par Venkatraj, Muthusamy;Ariën, Kevin;Heeres, Jan;Dirié, Bertrand;Joossens, Jurgen;Van Goethem, Sebastiaan;Van der Veken, Pieter;Michiels, Johan;Vande Velde, Christophe ;Vanham, Guido;Lewi, Paul;Augustyns, Koen
Référence Bioorganic & medicinal chemistry, 19, 20, page (5924-5934)
Publication Publié, 2011-10
Référence Bioorganic & medicinal chemistry, 19, 20, page (5924-5934)
Publication Publié, 2011-10
Article révisé par les pairs
Résumé : | 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. © 2011 Elsevier Ltd. All rights reserved. |