1. Academic Validation
  2. 3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility

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. doi: 10.1016/s0960-894x(03)00046-5.
W Cameron Black 1 Christine Brideau Chi Chung Chan Stella Charleson Wanda Cromlish Robert Gordon Erich L Grimm Gregory Hughes Serge Leger Chun Sing Li Denis Riendeau Michel Thérien Zhaoyin Wang Li Jing Xu Petpiboon Prasit
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8. [email protected]
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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