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.
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