Flavones. 1. Synthesis and antihypertensive activity of (3-phenylflavonoxy)propanolamines without beta-adrenoceptor antagonism

J Med Chem. 1987 May;30(5):788-92. doi: 10.1021/jm00388a007.

Abstract

The synthesis of a series of (3-phenylflavonoxy)propanolamines is described. These compounds were evaluated for potential antihypertensive activity in spontaneously hypertensive rats, as well as for in vivo and in vitro evidence of beta-adrenoceptor antagonism. Some of the compounds of this series exhibited effective antihypertensive properties but did not antagonize beta-adrenergic receptors. These active compounds represent a unique series of effective antihypertensive agents that, despite possessing structural characteristics typical of beta-blockers, does not have beta-adrenergic receptor blocking activity.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic beta-Antagonists
  • Animals
  • Antihypertensive Agents / chemical synthesis
  • Antihypertensive Agents / pharmacology
  • Chemical Phenomena
  • Chemistry
  • Flavonoids / chemical synthesis
  • Flavonoids / pharmacology
  • Flavonoids / therapeutic use*
  • Hypertension / drug therapy*
  • Male
  • Propanolamines / chemical synthesis
  • Propanolamines / pharmacology
  • Propanolamines / therapeutic use*
  • Rats
  • Rats, Inbred SHR
  • Rats, Inbred WKY
  • Receptors, Adrenergic, beta / drug effects*
  • Structure-Activity Relationship

Substances

  • Adrenergic beta-Antagonists
  • Antihypertensive Agents
  • Flavonoids
  • Propanolamines
  • Receptors, Adrenergic, beta