H^+/K^+-ATP酶抑制剂苯并咪唑类衍生物的研究

Studies on H\++/K\++ATPase Inhibitors Benzimidazole Derivatives

Ｈ＋／Ｋ＋ＡＴＰ酶是胃酸分泌的最后环节，在合成Ｈ＋／Ｋ＋ＡＴＰ酶抑制剂泮托拉唑的基础上，设计合成了１２个未见文献报道的苯并咪唑类衍生物，经红外光谱、核磁共振氢谱和元素分析确定了结构．初步药理筛选实验表明：化合物（５ｂ），（６ｂ），（６ｄ）具有抑制胃酸分泌的作用，其中化合物（６ｄ）作用最强．

H\++/K\++ATPase is the last passageway of gastric acid secretion.On the basis of synthesis of the H\++/K\++ATPase inhibitor pantoprazole,twelve benzimidazole derivatives were synthesized for the first time,and their structures were proved by IR,\+1HNMR and elementary analysis.Their antisecretory activities were evaluated in vivo,the compounds (5b),(6b) and (6d) have antisecretory activities and compound (6d) was the most potent.