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首页> 外文期刊>Organic Chemistry International >Synthesis and Characterization of a New Five and Six Membered Selenoheterocyclic Compounds Homologues of Ebselen
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Synthesis and Characterization of a New Five and Six Membered Selenoheterocyclic Compounds Homologues of Ebselen

机译:Ebselen的新的五和六元亚杂环杂环化合物的合成与表征

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摘要

The discovery of the antioxidant activity of selenoenzyme glutathione peroxidase (GPx) has attracted growing attention in the biochemistry of selenium. Among molecules which mimic the structure of the active site of the enzyme,N-phenyl-1,2-benzisoselenazolin-3-one1, Ebselen, exhibited useful anti-inflammatory properties. It has been extensively investigated and has undergone clinical trials as an anti-inflammatory agent. Unfortunately, Ebselen exhibits relatively poor catalytic activity, prompting attempts to design more efficacious GPx mimetics that would retain his low toxicity while manifesting improved catalytic properties. In this context, novel 1,2-benzoselenazine and 1,2-benzoselenazols, which are five and six membered homologues of Ebselen were synthesized and characterized. One structure has been proven by single crystal X-ray crystallography.
机译:硒酶谷胱甘肽过氧化物酶(GPx)的抗氧化活性的发现在硒的生物化学中引起了越来越多的关注。在模仿该酶活性位点结构的分子中,Nb-苯基-1,2-苯并硒基吲哚-3-甲酮Ebselen表现出有用的抗炎特性。它已被广泛研究,并已作为抗炎药进行了临床试验。不幸的是,Ebselen表现出相对较差的催化活性,促使人们尝试设计更有效的GPx模拟物,使其在保持低毒性的同时表现出改善的催化性能。在这种情况下,合成并表征了新的1,2-苯并硒氮杂和1,2-苯并硒氮杂,它们是埃布塞伦的五和六元同源物。单晶X射线晶体学已经证明了一种结构。

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