Sander, Kerstin and Kottke, Tim and Tanrikulu, Yusuf and Proschak, Ewgenij and Weizel, Lilia and Schneider, Erich H. and Seifert, Roland and Schneider, Gisbert and Stark, Holger (2009) 2,4-Diaminopyrimidines as histamine H-4 receptor ligands-Scaffold optimization and pharmacological characterization. BIOORGANIC & MEDICINAL CHEMISTRY, 17 (20). pp. 7186-7196. ISSN 0968-0896, 1464-3391
Full text not available from this repository. (Request a copy)Abstract
The human histamine H-4 receptor (hH(4)R) 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 hH(4)R 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. (C) 2009 Elsevier Ltd. All rights reserved.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | MICROWAVE-ASSISTED SYNTHESIS; CONSTITUTIVE ACTIVITY; MEDIATES CHEMOTAXIS; ANTAGONISTS; POTENT; H-2-RECEPTOR; CLONING; IDENTIFICATION; H-1-RECEPTOR; MECHANISM; Histamine; H4; GPCR; Topliss scheme; Lead optimization |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 03 Sep 2020 07:08 |
| Last Modified: | 03 Sep 2020 07:08 |
| URI: | https://pred.uni-regensburg.de/id/eprint/28268 |
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