Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents
Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents
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DOI：
10.1016/j.bmc.2016.01.010
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发表时间：
2016-02-15
影响因子：
3.5
通讯作者：
Chen, Li
中科院分区：
文献类型：
--
作者：
Fang, Lei;Chen, Mohao;Chen, Li
为了寻找新型多功能抗阿尔茨海默病药物，设计合成了一系列阿魏酸-咔唑杂合化合物。Ellman的试验表明，杂合化合物对胆碱酯酶显示出中等至有效的抑制活性。特别地，化合物5 k的AChE抑制效力（IC 50 1.9 μ M）甚至比加兰他敏高5倍。此外，目标化合物还表现出明显的抗氧化能力和神经保护作用，特别是对抗ROS诱导的毒性。值得注意的是，5 k的神经保护作用明显上级阿魏酸和咔唑的混合物，表明杂化化合物的治疗效果优于相应混合物的组合给药。(c)2016爱思唯尔有限公司版权所有。
In order to search for novel multifunctional anti-Alzheimer agents, a series of ferulic acid-carbazole hybrid compounds were designed and synthesized. Ellman's assay revealed that the hybrid compounds showed moderate to potent inhibitory activity against the cholinesterases. Particularly, the AChE inhibition potency of compound 5k (IC50 1.9 mu M) was even 5-fold higher than that of galantamine. In addition, the target compounds showed pronounced antioxidant ability and neuroprotective property, especially against the ROS-induced toxicity. Notably, the neuroprotective effect of 5k was obviously superior to that of the mixture of ferulic acid and carbazole, indicating the therapeutic effect of the hybrid compound is better than the combination administration of the corresponding mixture. (c) 2016 Elsevier Ltd. All rights reserved.