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Design and synthesis of novel senkyunolide analogues as neuroprotective agents
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2018-01-12 , DOI: 10.1016/j.bmcl.2018.01.018
Yuanying Fang , Rikang Wang , Qi Wang , Yongbing Sun , Saisai Xie , Zunhua Yang , Min Li , Yi Jin , Shilin Yang

A class of senkyunolide analogues bearing benzofuranone fragment were designed, synthesized and evaluated for their neuroprotective effect in models of oxygen glucose deprivation (OGD) and oxidative stress. All tested compounds showed neuroprotection profile based on the cell viability assay. In particular, derivatives 1f1i possessing furoxan-based nitric oxide releasing functionality exhibited significant biological activities in OGD models. More importantly, compound 1g containing short linker with furoxan displayed the most potent neuroprotection at the concentration of 100 μM (cell survival up to 145.2%). Besides, 1g also showed the middle level neuroprotective effect in model of oxidative stress.



中文翻译:

设计和合成新的senkyunolide类似物作为神经保护剂。

设计,合成并评估了一类带有苯并呋喃酮片段的senkyunolide类似物在氧葡萄糖剥夺(OGD)和氧化应激模型中的神经保护作用。基于细胞活力测定法,所有测试的化合物均显示出神经保护作用。特别是,具有基于呋喃喃的一氧化氮释放功能的衍生物1f1i在OGD模型中表现出显着的生物学活性。更重要的是,含有短接头与呋喃喃的化合物1g在浓度为100μM时显示出最有效的神经保护作用(细胞存活率高达145.2%)。此外,1g在氧化应激模型中也表现出中等水平的神经保护作用。

更新日期:2018-01-12
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