Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin

Derudas, Marco, Brancale, Andrea ORCID: https://orcid.org/0000-0002-9728-3419, Naesens, L., Neyts, J., Balzarini, J. and McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X 2010. Application of the phosphoramidate ProTide approach to the antiviral drug ribavirin. Bioorganic & Medicinal Chemistry 18 (7) , pp. 2748-2755. 10.1016/j.bmc.2010.02.015

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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
Date Type:	Publication
Status:	Published
Schools:	Pharmacy Systems Immunity Research Institute (SIURI)
Subjects:	R Medicine > RS Pharmacy and materia medica
Uncontrolled Keywords:	Ribavirin; ProTide; Carboxypeptidase Y; Human hint enzyme
Publisher:	Elsevier
ISSN:	0968-0896
Last Modified:	05 Jan 2024 05:55
URI:	https://orca.cardiff.ac.uk/id/eprint/6489

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