依达拉奉和 1-氨基金刚烷新共轭物的合成及其与大鼠 NMDA 受体的相互作用

IF 0.8 4区医学 Q4 CHEMISTRY, MEDICINAL

Pharmaceutical Chemistry Journal Pub Date : 2024-06-21 DOI:10.1007/s11094-024-03134-w

V. V. Grigoriev, A. Yu. Aksinenko, T. V. Goreva, A. V. Gabrelyan, T. A. Epishina

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引用次数: 0

摘要

我们合成了新的依达拉奉含金刚烷的衍生物，依达拉奉是治疗肌萎缩侧索硬化症的两种药物之一。新的依达拉奉衍生物中的吡唑酮环和金刚烷分子通过相应的醇甲磺酸盐胺化反应，与烷基和氮杂环丁烷连接。研究发现，其中一些新化合物能有效阻断大鼠体内的异构 NMDA 受体结合位点，但对通道内 NMDA 受体结合位点的活性很小。研究人员分析了伊芬地尔结合位点的阻断能力与分子上的连接体和取代基结构之间的结构-活性关系。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Synthesis of New Conjugates of Edaravone and 1-Aminoadamantanes and Their Interaction with NMDA Receptors in Rats

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Synthesis of New Conjugates of Edaravone and 1-Aminoadamantanes and Their Interaction with NMDA Receptors in Rats

New adamantane-containing derivatives of edaravone, one of two drugs used to treat amyotrophic lateral sclerosis, were synthesized. The pyrazolone ring and adamantane moiety in the new edaravone derivatives were conjugated by alkyl and azetidine linkers via amination of the corresponding alcohol mesylates. Some of the new compounds were found to be effective blockers of the allosteric NMDA receptor binding site in rats but exhibited little activity against the intrachannel NMDA receptor binding site. The structure–activity relationship between the ability to block the ifenprodil binding site and the structure of the linkers and substituents on the molecule was analyzed.

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来源期刊

Pharmaceutical Chemistry Journal CHEMISTRY, MEDICINAL-PHARMACOLOGY & PHARMACY

CiteScore

1.30

自引率

22.20%

发文量

226

审稿时长

3-8 weeks

期刊介绍： Pharmaceutical Chemistry Journal is a monthly publication devoted to scientific and technical research on the creation of new drugs and the improvement of manufacturing technology of drugs and intermediates. International contributors cover the entire spectrum of new drug research, including: methods of synthesis; results of pharmacological, toxicological, and biochemical studies; investigation of structure - activity relationships in prediction of new compounds; methods and technical facilities used; and problems associated with the development of ecologically safe and economically feasible methods of industrial production. In addition, analytical reviews of the international literature in the field provide coverage of the most recent developments around the world. Pharmaceutical Chemistry Journal is a translation of the Russian journal Khimiko-Farmatsevticheskii Zhurnal. The Russian Volume Year is published in English from April. All articles are peer-reviewed.