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Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jan 01; Vol. 18 (1), pp. 324-8. Date of Electronic Publication: 2007 Oct 17. - Publication Year :
- 2008
-
Abstract
- The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38alpha are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model.
- Subjects :
- Administration, Oral
Amides chemistry
Amides pharmacokinetics
Animals
Arthritis, Experimental drug therapy
Arthritis, Experimental metabolism
Biphenyl Compounds chemistry
Biphenyl Compounds pharmacokinetics
Crystallography, X-Ray
Models, Molecular
Molecular Conformation
Oxadiazoles chemistry
Oxadiazoles pharmacokinetics
Oxadiazoles pharmacology
Piperazines chemistry
Piperazines pharmacokinetics
Piperazines pharmacology
Protein Binding
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors pharmacokinetics
Rats
Structure-Activity Relationship
p38 Mitogen-Activated Protein Kinases chemistry
p38 Mitogen-Activated Protein Kinases metabolism
Amides pharmacology
Biphenyl Compounds pharmacology
Protein Kinase Inhibitors pharmacology
p38 Mitogen-Activated Protein Kinases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 1
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 17981461
- Full Text :
- https://doi.org/10.1016/j.bmcl.2007.10.043