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依布硒啉及其开环衍生物的合成与生物学评价。

Synthesis and biological evaluation of ebselen and its acyclic derivatives.

作者信息

Chang Tsu-Chung, Huang Mei-Lan, Hsu Wen-Lin, Hwang Jing-Min, Hsu Ling-Yih

机构信息

Department of Biochemistry, National Defense Medical Center, Neihu, Taipei, Taiwan, ROC.

出版信息

Chem Pharm Bull (Tokyo). 2003 Dec;51(12):1413-6. doi: 10.1248/cpb.51.1413.

Abstract

Five ebselen and three acyclic ebselen derivatives were synthesized. These compounds were screened for their glutathione peroxidase (GSH Px)-like activity and scavenging activity against 1,1-diphenyl-2-pycryl-hydrazyl (DPPH) and peroxynitrite radical. All tested compounds displayed similar significant GSH Px-like activity, which are slightly higher than that of ebselen. The peroxynitrite scavenging activity showed that the acyclic allylseleno 4c was five times more potent than ebselen.

摘要

合成了五种依布硒啉和三种无环依布硒啉衍生物。对这些化合物进行了谷胱甘肽过氧化物酶(GSH Px)样活性以及对1,1-二苯基-2-苦基肼(DPPH)和过氧亚硝酸盐自由基的清除活性的筛选。所有测试化合物均表现出相似的显著GSH Px样活性,略高于依布硒啉。过氧亚硝酸盐清除活性表明,无环烯丙基硒醚4c的效力是依布硒啉的五倍。

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