A potent and orally active HIV-1 integrase inhibitor

被引:24
|
作者
Egbertson, Melissa S. [1 ]
Moritz, H. Marie
Melamed, Jeffrey Y.
Han, Wei
Perlow, Debra S.
Kuo, Michelle S.
Embrey, Mark
Vacca, Joseph P.
Zrada, Matthew M.
Cortes, Amanda R.
Wallace, Audrey
Leonard, Yvonne
Hazuda, Daria J.
Miller, Michael D.
Felock, Peter J.
Stillmock, Kara A.
Witmer, Marc V.
Schleif, William
Gabryelski, Lori J.
Moyer, Gregory
Ellis, Joan D.
Jin, Lixia
Xu, Wei
Braun, Matthew P.
Kassahun, Kellem
Tsou, Nancy N.
Young, Steven D.
机构
[1] Merck Res Labs, Dept Med Chem, West Point, PA 19486 USA
[2] Merck Res Labs, Dept Biol Chem, West Point, PA 19486 USA
[3] Merck Res Labs, Dept Viral Vaccine Res, West Point, PA 19486 USA
[4] Merck Res Labs, Pharmaceut Res Dept, West Point, PA 19486 USA
[5] Merck Res Labs, Dept Drug Metab, West Point, PA 19486 USA
[6] Dept Med Chem, Rahway, NJ 07065 USA
关键词
HIV; AIDS; integrase; strand transfer; 1,6-naphthyridine;
D O I
10.1016/j.bmcl.2006.11.080
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A 1,6-naphthyridine inhibitor of HIV-1 integrase has been discovered with excellent inhibitory activity in cells, good pharmacokinetics, and an excellent ability to inhibit virus with mutant enzyme. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码:1392 / 1398
页数:7
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