Synthesis and biological evaluation of ebselen and its acyclic derivatives

被引:31
作者
Chang, TC
Huang, ML
Hsu, WL
Hwang, JM
Hsu, LY
机构
[1] Natl Def Med Ctr, Sch Pharm, Taipei, Taiwan
[2] Natl Def Med Ctr, Dept Biochem, Taipei, Taiwan
[3] Tri Serv Gen Hosp, Dept Radiat Oncol, Taipei 114, Taiwan
[4] Buddhist Tzu Chi Med Ctr, Canc Med Ctr, Hualien, Taiwan
[5] Buddhist Tzu Chi Med Ctr, Dept Radiat Oncol, Hualien, Taiwan
关键词
ebselen derivative; selenoorganic compound; antioxidant; peroxynitrite; glutathione peroxidase;
D O I
10.1248/cpb.51.1413
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
引用
收藏
页码:1413 / 1416
页数:4
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