Synthesis and pharmacological investigation of compounds containing a 2-thioxopyrrolidine-4,5-dione moiety

Pol J Pharmacol Pharm. 1986 May-Jun;38(3):309-19.

Abstract

The synthesis of two Schiff bases of aryl methyl ketones and ethylenediamine 1c, 1d, symmetric adducts of aryl isothiocyanates with Schiff bases 2d-2m and 2-thioxopyrrolidine-4,5-dione derivatives 4d-4m obtained by condensation of oxalyl chloride with Schiff bases of aroylthioacetic acid anilides and ethylenediamine is described. Some of 13 investigated compounds 4a, 4b, 4d-4l, 5a, 5b of 2-thioxopyrrolidine-4,5-dione type showed sedative and analgesic action.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 5-Hydroxytryptophan / pharmacology
  • Analgesics* / chemical synthesis
  • Analgesics* / toxicity
  • Animals
  • Anticonvulsants
  • Drug Interactions
  • Helplessness, Learned
  • Lethal Dose 50
  • Male
  • Mice
  • Motor Activity / drug effects
  • Pyrrolidines / chemical synthesis
  • Pyrrolidines / pharmacology*
  • Pyrrolidines / toxicity
  • Rats
  • Rats, Inbred Strains
  • Sleep / drug effects
  • Stereotyped Behavior / drug effects

Substances

  • Analgesics
  • Anticonvulsants
  • Pyrrolidines
  • 5-Hydroxytryptophan