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Design and Synthesis of an Aniline Derivative with Biological Activity on Heart Failure
Combinatorial Chemistry & High Throughput Screening ( IF 1.6 ) Pub Date : 2021-01-31 , DOI: 10.2174/1386207323666200709163008
Garcimarero-Espino E Alejandra 1 , Figueroa-Valverde Lauro 2 , Rosas-Nexticapa Marcela 3 , Lopez-Ramos Maria 2 , Diaz Cedillo Francisco 4 , Mateu-Armand Virginia 3 , Ortiz-Ake Yazmin 2
Affiliation  

Background: Several compounds have been synthesized as a therapeutic alternative for heart failure; however, its preparation requires special conditions.

Objective: The aim of this study, was to synthesize some aniline derivatives (4-9) from 3- ethynylaniline to evaluate their biological activity against heart failure.

Methods: The synthesis of aniline derivatives involved a series of reactions such as etherification, addition, and cyclization. The structure of all compounds obtained was confirmed by spectroscopic and spectrometric methods. In addition, to evaluate the biological activity of compounds, an ischemia/reperfusion injury model was used.

Results: The results showed that compound 8 decreases heart failure, which translates into a decrease in the infarction area compared to compounds 4-7 and 9.

Conclusion: This study reports a facile method for the preparation of aniline derivatives. This method offers some advantages such as; a simple procedure, low cost, and easy work up. In addition, compound 8 showed an interesting biological activity against heart failure. This phenomenon is particularly interesting because the biological activity induced by this compound could involve a molecular mechanism that is different from other drugs used for the treatment of heart failure.



中文翻译:

一种对心力衰竭具有生物活性的苯胺衍生物的设计与合成

背景:已经合成了几种化合物作为心力衰竭的治疗替代品;然而,它的制备需要特殊的条件。

目的:本研究的目的是从 3-乙炔基苯胺合成一些苯胺衍生物 (4-9) 以评估它们对心力衰竭的生物活性。

方法:苯胺衍生物的合成涉及醚化、加成、环化等一系列反应。所得所有化合物的结构均通过光谱和光谱方法确认。此外,为了评估化合物的生物活性,使用了缺血/再灌注损伤模型。

结果:结果表明,与化合物 4-7 和 9 相比,化合物 8 减少了心力衰竭,这意味着梗死面积减少。

结论:本研究报告了一种制备苯胺衍生物的简便方法。这种方法提供了一些优点,例如;程序简单,成本低,易于操作。此外,化合物 8 显示出一种有趣的抗心力衰竭的生物活性。这种现象特别有趣,因为这种化合物诱导的生物活性可能涉及一种不同于其他用于治疗心力衰竭的药物的分子机制。

更新日期:2021-02-11
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