Affiliation:
1. Federal State Budgetary Educational Institution of Higher Education "Perm State Pharmaceutical Academy" of the Ministry of Health of the Russian Federation
Abstract
Introduction. Correction of pathological anxiety is currently an important task of modern pharmacology, since anxiety disorders are among the most common mental illnesses. Taking into account the trend of a constant increase in the incidence of anxiety and depressive disorders (ADD) in the world, the urgency of searching for various tools for studying this group of diseases and creating safe, highly effective drugs for the pharmacotherapy of ADD is growing.Aim. The study of new derivatives of salts of 2,4-dioxobutanoic acids containing fragments of benzimidazole and pyrimidine cycles on behavioral reactions of animals.Materials and methods. The salts of 4-methoxyphenyl-4-oxobut-2-enoic acid with heterocyclic amines synthesized by us were used as objects of research. Behavioral reactions of animals to the introduction of the studied compounds were evaluated using a number of tests: "open field", light/dark box", "extrapolation escape task", "forced swim".Results and discussion. The results of the experiments made it possible to identify a potentially active compound 1b, which showed an improvement in a number of indicators of motor activity of animals and an anti-anxiety effect. In addition, with the introduction of substance 1b, there is a manifestation of antidepressant activity in an acute stress situation.Conclusion. The effect of compounds 1a, 1b obtained for the first time on the behavioral reactions of animals was studied. The "structure-activity" analysis was carried out with the establishment of the priority of further targeted synthesis of salts of 2,4-dioxobutane acid derivatives containing a fragment of 2-aminopyrimidine. A compound with a neuropsychotropic activity profile has been identified, which is recommended for further in-depth study.
Publisher
Center of Pharmaceutical Analytics Ltd
Subject
Drug Discovery,Pharmaceutical Science