香豆素衍生物的结构修饰：抗氧化和脂氧合酶（LOX）抑制活性的测定。
Structural modifications of coumarin derivatives: Determination of antioxidant and lipoxygenase (LOX) inhibitory activity.
作者信息
Roussaki Marina, Zelianaios Konstantinos, Kavetsou Eleni, Hamilakis Stylianos, Hadjipavlou-Litina Dimitra, Kontogiorgis Christos, Liargkova Thalia, Detsi Anastasia
机构信息
Laboratory of Organic Chemistry, School of Chemical Engineering, National Technical University of Athens, Heroon Polytechniou 9, Zografou Campus, GR 15773 Athens, Greece.
Laboratory of Organic Chemistry, School of Chemical Engineering, National Technical University of Athens, Heroon Polytechniou 9, Zografou Campus, GR 15773 Athens, Greece.
出版信息
Bioorg Med Chem. 2014 Dec 1;22(23):6586-6594. doi: 10.1016/j.bmc.2014.10.008.
In the present project, a series of coumarin analogues, were synthesised and evaluated for their antioxidant and soybean lipoxygenase inhibitory activity. A variety of structural modifications on the coumarin scaffold revealed interesting structure–activity relationships concerning the different biological assays. Prenyloxy-coumarins 9 and 10 displayed the best combined inhibition of lipid peroxidation and soybean lipoxygenase. Thiocoumarins 11 and 14 were identified as potent lipoxygenase inhibitors whereas hydrazone analogues 15 and 16 were efficient DPPH radical scavengers.
在本项目中，合成了一系列香豆素类似物，并对其抗氧化和大豆脂氧合酶抑制活性进行了评估。对香豆素骨架进行的各种结构修饰揭示了与不同生物学测定相关的有趣构效关系。异戊烯氧基香豆素9和10对脂质过氧化和大豆脂氧合酶表现出最佳的联合抑制作用。硫代香豆素11和14被鉴定为有效的脂氧合酶抑制剂，而异腙类似物15和16是高效的DPPH自由基清除剂。
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