作者:William A. Bolhofer、Charles N. Habecker、Adolph M. Pietruszkiewicz、Mary Lou Torchiana、Henry I. Jacoby、Clement A. Stone
DOI:10.1021/jm00189a015
日期:1979.3
A series of N-substituted 2-mercaptoacetamidines was synthesized and evaluated for gastric antisecretory activity in dogs stimulated with gastrin tetrapeptide. The most potent analogues showed 80--95% inhibition of acid secretion after an oral dose of 8 mg/kg. Thus, these compounds represent a new structural type having significant antisecretory activity. Disulfides had essentially the same antisecretory
合成了一系列的N-取代的2-巯基乙am,并评价了用胃泌素四肽刺激的狗的胃抗分泌活性。口服剂量为8 mg / kg后,最有效的类似物显示出80--95%的酸分泌抑制作用。因此,这些化合物代表具有显着抗分泌活性的新结构类型。二硫化物与相应的巯基乙acet具有基本相同的抗分泌能力,表明代谢相互转化。巯基的烷基化降低了效力。较高的羧am同系物,例如2-和3-巯基丙ion,具有非常低的活性。羟乙am和巯基乙酰胺的药效也很低。用这一系列化合物观察到的副作用包括呕吐,心动过速和胃出血。