2,3-Diarylbenzopyran derivatives as a novel class of selective cyclooxygenase-2 inhibitors

Bioorg Med Chem Lett. 2003 Feb 10;13(3):413-7. doi: 10.1016/s0960-894x(02)00952-6.

Abstract

A new series of cyclooxygenase-2(COX-2) inhibitors with naturally occurring flavone as the main skeleton has been synthesized and their biological activities were evaluated for cyclooxygenase inhibitory activity. Rational structural modifications were applied to potent COX-2 inhibitors to obtain the desired pharmacokinetic profiles for improved oral anti-inflammatory activity.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology
  • Benzopyrans / chemical synthesis*
  • Benzopyrans / pharmacology*
  • Carrageenan
  • Chemical Phenomena
  • Chemistry, Physical
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors / chemical synthesis*
  • Cyclooxygenase Inhibitors / pharmacokinetics
  • Cyclooxygenase Inhibitors / pharmacology*
  • Edema / chemically induced
  • Edema / prevention & control
  • Indicators and Reagents
  • Isoenzymes / metabolism*
  • Male
  • Membrane Proteins
  • Prostaglandin-Endoperoxide Synthases / metabolism*
  • Rats
  • Rats, Sprague-Dawley

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Benzopyrans
  • Cyclooxygenase 2 Inhibitors
  • Cyclooxygenase Inhibitors
  • Indicators and Reagents
  • Isoenzymes
  • Membrane Proteins
  • Carrageenan
  • Cyclooxygenase 1
  • Cyclooxygenase 2
  • Prostaglandin-Endoperoxide Synthases
  • Ptgs1 protein, rat