The study of the effect of 5-(4-(tret-butyl)phenyl)-4-R-amino-4H-1,2,4-triazole-3-thiols on the duration of thiopental-sodium narcosis for laboratory rats

Abstract

The purpose of the work was to investigate the effect of 5-(4-(tret-butyl)phenyl)-4-R-amino-4H-1,2,4-triazole-3-thiols on the duration of thiopental-sodium narcosis for laboratory rats and to identify the regularities of the dependence “chemical structure – biological effect”. Materials and methods. The objects of research were 15 new compounds, derivatives of 4-amino-5-(4-(tret-butyl)phenyl)-4H-1,2,4-triazole-3-thiols. These compounds are the crystal substances which are odorless, insoluble in water and soluble in organic solvents. The combined reception and interaction of the compounds with anesthetic agents for rats were considered. The time of the anesthetic thiopental sodium narcosis was marked by the time while the animal was in lateral position, since losing reversal’s reflex. Aminazine and caffeine-sodium benzoate (10 mg/kg and 50 mg/kg ) were used as a standard of comparison. Results and discussion. In the study we have found that 5-(4-(tret-butyl)phenyl)-4-R-amino-4H-1,2,4-triazole-3-thiols exhibit different effects – deprimo action or analeptic action. For example, the presence of fluorine in the structure of compound contributes to some analeptic activity and vice versa the transition to disubstituted fluoride molecules causes small deprimo action. However the presence of chlorine leads to the appearance of clear raising to a higher power actions regarding to sodium thiopental, that is more than standard of comparison – aminazine. It is interesting to observe the activity change of a series of nitro containing compounds. Conclusions. The leader compound has been identified among the investigated compounds. It exceeds the standard of comparing (aminazine) by indexes. Some regularities “chemical structure – biological effect” have been established. These results can be used in the future for targeted search of substances with analeptic or deprimo activity.

Keywords

• 4-triazole
• Organic Synthesis
• Drug Interactions
• Analeptics