| Literature DB >> 12570367 |
Linghang Zhuang1, John S Wai, Mark W Embrey, Thorsten E Fisher, Melissa S Egbertson, Linda S Payne, James P Guare, Joseph P Vacca, Daria J Hazuda, Peter J Felock, Abigail L Wolfe, Kara A Stillmock, Marc V Witmer, Gregory Moyer, William A Schleif, Lori J Gabryelski, Yvonne M Leonard, Joseph J Lynch, Stuart R Michelson, Steven D Young.
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.Entities:
Mesh：
Substances：
Year: 2003 PMID： 12570367 DOI： 10.1021/jm025553u
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446