Meeting report: 30th International Conference on Antiviral Research, in Atlanta, GA, USA

Vere Hodge, R Anthony

The final section of David's lecture described the investigation of a new carbocyclic nucleoside, 2 0 -Deoxy-2 0 -fluoro-3 0 -hydroxy-4 0 -(hydroxymethyl)-5 0methylene-carbocyclic adenosine (FMCA) ( Figure 5 ). The 14-step synthesis was shown. FMCA was tested in a cell culture HBV DNA replication assay against both wild-type (wt), lamivudine-resistant strains (M204V, M204I, L180M and L180M/M204V) and adefovir-resistant strain (M236T). FMCA, retained good activity against all these strains, the change in EC 50 values versus the wt virus was between 1.0-and 1.2-fold. In a separate cell culture assay, FMCA and its phosphoramidate prodrug (FMCA-P) were tested against an entecavir-resistant strain (L180M/M204V/ S202G). Both FMCA and its prodrug retained good activity (1.2-and 0.9-fold). Although the data were not shown, FMCA also retains activity against tenofovir-resistant strains.