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Synthesis and biological evaluation of 2,2-dimethylbenzopyran derivatives as potent neuroprotection agents

机译：2,2-二甲基苯并吡喃衍生物作为强效神经保护剂的合成及生物学评价

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The development of novel neuroprotection agents is of great significance for the treatment of ischemic stroke. In this study, a series of compounds comprising 2,2-dimethylbenzopyran groups and cinnamic acid groups have been synthesized. Preferential combination principles and bioisostere that improved the neuroprotective effect of the compounds were identified for this series via biological activity assay in vitro . Meanwhile, a functional reversal group of the acrylamide amide resulted in the most active compounds. Among them, BN- 07 significantly improved the morphology of neurons and obviously increased cell survival rate of primary neurons induced by oxygen glucose deprivation (OGD), superior to clinically used anti-ischemic stroke drug edaravone (Eda). Overall, our findings may provide an alternative strategy for the design of novel anti-ischemic stroke agents with more potency than Eda.
机译：新型神经保护剂的开发对缺血性中风的治疗具有重要意义。在这项研究中，合成了一系列包含2，2-二甲基苯并吡喃基和肉桂酸基的化合物。通过体外生物活性测定，确定了优先组合原则和生物甾体改善了这些化合物的神经保护作用。同时，丙烯酰胺酰胺的官能反转基团导致活性最高。其中，BN-07明显改善了由氧葡萄糖剥夺（OGD）诱导的原代神经元的神经元形态，并明显提高了原代神经元的细胞存活率，优于临床使用的抗缺血性中风药物依达拉奉（Eda）。总体而言，我们的发现可能为设计新型抗缺血性卒中药物提供比Eda更高效力的替代策略。

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