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

Publication ,  Journal Article
Black, WC; Brideau, C; Chan, CC; Charleson, S; Cromlish, W; Gordon, R; Grimm, EL; Hughes, G; Leger, S; Li, CS; Riendeau, D; Thérien, M ...
Published in: Bioorganic & medicinal chemistry letters
March 2003

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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Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

March 2003

Volume

13

Issue

6

Start / End Page

1195 / 1198

Related Subject Headings

  • Substrate Specificity
  • Structure-Activity Relationship
  • Solubility
  • Rats
  • Prostaglandin-Endoperoxide Synthases
  • Pain
  • Membrane Proteins
  • Medicinal & Biomolecular Chemistry
  • Isoenzymes
  • Humans
 

Citation

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Black, W. C., Brideau, C., Chan, C. C., Charleson, S., Cromlish, W., Gordon, R., … Prasit, P. (2003). 3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility. Bioorganic & Medicinal Chemistry Letters, 13(6), 1195–1198. https://doi.org/10.1016/s0960-894x(03)00046-5
Black, W Cameron, Christine Brideau, Chi Chung Chan, Stella Charleson, Wanda Cromlish, Robert Gordon, Erich L. Grimm, et al. “3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.Bioorganic & Medicinal Chemistry Letters 13, no. 6 (March 2003): 1195–98. https://doi.org/10.1016/s0960-894x(03)00046-5.
Black WC, Brideau C, Chan CC, Charleson S, Cromlish W, Gordon R, et al. 3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility. Bioorganic & medicinal chemistry letters. 2003 Mar;13(6):1195–8.
Black, W. Cameron, et al. “3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility.Bioorganic & Medicinal Chemistry Letters, vol. 13, no. 6, Mar. 2003, pp. 1195–98. Epmc, doi:10.1016/s0960-894x(03)00046-5.
Black WC, Brideau C, Chan CC, Charleson S, Cromlish W, Gordon R, Grimm EL, Hughes G, Leger S, Li CS, Riendeau D, Thérien M, Wang Z, Xu LJ, Prasit P. 3,4-Diaryl-5-hydroxyfuranones: highly selective inhibitors of cyclooxygenase-2 with aqueous solubility. Bioorganic & medicinal chemistry letters. 2003 Mar;13(6):1195–1198.
Journal cover image

Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

March 2003

Volume

13

Issue

6

Start / End Page

1195 / 1198

Related Subject Headings

  • Substrate Specificity
  • Structure-Activity Relationship
  • Solubility
  • Rats
  • Prostaglandin-Endoperoxide Synthases
  • Pain
  • Membrane Proteins
  • Medicinal & Biomolecular Chemistry
  • Isoenzymes
  • Humans