Design and Synthesis of 8-Hydroxy-1,6Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells

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Abstract

Naphthyridine 7 inhibits the strand transfer of the integration process catalyzed by integrase with an IC50 of 10 nM and inhibits 95% of the spread of HIV-1 infection in cell culture at 0.39 microM. It does not exhibit cytotoxicity in cell culture at < or =12.5 microM and shows a good pharmacokinetic profile when dosed orally to rats. The antiviral activity of 7 and its effect on integration were confirmed using viruses with specific integrase mutations.

Design and Synthesis of 8-Hydroxy-1,6Naphthyridines as Novel Inhibitors of HIV-1 Integrase in Vitro and in Infected Cells

Key Points

Abstract

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