Antiinflammatory activity of N-(2-benzoylphenyl)alanine derivatives

J Med Chem. 1984 Oct;27(10):1317-21. doi: 10.1021/jm00376a016.

Abstract

A series of N-(2-benzoylphenyl)alanine derivatives were synthesized and tested for antiinflammatory activity in the Evans blue-carrageenan induced pleural effusion assay. The target compounds were envisioned to bind to a receptor site on the cyclooxygenase enzyme by a mechanism first proposed by Appleton and Brown. Of the 21 compounds prepared, two were found to be one-tenth as potent as indomethacin in the pleurisy model and one compound was tested and found to be weakly active in the adjuvant arthritis model.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Arthritis / drug therapy*
  • Arthritis, Experimental / drug therapy*
  • Chemical Phenomena
  • Chemistry
  • Disease Models, Animal
  • Indicators and Reagents
  • Indomethacin / therapeutic use
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemical synthesis
  • Phenylalanine / therapeutic use
  • Pleurisy / drug therapy
  • Rats
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents
  • Indicators and Reagents
  • Phenylalanine
  • N-(2-benzoylphenyl)alanine
  • Indomethacin