Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) [letter]

M Venkatraj, KK Ariën, J Heeres, B Dirié, J Joossens, S Van Goethem, P Van der Veken, J Michiels, CML Vande Velde, G Vanham, PJ Lewi, K Augustyns

    Research output: Contribution to journalA1: Web of Science-article

    Abstract

    In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these series are three diarylpyridazinones 25a, 25l and 25n which demonstrated submicromolar activity against wild-type HIV-1 and moderate activity against the single mutant strain Ba-L V106A.
    Original languageEnglish
    JournalBioorganic and Medicinal Chemistry
    Volume19
    Issue number20
    Pages (from-to)5924-5934
    Number of pages11
    ISSN0968-0896
    DOIs
    Publication statusPublished - 2011

    Keywords

    • B780-tropical-medicine
    • Viral diseases
    • HIV-1
    • AIDS
    • Non-nucleoside
    • Reverse transcriptase inhibitors
    • Mutations
    • Strains
    • Diarylpyridinones
    • Diarylpyridazinones
    • Diarylphtalazinones
    • Laboratory techniques and procedures

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