The application of the phosphoramidate ProTide approach confers micromolar potency against Hepatitis C virus on inactive agent 4′-azidoinosine: Kinase bypass on …

C McGuigan, F Daverio, I Nájera, JA Martin…

Index: McGuigan, Christopher; Daverio, Felice; Najera, Isabel; Martin, Joseph A.; Klumpp, Klaus; Smith, David B. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 11 p. 3122 - 3124

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Citation Number: 16

Abstract

Novel phosphoramidate ProTides derived from 4′-azidoinosine have been prepared and evaluated in the replicon assay against hepatitis C Virus (HCV). The parent nucleoside analogue is inactive in this assay, while the ProTides are active at low μM levels in some cases. This is a rare example of an inosine nucleoside analogue with potent antiviral activity and further supports the notion of ProTides as a drug discovery motif.