Synthesis and biological activity of arylspiroborate salts derived from caffeic Acid phenethyl ester.

International Journal of Medicinal Chemistry Pub Date : 2015-01-01 Epub Date: 2015-03-05 DOI:10.1155/2015/418362
Martin J G Hébert, Andrew J Flewelling, Trevor N Clark, Natalie A Levesque, Jacques Jean-François, Marc E Surette, Christopher A Gray, Christopher M Vogels, Mohamed Touaibia, Stephen A Westcott
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引用次数: 4

Abstract

Two novel boron compounds containing caffeic acid phenethyl ester (CAPE) derivatives have been prepared and characterized fully. These new compounds and CAPE have been investigated for potential antioxidant and antimicrobial properties and their ability to inhibit 5-lipoxygenase and whether chelation to boron improves their biological activity. Sodium salt 4 was generally more active than ammonium salt 5 in the biological assays and surpassed the radical scavenging ability of CAPE. Compounds 4 and 5 were more active than CAPE and Zileuton in human polymorphonuclear leukocytes. These results clearly show the effectiveness of the synthesized salts as transporter of CAPE.

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咖啡酸苯乙酯衍生物芳基螺硼酸盐的合成及生物活性研究。
制备了两种含咖啡酸苯乙酯(CAPE)衍生物的新型硼化合物,并对其进行了表征。研究了这些新化合物和CAPE的潜在抗氧化和抗菌性能、抑制5-脂氧合酶的能力以及与硼的螯合是否能提高它们的生物活性。在生物实验中,钠盐4普遍比铵盐5更有活性,并且超过了CAPE的自由基清除能力。化合物4和5在人多形核白细胞中的活性高于CAPE和Zileuton。这些结果清楚地显示了合成盐作为CAPE转运体的有效性。
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期刊介绍: International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis. International Journal of Medicinal Chemistry is a peer-reviewed, Open Access journal that publishes original research articles as well as review articles in all areas of chemistry associated with drug discovery, design, and synthesis.
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