title: Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs).
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.
authors.affiliation: Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
authors.forename: Muthusamy
authors.initials: M
authors.lastname: Venkatraj
authors.forename: Kevin K
authors.initials: KK
authors.lastname: Ariën
authors.forename: Jan
authors.initials: J
authors.lastname: Heeres
authors.forename: Bertrand
authors.initials: B
authors.lastname: Dirié
authors.forename: Jurgen
authors.initials: J
authors.lastname: Joossens
authors.forename: Sebastiaan
authors.initials: S
authors.lastname: Van Goethem
authors.forename: Pieter
authors.initials: P
authors.lastname: Van der Veken
authors.forename: Johan
authors.initials: J
authors.lastname: Michiels
authors.forename: Christophe M L
authors.initials: CM
authors.lastname: Vande Velde
authors.forename: Guido
authors.initials: G
authors.lastname: Vanham
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Lewi
authors.forename: Koen
authors.initials: K
authors.lastname: Augustyns
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology*; D054303:HIV Reverse Transcriptase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D006801:Humans; D008958:Models, Molecular; D010793:Phthalazines / Q000737:chemistry / Q000494:pharmacology*; D011724:Pyridazines / Q000737:chemistry / Q000494:pharmacology*; D011728:Pyridones / Q000737:chemistry / Q000494:pharmacology*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D019380:Anti-HIV Agents; D010793:Phthalazines; D011724:Pyridazines; D011728:Pyridones; D018894:Reverse Transcriptase Inhibitors; C514824:reverse transcriptase, Human immunodeficiency virus 1; D054303:HIV Reverse Transcriptase