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

Abstract

Severe fatigue can occur due to overwork, lack of exercise, depression, insomnia, etc. It should be understood that fatigue, weakness, both emotional and physical, is not a disease. Often, actoprotective substances are used to reduce fatigue. To search for new substances with a different spectrum of pharmacological activity, 1,2,4-triazole derivatives have proven themselves well. The aim of work was to investigate actoprotective activity among previously synthesized 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. Results. Compounds Ia, Ib, IIb, IIk, IIj had been found to have a moderate actoprotective effect. But none compound had exceeded the comparison drug. Some conclusions were drawn regarding the dependence of “structure – actoprotective effect”: the most active compound was 2-aminoethanol 2-((5-(2-bromophenyl)-4-ethyl-4H-1,2,4-triazole-3-yl)thio)acetate (IIj); conversion to 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazole-3-yl)thio)acetate salts and selection as sodium, potassium, or 2-aminoethanol cations was resulted in to increase the actoprotective effect. Conclusions. As a result, the actoprotective activity of 18 new 2-((5-(2-bromophenyl)-4-substituted-4H-1,2,4-triazole-3-yl)thio)acetates was investigated. Some conclusions were drawn regarding the dependence of “structure – actoprotective effect”.

Keywords

• actoprotective activity
• 1 2 4-triazole
• acids
• salts
• heterocyclic compounds