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6,7-二氢-1H-环戊并[d]嘧啶-2,4(3H,5H)-二酮的7-硫代衍生物的合成及抗氧化活性

Synthesis and Antioxidant Activity of 7-Thio Derivatives of 6,7-Dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione.

作者信息

Kononevich Yuriy M, Bobkova Ludmila S, Smolski Alexander S, Demchenko Anatoly M

机构信息

A. N. Nesmeyanov Institute of Organoelement Compounds, Russian Academy of Sciences, Vavilova str. 28, 119991, Moscow, Russian Federation.

Institute of Pharmacology and Toxicology, National Academy of Medical Science of Ukraine, Ezhena Pot'je str. 14, 03680, Kyiv, Ukraine.

出版信息

Sci Pharm. 2014 Oct 29;83(1):41-8. doi: 10.3797/scipharm.1406-09. Print 2015 Jan-Mar.

Abstract

New 7-thio derivatives of 6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione have been synthesized by the reaction of 3-cyclohexyl-7-thio-6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione with alkylhalogenides. The synthesized compounds were tested for antioxidant activity on the model of Fe(2+)-dependent oxidation of adrenaline in vitro. It was found that the antiradical activity of 7-thio derivatives of 6,7-dihydro-1H-cyclopenta[d]pyrimidine-2,4(3H,5H)-dione significantly depends on the structure of the substituent which is part of the thioether fragment of the base molecule.

摘要

通过3-环己基-7-硫代-6,7-二氢-1H-环戊并[d]嘧啶-2,4(3H,5H)-二酮与卤代烷反应,合成了6,7-二氢-1H-环戊并[d]嘧啶-2,4(3H,5H)-二酮的新型7-硫代衍生物。在体外肾上腺素的铁(2+)依赖性氧化模型上对合成的化合物进行了抗氧化活性测试。结果发现,6,7-二氢-1H-环戊并[d]嘧啶-2,4(3H,5H)-二酮的7-硫代衍生物的抗自由基活性显著取决于作为碱基分子硫醚片段一部分的取代基的结构。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/d2ef/4729228/85dee09de4a2/SciPharm-83-41-g001.jpg

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