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Reducing ion channel activity in a series of 4-heterocyclic arylamide FMS inhibitors
- Source :
- Bioorganicmedicinal chemistry letters. 20(13)
- Publication Year :
- 2010
-
Abstract
- During efforts to improve the bioavailability of FMS kinase inhibitors 1 and 2, a series of saturated and aromatic 4-heterocycles of reduced basicity were prepared and evaluated in an attempt to also improve the cardiovascular safety profile over lead arylamide 1, which possessed ion channel activity. The resultant compounds retained excellent potency and exhibited diminished ion channel activity.
- Subjects :
- Models, Molecular
Nitrile
Molecular model
Stereochemistry
Clinical Biochemistry
Pharmaceutical Science
Stereoisomerism
Receptor, Macrophage Colony-Stimulating Factor
Biochemistry
Chemical synthesis
chemistry.chemical_compound
Structure-Activity Relationship
Heterocyclic Compounds
Drug Discovery
Structure–activity relationship
Molecular Biology
Protein Kinase Inhibitors
chemistry.chemical_classification
biology
Dose-Response Relationship, Drug
Molecular Structure
Organic Chemistry
Combinatorial chemistry
Amides
Bioavailability
Enzyme
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Oxidation-Reduction
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 20
- Issue :
- 13
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....8c5510c9a3e081ba95d9c48c2a863b4c