Synthesis, toxicological and pharmacological assessment of esters of carbonic and carbamic acids with 2-aryl-4-hydroxyethylmorpholines

The synthesis of 15 original morpholine derivatives from 4-hydroxyethyl-2-arylmorpholines is described. The structures of the synthesized esters were proved by LR, H-1-NMR and C-13-NMR data. Acute toxicity studies of the compounds were performed on mice. A comparative pharmacological study of the in vivo effect on the central nervous system was realized by certain screening tests: hexobarbital-induced sleeping time, locomotor activity and behavior despair test for antidepressants. The results indicate that some of the compounds are less toxic than the reference drug Moclobemide (Aurorix). Compound 2d, 2-(4-bromphenyl)-4-(2-phenyloxycarbonyloxyethyl)morpholine, has a low toxicity and weak dose-dependent antidepressive activity. This compound does not influence hexobarbital-induced sleeping time or locomotor activity of mice.