Faculty of Chemistry, Adam Mickiewicz University, Poznań, Poland.
Faculty of Biology, Adam Mickiewicz University, Poznań, Poland.
Nat Prod Res. 2022 Jul;36(13):3413-3419. doi: 10.1080/14786419.2020.1864364. Epub 2020 Dec 24.
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.
通过铜催化的叠氮-炔环加成（CuAAC）反应，我们合成了一系列新型的含三唑的禾谷类衍生物。所有新获得的化合物的结构都通过光谱分析和密度泛函理论（DFT）方法得到了确认。这些衍生物被筛选出来，以评估它们对自由基诱导的氧化溶血的保护能力，自由基是由 2,2'-偶氮双（2-甲基丙脒）二盐酸盐（AAPH）生成的。我们的工作表明，带有丙基或辛基连接基团和邻苯二甲酰亚胺基团的吲哚-三唑片段的衍生物具有折叠结构，能够有效地保护人红细胞免受氧化应激诱导的溶血。
