当前位置: X-MOL 学术Lett. Drug Des. Discov. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Design, Synthesis, and Biological Evaluation of Novel Tetramethylpyrazine- nitrone Derivatives as Antioxidants
Letters in Drug Design & Discovery ( IF 1 ) Pub Date : 2021-05-01 , DOI: 10.2174/1570180817999201117145311
Haiyun Chen 1 , Chunyan Yan 2 , Jie Cao 3 , Zheng Liu 4 , Yewei Sun 3 , Yuqiang Wang 3
Affiliation  

Background: Thrombolysis and endovascular thrombectomy are the two main therapeutic strategies for ischemic stroke in clinic. However, reperfusion injury causes oxidative stress leading to overproduction of reactive oxygen species, mitochondrial dysfunction and subsequent cell death.

Methods: We designed and synthesized two tetramethylpyrazine-nitrone derivatives (T-003 and T- 005) and investigated their abilities for scavenging free radicals and protective effects as well as neurite outgrowth promotion in vitro.

Results: Both of them showed potent radical-scavenging activity and neuroprotective effects against iodoacetic acid-induced cell injury. Furthermore, T-003 and T-005 significantly promoted neurite outgrowth in PC12 cells.

Conclusion: Our results suggest that compound T-003 and T-005 could be potent antioxidants for the treatment of neurological disease, particularly ischemic stroke.



中文翻译:

作为抗氧化剂的新型四甲基吡嗪-硝酮衍生物的设计、合成和生物学评价

背景:溶栓和血管内血栓切除术是临床上缺血性卒中的两种主要治疗策略。然而,再灌注损伤会导致氧化应激,导致活性氧过量产生、线粒体功能障碍和随后的细胞死亡。

方法:我们设计并合成了两种四甲基吡嗪-硝酮衍生物(T-003 和 T-005),并在体外研究了它们清除自由基和保护作用以及促进神经突生长的能力。

结果:两者均显示出有效的自由基清除活性和对碘乙酸诱导的细胞损伤的神经保护作用。此外,T-003 和 T-005 显着促进 PC12 细胞的神经突生长。

结论:我们的结果表明,化合物 T-003 和 T-005 可能是治疗神经系统疾病,尤其是缺血性中风的有效抗氧化剂。

更新日期:2021-05-01
down
wechat
bug