Holota S. Synthesis of aryl- and heterylsubstituted 4-thiazolidones and their biological activity

Object - reactions of [2+3]-cyclocondensation in synthesis of 4-thiazolidones, interaction of thiazolidines with oxocompounds, acid hydrolysis; the purpose - synthesis of new aryl- and heterylsubstituted 4-thiazolidones and search of effective and low-toxic physiologically active substances among them; methods - organic synthesis, IR-, NMR-, chromatomas-spectroscopies, traditional and high throughput pharmacological screening; novelty - the effective methods of synthesis of 5-substituted 4-thiazolidones with pyrazolone-5 and thiazole moieties, functional derivatives of 2-hetarylydene(hydrazono)-4-thiazolidone- 5-acetic acids, 6-substituted thiazolo[3,2-b]-1,2,4-triazol-5(6Н)-ones, 5-aroylmethyl-4-thiazolidones were worked out. Anti-inflammatory, anticancer, anticonvulsant, antimicrobial, antifungal and antituberculosis activities of synthesized compounds have been studied, "structure-activity" correlations have been carried out and "lead-compounds" with high level of above-mentioned activities have been identified; the outcomes - the row of new perspective and low-toxic compounds, which possess anti-inflammatory, anticancer, anticonvulsant, antimicrobial, antifungal and antituberculosis activities were identified; certain criteria for the search of biologically-active compounds among aryl- and heterylsubstituted 4-thiazolidones have been formulated; there are introduced into scientific and educational process of pharmaceutical chemistry and organic chemistry departments of National Pharmaceutical University; area - pharmacy.