Diaminopyrimidines, diaminopyridines and diaminopyridazines as histamine H4 receptor modulators
| Autor: | Zhao Bao-Ping, Kevin Tays, Brad M. Savall, Hui Cai, Michael David Gaul, James P. Edwards, Patricia McGovern, Robin L. Thurmond, Steven P. Meduna |
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| Rok vydání: | 2015 |
| Předmět: |
Pyrimidine
Pyridines Stereochemistry Organic Chemistry Clinical Biochemistry Pharmaceutical Science Biochemistry Pyrrolidine Receptors G-Protein-Coupled Pyridazine chemistry.chemical_compound chemistry Diamine Drug Discovery Pyridine Humans Receptors Histamine Molecular Medicine Amine gas treating Histamine H4 receptor Receptor Molecular Biology Receptors Histamine H4 |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 25:956-959 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2014.12.027 |
| Popis: | Previously disclosed H 4 receptor modulators, the triamino substituted pyridines and pyrimidines, contain a free primary amino (–NH 2 ) group. In this Letter we demonstrate that an exocyclic amine (NH 2 ) is not needed to maintain affinity, and also show a significant divergence in the SAR of the pendant diamine component. These des -NH 2 azacycles also show a distinct functional spectrum, that appears to be influenced by the diamine component; in the case of the 1,3-amino pyrimidines, the preferred diamine is the amino pyrrolidine instead of the more common piperazines. Finally, we introduce 3,5-diamino pyridazines as novel histamine H 4 antagonists. |
| Databáze: | OpenAIRE |
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