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Heteroarylnitrones as Drugs for Neurodegenerative Diseases: Synthesis, Neuroprotective Properties, and Free Radical Scavenger Properties.

  作者 Porcal, Williams;Hernandez, Paola;Gonzalez, Mercedes;Ferreira, Ana;Olea-Azar, Claudio;Cerecetto, Hugo;Castro, Ana;  
  选自 期刊  Journal of Medicinal Chemistry;  卷期  2008年51-19;  页码  6150-6159  
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[摘要]Compounds (More Than One Hetero Atom)) Section New 1,2,4-thiadiazolylnitrones and furoxanylnitrones were developed and evaluated as neuroprotective agents on a human neuroblastoma (SH-SY5Y) cells model. They inhibited at low micromolar concns. the oxidative damage and the death induced by exposure to hydrogen peroxide. These heteroarylnitrones showed excellent peroxyl free radical absorbance capacities, analyzed by oxygen radical absorbance capacity (ORAC) assay with fluorescein as the fluorescent probe, ranging from 1.5- to 16.5-fold the value of the ref. nitrone, a-phenyl-N-tert-butylnitrone (PBN). The ESR spectroscopy demonstrated the ability of these derivs. to directly trap and stabilize oxygen, carbon, and sulfur-centered free radicals. These results demonstrated the potential use of these heteroarylnitrones as neuroprotective agents in preventing the death of cells exposed to enhanced oxidative stress and damage.

 
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