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

James P. Guare, Peter J. Felock, Daria J. Hazuda, Joseph P. Vacca, Stuart R. Michelson, Linghang Zhuang, John Wai, Mark W. Embrey, Thorsten E. Fisher, Melissa S. Egbertson, Linda S. Payne, Abigail Wolfe, Kara A. Stillmock, Marc Witmer, Gregory Moyer, William A. Schleif, Lori J. Gabryelski, Yvonne Leonard, Joseph J. Lynch, Steven D. Young
2003-01-09
SCID:  54.1/7etwsk55 Discuss with AI
Abstract (AI)
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.
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2003-01-09
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James P. Guare
Peter J. Felock
Daria J. Hazuda
Joseph P. Vacca
Stuart R. Michelson
Linghang Zhuang
John Wai
Mark W. Embrey
Thorsten E. Fisher
Melissa S. Egbertson
Linda S. Payne
Abigail Wolfe
Kara A. Stillmock
Marc Witmer
Gregory Moyer
William A. Schleif
Lori J. Gabryelski
Yvonne Leonard
Joseph J. Lynch
Steven D. Young
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