设计并合成一种具有心力衰竭生物活性的苯胺衍生物。
Design and Synthesis of an Aniline Derivative with Biological Activity on Heart Failure.
机构信息
Facultad de Medicina, Universidad Veracruzana. Médicos y Odontólogos s/n, 91010, Xalapa, Veracruz, Mexico.
Laboratory of Pharmaco-Chemistry at the Faculty of Chemical Biological Sciences of the University Autonomous of Campeche, Av. Ex Hacienda Kala s/n, 24085 San Francisco de Campeche, Campeche, Mexico.
出版信息
Comb Chem High Throughput Screen. 2021;24(2):220-232. doi: 10.2174/1386207323666200709163008.
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.
背景
已经合成了几种化合物作为心力衰竭的治疗替代物；然而，其制备需要特殊条件。
目的
本研究旨在从 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一系列反应，如醚化、加成和环化。通过光谱和光谱方法确证了所有获得的化合物的结构。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，化合物 8 可减轻心力衰竭，与化合物 4-7 和 9 相比，其梗死面积减小。
结论
本研究报告了一种简便的苯胺衍生物制备方法。该方法具有操作简单、成本低、易于处理等优点。此外，化合物 8 对心力衰竭表现出有趣的生物活性。这种现象特别有趣，因为该化合物诱导的生物活性可能涉及与用于治疗心力衰竭的其他药物不同的分子机制。
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