1979 年 27 巻 7 号 p. 1596-1603
The hypoglycemic activity and physico-chemical properties (pKa, log P) of cyclic guanidines were measured. Qualitative structure-activity relationships were investigated in various mono-, bi-, and tricyclic guanidines and it became apparent that compounds which have a bulky group and a pKa value between 8-11 showed potent activity. It was possible to correlate hypoglycemic activity with the pKa values and partition coefficients of cyclic guanidines.