SYNTHESIS AND ANALGESIC ACTIVITY OF [1,3,4]-THIADIAZOLE-[1,3-DIONE]-ISOINDOLE DERIVATIVES

Background: During recent years, there has been a large investigation on different classes of thiadiazole compounds, many of which were found to possess an extensive spectrum of pharmacological activities. This study was undertaken to synthesize and evaluate the analgesic activity of [1,3,4]-thiadiazole-[1,3-dione]-isoindole derivatives. Methods: The purity of the synthesized compounds was checked by performing thin layer chromatography and determining melting points. All the synthesized compounds were subjected to spectral analysis such as FT-IR and UV-visible spectroscopy. The acute toxicity study was performed using the ‘up and down method’ while the in-vivo analgesic activity was evaluated using ‘Eddy’s hot plate method in mice, taking ibuprofen as standard. Data analysis was done using one-way ANOVA followed by Dunnett’s t-test. Results: The melting point values of each of the synthesized compounds were found to be between 145-238°C, and the molecular weight values were found to be between 204-496 gm. Spectral analysis of all the synthesized compounds has shown satisfactory results. R_f values of all the synthesized compounds were found to be different and supporting the fact of formation of new compounds and also the purity of the compounds. The LD₅₀ value of the compounds (A₅1-A₅4) was less than 1750mg/kg. When compared to ibuprofen, two of the compounds showed good analgesic activity. Conclusions: The results suggest that such compounds exert an analgesic effect. Therefore, promising results can be expected from future investigations of these compounds.