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

Article abstract of DOI:10.1016/S0223-5234(97)89855-8

The synthesis of 15 original morpholine derivatives from 4-hydroxyethyl-2-arylmorpholines is described.The structures of the synthesized esters were proved by IR, 1H-NMR and 13C-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).Compounds 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. - Keywords: 4-hydroxyethyl-2-arylmorpholine ester; acute toxicity; antidepressant activity; Moclobemide.