Hepatitis Research Today is a free monthly online journal that collates and summarizes the latest research about Hepatitis, including details on hepatitis a, b, c, causes, symptoms. | ||||||||
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6-Hydrazinopurine 2'-methyl ribonucleosides and their 5'-monophosphate prodrugs as potent hepatitis C virus inhibitors.Gunic E, Chow S, Rong F, Ramasamy K, Raney A, Li DY, Huang J, Hamatake RK, Hong Z, Girardet JL Valeant Research and Development, 3300 Hyland Avenue, Costa Mesa, CA 92626, USA. A series of 6-hydrazinopurine 2'-methyl ribonucleosides was synthesized and tested for its inhibitory activity against the hepatitis C virus (HCV). The lack of antiviral activity of these nucleosides was associated with a poor affinity for adenosine kinase, which prompted us to synthesize several of their 5'-monophosphate prodrugs. Some of these prodrugs exhibited more than 1000-fold improvement in anti-HCV activity when compared to their parent nucleosides (EC(50) of 24 nM vs 92 microM for the parent). Published 6 April 2007 in Bioorg Med Chem Lett, 17(9): 2456-8.
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