Linghang Zhuang, J. Wai, Mark W. Embrey
Jan 9, 2003
Citations
3
Influential Citations
232
Citations
Quality indicators
Journal
Journal of medicinal chemistry
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.