Developments in non-anticholinergic anti-ulcer agents

Conformational and structural relations among antipeptic ulcer compounds

“…thiocyanate and methyl isothiocyanate26 are 2.78 and 2.82 Á, respectively, while rgNin thioacetamide is 2.66 A and approximately 2.8 A in the benzisothiazole (2). Perhaps there is a separate antisecretory mechanism related to r §N in the compounds above which acts jointly with the principally proposed distance criterion, but to a somewhat lesser degree.…”

“…It was not possible to devise a single, unified model which incorporates compounds [1][2][3][4][5][6] I summarizes the activities of these compounds vs. various secretory stimulants, from which it appears that 2,2'-bipyridine (3) is unique in that it does not inhibit insulinor histamine-stimulated secretory response. If all compounds related to 310 behave similarly to 3, omission of these compounds from the model is justified.…”

Novel pharmacological activity of a series of substituted pyridines

“…3 A number of experimental agents and approaches to the peptic ulcer problem have been reviewed. [4][5][6][7] A potentially useful clinical agent could be one which effectively reduces the volume and acidity of gastric secretion through mechanisms other than the blockade of the cholinergic system. Compounds devoid of anticholinergic activity, as demonstrated by their failure to antagonize the blood pressure effect of acetylcholine, were tested in a modified pylorus-ligated rat8•9 technique.…”