Structure – biological activity relationship of thiazolidinone derivatives

Abstract

1. First synthesized compounds biological activity scale The aim – search for the new biologically active substances in group of 2,4- thiazolidinones. It has been synthesized 426 new compounds (Table 1). Their structure was confirmed by methods of chemical and instrumental analysis, and biological activity was tested using microbiological and pharmacological activity analysis techniques. Table 1. Biological activity of new thiazolidinone derivatives2. Pharmacophore structure and biological activity relationship Structures of new compounds were provided with sulfonamides, benzoic and salicylic acid, morpholine, 5-nitrobenzothiazole, aminoguanidine, guanylhydrazine and β-hydrazide fragments, predicting their pharmacophoric features (Table 2).Table 2. Pharmacophoric groups and biological activity of thiazolidinone derivatives.3. The biological activity scale of new compounds The new compounds were tested evaluating their antimicrobial (antibacterial, antifungal, antiviral, tuberculostatic), diuretic, neurotropic, anticonvulsive, pesticidal and ascaricidal activity. Majority of thiazolidinone derivatives were proved to be antimicrobial, diuretic ant neurotropic substances. Conclusion. Obtained experimental results proved our primary hypothesis to use 4-thiazolidinone scaffold with different substituenst for obtaining new biologically and pharmacologically active compounds.