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
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Research Support, Non-U.S. Gov't
MeSH terms
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Amphetamine / antagonists & inhibitors
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Amphetamine / pharmacology
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Animals
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Blood Pressure / drug effects
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Brain / drug effects
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Brain / enzymology*
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Clonidine / pharmacology
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Female
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Hydrazines / chemical synthesis*
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Hydrazines / pharmacology
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Hydrazines / toxicity
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Hydrolysis
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In Vitro Techniques
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Kynuramine
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Lethal Dose 50
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Male
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Mice
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Mitochondria / drug effects
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Mitochondria / enzymology*
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Monoamine Oxidase Inhibitors / chemical synthesis*
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Monoamine Oxidase Inhibitors / pharmacology
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Monoamine Oxidase Inhibitors / toxicity
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Motor Activity / drug effects
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Rats
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Rats, Sprague-Dawley
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Spectrometry, Fluorescence
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Thiazoles / chemical synthesis*
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Thiazoles / pharmacology
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Thiazoles / toxicity
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Tyramine / pharmacology
Substances
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Hydrazines
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Monoamine Oxidase Inhibitors
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Thiazoles
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Kynuramine
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Amphetamine
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Clonidine
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Tyramine