Bifunctional aryloxyphosphoramidate prodrugs of 2'-C-Me-uridine: synthesis and anti-HCV activity
| Autor: | Roger G. Ptak, Piet Herdewijn, Chunsheng Huang, Munmun Maiti, Steven De Jonghe, Ling-Jie Gao, Michael G. Murray |
|---|---|
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Sofosbuvir Stereochemistry Chemistry Techniques Synthetic Hepacivirus Virus Replication Biochemistry Antiviral Agents Article 03 medical and health sciences chemistry.chemical_compound Me-uridine medicine Humans Phosphoric Acids Prodrugs Physical and Theoretical Chemistry Bifunctional Uridine Anti hiv Organic Chemistry virus diseases Phosphoramidate Prodrug Amides Hepatitis C digestive system diseases 030104 developmental biology chemistry Microsome Microsomes Liver Nucleoside medicine.drug |
| Zdroj: | Organicbiomolecular chemistry. 14(37) |
| ISSN: | 1477-0539 |
| Popis: | In an attempt to identify novel nucleoside phosphoramidate analogues for improving the anti-HCV activity of 2’-C-Me-uridine, we have synthesized for the first time a series of L-glutamic acid, L-serine, L-threonine and L-tyrosine containing aryloxyphosphoramidate prodrugs of 2’-C-Me-uridine. Evaluation of their activity against HCV revealed that they displayed very potent anti-HCV activity, with EC50 values that are in the same range as of Sofosbuvir. ispartof: Organic & Biomolecular Chemistry vol:14 issue:37 pages:8743-8757 ispartof: location:England status: published |
| Databáze: | OpenAIRE |
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