香豆素衍生物的高效微波合成及其抗氧化和抗炎特性评估

Anziya P A, S. T S, A. K, Anjali Krishna, Sini Baby, Divine P Daniel
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引用次数: 0

摘要

微波辐射是一种电磁辐射,在有机合成中被用作加热源。香豆素是一种苯并吡喃酮衍生物,具有抗凝、抗菌、镇痛、消炎等多种药理活性。研究的主要目的是比较用微波辅助方法合成一些香豆素衍生物的方法。我们合成了两种不同的香豆素衍生物,并对它们的抗炎活性和抗氧化活性进行了评估。3- 乙酰基香豆素(3-acetyl-2H-Chromen-2-one)是在哌啶存在下通过与水杨醛和乙酰乙酸乙酯反应合成的,3-乙酰基-6-溴香豆素(3-acetyl-6-bromo-2H-Chromen-2-one)是通过使用 5-溴水杨醛合成的。合成的化合物通过 MP、TLC、IR 和 NMR 进行了表征。化合物的抗氧化活性是通过三氯化铁还原力、一氧化氮和过氧化氢清除法进行测定的。化合物的抗炎活性是通过使用 BSA 法进行蛋白质变性得出的。在合成的两种化合物中,溴代乙酰香豆素的抗氧化和抗炎活性高于标准化合物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Efficient microwave synthesis of coumarin derivatives with evaluation of their antioxidant and anti-inflammatory properties
Microwave radiation, an electromagnetic radiation, is used as a source of heating in organic synthesis. Coumarin, a benzopyrone derivative, shows various pharmacological activities such as anticoagulant, antimicrobial, analgesic, anti-inflammatory. The prime objective was to compare the synthesis of some coumarin derivatives by microwave assisted methods. Two different coumarin derivatives were synthesized and evaluated for their anti-inflammatory activity and anti-oxidant activity. 3-Acetylcoumarin (3-acetyl-2H-Chromen-2- one) was synthesized by reaction with salicylaldehyde and ethyl acetoacetate in presence of piperidine and the 3-acetyl-6-bromocoumarin (3-acetyl-6-bromo-2H-chromen-2-one) was synthesized by using 5-bromo-salicyladehyde. The synthesized compounds were characterized by MP, TLC, IR and NMR. The antioxidant activity of the compounds was done by reducing power by ferric chloride, nitric oxide and hydrogen peroxide scavenging method. The anti-inflammatory activity of the compounds was done by protein denaturation using BSA method. Out of the two compounds synthesized, bromine-substituted acetyl coumarin showed more anti-oxidant and anti-inflammatory activity when compared to standard.
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