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5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure–activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog
5-Heteroatom substituted pyrazoles as canine COX-2 inhibitors. Part 1: Structure–activity relationship studies of 5-alkylamino pyrazoles and discovery of a potent, selective, and orally active analog
- Source :
- Bioorganic & Medicinal Chemistry Letters. 16:288-292
- Publication Year :
- 2006
- Publisher :
- Elsevier BV, 2006.
-
Abstract
- Structure-activity relationship (SAR) studies of the novel 2-[3-di and trifluoromethyl-5-alkylamino pyrazo-1-yl]-5-methanesulfonyl (SO(2)Me)/sulfamoyl (SO(2)NH(2))-pyridine derivatives for canine COX enzymes are described. The studies led to the identification of 2e as lead with potent in vitro activity, selectivity, and in vivo activity in dogs and cats.
- Subjects :
- Stereochemistry
Clinical Biochemistry
Heteroatom
Drug Evaluation, Preclinical
Administration, Oral
Pharmaceutical Science
In Vitro Techniques
Biochemistry
Chemical synthesis
Sulfone
Structure-Activity Relationship
chemistry.chemical_compound
Dogs
In vivo
Drug Discovery
Animals
Structure–activity relationship
Molecular Biology
chemistry.chemical_classification
Cyclooxygenase 2 Inhibitors
Molecular Structure
biology
Organic Chemistry
In vitro
Disease Models, Animal
Enzyme
chemistry
Cyclooxygenase 2
Enzyme inhibitor
Cats
biology.protein
Pyrazoles
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 16
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....f287d246c2a3746f106e9752c3bac59e
- Full Text :
- https://doi.org/10.1016/j.bmcl.2005.10.006