Experimental antiulcer drugs. 1. Indole-1-alkanamides and pyrrole-1-alkanamides

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Abstract
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, -1-propionamide and -1-butyramide. Replacement of either methyl group by a H atom or an ethyl radical resulted in greatly diminished activity. In the acetamide and propionamide series the 3-hydroxymethyl-2-methyl derivatives exhibted activity but only when administered by the s.c. route. 2,3-Dimethylindole was active and 2,3,4,5-tetramethylpyrrole-1-acetamide was moderately active. A number of the active 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.

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