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具有抗氧化性能的褪黑素类似物新型吲哚酰肼/腙衍生物:合成与构效关系

Melatonin analogue new indole hydrazide/hydrazone derivatives with antioxidant behavior: synthesis and structure-activity relationships.

作者信息

Gürkök Gökce, Coban Tulay, Suzen Sibel

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, Tandogan, Ankara, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2009 Apr;24(2):506-15. doi: 10.1080/14756360802218516.

Abstract

Melatonin (MLT) is a hormone produced in the brain by the pineal gland, from the amino acid tryptophan. It is also an antioxidant hormone with a particular role in the protection of nuclear and mitochondrial DNA. In recent years, many physiological properties of MLT have been described resulting in much attention in the development of synthetic compounds possessing the indole ring. Sixteen MLT analogue indole hydrazide/hydrazone derivatives were synthesized and in vitro antioxidant activity was investigated. Most of the compounds showed significantly higher activity than MLT at 10(-3) M and 10(-4) M concentrations.

摘要

褪黑素(MLT)是一种由松果体在大脑中从氨基酸色氨酸产生的激素。它也是一种抗氧化激素,在保护核DNA和线粒体DNA方面具有特殊作用。近年来,已经描述了MLT的许多生理特性,这使得具有吲哚环的合成化合物的开发备受关注。合成了16种MLT类似物吲哚酰肼/腙衍生物,并研究了其体外抗氧化活性。大多数化合物在10^(-3) M和10^(-4) M浓度下显示出比MLT显著更高的活性。

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