Biological Activities of Drugs. VI. Structure-Activity Relationship of Sulfonamide Carbonic Anhydrase Inhibitors. (1)

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A study was made of correlation of carbonic anhydrase inhibitory activity with the chemical structures of 19 derivatives of benzenesulfonamide and 3 heterocyclic sulfonamides in reference to the physicochemical properties of the compounds. A linear correlation was observed for Hammett's σ factor against pK_a, chemical shift of the sulfamoyl protons, and valence-force constant of the S=O bond. Inhibitory activity increased with a decrease of pK_a, and with an increase of Hammett's σ factor, chemical shift of the sulfamoyl protons, and the S=O valence-force constant of the sulfamoyl group. A close correlation was also found between the inhibitory activity and water solubility of the unionized molecules of benzenesulfonamides except for p-CH_3NH and o-NO_2 derivatives.
社団法人日本薬学会の論文
1969-05-25