Synthesis and biological activity of pyridopyridazin-6-one p38 MAP kinase inhibitors. Part 1

The development and synthesis of potent p38α MAP kinase inhibitors containing a pyridazinone platform is described. Evolution of the p38α selective pyridopyridazin-6-one series from the p38α/β dual inhibitor 2H-quinolizin-2-one series will be discussed in full detail.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2011-01, Vol.21 (1), p.411-416
Hauptverfasser:	Tynebor, Robert M., Chen, Meng-Hsin, Natarajan, Swaminathan R., O’Neill, Edward A., Thompson, James E., Fitzgerald, Catherine E., O’Keefe, Stephen J., Doherty, James B.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Binding Sites bioactive properties Biological and medical sciences Bones, joints and connective tissue. Antiinflammatory agents Catalytic Domain Computer Simulation enzyme inhibitors Medical sciences mitogen-activated protein kinase Mitogen-Activated Protein Kinase 14 - antagonists & inhibitors Mitogen-Activated Protein Kinase 14 - metabolism p38 inhibitors Pharmacology. Drug treatments Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacokinetics Protein Structure, Tertiary Pyridazines - chemical synthesis Pyridazines - chemistry Pyridazines - pharmacokinetics Pyridopyridazin-6-one Rats Rheumatoid arthritis Selective Structure-Activity Relationship synthesis
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