1258631-01-4Relevant academic research and scientific papers
Ligand based design of novel histamine H4 receptor antagonists; Fragment optimization and analysis of binding kinetics
Smits, Rogier A.,Lim, Herman D.,Van Der Meer, Tiffany,Kuhne, Sebastiaan,Bessembinder, Karin,Zuiderveld, Obbe P.,Wijtmans, Maikel,De Esch, Iwan J.P.,Leurs, Rob
supporting information; experimental part, p. 461 - 467 (2012/02/04)
The histamine H4 receptor is a G protein-coupled receptor that has attracted much interest for its role in inflammatory and immunomodulatory functions. In our search for new H4R ligands, a low affinity isoquinoline fragment was optimized to 7-(furan-2-yl)-4-(piperazin-1-yl) quinazolin-2-amine (VUF11489), as a new H4R antagonist. Analysis of its binding kinetics at the human H4R showed this compound to have a very different dissociative half-life in comparison with reference antagonist JNJ7777120.
QUINAZOLINE DERIVATIVES AS HISTAMINE H4-RECEPT0R INHIBITORS FOR USE IN THE TREATMENT OF INFLAMMATORY DISORDERS
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Page/Page column 21, (2010/12/31)
Compounds that modulate the histamine H4 receptor, and which may be useful for treating or preventing disorders and conditions mediated by the histamine H4 receptor, e.g. inflammation, are of Formula (I):
