Pharmacological properties of some aminoalkanolic derivatives of xanthone

Pharmazie. 2001 Jul;56(7):567-72.

Abstract

A series of appropriate aminoisopropanoloxy derivatives of 2-, 3- or 6-xanthone was synthesized and evaluated for anticonvulsant activity in the maximal electroshock seizure (MES) and subcutaneous pentylenetetrazole seizure threshold (ScMet) assays and for neurotoxicity (TOX). The most interesting result was the anticonvulsant activity of (+/-)-3-(2-propylamino)-1- [(2-methyl)-6-xanthonoxy]-2-propanol hydrochloride (10), which displayed anti-MES activity with a protective index (TD50/ED50) of 0.80. Some of the obtained compounds were also tested for their effect on the circulatory system (influence on the non-working heart perfusion, protection against adrenaline induced-arrhythmia) and acute toxicity.

MeSH terms

  • Animals
  • Anti-Arrhythmia Agents / chemical synthesis
  • Anti-Arrhythmia Agents / pharmacology
  • Anticonvulsants / chemical synthesis*
  • Anticonvulsants / pharmacology*
  • Anticonvulsants / toxicity
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / prevention & control
  • Coronary Circulation / drug effects
  • Electroshock
  • Epinephrine / pharmacology
  • Hemodynamics / drug effects
  • Lethal Dose 50
  • Male
  • Mice
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Seizures / prevention & control
  • Xanthines / chemical synthesis*
  • Xanthines / pharmacology*
  • Xanthines / toxicity

Substances

  • Anti-Arrhythmia Agents
  • Anticonvulsants
  • Xanthines
  • Epinephrine