Molecular Pharmacology, Vol 2, 259-265, Copyright © 1966 by the American Society for Pharmacology and Experimental Therapeutics

Prediction of in Vitro Activity of Sulfonamides, Using Hammett Constants or Spectrophotometric Data of the Basic Amines for Calculation

¹ Chemical Department of the Borstel Research Institute for Experimental Biology and Medicine, 2061 Borstel, Germany

A homologous series of substituted benzenesulfonamides has been synthesized, and the minimum inhibitory concentration (MIC) against two strains of bacteria has been determined. It is shown that there is an approximately linear relationship between the MIC of the substituted benzenesulfonamides and the -Hammett values as well as the b values calculated from infrared-spectrophotometric data of the substituted anilines used for the synthesis of the benzenesulfonamides. Thereby it is possible to predict the in vitro activity of sulfonamides using either Hammett or b values of the basic amines.

Note:
ACKNOWLEDGMENTS The author is indebted to Dr. E. Krüger-Thiemer for helpful discussion throughout the work and for helpful criticism and suggestions concerning the manuscript. He is also pleased to acknowledge the excellent assistance of Miss Ellen Wempe and Miss Helga Henke. This investigation was reported, in part, at the IVth International Congress of Chemotherapy, Washington, D.C., October 17-21, 1965.