Comparative structure-activity relationship studies of 1-(5-methylsulfonylpyrid-2-yl)-5-alkyl and (hetero)aryl triazoles and pyrazoles in canine COX inhibition
| Autor: | Donald W. Mann, Carol F. Petras, Chao Li, Subas M. Sakya, Andrei Shavnya, Michael P. Lynch, Burton H. Jaynes, Cheng Hengmiao, Bryson Rast, David A. Koss, Jin Li, Michelle L. Haven, Scott B. Seibel |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Alkylation
Stereochemistry Clinical Biochemistry Triazole Pharmaceutical Science Pyrazole Biochemistry Chemical synthesis chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Dogs Drug Discovery Side chain Structure–activity relationship Animals Sulfhydryl Compounds Molecular Biology biology Cyclooxygenase 2 Inhibitors Molecular Structure Chemistry Aryl Organic Chemistry Active site Triazoles Enzyme inhibitor Cyclooxygenase 2 biology.protein Molecular Medicine Pyrazoles Ethers |
| Zdroj: | Bioorganicmedicinal chemistry letters. 18(3) |
| ISSN: | 1464-3405 |
| Popis: | Structure–activity relationship (SAR) studies of novel 5-alkyl and 5-aryl/heteroaryl substituted 1,2,4-triazoles are described. The in vitro activity is compared to the pyrazole class of compounds with analogous side chains to delineate the contribution of the triazole ring nitrogen in binding to the active site. Both series are quite potent and selective in the canine whole blood (CWB) COX-2 assay, suggesting the increased binding contribution of the hydrophobic side chains. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect