3-[4-(Methylsulfonyl)phenyl]-5-(trifluoromethyl)(2-pyridyl) Phenyl Ketone as a Potent and Orally Active Cyclooxygenase-2 Selective Inhibitor: Synthesis and Biological Evaluation
✍ Scribed by Khanapure, Subhash P.; Augustyniak, Michael E.; Earl, Richard A.; Garvey, David S.; Letts, L. Gordon; Martino, Allison M.; Murty, Madhavi G.; Schwalb, David J.; Shumway, Matthew J.; Trocha, Andrzej M.
- Book ID
- 111898040
- Publisher
- American Chemical Society
- Year
- 2005
- Tongue
- English
- Weight
- 104 KB
- Volume
- 48
- Category
- Article
- ISSN
- 0022-2623
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## Abstract Four series of 5‐methylsulfonyl‐1‐phenyl‐1__H__‐indole‐2‐carboxylic acid alkyl esters (family **A**), ‐2‐carbonitriles (family **B**), ‐2‐carboxamides (family **C**), and 2‐benzoyl‐5‐methylsulfonyl‐1‐phenyl‐1__H__‐indoles (family **D**) were prepared and evaluated for their ability to i
## Abstract For Abstract see ChemInform Abstract in Full Text.
Fourteen new 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5-LOX with IC 50 in the range of 0.10-9.87 lM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (I