3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
Article Details
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Black WC, Brideau C, Chan CC, Charleson S, Cromlish W, Gordon R, Grimm EL, Hughes G, Leger S, Li CS, Riendeau D, Therien M, Wang Z, Xu LJ, Prasit P
3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.
Bioorg Med Chem Lett. 2003 Mar 24;13(6):1195-8.
- PubMed ID
- 12643942 [ View in PubMed]
- Abstract
The introduction of a hydroxyl group into the 5-position of the diaryl furanone system provides highly selective inhibitors of cyclooxygenase-2. These molecules can be converted into their sodium salts which are water soluble, facilitating intravenous formulation. These salts show excellent potency in rat models of pain, fever and inflammation.
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 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