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

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282 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)1506-1508
Number of pages3
JournalJournal of Medicinal Chemistry
Volume49
Issue number5
DOIs
Publication statusPublished - 2006 Mar 5
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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  • Cite this

    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