Study of anticonvulsant properties of 1,2,4-triazole derivatives and prospects for their use in pharmacy
DOI:
https://doi.org/10.14739/2409-2932.2025.2.320738Keywords:
1,2,4-triazole, synthesis, physicochemical properties, structure-activity relationship, anticonvulsant effect, in silico, in vivo studies, activity predictionAbstract
Anticonvulsant drugs (antiepileptic drugs) are a group of medications used to treat epilepsy and to control other disorders associated with seizures or convulsive episodes. The choice of a particular drug depends on the type of seizure, the patient’s age, comorbidities, and possible side effects. Treatment with these drugs requires constant medical monitoring to achieve optimal impact and to minimize risks. Therefore, solving the problem of creating new original medicines with minimal adverse effects remains an urgent task, with theoretical and practical justification.
The aim of the work was to analyze and summarize the world achievements in recent years in the study of anticonvulsant properties of 1,2,4-triazole derivatives and to prove the need and feasibility of further research in the chosen direction of scientific research.
Materials and methods. A comprehensive literature search was conducted using a range of scientometric databases indexing peer-reviewed sources in the fields of biomedicine, chemistry, and pharmacology, including PubMed, SciFinder, Web of Science, Google Scholar, ScienceDirect, and Scopus. To achieve this goal, theoretical methods were used: information search, review, comparison, generalization. Additionally, combined search queries using logical operators such as AND, OR, NOT were used to narrow or expand the search results. For example, the query “1,2,4-triazole AND anticonvulsant activity” found publications discussing the anticonvulsant properties of these compounds.
Results. The studies described in this work indicate the significant potential of S-derivatives of 5-(furan-2-yl)-4R1-1,2,4-triazol-3-thiones as anticonvulsants, considering the preliminary results of theoretical computer prediction, as well as the establishment of regularities between the structure of the synthesized compounds and their anticonvulsant effect. Experimental studies have shown that the two compounds exhibit anticonvulsant activity and are similar to Mydocalm in terms of the strength of their pharmacological effect. It was found that the anticonvulsant activity of 2-[5-(furan-2-yl)-4-phenyl-4H-1,2,4-triazol-3-ylthio]-1-(4-chlorophenylethanone) exceeds the effectiveness of comparison drugs, such as Mydocalm and phenobarbital, by 1.23 and 1.27 times, respectively, when using the corazole model of seizures in rats. The team of authors managed to synthesize several new 7-substituted-5-phenyl-[1,2,4]triazolo[1,5-a]pyrimidines through the inclusion of a triazole fragment in the pyrimidine ring, which is expected to have a synergistic effect in the treatment patients with epilepsy.
Conclusions. 1,2,4-triazole derivatives are of considerable interest for the development of new drugs with anticonvulsant activity, which can act through several molecular mechanisms. Thus, the analysis of scientific sources can suggest strategies for expanding.
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