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首页> 外文期刊>Pharmaceutical research >Scavenging of the one-electron reduction product from nisoldipine with relevant thiols: electrochemical and EPR spectroscopic evidences.
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Scavenging of the one-electron reduction product from nisoldipine with relevant thiols: electrochemical and EPR spectroscopic evidences.

机译:用相关硫醇清除尼索地平的单电子还原产物:电化学和EPR光谱学证据。

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PURPOSE: To determine the formation of the one-electron reduction product from nisoldipine and its reactivity with relevant thiols in mixed medium. METHODS: Cyclic voltammetry (CV) and electron paramagnetic resonance (EPR) techniques were used to determine the one-electron reduction product corresponding to the nitro radical anion. CV was employed to assess both the rate constants corresponding to the decay of the radicals and its interaction with relevant thiols. RESULTS: The nisoldipine radical anion follows second order kinetics, with an association rate constant of 283+/-16 l mol(-1) sec(-1). Nitro radical anion from nisoldipine significantly reacted with thiol compounds. This reactivity was significantly higher than the natural decay of the radical in mixed medium. EPR spectra recorded in situ using DMF/ 0.1 N NaOH (pH 13) confirmed the formation of the nitro radical anion, giving a well-resolved spectra in 35 lines using 0.1 G modulation. CONCLUSIONS: Electrochemical and EPR data indicated that all the tested thiols scavenged the nitro radical anion from nisoldipine. The following tentative order of reactivity towards the thiols can be proposed: cysteamine approximately glutathione > N-acetylcysteine > captopril > penicillamine.
机译:目的:确定尼索地平形成的单电子还原产物及其在混合介质中与相关硫醇的反应性。方法:采用循环伏安法(CV)和电子顺磁共振(EPR)技术确定对应于硝基自由基阴离子的单电子还原产物。使用CV评估与自由基的衰变相对应的速率常数及其与相关硫醇的相互作用。结果:尼索地平自由基阴离子遵循二级动力学,缔合速率常数为283 +/- 16 l mol(-1)sec(-1)。尼索地平的硝基自由基阴离子与硫醇化合物显着反应。该反应性显着高于混合介质中自由基的自然衰变。使用DMF / 0.1 N NaOH(pH 13)原位记录的EPR光谱证实了硝基自由基阴离子的形成,使用0.1 G调制在35条谱线中得到了良好分辨的光谱。结论:电化学和EPR数据表明,所有测试的硫醇都清除了尼索地平中的硝基自由基阴离子。可以提出对硫醇的以下暂定反应顺序:半胱胺近似于谷胱甘肽> N-乙酰基半胱氨酸>卡托普利>青霉素。

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