在实验动物行为研究中评估 2,4-二氧代丁酸盐的新衍生物

A. I. Krasnova, V. D. Polezhaeva, N. A. Pulina
{"title":"在实验动物行为研究中评估 2,4-二氧代丁酸盐的新衍生物","authors":"A. I. Krasnova, V. D. Polezhaeva, N. A. Pulina","doi":"10.33380/2305-2066-2023-12-4(1)-1591","DOIUrl":null,"url":null,"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.","PeriodicalId":11259,"journal":{"name":"Drug development & registration","volume":"14 19","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2023-12-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Evaluation of New Derivatives of 2,4-dioxobutanoic Acid Salts in Behavioral Studies of Laboratory Animals\",\"authors\":\"A. I. Krasnova, V. D. Polezhaeva, N. A. Pulina\",\"doi\":\"10.33380/2305-2066-2023-12-4(1)-1591\",\"DOIUrl\":null,\"url\":null,\"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.\",\"PeriodicalId\":11259,\"journal\":{\"name\":\"Drug development & registration\",\"volume\":\"14 19\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2023-12-26\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Drug development & registration\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.33380/2305-2066-2023-12-4(1)-1591\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Drug development & registration","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.33380/2305-2066-2023-12-4(1)-1591","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 0

摘要

简介由于焦虑症是最常见的精神疾病之一,因此矫正病理性焦虑是现代药理学的一项重要任务。考虑到全球焦虑症和抑郁症(ADD)发病率持续上升的趋势,寻找各种工具来研究这一类疾病,并为 ADD 的药物治疗创造安全、高效的药物的紧迫性与日俱增。研究含有苯并咪唑和嘧啶循环片段的 2,4-二氧代丁酸盐的新衍生物对动物行为反应的影响。研究对象是由我们合成的 4-甲氧基苯基-4-氧代丁-2-烯酸与杂环胺的盐类。通过一系列测试评估了动物对引入所研究化合物的行为反应:"结果和讨论。实验结果表明,1b 是一种潜在的活性化合物,它能改善动物运动活动的多项指标,并具有抗焦虑作用。此外,随着物质 1b 的引入,在急性应激情况下还表现出抗抑郁活性。研究了首次获得的化合物 1a、1b 对动物行为反应的影响。通过 "结构-活性 "分析,确定了进一步定向合成含有 2-氨基嘧啶片段的 2,4-二氧代丁烷酸衍生物盐的优先顺序。已经确定了一种具有神经精神活性的化合物,建议对其进行进一步深入研究。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
查看原文
分享 分享
微信好友 朋友圈 QQ好友 复制链接
本刊更多论文
Evaluation of New Derivatives of 2,4-dioxobutanoic Acid Salts in Behavioral Studies of Laboratory Animals
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.
求助全文
通过发布文献求助,成功后即可免费获取论文全文。 去求助
来源期刊
自引率
0.00%
发文量
0
期刊最新文献
Development and validation of UV-spectrophotometry method for quantitative determination of amorphous darunavir Identification of luteolin-7-glucoside metabolites after oral administration and development of a method for their quantitative analysis Analysis of the distribution and persistence of organophosphorus pesticides malathion and diazinon in herbal plants Evaluation of drug release from topical dosage forms and permeability prediction through the skin barrier (review) A biorelevant test for tablets glycine sublingual in the «simulated saliva» dissolution medium
×
引用
GB/T 7714-2015
复制
MLA
复制
APA
复制
导出至
BibTeX EndNote RefMan NoteFirst NoteExpress
×
×
提示
您的信息不完整,为了账户安全,请先补充。
现在去补充
×
提示
您因"违规操作"
具体请查看互助需知
我知道了
×
提示
现在去查看 取消
×
提示
确定
0
微信
客服QQ
Book学术公众号 扫码关注我们
反馈
×
意见反馈
请填写您的意见或建议
请填写您的手机或邮箱
已复制链接
已复制链接
快去分享给好友吧!
我知道了
×
扫码分享
扫码分享
Book学术官方微信
Book学术文献互助
Book学术文献互助群
群 号:481959085
Book学术
文献互助 智能选刊 最新文献 互助须知 联系我们:info@booksci.cn
Book学术提供免费学术资源搜索服务,方便国内外学者检索中英文文献。致力于提供最便捷和优质的服务体验。
Copyright © 2023 Book学术 All rights reserved.
ghs 京公网安备 11010802042870号 京ICP备2023020795号-1