Synthesis, Toxicological, and Pharmacological Assessment of Derivatives of 2-Aryl-4-(3-arylpropyl)morpholines
作者:Petya Avramova、Nicolai Danchev、Rossen Buyukliev、Tatiana Bogoslovova
DOI:10.1002/(sici)1521-4184(199811)331:11<342::aid-ardp342>3.0.co;2-6
日期:1998.11
The synthesis of nine original morpholine derivatives, i.e.2-aryl-4-(3-arylpropyl)morpholines, is described. The structure of all synthesised derivatives was proved by IR and H-1-NMR, and some C-13-NMR. Acute toxicity studies of the compounds of them by were performed on mice. A comparative pharmacological study of the in vivo effects on the central nervous system was undertaken using the screening tests: hexobarbital induced sleeping time; locomotor activity; and behaviour despair (for antidepressive activity). The most active compound 4-(2-benzoylethyl)-2-phenyl-3-methyl) morpholine 4e was studied for MAO-A and MAO-B inhibition in vitro in rat brain mitochondria preparations.