3-正丁苯酞-依达拉奉复合物治疗脑缺血的设计、合成及生物学评价

Hu Xia-min, Wei Dong, Qian Zhang, Qiong Yuan, Zhi-wen Cui, Cheng Gao, YU ZHI-JUN, Zhen-li Min
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引用次数: 1

摘要

合成了一系列3-正丁基苯乙烯-依达拉奉杂化合物,并通过分析和光谱(IR、1h NMR、13c NMR、MS和元素分析)对其结构进行了鉴定。用浊度法和Fenton法对合成的化合物体外抗血小板活性进行了评价。结果表明,化合物11a具有与3-正丁基苯乙烯相似的抗血小板聚集活性,其·OH清除活性(ic50值为2.87 mM)高于依达拉奉(ic50值为3.57 mM)。
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Design, Synthesis and Biological Evaluation of 3-n-Butylphthlide-Edaravone Hybrids as Potential Agents for the Treatment of Cerebral Ischemia
: A series of 3- n -butylphthlide-edaravone hybrids was synthesized and their structures were elucidated on the basis of analytical and spectral (IR, 1 H NMR, 13 C NMR, MS and elemental analyses) data. These synthesized compounds were evaluated for their in vitro antiplatelet by the turbidimetric method and antioxidant activities by the Fenton method. The results indicated that compound 11a showed similar potency of antiplatelet aggregation as 3- n -butylphthlide and stronger ·OH scavenging activity (IC 50 value of 2.87 mM) than edaravone (IC 50 value of 3.57 mM).
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