Synthesis and adrenolytic activity of new propanolamines

Molecules. 2010 May 28;15(6):3887-904. doi: 10.3390/molecules15063887.

Abstract

The synthesis of (2R,S)-1-(6-methoxy-4-(methoxymethyl)-1H-indol-5-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol and (2R,S)-1-(4-methoxy-6-(methoxymethyl)-1H-indol-5-yloxy)-3-(2-(2-methoxyphenoxy)ethylamino)propan-2-ol is described. The compounds were tested for electrographic, antiarrhythmic, hypotensive, and spasmolytic activity, as well as for alpha(1)-, alpha(2)- and beta(1)-adrenoceptor binding affinity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adrenergic Antagonists / chemical synthesis*
  • Adrenergic Antagonists / chemistry
  • Adrenergic Antagonists / pharmacology*
  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-2 Receptor Antagonists
  • Adrenergic beta-1 Receptor Antagonists
  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis
  • Anti-Arrhythmia Agents / chemistry
  • Anti-Arrhythmia Agents / therapeutic use
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / drug therapy
  • Blood Pressure / drug effects
  • Electrocardiography
  • Epinephrine / toxicity
  • Ileum / drug effects
  • In Vitro Techniques
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Propanolamines / chemical synthesis*
  • Propanolamines / chemistry
  • Propanolamines / therapeutic use*
  • Rabbits
  • Rats

Substances

  • Adrenergic Antagonists
  • Adrenergic alpha-1 Receptor Antagonists
  • Adrenergic alpha-2 Receptor Antagonists
  • Adrenergic beta-1 Receptor Antagonists
  • Anti-Arrhythmia Agents
  • Propanolamines
  • Epinephrine