Synthesis of 4-methylcoumarin derivatives containing 4,5-dihydropyrazole moiety to scavenge radicals and to protect DNA

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• 作者：Chuan Xiao^a ; Xu-Yang Luo^a ; De-Jun Li^a ; Hang Lu^a ; Zai-Qun Liu^a ; Zhi-Guang Song^a ; ^{szg@jlu.edu.cn} ; Ying-Hua Jin^b
• 关键词：Synthesis ; 4-Methylcoumarins ; 4 ; 5-Dihydroxypyrazole ; Free radical ; Antioxidant ; Oxidation of DNA
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：July, 2012
• 年：2012
• 卷：53
• 期：Complete
• 页码：159-167
• 全文大小：1058 K

文摘

A series of 4-methylcoumarin derivatives containing 4,5-dihydropyrazole moiety were synthesized and their antioxidant activities were evaluated in AAPH (2,2¡ä-azobis(2-amidinopropane hydrochloride))-induced oxidation of DNA, and in trapping DPPH (2,2¡ä-diphenyl-1-picrylhydrazyl) and ABTS^+? (2,2¡ä-azinobis(3-ethylbenzothiazoline-6-sulfonate) cationic radical), respectively. Among coumarin derivatives, 3a-d and 4a-c exhibited the termination of radical propagation-chains in AAPH-induced oxidation of DNA. The ortho dihydroxyphenyl substitution at 5 position and 1-unsubstitution of the 4,5-dihydroxylpyrazole was found enhancing the antioxidant activities of these coumarin derivatives.