Synthesis and antiulcer activity of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo [1,5-a]pyrimidine-7-ones

Farmaco Sci. 1986 Jun;41(6):417-29.

Abstract

A series of (E)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo-[1,5-a]pyrimidine-7-ones were synthesized and evaluated for the inhibition of stress-induced gastric ulcers in the rat after oral administration. Several molecules were found to be very active. The particularly interesting compound (E)-1-(3-chlorophenyl)-5-[2-(3-pyridyl)ethenyl]-1H,7H-pyrazolo[1,5-a]- pyrimidine-7-one was chosen for wider pharmacological investigation.

MeSH terms

  • Animals
  • Anti-Ulcer Agents / chemical synthesis*
  • Chemical Phenomena
  • Chemistry
  • Gastric Juice / metabolism
  • Male
  • Parasympatholytics
  • Pyrazoles / chemical synthesis*
  • Pyrazoles / pharmacology
  • Pyrimidinones / chemical synthesis*
  • Pyrimidinones / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Stomach Ulcer / etiology
  • Stomach Ulcer / prevention & control*
  • Stress, Psychological / complications

Substances

  • Anti-Ulcer Agents
  • Parasympatholytics
  • Pyrazoles
  • Pyrimidinones