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In order to support bioanalytical LC/MS method development and plasma sample analysis in preclinical and clinical studies of the anti-hepatitis C-virus nucleotides, PSI-7977 and PSI-352938, the corresponding stable isotope labeled forms were prepared. These labeled compounds were prepared by addition reaction of the freshly prepared Grignard reagent 13CD3MgI to the corresponding 2 ′-ketone nucleosides followed by fluorination of the resulting carbinol with DAST. As expected, these 2 ′-C-(trideuterated-13C-methyl) nucleotide prodrugs showed similar anti-HCV activity to that of the corresponding unlabeled ones. [ABSTRACT FROM AUTHOR]

In order to study structure-activity relationships among the derivatives and congeners of 5′,9-anhydro-3-(β-D-ribofuranosyl)xanthine for anti-hepatitis C virus activity, a series of 5′,9-anhydro-purine-isonucleosides with a substituent (s) at 6- or/and 8-position of the purine moiety were synthesized, and their anti-hepatitis C virus activity and cytotoxicity were evaluated and discussed. [ABSTRACT FROM AUTHOR]

A new approach to the synthesis of 2′,3′-didehydro-2′,3′-dideoxynucleosides was described in excellent yield through unusual olefin formation by PhSe-F trans -elimination. [ABSTRACT FROM AUTHOR]

Novel racemic, D- and L-β-dioxolane N4 -hydroxycylosine nucleosides have been synthesized and evaluated for their activity against hepatitis B virus. None of the synthesized nucleosides demonstrated selective anti-HBV activity. [ABSTRACT FROM AUTHOR]