Hepatoprotective activity of 1,2,4-triazole-3-thione derivatives, which contains on C5 atomic carbon hydroxy(phenyl)methyl dependent





1, 2, 4-triazole derivatives, hepatoprotective activity, carbontetrachloride, Alanine Aminotransferase, Aspartate Aminotransferase


Topicality. Actually it is very important to create highly effective but relatively inexpensive medications for the prevention and treatment the digestive system diseases. It would be appropriate to mention that we carried out an analysis of studies and examined hepatoprotective effects of 1,2,4-triazole derivatives, high rates of hepatoprotective effects were detected. Therefore, the search for hepatoprotectors in the series of 1,2,4-triazole derivatives has not only theoretical but also practical significance.

Aim. To study the first synthesized derivatives of 1,2,4-triazole-3-thione, containing substituents on C5 by carbon atom in conditions of tetrachormethane hepatitis.

Materials and methods. To model toxic hepatitis, a hepatotoxic xenobiotic, carbon tetrachloride, was used. The study of liver biochemical indicators was carried out in 24 hours later after the last injection of carbon tetrachloride. The ability of test compounds to restore the integrity of hepatocyte membranes was determined by anti-cytolytic effect (Alanine Aminotransferase (ALT), Aspartate Aminotransferase (AST) activity decrease). According to the results of the study, it was found that among 43 test compounds, 5 are able to prevent survival at 85.71 %.

Results and discussion. Thus, among the substances studied, compound 2c, which contributed 85.71 % of the survival of the experimental animals and decrease 33.43 % in ALT and 34.33 % in AST. In this case a very weak inverse dependence of the above was observed (r = -0.31).

Conclusions. As a result, some chemical structure patterns of the hepatoprotective action of 1,2,4-triazole derivatives were established, so the survival of the experimental animals decreased with the introduction of a phenyl substituent of the starting thiones with N4.

Author Biographies

A. M. Rud, Zaporizhzhіa State Medical University

Aspirant, Physical and Colloidal Chemistry Department

A. G. Kaplaushenko, Zaporizhzhia State Medical University

Dr.hab., Head of the Physical and Colloidal chemistry Department

Ye. S. Pruglo, Zaporizhzhia State Medical University

Ph.D., Associate Professor, Department of Clinical Pharmacy, Pharmacotherapy and MFE of FPE

Yu. G. Sameliuk, Zaporizhzhia State Medical University

Teaching Assistant, Physical and Colloidal Chemistry Department

Yu. S. Frolova, Zaporizhzhia State Medical University

Teaching Assistant, Physical and Colloidal Chemistry Department


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Pharmacology and biochemistry