8-methylguanosine and phosphoramidic-acid

8-methylguanosine has been researched along with phosphoramidic-acid* in 1 studies

Other Studies

1 other study(ies) available for 8-methylguanosine and phosphoramidic-acid

Article	Year
The phosphoramidate ProTide approach greatly enhances the activity of beta-2'-C-methylguanosine against hepatitis C virus. Bioorganic & medicinal chemistry letters, 2009, Aug-01, Volume: 19, Issue:15 Beta-2'-C-methyl purines (1, 2) are known inhibitors of hepatitis C virus (HCV). We herein report the synthesis, biological and enzymatic evaluation of their 5'-phosphoramidate ProTides. Described herein are seven l-alanine phosphoramidate derivatives with variations to the amino acid ester. The 1-naphthyl phosphoramidate of beta-2'-methylguanosine containing the benzyl ester (20) was the most active at 0.12microM, an 84-fold of increase in activity compared to the parent nucleoside (2) with no increase of cytotoxicity. The carboxypeptidase mediated hydrolysis of several ProTides showed a predictive correlation with their activity versus HCV in replicon. Topics: Amides; Amino Acids; Antiviral Agents; Chemistry, Pharmaceutical; Drug Design; Esters; Guanosine; Hepacivirus; Hepatitis C; Humans; Hydrolysis; Magnetic Resonance Spectroscopy; Models, Chemical; Phosphoric Acids; Prodrugs	2009

Article

Year

The phosphoramidate ProTide approach greatly enhances the activity of beta-2'-C-methylguanosine against hepatitis C virus.

Bioorganic & medicinal chemistry letters, 2009, Aug-01, Volume: 19, Issue:15

Beta-2'-C-methyl purines (1, 2) are known inhibitors of hepatitis C virus (HCV). We herein report the synthesis, biological and enzymatic evaluation of their 5'-phosphoramidate ProTides. Described herein are seven l-alanine phosphoramidate derivatives with variations to the amino acid ester. The 1-naphthyl phosphoramidate of beta-2'-methylguanosine containing the benzyl ester (20) was the most active at 0.12microM, an 84-fold of increase in activity compared to the parent nucleoside (2) with no increase of cytotoxicity. The carboxypeptidase mediated hydrolysis of several ProTides showed a predictive correlation with their activity versus HCV in replicon.

Topics: Amides; Amino Acids; Antiviral Agents; Chemistry, Pharmaceutical; Drug Design; Esters; Guanosine; Hepacivirus; Hepatitis C; Humans; Hydrolysis; Magnetic Resonance Spectroscopy; Models, Chemical; Phosphoric Acids; Prodrugs

2009