Antiviral activity of 2,3′-anhydro and related pyrimidine nucleosides against hepatitis B virus

Various 2,3′-anhydro analogs of 5-substituted 1-(2-deoxy-β-d-lyxofuranosyl)uracils (10–15) and a related 1-(3-O-mesyl-2-deoxy-β-d-lyxofuranosyl) pyrimidine nucleoside analog (18) have been synthesized for evaluation as a new class of potential anti-HBV agents. The compounds 10, 12, and 15 demonstrated most potent anti-HBV activities against duck HBV (DHBV) and human HBV with EC50 values in the range of 2.5–10 and 5–10 μg/mL, respectively, at non-toxic concentrations (CC50 = >200 μg/mL). The nucleoside 18 also demonstrated significant anti-HBV activity against DHBV with an EC50 value of 2.5 μg/mL, however, it was less active against HBV in 2.2.15 cells (EC50 = >10 μg/mL).

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