2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
Article Details
- CitationCopy to clipboard
Friesen RW, Brideau C, Chan CC, Charleson S, Deschenes D, Dube D, Ethier D, Fortin R, Gauthier JY, Girard Y, Gordon R, Greig GM, Riendeau D, Savoie C, Wang Z, Wong E, Visco D, Xu LJ, Young RN
2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors.
Bioorg Med Chem Lett. 1998 Oct 6;8(19):2777-82.
- PubMed ID
- 9873621 [ View in PubMed]
- Abstract
A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a substituent at C5 of the central pyridine. 5- Chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Etoricoxib Prostaglandin G/H synthase 2 IC 50 (nM) 1100 N/A N/A Details Etoricoxib Prostaglandin G/H synthase 2 IC 50 (nM) 81 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 500 N/A N/A Details Indomethacin Prostaglandin G/H synthase 2 IC 50 (nM) 26 N/A N/A Details