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2-芳基-3-(嘧啶-2-基)-噻唑烷酮的高效合成及抗氧化评价。

Efficient synthesis and antioxidant evaluation of 2-aryl-3-(pyrimidin-2-yl)-thiazolidinones.

机构信息

Laboratório de Química (LAQUIABIO), Universidade Federal de Pelotas, Pelotas, Rio Grande do Sul, Brazil.

出版信息

J Biochem Mol Toxicol. 2013 Sep;27(9):445-50. doi: 10.1002/jbt.21506. Epub 2013 Jun 24.

Abstract

In the present study, we reported the efficient synthesis of 11 3-(pyrimidin-2-yl)-thiazolidinones in good yields using molecular sieve as the desiccant agent. In addition, we have evaluated the antioxidant capacity of the synthesized compounds by the 2,2-diphenyl-2-picrylhydrazyl hydrate (DPPH•) and the 2,2-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) diammonium salt (ABTS(+•) ) radicals scavenging assay. Six compounds showed antioxidant activity towards DPPH• (EC50 between 16.13 and 49.94 µg/mL) and also demonstrated excellent activity regarding ABTS(+•) (TEAC: 10.32-53.52). These results showed that compounds 3-(pyrimidin-2-yl)-thiazolidinones may be easily synthesized by a less expensive procedure and could be a good starting point to the development of new antioxidant compounds.

摘要

在本研究中,我们报告了使用分子筛作为干燥剂,以良好的产率高效合成 11 个 3-(嘧啶-2-基)-噻唑烷-2,4-二酮的方法。此外,我们通过 2,2-二苯基-2-苦基肼基(DPPH•)和 2,2-联氮双(3-乙基苯并噻唑啉-6-磺酸)二铵盐(ABTS(+•))自由基清除试验评估了合成化合物的抗氧化能力。六种化合物对 DPPH•(EC50 在 16.13 到 49.94 µg/mL 之间)具有抗氧化活性,并且对 ABTS(+•)(TEAC:10.32-53.52)也具有出色的活性。这些结果表明,3-(嘧啶-2-基)-噻唑烷-2,4-二酮类化合物可以通过更经济的方法轻易合成,并且可能是开发新抗氧化化合物的良好起点。

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