Actoprotective activity research of 2-((5-(2-bromophenyl)- 4-substituted-4H-1,2,4-triazole-3-yl)thio)acetates

Materials and methods. The compounds used to study pharmacological activity were synthesized at the Department of Natural Sciences for International Students and Toxicological Chemistry ZSMU. White nonlinear rats weighing 200–260 g of 7 animals per group were used to study the actoprotective activity of 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazole-3-yl)thio)acetates. As a method for the study of pharmacological activity was used the method of forced swimming with a load of 10 % by weight of the rat. Statistical results were calculated using Kolmogorov–Smirnov test and Shapiro-Wilk test.


Materials and methods
The compounds used to study pharmacological activity were synthesized at the Department of Natural Sciences for International Students and Toxicological Chemistry, ZSMU [13].
As a method for the study of pharmacological activity was used the method of forced swimming [14] with a load of 10 % by weight of the rat.
Loads were fixed at the base of the tail of the animals. After immersing the animals underwater for 10 seconds, the laboratory rats' swimming time was measured until depletion in seconds. The rats were immersed individually in a large container with a water layer in excess of 60 cm. The water temperature was maintained at 24-27 °C. The tested compounds, as well as the standard of comparison -Riboxin ® (manufactured by Kyiv Vitamin Plant) were injected intraperitoneally 20 minutes before the start of immersion of animals at a dose of 100 mg/kg. For comparison, we also used a control group of animals with intraperitoneal injection of saline 20 minutes before immersion.
Statistical results were calculated using Kolmogorov-Smirnov test and Shapiro-Wilk test.

Results
As a result, the actoprotective activity of 18 new compounds was investigated. Compounds Ia, Ib, IIb, IIk, IIj had been found to have an actoprotective effect. But none compound exceeded the comparison drug. Some conclusions have been made regarding the dependence "structure -actoprotective activity".
It increase actoprotective activity to 8.27 % compared to control ( Table 2).
The substitution of sodium cation with potassium cation or 2-aminoethanol resulted in a nearly 2-fold reduction in the actoprotective effect.
Compounds Ia, Ib, IIb, IIk, IIj had been found to have a moderate actoprotective effect. But none compound exceeded the comparison drug.