Biological Activities of Drugs. VIII. Structure-Activity Relationship of Sulfonamide Carbonic Anhydrase Inhibitors. (3)

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Hansch-Fujita's method was applied to a structure-activity analysis of 22 sulfonamide derivatives with an inhibitory activity against carbonic anhydrase. Electronic parameters such as Hammett's σ factor, △pK_a, △ppm and △fr, and hydrophobic parameters such as π, π_c and β were employed. △pK_a, △ppm, △f_rπ, π_c and β were derived from dissociation constant, NMR chemical shift of sulfamoyl protons, S=O valence-force constant, n-octyl alcohol-water partition coefficient, chloroform-water partition coefficient and association constant to albumin, respectively. This analysis proved to be useful in predicting not only the activity of substituted benzenesulfonamides except o-substituted derivatives, but also that of 1,3,4-thiadiazole-5-sulfonamide derivatives. The activity of o-substituted derivatives was satisfactorily predicted with the use of polar parameter σ and steric constant E_s.
社団法人日本薬学会の論文
1969-12-25