Pyridazine based inhibitors of p38 MAPK
| Autor: | Cheryl D. Schwartz, Edward A. O'Neill, David A. Claremon, Nigel J. Liverton, Gerald S. Ponticello, Stephen J. O'Keefe, Margaret Pang, Charles J. Mcintyre |
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| Rok vydání: | 2002 |
| Předmět: |
Stereochemistry
p38 mitogen-activated protein kinases Clinical Biochemistry Anti-Inflammatory Agents Pharmaceutical Science p38 Mitogen-Activated Protein Kinases Biochemistry Chemical synthesis Pyridazine Inhibitory Concentration 50 Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Humans Enzyme Inhibitors Molecular Biology chemistry.chemical_classification biology Aryl Organic Chemistry In vitro Pyridazines Enzyme chemistry Nitrogen atom Enzyme inhibitor biology.protein Molecular Medicine Mitogen-Activated Protein Kinases |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 12:689-692 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(01)00834-4 |
| Popis: | Trisubstituted pyridazines were synthesized and evaluated as in vitro inhibitors of p38 MAPK. The most active isomers were those possessing an aryl group α and a heteroaryl group β relative to the nitrogen atom in the 2-position of the central pyridazine. Additionally, substitution in the 6-position of the central pyridazine with a variety of dialkylamino substituents afforded a set of inhibitors having good (p38 IC 50 1–20 nM) in vitro activity. |
| Databáze: | OpenAIRE |
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