Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
Article Details
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Lau CK, Brideau C, Chan CC, Charleson S, Cromlish WA, Ethier D, Gauthier JY, Gordon R, Guay J, Kargman S, Li CS, Prasit P, Riendeau D, Therien M, Visco DM, Xu L
Synthesis and biological evaluation of 3-heteroaryloxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors.
Bioorg Med Chem Lett. 1999 Nov 15;9(22):3187-92.
- PubMed ID
- 10576685 [ View in PubMed]
- Abstract
A series of 3-heteroaryloxy4-phenyl-2-5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Celecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 2 N/A N/A Details Celecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 1000 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 Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 20 N/A N/A Details Rofecoxib Prostaglandin G/H synthase 2 IC 50 (nM) 500 N/A N/A Details