Biological Activity of Drugs. XI. Relation of Structure to the Bacteriostatic Activity of Sulfonamides. (2)

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Hydrophobicity constant π, which was introduced by Hansch, of sulfonamides was measured in the systems of n-octyl alcohol-water (designated π_0) and chloroform-water (designated π_c). A good linear correlation was obtained between π_0 and π_c. π_c could be expressed in terms of log S_w, solubility of unionized molecules in water, and log S_c, solubility in chloroform. Binding of sulfonamides to human plasma protein, rabbit plasma and rabbit blood was measured following an equilibrium. dialysis method. A good correlation was obtained in any couple of the three measurements. The protein binding was found to be subjected to molecular weight of sulfonamides. Thus, an analysis was performed of the structure-activity relationship of sulfonamides between the bacteriostatic activity against Escherichia coli and the drug's physicochemical parameters including molecular weight.
社団法人日本薬学会の論文
1970-04-25