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2, 4-Diaminopyrimidines as histamine H 4 receptor ligands—scaffold optimization and pharmacological characterization

…, L Weizel, EH Schneider, R Seifert, G Schneider…

文献索引:Sander, Kerstin; Kottke, Tim; Tanrikulu, Yusuf; Proschak, Ewgenij; Weizel, Lilia; Schneider, Erich H.; Seifert, Roland; Schneider, Gisbert; Stark, Holger Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 20 p. 7186 - 7196

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被引用次数: 50

摘要

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 ...