Design, Synthesis, and Biological Evaluation of Novel Tetramethylpyrazine- nitrone Derivatives as Sntioxidants

(E-pub Ahead of Print)

Author(s): Haiyun Chen*, Chunyan Yan*, Jie Cao, Zheng Liu, Yewei Sun, Yuqiang Wang

Journal Name: Letters in Drug Design & Discovery

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Background: Thrombolysis and endovascular thrombectomy acted as two mainly therapeutic strategies for the ischemic stroke in clinic. However, reperfusion injury caused oxidative stress leading 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 and Discussion: Both of them showed potent radical-scavenging activity and neuroprotective effects against iodoacetic acid-induced cells 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.

Keywords: Ischemic stroke, oxidative stress, tetramethypyrazine-nitrone derivatives, radical-scavenging activity, neurite outgrowth, antioxidants

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(E-pub Ahead of Print)
DOI: 10.2174/1570180817999201117145311
Price: $95

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