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Journal of Medicinal Chemistry 2020-Sep

Recent Advances on Nitrones Design for Stroke Treatment

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José Marco-Contelles

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The recent advances of tetramethylpyrazine nitrones and quinolylnitrones for the treatment of stroke have been reviewed and compared with other agents, showing promising therapeutic applications. As a result of a functional transformation of natural product ligustrazine, (Z)-N-tert-butyl-1-(3,5,6-trimethylpyrazin-2-yl)methanimine oxide (6) is a multi-target small nitrone showing potent thrombolytic activity and free radicals scavenging power, in addition to non-toxicity and blood brain barrier permeability. Similarly, antioxidant (Z)-N-tert-butyl-1-(2-chloro-6-methoxyquinolin-3-yl)methanimine oxide (17) is a novel agent for cerebral ischemia therapy as it is able to scavenge different types of free radical species showing strong neuroprotection, and reduced infarct size.

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