Lelyukh M. Synthesis and biological activity of thiazolidine derivatives with thia(oxa)diazole fragments in molecules

The object - oxidative cyclization, acylayion, N- and S-alkylation reactions, formilation, hydrazinolysis, [2+3]-cyclocondensation, Knoevenagel condensation; the purpose - the search of new potential biologically active substances as potential drugs, among synthesized non-condensed 1,3,4-thia(oxa)diazole or imidazo[2,1-b][1,3,4]thiadiazole substituted 4- thiazolidinone and 2,3-dihydrothiazole derivatives; methods X-ray analysis, pharmacological screening, COMPARE analysis, molecular docking; results - the cyclization of 2-chloro-N-(5-aryl-1,3,4-oxadiazole-2-yl)acetamides with ammonium thiocyanate the group of novel 2-iminothiazolidin-4-ones and its 5-arylidene derivatives were synthesized; based on the acylation and N-alkylation reaction the group of not described amides of mono- and dicarboxylic acids of 2,4-dioxothiazolidinone row with thia(oxa)diazole fragments in molecules were obtained; the condensation of 2-(2,3-dioxo-1,3-dihydroindol-1-yl)-N-(5-aryl-1,3,4-oxadiazole-2-yl)acetamides with methylene active 4-thiazolidinones resulted in series of novel 5-isatinylidene derivatives; a series of 2-hydrazonoderivatives of 4-thiazolidinone and 2,3-dihydrothiazole with imidazo[2,1-b][1,3,4]thiadiazole moiety in position 2 were for the first time obtained on the base on the [2+3]-cyclocondensation of appropriate thiosemicarbazones with various equivalents of dielectrophilic synthon; the directed synthesis of 165 new compounds was conducted; low-toxic compounds were identified, from which 3 compounds with antitumor activity, 10 compounds with antitrypanosomal activity, 3 compounds with antiviral activity and 2 compounds with antifibrotic activity; introduced - into scientifically research work and educational processes of the departments of pharmaceutical direction; direction - pharmacy.