SYNTHESIS AND ANTIDEPRESSANT ACTIVITY OF 2-BROMO-1-(THIETAN-3-YL) IMIDAZOLE-4, 5-DICARBOXYLIC ACID DERIVATIVES
Journal Title: International Journal of Pharmacy and Pharmaceutical Sciences - Year 2017, Vol 9, Issue 8
Abstract
Objective: Synthesis of the salts and diylidenehydrazidеs of 2-bromo-1-(thietan-3-yl) imidazole-4,5-dicarboxylic acid to evaluate the antidepressant activities.Methods: The structures of the synthesised compounds were confirmed by elemental analysis and 1РNMR spectral data. The melting points of the compounds were determined on a Stuart SMP30 apparatus. The X-ray diffraction data for compound IIc were obtained at room temperature on a Xcalibur Gemini Еos. The antidepressant activity was investigated in the tail suspension and forced swimming tests. The locomotor activity and anxiety were studied in the open field test.Results: All synthesised compounds showed antidepressant activity after single intraperitoneal injection to male mice at doses equimolar to 10 mg/kg of imipramine. One of the compounds, 2-bromo-1-(thietan-3-yl) imidazole-4,5-dicarboxylic acid di[(4-hydroxy-3-methoxyphenyl) methylidenehydrazide], reduced the anxiety and decreased the locomotor activity at statistically significant levels. Other compounds did not have sedative and/or stimulating effects.Conclusion: Among the synthesised 2-bromo-1-(thietan-3-yl) imidazole-4,5-dicarboxylic acid derivatives, compounds with marked antidepressant activity were identified. An obvious advantage of these products is low toxicity.
Authors and Affiliations
Ferkat Khaliullin, Irina Nikitina, Anfisa Valieva, Albina Miftakhova, Leonard Khalilov, Ekaterina Mescheryakova
Keywords
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- EP ID EP575572
- DOI 10.22159/ijpps.2017v9i8.17613
- Views 85
- Downloads 0
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