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新型 3-烷酰基/芳酰基/杂芳酰基-2H-色烯-2-硫酮:合成及抗氧化活性评价。

Novel 3-alkanoyl/aroyl/heteroaroyl-2H-chromene-2-thiones: synthesis and evaluation of their antioxidant activities.

机构信息

Department of Chemistry, Manipur University, Canchipur, Imphal 795003, Manipur, India.

出版信息

Eur J Med Chem. 2010 Jun;45(6):2250-7. doi: 10.1016/j.ejmech.2010.01.070. Epub 2010 Feb 2.

Abstract

A facile, convenient and high yielding synthesis of a combinatorial library of 3-alkanoyl/aroyl/heteroaroyl-2H-chromene-2-thiones has been developed by the condensation of easily accessible beta-oxodithioesters and salicylaldehyde/substituted 2-hydroxybenzaldehydes under solvent-free conditions. The assessment of radical scavenging capacity of the compounds towards the stable free radical 2,2-diphenyl-1-picrylhydrazyl (DPPH) was measured and these compounds were found to scavenge DPPH free radical efficiently. Five selected compounds were able to protect curcumin from the attack of sulfur free radical generated by radiolysis of glutathione (GSH). The newly synthesized compounds exhibited profound antioxidant activities. Five of them rendered comparatively high antioxidant capacity.

摘要

通过在无溶剂条件下,使易于获得的β-氧代二硫代酯与水杨醛/取代的 2-羟基苯甲醛缩合,开发了一种方便、高产的 3-酰基/芳酰基/杂芳酰基-2H-色烯-2-硫酮组合文库的简便合成方法。评估了化合物对稳定自由基 2,2-二苯基-1-苦基肼(DPPH)的清除能力,发现这些化合物能够有效地清除 DPPH 自由基。五种选定的化合物能够保护姜黄素免受谷胱甘肽(GSH)辐射分解产生的硫自由基的攻击。新合成的化合物表现出很强的抗氧化活性。其中五种具有较高的抗氧化能力。

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