Synthesis and CNS activity of new 1-alkyl-2-aryl-7-hydroxy-5(1H)oxo-imidazo[1,2-a]pyrymidines

Acta Pol Pharm. 1996 May-Jun;53(3):209-12.

Abstract

Cyclocondensation of 1,5-disubstituted 2-aminoimidazolines with diethyl malonate in the presence of sodium methanolate leading to imidazol[1,2-alpyrimidine-5,7-dion system is presented. Prevailing of 7-hydroxy-5(1H)oxo form between three possible tautomers is discussed based on spectral data. CNS activity of nine compounds is evaluated.

MeSH terms

  • Animals
  • Apomorphine / toxicity
  • Catalepsy / chemically induced
  • Catalepsy / drug therapy
  • Drug Design
  • Drug Evaluation, Preclinical
  • Haloperidol / toxicity
  • Hypothermia / chemically induced
  • Hypothermia / drug therapy
  • Lethal Dose 50
  • Magnetic Resonance Spectroscopy
  • Male
  • Malonates / chemistry
  • Mice
  • Motor Activity / drug effects
  • Pain / drug therapy
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology
  • Pyrimidines / therapeutic use
  • Rats
  • Rats, Wistar
  • Reserpine / toxicity
  • Seizures / drug therapy
  • Sleep / drug effects
  • Stereotyped Behavior / drug effects
  • Structure-Activity Relationship

Substances

  • Malonates
  • Pyrimidines
  • Reserpine
  • Haloperidol
  • Apomorphine
  • diethylmalonic acid