Synthesis, toxicological and pharmacological assessment of morpholinooximes

Pharmazie. 1999 Jun;54(6):409-11.

Abstract

The synthesis, pharmacology and toxicology of four morpholine derivatives from 1-(2-arylmorpholino)-3-phenyl-3-propanonoxime and the synthesis of two anilides are described. The structures of the synthesized derivatives were proved by IR, 1H NMR and occasionally with 13C NMR. The acute toxicity of the compounds in mice was determined. A comparative pharmacological study of the in vivo effect on the central nervous system was realised by the following screening tests: pentobarbital induced sleeping time, locomotor activity and behaviour despair test for antidepressive activity. The most active compound was 1-(2-phenylmorpholino)-3-phenyl-3-propanonoxime (2b) which showed low toxicity and antidepressive activity at a dose of 1/10 LD50.

MeSH terms

  • Animals
  • Antidepressive Agents / chemical synthesis*
  • Antidepressive Agents / pharmacology
  • Antidepressive Agents / toxicity
  • Lethal Dose 50
  • Male
  • Mice
  • Morpholines / chemical synthesis*
  • Morpholines / pharmacology
  • Morpholines / toxicity
  • Motor Activity / drug effects
  • Oximes / chemical synthesis*
  • Oximes / pharmacology
  • Oximes / toxicity
  • Pentobarbital / pharmacology
  • Sleep / drug effects
  • Time Factors

Substances

  • 1-(2-phenylmorpholino)-3-phenyl-3-propanonoxime
  • Antidepressive Agents
  • Morpholines
  • Oximes
  • Pentobarbital