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3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility |
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| Authors: | Black W Cameron Brideau Christine Chan Chi Chung Charleson Stella Cromlish Wanda Gordon Robert Grimm Erich L Hughes Gregory Leger Serge Li Chun Sing Riendeau Denis Thérien Michel Wang Zhaoyin Xu Li Jing Prasit Petpiboon |
| Affiliation: | Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8. blackc@merck.com |
| 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. |
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