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Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).

Publication ,  Journal Article
Nicoll-Griffith, DA; Yergey, JA; Trimble, LA; Silva, JM; Li, C; Chauret, N; Gauthier, JY; Grimm, E; Léger, S; Roy, P; Thérien, M; Wang, Z ...
Published in: Bioorganic & medicinal chemistry letters
December 2000

Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx) were prepared by synthetic or biosynthetic methods. Metabolites include products of oxidation, glucuronidation, reduction and hydrolytic ring opening. Based on an in vitro whole blood assay, none of the known human metabolites of rofecoxib inhibits COX-1 nor contributes significantly to the inhibition of COX-2.

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Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

December 2000

Volume

10

Issue

23

Start / End Page

2683 / 2686

Related Subject Headings

  • Sulfones
  • Rats
  • Prostaglandin-Endoperoxide Synthases
  • Membrane Proteins
  • Medicinal & Biomolecular Chemistry
  • Lactones
  • Isoenzymes
  • Humans
  • Drug Evaluation, Preclinical
  • Cyclooxygenase Inhibitors
 

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Nicoll-Griffith, D. A., Yergey, J. A., Trimble, L. A., Silva, J. M., Li, C., Chauret, N., … Riendeau, D. (2000). Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx). Bioorganic & Medicinal Chemistry Letters, 10(23), 2683–2686. https://doi.org/10.1016/s0960-894x(00)00538-2
Nicoll-Griffith, D. A., J. A. Yergey, L. A. Trimble, J. M. Silva, C. Li, N. Chauret, J. Y. Gauthier, et al. “Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).Bioorganic & Medicinal Chemistry Letters 10, no. 23 (December 2000): 2683–86. https://doi.org/10.1016/s0960-894x(00)00538-2.
Nicoll-Griffith DA, Yergey JA, Trimble LA, Silva JM, Li C, Chauret N, et al. Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx). Bioorganic & medicinal chemistry letters. 2000 Dec;10(23):2683–6.
Nicoll-Griffith, D. A., et al. “Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx).Bioorganic & Medicinal Chemistry Letters, vol. 10, no. 23, Dec. 2000, pp. 2683–86. Epmc, doi:10.1016/s0960-894x(00)00538-2.
Nicoll-Griffith DA, Yergey JA, Trimble LA, Silva JM, Li C, Chauret N, Gauthier JY, Grimm E, Léger S, Roy P, Thérien M, Wang Z, Prasit P, Zamboni R, Young RN, Brideau C, Chan CC, Mancini J, Riendeau D. Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx). Bioorganic & medicinal chemistry letters. 2000 Dec;10(23):2683–2686.
Journal cover image

Published In

Bioorganic & medicinal chemistry letters

DOI

EISSN

1464-3405

ISSN

0960-894X

Publication Date

December 2000

Volume

10

Issue

23

Start / End Page

2683 / 2686

Related Subject Headings

  • Sulfones
  • Rats
  • Prostaglandin-Endoperoxide Synthases
  • Membrane Proteins
  • Medicinal & Biomolecular Chemistry
  • Lactones
  • Isoenzymes
  • Humans
  • Drug Evaluation, Preclinical
  • Cyclooxygenase Inhibitors