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Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase
- Source :
- Bioorganicmedicinal chemistry letters. 21(14)
- Publication Year :
- 2011
-
Abstract
- A series of inhibitors of mammalian 15-lipoxygenase (15-LO) based on a 3,4,5-tri-substituted pyrazole scaffold is described. Replacement of a sulfonamide functionality in the lead series with a sulfamide group resulted in improved physicochemical properties generating analogs with enhanced inhibition in cell-based and whole blood assays.
- Subjects :
- Clinical Biochemistry
Pharmaceutical Science
CHO Cells
Pyrazole
Biochemistry
Chemical synthesis
chemistry.chemical_compound
Lipoxygenase
Structure-Activity Relationship
Cricetulus
Cricetinae
Drug Discovery
Hydroxyeicosatetraenoic Acids
Structure–activity relationship
Animals
Arachidonate 15-Lipoxygenase
Humans
Lipoxygenase Inhibitors
Molecular Biology
Sulfamide
chemistry.chemical_classification
Sulfonamides
biology
Organic Chemistry
Amides
Sulfonamide
Enzyme
chemistry
Enzyme inhibitor
biology.protein
Molecular Medicine
Pyrazoles
Rabbits
Subjects
Details
- ISSN :
- 14643405
- Volume :
- 21
- Issue :
- 14
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....7d913c6022d0118d72a258707bb441c9