In vivo Analgesic Activity of New N-arylphthalimides Derivatives in Mice.

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2023-01-01 DOI:10.2174/2772270817666230302145537

Asghar Davood, Atefeh Saadabadi, Porya Torkaman, Ehsan Salehi, Hamed Shafaroodi

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引用次数: 0

Abstract

Background: A series of phthalimides related to thalidomide have been studied for analgesic activity in the formalin test. The formalin test was performed in mice in a nociceptive pattern to evaluate analgesic activity.

Methods: In this study, nine derivatives of phthalimides were evaluated in terms of exerting analgesic effects in mice. They exerted significant analgesic effects compared to indomethacin and negative control. These compounds were synthesized and characterized by TLC, followed by IR and H¹NMR in the previous studies. Two distinct periods of high licking activity were used to analyze both acute and chronic pain. All compounds were compared with indomethacin and carbamazepine as positive control and vehicle as a negative control.

Results: All of the tested compounds exhibited significant analgesic activity in both the first and second phases of the test compared to the control group (DMSO), although they did not show more activity than the reference drug (indomethacin) but were comparable to indomethacin.

Conclusion: This information may be useful in the development of a more potent phthalimide as an analgesic agent that acts as a sodium channel blocker and COX inhibitor.

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新型n -芳基邻苯二胺衍生物在小鼠体内的镇痛活性。

背景:研究了一系列与沙利度胺相关的邻苯二胺在福尔马林试验中的镇痛活性。在小鼠中进行福尔马林试验，以评估痛觉模式的镇痛活性。方法:对9种邻苯二甲酸亚胺衍生物的小鼠镇痛作用进行了研究。与吲哚美辛和阴性对照相比，它们具有显著的镇痛效果。这些化合物在之前的研究中已经合成并通过TLC、IR和H1NMR进行了表征。两个不同时期的高舔活动被用来分析急性和慢性疼痛。所有化合物与吲哚美辛和卡马西平为阳性对照，对照物为阴性对照。结果:与对照组(DMSO)相比，所有被测化合物在试验的第一和第二阶段都表现出显著的镇痛活性，尽管它们没有表现出比参比药物(吲哚美辛)更强的活性，但与吲哚美辛相当。结论:这些信息可能有助于开发更有效的邻苯二胺作为钠通道阻滞剂和COX抑制剂的镇痛剂。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.