MAOI activity of some novel series of substituted thiazol-2-yl-hydrazines

Pharmazie. 1992 Dec;47(12):902-10.

Abstract

Three series of 2-thiazolylhydrazines were synthetized and evaluated for their MAO inhibitory (MAOI) activity, both by in vivo tests, to assay their influence on several MAOI activity-related parameters (the variation on blood pressure induced by tyramine and clonidine and L-amfetamine-induced hypermotility) and in vitro tests, to assay their effect on rat brain mitochondria by a kinuramine fluorimetric assay. In vivo, all the tested compounds significatively influenced the evaluative parameters used. As regards in vitro test, all compounds displayed MAOI activity at a concentration of 1.10(-4) mol.l-1, which was significant in several cases. In the discussion of the results, the influence of the structure on the biological activity of the prepared compounds was delineated.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amphetamine / antagonists & inhibitors
  • Amphetamine / pharmacology
  • Animals
  • Blood Pressure / drug effects
  • Brain / drug effects
  • Brain / enzymology*
  • Clonidine / pharmacology
  • Female
  • Hydrazines / chemical synthesis*
  • Hydrazines / pharmacology
  • Hydrazines / toxicity
  • Hydrolysis
  • In Vitro Techniques
  • Kynuramine
  • Lethal Dose 50
  • Male
  • Mice
  • Mitochondria / drug effects
  • Mitochondria / enzymology*
  • Monoamine Oxidase Inhibitors / chemical synthesis*
  • Monoamine Oxidase Inhibitors / pharmacology
  • Monoamine Oxidase Inhibitors / toxicity
  • Motor Activity / drug effects
  • Rats
  • Rats, Sprague-Dawley
  • Spectrometry, Fluorescence
  • Thiazoles / chemical synthesis*
  • Thiazoles / pharmacology
  • Thiazoles / toxicity
  • Tyramine / pharmacology

Substances

  • Hydrazines
  • Monoamine Oxidase Inhibitors
  • Thiazoles
  • Kynuramine
  • Amphetamine
  • Clonidine
  • Tyramine