BACKGROUND: The human histamine H(4) receptor (hH(4)R) is a promising new target in the therapy of inflammatory or immune system diseases. METHODS: For the development of new hH(4)R ligands, a broad virtual screening was performed and two hits were identified. Their annelated heterocyclic core was optimized with regard to affinity and potency. RESULTS: Pharmacological characterization of the resulting diaminopyrimidines revealed different agonist and antagonist properties within the same scaffold.
BACKGROUND: The humanhistamine H(4) receptor (hH(4)R) is a promising new target in the therapy of inflammatory or immune system diseases. METHODS: For the development of new hH(4)R ligands, a broad virtual screening was performed and two hits were identified. Their annelated heterocyclic core was optimized with regard to affinity and potency. RESULTS: Pharmacological characterization of the resulting diaminopyrimidines revealed different agonist and antagonist properties within the same scaffold.
Authors: Yusuf Tanrikulu; Ewgenij Proschak; Tim Werner; Tim Geppert; Nickolay Todoroff; Alexander Klenner; Tim Kottke; Kerstin Sander; Erich Schneider; Roland Seifert; Holger Stark; Timothy Clark; Gisbert Schneider Journal: ChemMedChem Date: 2009-05 Impact factor: 3.466