Cytoprotective effects of 4,6-bis(1H-pyrazol-1-yl)pyrimidine and related compounds on HCI.ethanol-induced gastric lesions in rats.
Bis(1H-pyrazol-1-yl)- and bis(1H-imidazol-1-yl)pyrimidines were synthesized and evaluated for cytoprotective effects. Among them, 4,6-bis(1H-pyrazol-1-yl)pyrimidine (3) showed a potent inhibitory effect on the HCl.ethanol-, ethanol-, and water immersion stress-induced gastric lesions in rats, and a very low acute toxicity. One of the major factors responsible for the cytoprotective effects of 3 is the increase in the bicarbonate secretion. This compound appears to be a promising cytoprotective drug for the treatment of gastric mucosal ulcers.
Ikeda
M
M
Kyoto Pharmaceutical University, Japan.
Maruyama
K
K
Nobuhara
Y
Y
Yamada
T
T
Okabe
S
S
D000818:Animals; D000897:Anti-Ulcer Agents / Q000627:therapeutic use*; D001639:Bicarbonates / Q000378:metabolism; D000431:Ethanol / Q000633:toxicity*; D005753:Gastric Mucosa / Q000098:blood supply / Q000378:metabolism; D016480:Helicobacter pylori / Q000187:drug effects; D010437:Peptic Ulcer / Q000188:drug therapy*; D011720:Pyrazoles / Q000737:chemistry* / Q000627:therapeutic use; D011743:Pyrimidines / Q000737:chemistry* / Q000627:therapeutic use; D051381:Rats; D012039:Regional Blood Flow / Q000187:drug effects
D000897:Anti-Ulcer Agents; D001639:Bicarbonates; D011720:Pyrazoles; D011743:Pyrimidines; C043452:dulcerozine; D000431:Ethanol