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首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >Synthesis and biological evaluation of novel condensed pyrimidinylmethylsulfinylbenzimidazoles as antiulcer agent
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Synthesis and biological evaluation of novel condensed pyrimidinylmethylsulfinylbenzimidazoles as antiulcer agent

机译：新型缩合嘧啶基甲基亚磺酰基苯并咪唑类抗溃疡剂的合成及生物学评价

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摘要

Current therapies to treat gastroesophageal reflux disease (GERD), peptic ulcer disease (PUD), and other acid-related diseases either prevent stimulation of the parietal cell (H2-receptor antagonists) or inhibit gastric H+/ K+-ATPase (proton pump inhibitors). The inhibition of acid production by proton pump inhibitors (PPI's) provides more effective relief of symptoms and healing. A series of novel 4-substituted-2-(lH-benzimidazol-2-yl)methylsulfi-nylpyrimidines were synthesized as target compounds and antiulcer activity was done using parameters like total acidity, pH, and total gastric acid volume by pylorus liga-tion method on Wistar rats. Three different dose levels were employed for testings. The target compounds 4-substituted-2-(lH-benzimidazol-2-yl)methylsulfinylpyr-imidines were effective for ulcer treatment and among them compounds 10c, l0d, 8b, and 8c exhibited potent antisecretory activity. Overall, compounds 10c, l0d, 8b, and 8c can be looked upon as potential leads for further development and investigations.
机译：目前用于治疗胃食管反流病（GERD），消化性溃疡病（PUD）和其他与酸有关的疾病的治疗方法是防止刺激壁细胞（H2-受体拮抗剂）或抑制胃H + / K + -ATPase（质子泵抑制剂） 。质子泵抑制剂（PPI's）对酸产生的抑制作用可以更有效地缓解症状和治愈疾病。合成了一系列新型的4-取代-2-（1H-苯并咪唑-2-基）甲基亚磺酰基-嘧啶作为目标化合物，并通过幽门结扎法使用总酸度，pH和总胃酸量等参数进行了抗溃疡活性的研究。 Wistar大鼠的方法。测试使用了三种不同的剂量水平。目标化合物4-取代的2-（1-H-苯并咪唑-2-基）甲基亚磺酰基吡啶-亚胺对于溃疡治疗是有效的，并且其中的化合物10c，10d，8b和8c显示出有效的抗分泌活性。总体而言，化合物10c，10d，8b和8c可被视为进一步开发和研究的潜在线索。

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