【摘 要】
:
To search for potent anti-isehemic stroke agents,a series of tetramethylpyrazine (TMP)/resveratrol (RES) hybrids 6a-t were designed and synthesized.These hybrids inhibited adenosine diphosphate (ADP)-or arachidonic acid (AA)-induced platelet aggregation,a
【机 构】
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State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Discovery for Metabolic Di
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To search for potent anti-isehemic stroke agents,a series of tetramethylpyrazine (TMP)/resveratrol (RES) hybrids 6a-t were designed and synthesized.These hybrids inhibited adenosine diphosphate (ADP)-or arachidonic acid (AA)-induced platelet aggregation,among them,6d,6g-i,6o and 6q were more active than TMP.The most active compound 6h exhibited more potent antiplatelet aggregation activity than TMP,RES,as well as positive control ticlopidine (Ticlid) and aspirin (ASP).Furthermore,6h exerted strong antioxidative activity in a dose-dependent manner in rat pheochromocytoma PC12 cells which were treated with hydrogen peroxide (H2O2) or hydroxyl radical (·OH).Importantly,6h significantly protected primary neuronal cells suffered from oxygen-glucose deprivation/reoxygenation (OGD/R) injury,comparable to an anti-ischemic drug edaravone (Eda).Together,our findings suggest that 6h may be a promising candidate warranting further investigation for the intervention of ischemic stroke.
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