| Literature DB >> 19493593 |
Malte Meppen1, Barbara Pacini, Renzo Bazzo, Uwe Koch, Joseph F Leone, Kenneth A Koeplinger, Michael Rowley, Sergio Altamura, Annalise Di Marco, Fabrizio Fiore, Claudio Giuliano, Odalys Gonzalez-Paz, Ralph Laufer, Vincenzo Pucci, Frank Narjes, Cristina Gardelli.
Abstract
The currently approved treatment for hepatitis C virus infections is a combination of Ribavirin and pegylated Interferon. It leads to a sustained virologic response in approximately only half of the patients treated. For this reason there is an urgent need of new therapeutic agents. 2'-C-Methylcytidine is the first nucleoside inhibitor of the HCV NS5B polymerase that was efficacious in reducing the viral load in patients infected with HCV. The application of a monophosphate prodrug approach based on unprecedented cyclic phosphoramidates is reported. Our SAR studies led to compounds that are efficiently converted to the active triphosphate in human hepatocytes.Entities:
Mesh：
Substances：
Year: 2009 PMID： 19493593 DOI： 10.1016/j.ejmech.2009.04.043
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514