Synthesis and some central pharmacological properties of new derivatives of 2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic acid

Pol J Pharmacol Pharm. 1992 Jan-Feb;44(1):67-78.

Abstract

Twenty one derivatives of 2,3-dihydroimidazo[1,2-a]pyrimidine-6-carboxylic acid (6 n-butyl amides and 15 free acids) bearing the aromatic ring in position 1 or 2 were obtained. They were synthesized by aminolysis or hydrolysis of respective ethyl esters. Pharmacological studies on the central action of eight compounds 1, 2, 4, 5, 7, 8, 9 and 10 were carried out on mice and rats. The most active compounds, producing sedation and hypothermia, and 1, 2 and 5. The compounds decreased amphetamine-induced hyperactivity. Besides, compound 2 exerted analgesic effect in mice.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Body Temperature / drug effects
  • Brain / drug effects*
  • Brain / physiopathology
  • Cold Temperature
  • Electroshock
  • Imidazoles / chemical synthesis
  • Imidazoles / pharmacology*
  • Imidazoles / toxicity
  • Lethal Dose 50
  • Male
  • Mice
  • Motor Activity / drug effects
  • Pain / drug therapy
  • Pyrimidines / chemical synthesis
  • Pyrimidines / pharmacology*
  • Pyrimidines / toxicity
  • Rats
  • Rats, Wistar

Substances

  • Imidazoles
  • Pyrimidines