Antiinflammatory agents. 3. Synthesis and pharmacological evaluation of 2-amino-3-benzoylphenylacetic acid and analogues

J Med Chem. 1984 Nov;27(11):1379-88. doi: 10.1021/jm00377a001.

Abstract

A series of substituted derivatives of 2-amino-3-benzoylphenylacetic acid (amfenac) has been synthesized and evaluated for antiinflammatory, analgesic, and cyclooxygenase inhibiting activity. Several derivatives including 157 (4'-chloro), 158 (4'-bromo), and 182 (5-chloro, 4'-bromo) were more potent than indomethacin in these assays.

MeSH terms

  • Analgesia
  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Arthritis, Experimental / drug therapy
  • Chemical Phenomena
  • Chemistry
  • Cyclooxygenase Inhibitors
  • Female
  • Indomethacin / therapeutic use
  • Intestines / drug effects
  • Isomerism
  • Male
  • Phenylacetates / chemical synthesis*
  • Phenylacetates / therapeutic use
  • Phenylacetates / toxicity
  • Rats
  • Rats, Inbred Strains
  • Stomach / drug effects

Substances

  • Anti-Inflammatory Agents
  • Cyclooxygenase Inhibitors
  • Phenylacetates
  • amfenac
  • Indomethacin