Novel 2-(4-methylsulfonylphenyl)pyrimidine derivatives as highly potent and specific COX-2 inhibitors
-
Add time:08/17/2019 Source:sciencedirect.com
New series of 2-(4-methylsulfonylphenyl) and 2-(4-sulfamoylphenyl)pyrimidines were synthesized and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). COX-1 and COX-2 inhibitory activity of these compounds was determined using purified enzyme (PE) and human whole blood (HWB) assays. Extensive structure–activity relationship (SAR) work was carried out within these series, and a wide number of potent and specific COX-2 inhibitors were identified (HWB COX-2 IC50 = 2.4–0.3 nM and 80- to 780-fold more selective than rofecoxib).
We also recommend Trading Suppliers and Manufacturers of 4-FLUORO-N-(2-[4-(7-HYDROXY-NAPHTHALEN-1-YL)-PIPERAZIN-1-YL]-ETHYL)-BENZAMIDE (cas 135722-26-8). Pls Click Website Link as below: cas 135722-26-8 suppliers
Prev:Research paperDesign, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization
Next:Aldol reactions of 2-thioxotetrahydropyrimidin-4(1H)-ones: stereoregulations from endo- and exocyclic chiral centres) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- Access to 2′,3′-dihydro-1′H-spiro[indoline-3,4′-pyridin]-2-ones via amino acid derived phosphine-catalyzed asymmetric [4+2] annulation with easily available oxindole-derived α,β-unsaturated imines08/19/2019
- Aldol reactions of 2-thioxotetrahydropyrimidin-4(1H)-ones: stereoregulations from endo- and exocyclic chiral centres08/18/2019
- Research paperDesign, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization08/16/2019
