1196993-99-3Relevant academic research and scientific papers
2,4-Diaminopyrimidines as histamine H4 receptor ligands-Scaffold optimization and pharmacological characterization
Sander, Kerstin,Kottke, Tim,Tanrikulu, Yusuf,Proschak, Ewgenij,Weizel, Lilia,Schneider, Erich H.,Seifert, Roland,Schneider, Gisbert,Stark, Holger
experimental part, p. 7186 - 7196 (2010/03/03)
The human histamine H4 receptor (hH4R) is a promising new target in the therapy of inflammatory diseases and disorders of the immune system. For the development of new H4R antagonists a broad ligand-based virtual screening was performed resulting in two hits. The dissection of their common annelated aromatic core into its heteromonocyclic components showed that 2,4-diaminopyrimidine is a potent hH4R affinity scaffold, which was comprehensively investigated. Structure-activity relationship studies revealed that slight structural changes evoke extensive differences in functional activities and potencies: while o- and p-substituted benzyl amines mainly showed partial agonism, m-substituted and rigidified ones exhibited inverse agonist efficacy.
