Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase

Bioorganic & Medicinal Chemistry Letters
2009.0

Abstract

The identification and evolution of a series of potent and selective p38 inhibitors is described. p38 inhibitors based on a N-benzyl pyridinone high-throughput screening hit were prepared and their SAR explored. Their design was guided by ligand bound co-crystals of p38alpha. These efforts resulted in the identification of 12r and 19 as orally active inhibitors of p38 with significant efficacy in both acute and chronic models of inflammation.

DOI： 10.1016/j.bmcl.2009.08.082

Knowledge Graph

Similar Paper

Discovery of N-substituted pyridinones as potent and selective inhibitors of p38 kinase
Bioorganic & Medicinal Chemistry Letters 2009.0
The Discovery of VX-745: A Novel and Selective p38α Kinase Inhibitor
ACS Medicinal Chemistry Letters 2011.0
Novel, potent and selective anilinoquinazoline and anilinopyrimidine inhibitors of p38 MAP kinase
Bioorganic & Medicinal Chemistry Letters 2004.0
Synthesis and pharmacological characterization of a potent, orally active p38 kinase inhibitor
Bioorganic & Medicinal Chemistry Letters 2002.0
Benzimidazolone p38 inhibitors
Bioorganic & Medicinal Chemistry Letters 2004.0
Pyridinylquinoxalines and Pyridinylpyridopyrazines as Lead Compounds for Novel p38α Mitogen-Activated Protein Kinase Inhibitors
Journal of Medicinal Chemistry 2010.0
Discovery of a new class of p38 kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2000.0
1-Phenyl-5-pyrazolyl ureas: potent and selective p38 kinase inhibitors
Bioorganic & Medicinal Chemistry Letters 2000.0
The discovery of kinase inhibitors by a combination of diversity-oriented synthesis and selective screening
MedChemComm 2016.0
A novel series of p38 MAP kinase inhibitors for the potential treatment of rheumatoid arthritis
Bioorganic & Medicinal Chemistry Letters 2004.0