2. Academic Validation
  3. Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs)

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

  • Bioorg Med Chem. 2011 Oct 15;19(20):5924-34. doi: 10.1016/j.bmc.2011.08.060.
Muthusamy Venkatraj 1,  Kevin K Ariën,  Jan Heeres,  Bertrand Dirié,  Jurgen Joossens,  Sebastiaan Van Goethem,  Pieter Van der Veken,  Johan Michiels,  Christophe M L Vande Velde,  Guido Vanham,  Paul J Lewi,  Koen Augustyns
Affiliations

Affiliation

  • 1 Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
PMID: 21930388 DOI: 10.1016/j.bmc.2011.08.060
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.

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