Synthesis, Toxicological, and Pharmacological Assessment of Derivatives of 2-Aryl-4-(3-arylpropyl)morpholines

Abstract

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.

Crystal structure of N-propynoyl-(5R)-3-methyl- 5-phenylmorpholin-2-one, C14H13NO3

“…N-Substituted morpholines show activity as antidepressants, antidiabetics,a nti-emetics, platelet aggregation inhibitors, antihyperlipoproteinemics, bronchodilators and growth stimulantsand areusedinthe treatment of inflammatory diseases, pain, migraine and asthma [1][2][3][4][5].…”

Synthesis of new 1,2,4-triazole compounds containing Schiff and Mannich bases (morpholine) with antioxidant and antimicrobial activities

“…They have been reported to have antimicrobial, antiemetic, platelet aggregation inhibitory, antihyperlipo, proteinemic, and bronchodilator activity. In addition, they are also used in the treatment of pain, migraine, and asthma [19][20][21][22] . In recent years, the thiophene chemistry have attracted more interest because of the biological significance.…”

Design, Synthesis and Spectral Characterization of Novel 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides

“…They are reported to exert a number of important physiological activities such as antidiabetic, 21,22 antiemetic, 23,24 platelet aggregation inhibitors and antihyperlipo-proteinemics, 21 bronchodilators and growth stimulants 25 and antidepressants. 26 These were also used in the HN O Scheme 1. Synthetic route for the formation of 2-morpholino-N-(4,6-diarylpyrimidin-2-yl)acetamides treatment of inflammatory diseases, pain, migraine and asthma.…”