BIOLOGICAL STUDIES OF THIAZOLES OF NEW STRUCTURE

To test and evaluate a series of thiazoles of new structure, synthesized by us, for various biological activities and toxicity. During the work, a number of activities (anti-inflammatory, hypotensive, psychostimulant properties) were discovered among thiazole derivatives, which expands the scope of their application.

For the biological activity studies, we have taken the series of thiazole derivatives were synthesized by us, on the base of substituted glutaric acid. For the experiments, we took white mice of the same weight not more than 20 g and breed, adult rats 160-180 g. The experiments were carried out on 6 batches, 10 animals in each. Animals were kept in a barrier-type room under conditions corresponding to the standards.

Synthesis: On the base of diesters of (2-substituted-2-(2-bromacetyl) pentanedioic acid by the Hanch's method we obtained the corresponding thiazole derivatives․ Through complete hydrazinolysis of the latter, we obtained the corresponding dihydrazide derivatives. Anti-inflammatory activity was determined using the formalin-induced inflammation method. The hypotensive activity of compounds 4d and 4e was studied in a generally accepted manner - on anesthetized (Nembutal 50 mg/kg) rats and compare with known drug Bendazol (Dibazol). Toxicity parameters were calculated using the methods of Pershin, Miller and Teintner.

The synthesized compounds showed promising pharmacological effects such as anti-inflammatory, psychostimulant, and hypotensive activities. Locomotor and exploratory activity, body temperature, fear and aggression responses, seizure response to maximal electroshock (50 mA, 0.2 sec., 50 Hz), response to corazol. This study suggests that these thiazole derivatives may be of interest for further research due to their pharmacological properties, low toxicity (700 to 2200 mg/kg,) and diversity of biological activities.