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The discovery of (R)-2-(sec-butylamino)-N-(2-methyl-5-(methylcarbamoyl)phenyl) thiazole-5-carboxamide (BMS-640994)-A potent and efficacious p38alpha MAP kinase inhibitor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Mar 15; Vol. 18 (6), pp. 1762-7. Date of Electronic Publication: 2008 Feb 16. - Publication Year :
- 2008
-
Abstract
- A novel structural class of p38alpha MAP kinase inhibitors has been identified via iterative SAR studies of a focused deck screen hit. Optimization of the lead series generated 6e, BMS-640994, a potent and selective p38alpha inhibitor that is orally efficacious in rodent models of acute and chronic inflammation.
- Subjects :
- Animals
Arthritis drug therapy
Caco-2 Cells
Cell Membrane Permeability drug effects
Cells, Cultured
Crystallography, X-Ray
Cytochrome P-450 Enzyme Inhibitors
Cytochrome P-450 Enzyme System metabolism
Ether-A-Go-Go Potassium Channels antagonists & inhibitors
Humans
Lipopolysaccharides pharmacology
Male
Mice
Microsomes, Liver drug effects
Mitogen-Activated Protein Kinase 14 metabolism
Molecular Structure
Monocytes cytology
Monocytes drug effects
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacokinetics
Rats
Rats, Inbred Lew
Structure-Activity Relationship
Thiazoles chemical synthesis
Thiazoles pharmacokinetics
Tumor Necrosis Factor-alpha metabolism
Mitogen-Activated Protein Kinase 14 antagonists & inhibitors
Protein Kinase Inhibitors pharmacology
Thiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18313298
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.02.031