"Identification of BMS-200475 as a Novel and Potent Inhibitor of Hepatitis B Virus."

According to an abstract submitted by the authors to the 11th International Conference on AIDS, held July 7-12, 1996, in Vancouver, British Columbia, "BMS-200475, a cyclopentyl guanosine analog with an exo carbon-carbon double bond, was identified as a potent inhibitor (EC₅₀ = 5 nM, CC₅₀ =30 (mu)M) of hepatitis B virus (HBV) replication using HepG2.2.15 cells. BMS-200475 showed no significant activity against a panel of unrelated RNA and DNA viruses (EC₅₀ >10 (mu)M). BMS-200475 was phosphorylated to its active triphosphate form by cellular enzymes. In vitro biochemical assays demonstrated that BMS-200475-TP is a potent inhibitor of HBV polymerase,...

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