Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.

doi:10.1021/JM025553U

Paper

Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.

Published Jan 9, 2003 · Linghang Zhuang, J. Wai, Mark W. Embrey

Journal of medicinal chemistry

Q1 SJR score

236

Citations

3

Influential Citations

Full textSemantic Scholar

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.

In Vitro Study

Highly Cited

Study Snapshot

Naphthyridine 7 effectively inhibits HIV-1 infection spread in cell culture, with a pharmacokinetic profile suitable for oral administration to rats.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Sign up to use Study Snapshot

Consensus is limited without an account. Create an account or sign in to get more searches and use the Study Snapshot.

Create an account

Design and synthesis of 8-hydroxy-[1,6]naphthyridines as novel inhibitors of HIV-1 integrase in vitro and in infected cells.

Sign up to use Study Snapshot

References

Citations