[1] It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine (Tagamet).

[2] After discovering that burimamide is largely inactive at physiological pH, due to the presence of its electron-donating side chain, the following steps were undertaken to stabilize burimamide: These changes increased the bioavailability metiamide so that it is ten times more potent than burimamide in inhibiting histamine-stimulated release of gastric acid.

[2] The clinical trials that began in 1973 demonstrated the ability of metiamide to provide symptomatic relief for ulcerous patients by increasing healing rate of peptic ulcers.

However, during these trials, an unacceptable number of patients dosed with metiamide developed agranulocytosis (decreased white blood cell count).

In the strongly acid medium, the amine is completely protonated; this allows the thiol to express its nucleophilicity without competition and the acid also activates the alcoholic function toward displacement.