MAOI activity of some novel series of substituted thiazol-2-yl-hydrazines.
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.
Mazzone
G
G
Institute of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Catania, Italy.
Pignatello
R
R
Panico
A
A
Mazzone
S
S
Puglisi
G
G
Pennisi
G
G
Raciti
G
G
Mazzone
P
P
Matera
M
M
D000661:Amphetamine / Q000037:antagonists & inhibitors / Q000494:pharmacology; D000818:Animals; D001794:Blood Pressure / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000201:enzymology*; D003000:Clonidine / Q000494:pharmacology; D005260:Female; D006834:Hydrazines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D006868:Hydrolysis; D066298:In Vitro Techniques; D007735:Kynuramine; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008928:Mitochondria / Q000187:drug effects / Q000201:enzymology*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D017207:Rats, Sprague-Dawley; D013050:Spectrometry, Fluorescence; D013844:Thiazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D014439:Tyramine / Q000494:pharmacology
D006834:Hydrazines; D008996:Monoamine Oxidase Inhibitors; D013844:Thiazoles; D007735:Kynuramine; D000661:Amphetamine; D003000:Clonidine; D014439:Tyramine