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New triazole-bearing gramine derivatives – synthesis, structural analysis and protective effect against oxidative haemolysis
Natural Product Research ( IF 2.2 ) Pub Date : 2020-12-24 , DOI: 10.1080/14786419.2020.1864364
W Kozanecka-Okupnik 1 , A Sierakowska 1 , N Berdzik 1 , I Kowalczyk 1 , L Mrówczyńska 2 , B Jasiewicz 1
Affiliation  

Abstract

The new series of triazole-bearing gramine derivatives were synthesized through a CuAAC procedure. The structures of all newly obtained compounds were confirmed by spectroscopic analysis and DFT methods. The obtained derivatives were screened for their protective potency against oxidative haemolysis induced by free radicals generated from 2,2’-azobis(2-methylpropionamidine) dihydrochloride (AAPH). Our work demonstrates that derivatives with propyl or octyl linker and phthalimide group associated with indole-triazole moiety, which have a folded structure, effectively protect human erythrocytes against oxidative stress-induced haemolysis.



中文翻译:

新的含有三唑的禾本科衍生物——合成、结构分析和对氧化溶血的保护作用

摘要

通过CuAAC程序合成了新系列的含有三唑的禾本科衍生物。所有新获得的化合物的结构均通过光谱分析和 DFT 方法确认。筛选获得的衍生物对由 2,2'-偶氮二(2-甲基丙脒) 二盐酸盐 (AAPH) 产生的自由基引起的氧化溶血的保护效力。我们的工作表明,具有丙基或辛基接头和邻苯二甲酰亚胺基团的衍生物与具有折叠结构的吲哚-三唑部分相关,可有效保护人类红细胞免受氧化应激诱导的溶血。

更新日期:2020-12-24
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