Synthesis and cytoprotective antiulcer activity of 2- or 4-(1H-pyrazol-1-yl)pyrimidine derivatives related to mepirizole and dulcerozine.
(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.
Ikeda
M
M
Kyoto Pharmaceutical University, Japan.
Maruyama
K
K
Nobuhara
Y
Y
Yamada
T
T
Okabe
S
S
D000284:Administration, Oral; D000818:Animals; D000897:Anti-Ulcer Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000627:therapeutic use*; D004195:Disease Models, Animal; D004840:Epirizole / Q000737:chemistry* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D010437:Peptic Ulcer / Q000188:drug therapy; D011743:Pyrimidines / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
D000897:Anti-Ulcer Agents; D011743:Pyrimidines; C043452:dulcerozine; D004840:Epirizole