Bell M R, Zalay A W, Oesterlin R, Clemans S D, Dumas D J, Bradford J C, Rozitis J
J Med Chem. 1977 Apr;20(4):537-40. doi: 10.1021/jm00214a015.
The synthesis and gastric antisecretory activity of a series of indole-1-alkanamides and pyrrole-1-alkanamides are presented. A marked elevation of the pH of the gastric secretions of the rat was observed after oral administration of 100 mg/kg of 2,3-dimethylindole-1-acetamide (2), -1-propionamide (8), and -1-butyramide (13). Replacement of either methyl group by a hydrogen atom or an ethyl radical resulted in greatly diminished activity. In the acetamide and propionamide series the 3-hydroxymethyl-2-methyl (14 and 15) derivatives exhibited activity but only when administered by the subcutaneous route. 2,3-Dimethylindole (18) was active and 2,3,4,5-tetramethylpyrrole-1-acetamide was moderately active. A number of the activ compounds were tested in the mouse mydriasis test for anticholinergic activity and found to be inactive. They were also found to be inactive in blocking histamine-induced acid secretion in the dog.
本文介绍了一系列吲哚 -1-烷酰胺和吡咯 -1-烷酰胺的合成及其胃抗分泌活性。口服给予大鼠100mg/kg的2,3 - 二甲基吲哚 -1-乙酰胺（2）、-1-丙酰胺（8）和 -1-丁酰胺（13）后，观察到大鼠胃液pH值显著升高。用氢原子或乙基取代任一甲基都会导致活性大大降低。在乙酰胺和丙酰胺系列中，3-羟甲基 -2-甲基（14和15）衍生物具有活性，但仅在皮下给药时才有活性。2,3 - 二甲基吲哚（18）有活性，2,3,4,5 - 四甲基吡咯 -1-乙酰胺有中等活性。对许多活性化合物进行了小鼠散瞳试验以检测其抗胆碱能活性，结果发现它们无活性。还发现它们在阻断犬组胺诱导的胃酸分泌方面也无活性。
