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

285 引用 (Scopus)

抜粋

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.

元の言語English
ページ(範囲)1506-1508
ページ数3
ジャーナルJournal of Medicinal Chemistry
49
発行部数5
DOI
出版物ステータスPublished - 2006 3 5
外部発表Yes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

フィンガープリント Novel HIV-1 integrase inhibitors derived from quinolone antibiotics' の研究トピックを掘り下げます。これらはともに一意のフィンガープリントを構成します。

  • これを引用

    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. (2006). Novel HIV-1 integrase inhibitors derived from quinolone antibiotics. Journal of Medicinal Chemistry, 49(5), 1506-1508. https://doi.org/10.1021/jm0600139