosphate.

Item Type: Article
Schools and Departments: School of Life Sciences > Chemistry
Depositing User: Marco Derudas
Date Deposited: 23 Jul 2015 06:20
Last Modified: 23 Jul 2015 06:20
URI: http://sro.sussex.ac.uk/id/eprint/55689
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