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Mode of action and quantitative structure–activity relationship of sulfonamides in biological systems of different complexity (enzymes, bacteria, rat, and human)
Author(s) -
Seydel J. K.
Publication year - 1981
Publication title -
international journal of quantum chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.484
H-Index - 105
eISSN - 1097-461X
pISSN - 0020-7608
DOI - 10.1002/qua.560200113
Subject(s) - lipophilicity , chemistry , steric effects , sulfonamide , enzyme , pharmacokinetics , bacteria , molecule , mode of action , quantitative structure–activity relationship , computational chemistry , stereochemistry , biochemistry , organic chemistry , pharmacology , biology , genetics
The mode of action of sulfonamides is evaluated and described and the structural dependency of the inhibitory effect of sulfonamides against isolated enzymes as well as against whole cell bacteria is quantitatively described as a function of the variation of electronic and steric influences of the various substituents. In addition the structural dependence of various pharmacokinetic properties as rate of absorption, distribution, metabolism, and excretion on structural changes in the sulfonamide molecules is quantitatively derived. In contrast to the preconditions for inhibitory activity, changes in lipophilicity play the dominant role in pharmacokinetics of sulfonamides.