SYNTHESIS AND ANTI-INFLAMMATORY PROPERTIES OF SOME C5 SUBSTITUTED 3-METHYL-4-THIOXO-THIAZOLIDIN-2-ONES ; СИНТЕЗ И ПРОТИВОВОСПАЛИТЕЛЬНЫЕ СВОЙСТВА НЕКОТОРЫХ С5 ЗАМЕЩЕННЫХ 3-МЕТИЛ-4-ТИОКСО-ТИАЗОЛИДИН-2-ОНОВ ; СИНТЕЗ ТА ПРОТИЗАПАЛЬНІ ВЛАСТИВОСТІ ДЕЯКИХ С5 ЗАМІЩЕНИХ 3-МЕТИЛ-4-ТІОКСО-ТІАЗОЛІДИН-2-ОНІВ

Introduction. The study of the reactivity of 4-thiazolidone derivatives and the implementation of their chemical transformations is a promising area for the search for new biologically active substances. This is due to the wide range of biological activity of this class of compounds, as well as the presence of a number of reactive centers, which allows for various modifications of the original structure. Taking into account these circumstances, the synthesis of new substances as potential drug-like molecules among this class of compounds is relevant. The aim of the study – to synthesize some C5 substituted derivatives of 3-methyl-4-thioxo-thiazolidin-2-one for pharmacological screening in vivo of their anti-inflammatory activity. Research Methods. Organic synthesis, 1H NMR spectroscopy, elemental analysis, pharmacological screening were performed. Results and Discussion. The synthetic part of the work consisted in the structural modification of 3-methyl-4-thioxo-thiazolidin-2-one. The active methylene group at the C5 position of the said scafold exhibits CH-acidic properties and allows to carry out the azo coupling reaction with aryldiazonium salts to give the corresponding 3-methyl-5-(aryl-hydrazones)-4-thioxo-thiazolidin-2-ones. The structure of the obtained compounds and the interpretation of the performed chemical studies were confirmed by the data of elemental analysis and 1H NMR spectroscopy. The study of the effect of synthesized substances on the course of the exudative phase of inflammation was performed on the basis of the carrageenan model of inflammatory edema of the paws of white rats. The presence of an inflammatory reaction was established with a change in the volume of the limb by the oncometric method at the beginning of the experiment and 4 hours after the introduction of the phlogogenic agent. For comparison, the anti-inflammatory effect of Ibuprofen was studied under similar conditions. The synthesized compounds have anti-inflammatory properties, and some of them in terms of activity are ...