Abstract
The article summarizes and compares data on the properties and biological activity of o-benzoic sulfimide and sulfanilamide compounds. Attention is given to the biochemical conditions under which o-benzoic sulfimide and sulfanilamides have similar activity groups. The results of the experimental and theoretical studies aimed at understanding the molecular organization and biological activity of folic acid and its homologous complexes are analyzed. A hypothesis about the possible mechanisms of the formation of such complexes with the participation of o-benzoic sulfimide is presented. The perspectives for the use of o-benzoic sulfimide and its homologues in biomedicine are evaluated.
Highlights
Introduction oBenzoic sulfimide (1,1-dioxo-1,2-benzothiazol-3-one), better known as saccharin (Figure 1), was accidentally discovered by a chemist Constantin Fahlberg in 1879 when studying the oxidation of o-toluenesulfonamide for work on coal tar derivatives in the laboratory of Prof
In order to understand the mechanism of the antimicrobial action of saccharin, it is necessary to start with the fact that the cyclic form of o-benzoic sulfimide does not have active radicals that could help it quickly engage in crucial metabolic processes in pro- and eukaryotic cells
Saccharin has antibacterial activity only if it is transformed by the enzyme systems of micro- and/or macroorganisms. o-sulphamoylbenzoic acid can be absorbed by both symbiotic and pathogenic microflora. It starts to compete with native p-aminobenzoic acid in the bacterial cell and is mistakenly included by the bacterial enzyme complexes in the composition of pseudofolic acid (Figure 5, XV), which cannot provide normal biosynthesis of nucleic acids and many bacterial proteins
Summary
In order to understand the mechanism of the antimicrobial action of saccharin, it is necessary to start with the fact that the cyclic form of o-benzoic sulfimide does not have active radicals that could help it quickly engage in crucial metabolic processes in pro- and eukaryotic cells. This leads to the conclusion that the cyclic form of saccharin is probably a prodrug that needs to be bioactivated.
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