[(Arylcarbonyl)oxy]propanolamines. 1. Novel beta-blockers with ultrashort duration of action

J Med Chem. 1984 Aug;27(8):1007-16. doi: 10.1021/jm00374a013.

Abstract

Novel [(arylcarbonyl)oxy]propanolamines were synthesized and investigated as potential ultrashort-acting beta-adrenergic receptor blockers. Many of these analogues exhibited good potency and short duration. The N-ureidoalkyl analogue 85 (ACC-9089) has a potency equal to propranolol and a duration of action of about 21 min in the dog. It has been selected as a candidate for further clinical study. Structure-activity relationships and structure-duration relationships for these new beta-blockers are also discussed.

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis*
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Dogs
  • Guinea Pigs
  • Half-Life
  • Heart Rate / drug effects
  • Humans
  • In Vitro Techniques
  • Isoproterenol / pharmacology
  • Propanolamines / chemical synthesis*
  • Propanolamines / pharmacology
  • Structure-Activity Relationship
  • Time Factors
  • Trachea / drug effects

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines
  • Isoproterenol