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
  • 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.