Study of acute toxicity of new thiophene-containing derivatives of 1,2,4-triazole

Abstract

Acute toxicity studies are an integral part of preclinical studies of any new biologically active compound. It should be noted that it is this stage of research that is crucial regarding the possibility of further use of a pharmacologically active substance as a drug. This indicator also helps to determine the initial dose for clinical trials and establish a range of potentially safe doses. The data obtained will help determine the direction of new chemical syntheses, replenish the relevant libraries in silico, as well as reveal many other fundamentally important parameters that characterize the interaction in the compound – living organism system. The aim of this research is to study the acute toxicity of 2-((4-phenyl-5-(thiophene-3-ylmethyl)-1,2,4-triazole-3-yl)thio)sodium acetate. Materials and methods. Previously, a prediction was made using the GUSAR computer program, which helped determine the dose intervals. Acute toxicity was determined by the experimental method of Kerber in vivo using white nonlinear Wistar rats. The rats were weighed, labeled, and divided into five groups of six individuals of each. Results. After the introduction of compound moving activity decreased, drowsiness, pupil miosis, and thirst were observed. In the fifth group, with the maximum dilution, all rats died within two hours after administration of the test compound. During the death, convulsions were observed. In the fourth group five animals died, and in the third – two rats died. In the first two groups, all the rats survived. During follow-up, the animals behaved normally. Based on the results of the research, calculations were made and the LD50 indicator was determined. Conclusions. According to the results, the studied compound belonged to the V class of toxicity (almost non-toxic), and the resulting LD50 value was 1125 mg/kg. This indicator confirmed the prospects for further study of this compound.

Oxidation reactions of cyclopent-2-en-1-yl thiophene derivatives

“…Khilkovets and I.M. Bilai (40) indicates a sufficient level of safety of thiophenecontaining compounds.…”