Studies on Antiulcer Agents. I. Synthesis and Pharmacological Properties of Ethyl 2-[(1H-Benzimidazol-2-yl)sulfinylmethyl]-4-dimethylamino-5-pyrimidinecarboxylate, a New H+/K+-ATPase Inhibitor Possessing Mucosal Protective Activity

Kohji TERASHIMA; Hiroshi SHIMAMURA; Akito KAWASE; Yuji TANAKA; Keiji UENISHI; Isami KIMURA; Yasuhiro ISHIZUKA; Makoto SATO

doi:10.1248/cpb.43.166

Studies on Antiulcer Agents. I. Synthesis and Pharmacological Properties of Ethyl 2-[(1H-Benzimidazol-2-yl)sulfinylmethyl]-4-dimethylamino-5-pyrimidinecarboxylate, a New H⁺/K⁺-ATPase Inhibitor Possessing Mucosal Protective Activity

寺島幸司, 嶋村浩, 川瀬明人, 田中裕二, 上西啓司, 木村伊佐美, 石塚泰博, 佐藤誠

著者情報

キーワード: pyrimidine derivative, H⁺/K⁺-ATPase inhibitor, mucosal protection, antisecretion, antiulcer agant

ジャーナルフリー

1995 年 43 巻 1 号 p. 166-168

DOI https://doi.org/10.1248/cpb.43.166

詳細

抄録

Ethyl 2-[(1H-benzimidazol-2-yl)sulfinylmethyl]-4-dimethylamino-5-pyrimidinecarboxylate (2) has been synthesized and evaluated for antiulcer properties. Compound 2 is a H⁺/K⁺-ATPase inhibitor that affords mucosal protection against absolute ethanol-induced gastric lesions in rats after oral and parenteral administrations. On the other hand, omeprazole, a representative H⁺/K⁺-ATPase inhibitor, showed mucosal protective action only after oral administration, indicating that it required gastric acid secretion to generate activity. The antiulcer activity of 2 in animal models, such as water-immersion stress-induced gastric ulcer in rats and acidified aspirin-induced gastric ulcer in rats, was three times higher than that of cimetidine.

責任著者(Corresponding author)

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