Synthesis and cytoprotective antiulcer activity of 2- or 4-(1H-pyrazol-1-yl)pyrimidine derivatives related to mepirizole and dulcerozine

Chem Pharm Bull (Tokyo). 1996 Sep;44(9):1700-6. doi: 10.1248/cpb.44.1700.

Abstract

(1H-Pyrazol-1-yl)-, (1H-imidazol-1-yl)-, and (1H-1,2,4-triazol-1-yl)pyrimidines were prepared and evaluated for cytoprotective antiulcer activity. Among them, 4-methoxy-6-methyl-2-(1H-pyrazol-1-yl)pyrimidine (18) showed potent inhibition of the HCl-ethanol-induced and water-immersion stress-induced ulcers in rats, as well as low acute toxicity.

MeSH terms

  • Administration, Oral
  • Animals
  • Anti-Ulcer Agents / chemical synthesis*
  • Anti-Ulcer Agents / chemistry
  • Anti-Ulcer Agents / therapeutic use*
  • Disease Models, Animal
  • Epirizole / chemistry*
  • Epirizole / pharmacology
  • Magnetic Resonance Spectroscopy
  • Male
  • Peptic Ulcer / drug therapy
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship

Substances

  • Anti-Ulcer Agents
  • Pyrimidines
  • dulcerozine
  • Epirizole