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'Reverse' alpha-ketoamide-based p38 MAP kinase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Oct 15; Vol. 18 (20), pp. 5456-9. Date of Electronic Publication: 2008 Sep 11. - Publication Year :
- 2008
-
Abstract
- We have identified a second series of potent p38 inhibitors. As with our first generation series, these compounds are based on an alpha-ketoamide scaffold. The reversal of the ketoamide order, however, introduces more chemical flexibility and in addition results in improve potencies against p38.
- Subjects :
- Allosteric Site
Anti-Inflammatory Agents pharmacology
Chemistry, Pharmaceutical methods
Cytokines metabolism
Drug Design
Humans
Inflammation drug therapy
Inhibitory Concentration 50
Models, Chemical
Models, Molecular
Structure-Activity Relationship
Amides chemistry
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Ketones chemistry
p38 Mitogen-Activated Protein Kinases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 20
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18835164
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.09.028