Details

Autor(en) / Beteiligte

• Zhuang, Linghang
• Wai, John S
• Embrey, Mark W
• Fisher, Thorsten E
• Egbertson, Melissa S
• Payne, Linda S
• Guare, James P
• Vacca, Joseph P
• Hazuda, Daria J
• Felock, Peter J
• Wolfe, Abigail L
• Stillmock, Kara A
• Witmer, Marc V
• Moyer, Gregory
• Schleif, William A
• Gabryelski, Lori J
• Leonard, Yvonne M
• Lynch, Joseph J
• Michelson, Stuart R
• Young, Steven D

Titel

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

Ist Teil von

• Journal of medicinal chemistry, 2003-02, Vol.46 (4), p.453-456

Ort / Verlag

Washington, DC: American Chemical Society

Erscheinungsjahr

2003

Link zum Volltext

Quelle

MEDLINE

Beschreibungen/Notizen

• 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 μM. It does not exhibit cytotoxicity in cell culture at ≤12.5 μM 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.