Novel HIV-1 integrase inhibitors derived from quinolone antibiotics

Motohide Sato, Takahisa Motomura, Hisateru Aramaki, Takashi Matsuda, Masaki Yamashita, Yoshiharu Ito, Hiroshi Kawakami, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Satoru Ikeda, Eiichi Kodama, Masao Matsuoka, Hisashi Shinkai

研究成果: Article査読

318 被引用数 (Scopus)

抄録

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.

本文言語English
ページ(範囲)1506-1508
ページ数3
ジャーナルJournal of Medicinal Chemistry
49
5
DOI
出版ステータスPublished - 2006 3月 5
外部発表はい

ASJC Scopus subject areas

  • 分子医療
  • 創薬

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