Hybrid molecules of scutellarein and 3, 5, 6-trimethylpyrazine-2-formic acid linked with polar amino acid for ischemic stroke
Hybrid molecules of scutellarein and 3, 5, 6-trimethylpyrazine-2-formic acid linked with polar amino acid for ischemic stroke
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DOI:
10.1007/s00044-022-02892-0
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发表时间:
2022-04-22
影响因子:
2.6
通讯作者:
Dong,Yongxi
中科院分区:
文献类型:
--
作者:
Wu,Shuxia;Liu,Mingji;Dong,Yongxi
Scutellarin has been found to possess a certain protective activity against oxidative damage, and scutellarein has been proved to be the main absorption component of scutellarin in the small intestine. Tertramethylpyrazine is a commonly used antiplatelet drug, and its active metabolite 3, 5, 6-trimethylpyrazine-2-formic acid displays similar pharmacological activities with lower toxicity. Based on the principle of molecular hybridization and previous work, five hybrid molecules of scutellarein and 3, 5, 6-trimethylpyrazine-2-formic acid linked with polar amino acids were synthesized, and their anti-oxidative and antiplatelet aggregation activities were evaluated. The results showed that these hybrid molecules had better protective activity against oxidative damage and antiplatelet aggregation activity than the original drugs, and these results also demonstrated that molecular hybridization strategy could be applicable to develop better agents for ischemic stroke.Graphical abstract