Synthesis and biological activity of pyridopyridazin-6-one p38α MAP kinase inhibitors. Part 2.

Authors :: Tynebor RM
Chen MH
Natarajan SR
O'Neill EA
Thompson JE
Fitzgerald CE
O'Keefe SJ
Doherty JB
Source :: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Sep 15; Vol. 22 (18), pp. 5979-83. Date of Electronic Publication: 2012 Aug 02.
Publication Year :: 2012
Abstract: This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38α activity and 24h coverage in the rat arthritis efficacy model.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)

Subjects :: Animals
Dogs
Dose-Response Relationship, Drug
Haplorhini
Humans
Mitogen-Activated Protein Kinase 14 metabolism
Molecular Structure
Protein Kinase Inhibitors administration & dosage
Pyridazines administration & dosage
Pyridines administration & dosage
Rats
Structure-Activity Relationship
Mitogen-Activated Protein Kinase 14 antagonists & inhibitors
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacology
Pyridazines chemical synthesis
Pyridazines pharmacology
Pyridines chemical synthesis
Pyridines pharmacology

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