Terashima K, Shimamura H, Kawase A, Tanaka Y, Uenishi K, Kimura I, Ishizuka Y, Sato M
Research Laboratories, Roussel Morishita Co., Ltd., Shiga, Japan.
Chem Pharm Bull (Tokyo). 1995 Jan;43(1):166-8. doi: 10.1248/cpb.43.166.
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.
已合成了2-[（1H-苯并咪唑-2-基）亚磺酰甲基]-4-二甲基氨基-5-嘧啶羧酸乙酯（2）并对其抗溃疡特性进行了评估。化合物2是一种H⁺/K⁺-ATP酶抑制剂，经口服和肠胃外给药后，能为大鼠提供针对无水乙醇诱导的胃部损伤的黏膜保护作用。另一方面，代表性的H⁺/K⁺-ATP酶抑制剂奥美拉唑仅在口服后才显示出黏膜保护作用，这表明它需要胃酸分泌来产生活性。在动物模型中，如大鼠水浸应激性胃溃疡和大鼠酸化阿司匹林诱导的胃溃疡，2的抗溃疡活性比西咪替丁高3倍。
