Discovered in 1926 it was marketed in Europe by Schering AG of Berlin as a synthetic drug with insulin-like properties that could be taken orally.

The folk remedy French lilac (Galega officinalis), was used to treat the symptoms of diabetes, and towards the end of the nineteenth century it was discovered to contain galegine, a derivative of guanidine.

Karl Slotta at the Chemistry Institute of the University of Vienna synthesized derived compounds that had a polymethylene chain with a guanidine group at each end.

that trypanosomes require a plentiful supply of glucose in order to reproduce, researchers tested Synthalin and related compounds to see if they could be effective treatments.

[citation needed] Further modifications to the chemical structure led to the diamidine class of drugs, of which pentamidine is still used against trypanosomiasis.