Synthesis, toxicological, and pharmacological assessment of derivatives of 2-aryl-4-(3-arylpropyl)morpholines.
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 1H-NMR, and some of them by 13C-NMR. Acute toxicity studies of the compounds 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.
Avramova
P
P
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sofia, Bulgaria.
Danchev
N
N
Buyukliev
R
R
Bogoslovova
T
T
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D007928:Lethal Dose 50; D008297:Male; D051379:Mice; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D009025:Morpholines / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D012890:Sleep / Q000187:drug effects; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D008996:Monoamine Oxidase Inhibitors; D009025:Morpholines