Novel HIV-1 integrase inhibitors derived from quinolone antibiotics

被引：299

作者：

Sato, M

Motomura, T

Aramaki, H

Matsuda, T

Yamashita, M

Ito, Y

Kawakami, H

Matsuzaki, Y

Watanabe, W

Yamataka, K

Ikeda, S

Kodama, E

Matsuoka, M

Shinkai, H

机构：

[1] JT Inc, Cent Pharmaceut Res Inst, Takatsuki, Osaka 5691125, Japan

[2] Kyoto Univ, Inst Virus Res, Sakyo Ku, Kyoto 6068507, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2006年 / 49卷 / 05期

关键词：

D O I：

10.1021/jm0600139

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The viral enzyme integrase is essential for the replication of human immunodeficiency virus type 1 (HIV-1) and represents a remaining target for antiretroviral drugs. Here, we describe the modification of a quinolone antibiotic to produce the novel integrase inhibitor JTK-303 (GS 9137) that blocks strand transfer by the viral enzyme. It shares the core structure of quinolone antibiotics, exhibits an IC50 of 7.2 nM in the strand transfer assay, and shows an EC50 of 0.9 nM in an acute HIV-1 infection assay.

引用

页码：1506 / 1508

页数：3

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