Synthesis and beta-adrenergic blocking activity of oxipropanolamines of 3,4-dihydro-3-oxo-2H(1,4)benzothiazine

Farmaco Sci. 1987 Jan;42(1):61-75.

Abstract

The synthesis of a series of oxypropanolamines of 3,4-dihydro-3-oxo-2H(1,4)benzothiazine is reported. Some of these compounds proved more potent than propranolol and carteolol as beta-adrenergic blocking agents in in vitro tests. The 8-(3-tert-butylamino-2-hydroxy)propoxy-3,4-dihydro-3-oxo-2H(1,4) benzothiazine fumarate (XVI a), which gave better results, confirmed its remarkable activity in in vivo tests.

MeSH terms

  • Adrenergic beta-Antagonists / chemical synthesis*
  • Animals
  • Chemical Phenomena
  • Chemistry
  • Female
  • Guinea Pigs
  • Heart Rate / drug effects
  • In Vitro Techniques
  • Isoproterenol / antagonists & inhibitors
  • Male
  • Mice
  • Propanolamines / chemical synthesis*
  • Propanolamines / pharmacology
  • Propanolamines / toxicity
  • Rats
  • Rats, Inbred SHR
  • Thiazines / chemical synthesis*
  • Thiazines / pharmacology
  • Thiazines / toxicity

Substances

  • Adrenergic beta-Antagonists
  • Propanolamines
  • Thiazines
  • Isoproterenol