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
  • 1. Merck Frosst Centre for Therapeutic Research, PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8. [email protected]
PMID: 12643942 DOI: 10.1016/s0960-894x(03)00046-5
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.