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Synthesis and evaluation of novel phosphoramidate prodrugs of 2′-methyl cytidine as inhibitors of hepatitis c virus NS5B polymerase

Authors :
Claudio Giuliano
Michael Rowley
Annalise Di Marco
Fabrizio Fiore
Monica Donghi
Cristina Gardelli
Barbara Attenni
Vincenzo Pucci
Frank Narjes
Ralph Laufer
Joseph F. Leone
Source :
Bioorganic & Medicinal Chemistry Letters. 19:1392-1395
Publication Year :
2009
Publisher :
Elsevier BV, 2009.

Abstract

A variety of new prodrugs of 2'-methyl cytidine based on acyloxy ethylamino phosphoramidates have been synthesized and tested in vitro and in vivo for their biological activity. Compared with the parent drug a 10- to 20-fold increase in formation of nucleotide triphosphate in rat and human hepatocytes could be achieved.

Details

ISSN :
0960894X
Volume :
19
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....8bd9d8136571293bd1dc41a8ee79d59f