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

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 HIV(TEKI) and HIV-1(NL4)(-)(3) replication in PBMC (TI >4,000 and >10,000, respectively).

SUBMITTER: Nair V

PROVIDER: S-EPMC2518396 | biostudies-literature | 2006 Jan

REPOSITORIES: biostudies-literature

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

Nair Vasu V Chi Guochen G Ptak Roger R Neamati Nouri N

Journal of medicinal chemistry 20060101 2

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 HIV(TEKI) and HIV-1(NL4)(-)(3) replication in PBMC (TI >4,000 and >10,000, respec ...[more]

PMID: 16420027

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