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Hybrid molecules of scutellarein and tertramethylpyrazine's active metabolites for ischemic stroke
Yongxi Dong1, Xiaohe Zhang2, Mingji Liu3
1College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China; State Key Laboratory of Functions and Applications of Medicinal Plants, Guizhou Medical University, Guiyang 550014, China; School of Pharmacy, Guizhou Medical University, Guiyang 550025, China; Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guiyang 550004, China.
Abstract:
A series of hybrid molecules of scutellarein and tertramethylpyrazine's active metabolites have been synthesized. Compared to the original compound, these prepared compounds exhibited higher water solubility, more appropriate logP and better stability. Importantly, compounds 11b, 11d and 11e showed improved neuroprotective activity against the H2O2-induced cell death in PC12 cells, and better antithrombosis activity. The optimized compound 11b was further evaluated by cerebral ischemia/ reperfusion in the middle cerebral artery occlusion (MCAO) model, the results showed that the compound could significantly reduce the infarct area and decrease the neuronal cell damage in CA1 pyramidal neurons. Overall, we demonstrated that the twin drug strategy could be applied in the development of agents for the treatment of ischemic stroke.