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

  1. Author:
    Nair, V.
    Chi, G.
    Ptak, R.
    Neamati, N.

  2. Author Address

    Univ Georgia, Ctr Drug Discovery, Athens, GA 30602 USA. Univ Georgia, Dept Pharmaceut & Biomed Sci, Athens, GA 30602 USA. So Res Inst, Infect Dis Res Dept, Frederick, MD 21701 USA. Univ So Calif, Dept Pharmaceut Sci, Los Angeles, CA 90089 USA.;Nair, V, Univ Georgia, Ctr Drug Discovery, Athens, GA 30602 USA.;vnair@rx.uga.edu
    1. Year: 2006
    2. Date: Jan
  2. Journal: Journal of Medicinal Chemistry
    1. 49
    2. 2
    3. Pages: 445-447
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    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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External Sources

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  2. DOI: 10.1021/jm0508890
  3. View record in Web of Science®
  4. WOS: 000234836200002

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