1,3-Diethylbenzimidazolium Triodide in Pharmacotherapy of Chronic Compensated Tonsillopharyngitis

Abstract

The article presents the results of a clinical and bacteriological assessment of the pharmacological efficacy of 1,3-diethylbenzimidazolium triiodide in chronic compensated tonsillopharyngitis. As a result of a 10-day course of treatment, an improvement in the clinical status of patients was achieved, as well as a significant positive effect on the composition of the pharyngeal microbiocenosis. In particular, the content of Staphylococcus aureus, β-hemolytic streptococci, Escherichia signifi cantly decreased, and Enterobacteria, non-fermenting bacteria, and Streptococci pneumonia completely disappeared from the microbial focus. However, the conducted 10-day treatment did not lead to the complete disappearance of α-hemolytic and non-hemolytic streptococci from the microbial population. This may be explained by the reparative effect of Stellanin® on the lymphoid formations of the pharynx, contributing to the restoration of colonization resistance.

Regio‐ and Chemoselectivity of Tandem N‐Ketoalkylation/Cyclization of 2‐Thioxoimidazoline‐4‐One

“…To synthesize triiodides based on the thiohydantoin cation, we performed the reaction of compounds 3 a – c with elemental iodine in acetone. In the literature, the drugs based on the diethylbenzimidazolium triiodide salts are poorly described [33] although the combination of elemental iodine with organic component might extend the biological activity of the products. The triiodide salts 4 b,c were isolated in close to 90 % yield (Scheme 2), whereas triiodide salt 4a could not be isolated as an individual product but only as an inseparable mixture with the product of intramolecular cyclization 5 , as proved by the presence of the signals of the methylene groups at 4.82 ( 1 H) and 52.0 ppm ( 13 C) in 4 a and those at 7.43 ( 1 H) and 111.1 ppm ( 13 C) of the =CH group in the thiazole ring in 5 .…”

“…The need for the salts of heterocyclic compounds is determined by the growing interest in these compounds due to wide application in different fields of science and technology. [32][33][34] With this in mind, the aim of the present work was to investigate the reactions of thiohydantoin with aliphatic, aromatic, and heteroaromatic α-iodoketones, and to explore the possibility of cyclization of the expected alkylation products. Earlier, we have shown that α-iodoketones, due to the high reactivity of the CÀ I bond, readily alkylate heterocyclic compounds with the carbonyl group in the molecule in the absence of bases or catalysts; the degree and regioselectivity of alkylation have also been investigated depending on the structure of the heterocycle.…”

“…To the best of our knowledge, prior to the present study, there had been no report on the alkylation of thiohydantoin or its derivatives with α‐iodoketones that might lead to the corresponding salts. The need for the salts of heterocyclic compounds is determined by the growing interest in these compounds due to wide application in different fields of science and technology [32–34] . With this in mind, the aim of the present work was to investigate the reactions of thiohydantoin with aliphatic, aromatic, and heteroaromatic α‐iodoketones, and to explore the possibility of cyclization of the expected alkylation products.…”