HIV integrase inhibitors with nucleobase scaffolds: Discovery of a highly potent anti-HIV agent

被引：68
|
作者：
Nair, V [1 ]
Chi, G
Ptak, R
Neamati, N
机构：
[1] Univ Georgia, Ctr Drug Discovery, Athens, GA 30602 USA
[2] Univ Georgia, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 USA
[3] So Res Inst, Infect Dis Res Dept, Frederick, MD 21701 USA
[4] Univ So Calif, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 02期
关键词：
D O I：
10.1021/jm0508890
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
HIV integrase is essential for HIV replication. However, there are currently no integrase inhibitors in clinical use for AIDS. We have discovered a conceptually new beta-diketo acid that is a powerful inhibitor of both the 3'-processing and strand transfer steps of HIV-1 integrase. The in vitro anti-HIV data of this inhibitor were remarkable as exemplified by its highly potent antiviral therapeutic efficacy against HIVTEKI and HIV-1(NL4-3) replication in PBMC (TI > 4,000 and > 10,000, respectively).
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收藏
页码：445 / 447
页数：3
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