Discriminant-analytical investigation on the structural dependence of hyperglycemic and hypoglycemic activity in a series of substituted o-toluenesulfonylthioureas and o-toluenesulfonylureas

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Abstract
The influence of a series of substituted o-toluenesulfonylthioureas and o-toluenesulfonylureas on the level of blood sugar was investigated in rats. The compounds were divided into 3 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, RM [log(1/Rf-1)] 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. Two different mechanisms of action with opposite effect overlap in the case of the series studied.

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