【摘 要】
：
The development of novel anti-thrombotic agents with strong free radical scavenging activity is of great significance for the treatment of ischemic stroke.1 In the present study,3-alkyl/arylalkyl-subs
【机 构】
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Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009
【出 处】
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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
The development of novel anti-thrombotic agents with strong free radical scavenging activity is of great significance for the treatment of ischemic stroke.1 In the present study,3-alkyl/arylalkyl-substituted benzo[c]thiophen-l(3H)-ones(5a-h) were designed and synthesized.The most active compound 5d significantly inhibited the adenosine diphosphate(ADP)-and arachidonic acid(AA)-induced in vitro platelet aggregation,superior to clinically used anti-ischemic stroke drugs 3-n-butylphthalide (NBP) and Edaravone(Eda).More importantly,in comparison with both NBP and Eda,5d exhibited stronger anti-thrombotic and free radical scavenging activities,and better or comparable neuroprotective effects against ischemia/reperfusion(I/R) in rats,including amelioration of neurobehavioral function,reduction of infarct volume and brain water content,attenuation of cerebral damage and normalization of the levels of oxidative enzymes.Overall,our findings may provide an alternative strategy for the discovery of novel anti-ischemic stroke agents more potent than drugs like NBP and Eda.
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