Dibenzotropone- and dibenzosuberonecarboxylic acids with bronchodilator activity

J Med Chem. 1979 Nov;22(11):1357-63. doi: 10.1021/jm00197a015.

Abstract

The syntheses of 44 5H-dibenzo[a,d]cyclohepten-5-one derivatives bearing a carboxyl gropu at the 1, 2, 3, or 10 position and various substituents at the 7, 8, or 9 position are described. Some of the compounds showed significant bronchodilator activity in guinea pigs and protected the animals against a histamine challenge administered either by aerosol or intravenously. The most active compounds were 10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-one-2-carboxylic acids bearing a methyl or halogen substituent at the 9 position. These compounds were approximately as active as aminophylline by intraperitoneal administration.

MeSH terms

  • Airway Resistance / drug effects
  • Animals
  • Bronchodilator Agents / chemical synthesis*
  • Carboxylic Acids / chemical synthesis*
  • Carboxylic Acids / pharmacology
  • Female
  • Guinea Pigs
  • Histamine Antagonists
  • In Vitro Techniques
  • Structure-Activity Relationship
  • Trachea / drug effects

Substances

  • Bronchodilator Agents
  • Carboxylic Acids
  • Histamine Antagonists