稳定的芳基和杂芳基磺酰基酰胺肟的合成及其抗氧化和脂质过氧化活性评价。
Synthesis of stable aromatic and heteroaromatic sulfonyl-amidoximes and evaluation of their antioxidant and lipid peroxidation activity.
机构信息
Laboratory of Organic, Bioorganic and Natural Products Chemistry, Molecular Biology and Genetics Department, Democritus University of Thrace, 68100 Alexandroupolis, Greece.
Department of Pharmaceutical Chemistry, School of Pharmacy, Faculty of Health Sciences, Aristotle University of Thessaloniki, 54124 Thessaloniki, Greece.
出版信息
Eur J Med Chem. 2014 Jun 10;80:145-53. doi: 10.1016/j.ejmech.2014.04.040. Epub 2014 Apr 13.
We describe herein the synthesis of stable aromatic and heteroaromatic sulfonyl-amidoximes, from the reaction of amidoximes with the corresponding sulfonyl chlorides, in low to excellent yields. Evaluation of their antioxidant activity has shown that 17 out of 28 compounds highly compete DMSO for hydroxyl radicals, while five of them inhibit lipid peroxidation. Combining the reducing and anti-lipid peroxidation ability it seems that compounds 13 and 31 could be used as lead molecules.
我们在此描述了稳定的芳基和杂芳基磺酰基-羟胺的合成方法，即羟胺与相应的磺酰氯反应，产率低至优良。评估它们的抗氧化活性表明，28 种化合物中有 17 种对羟基自由基的竞争能力与 DMSO 相当，其中 5 种化合物抑制脂质过氧化。结合还原和抗脂质过氧化能力，化合物 13 和 31 似乎可以用作先导分子。
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