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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期

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

页码：1392 / 1398

页数：7

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