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已知2-苯基-2-(2-吡啶基)硫酰胺是一有效非抗胆碱能胃分泌抑制剂,继之,又报道结构不同的哒嗪酮甲基硫酰胺类具有显著的抑制胃分泌活性。为寻找高效、长效、非抗胆碱能的抗溃疡药,作者结合两者结构特点,合成了一新型3-(2H)哒嗪酮类衍生物。其方法是3-(2H)哒嗪酮类的2-N位上用Br(CH_2)_nCN烷化,腈基单用H_2S或与伯、仲胺处理转变为硫酰胺基即得。经大鼠进行抑制胃分泌活性试验表明,2-N位有硫酰胺侧链的3-(2H)哒嗪酮类均显相当强烈的抑制作用。其中化合物48、49、51、52等最为有效。
It is known that 2-phenyl-2- (2-pyridyl) sulfamide is a potent non-anticholinergic gastric secretion inhibitor. Subsequently, it was also reported that pyridazinone methylsulfamides with different structures showed significant inhibition Gastrin secretion activity. In order to find an effective, long-acting, non-anticholinergic anti-ulcer drug, the authors synthesized a novel 3- (2H) pyridazinone derivative based on their structural characteristics. The method is that 3- (2H) pyridazinones are alkylated with Br (CH_2) _nCN at the 2-N position, nitrile groups are treated with H_2S or primary and secondary amines to be converted to sulfamides. Inhibition of gastric secretion activity in rats showed that 2-N-position sulfanilamide side chains of 3- (2H) pyridazinones showed a very strong inhibitory effect. Among them, compounds 48, 49, 51, 52 and the like were the most effective.