Discovery of 4 '-azido-2 '-deoxy-2 '-C-methyl cytidine and prodrugs thereof: A potent inhibitor of Hepatitis C virus replication

Abstract

4'-Azido-2'-deoxy-2'-methylcytidine (14) is a potent nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase, displaying an EC50 value of 1.2 mu M and showing moderate in vivo bioavailability in rat (F = 14%). Here we describe the synthesis and biological evaluation of 4'-azido-2'-deoxy-2'-methylcytidine and prodrug derivatives thereof. (C) 2012 Elsevier Ltd. All rights reserved.

Keywords

Hepatitis C virus; NS5B polymerase; Antivirals; Nucleoside; Prodrug; Phosphoramidate

Published in

Bioorganic and Medicinal Chemistry Letters
2012, volume: 22, number: 9, pages: 3265-3268
Publisher: PERGAMON-ELSEVIER SCIENCE LTD

SLU Authors

• Nilsson, Magnus

  • Medivir AB

• Agback, Tatiana

  • Medivir AB

UKÄ Subject classification

Medicinal Chemistry
Pharmacology and Toxicology

Publication identifier

• DOI: https://doi.org/10.1016/j.bmcl.2012.03.021

Permanent link to this page (URI)

https://res.slu.se/id/publ/99459