DISCRIMINANT-ANALYTICAL INVESTIGATION ON THE STRUCTURAL DEPENDENCE OF HYPERGLYCEMIC AND HYPOGLYCEMIC ACTIVITY IN A SERIES OF SUBSTITUTED ORTHO-TOLUENESULFONYLTHIOUREAS AND ORTHO-TOLUENESULFONYLUREAS

The influence of a series of substituted o-toluenesulfonylthioureas and o-toluenesulfonylureas on the level of blood sugar was investigated in rats. According to the observed response the compounds were divided intothree classes corresponding to hypoglycemic, hyperglycemic, and no activity. The distribution of the compounds over these classes can be described by discriminant functions using substituent constants, values, and indicator variables. Most important for the separation of classes are hydrophobic and/or steric properties as well as the presence or absence of the thioamide group. The results indicate that two different mechanisms of action with opposite effect overlap in the case of the series studied. © 1979, American Chemical Society. All rights reserved.