Ferulic acid-carbazole hybrid compounds: Combination of cholinesterase inhibition, antioxidant and neuroprotection as multifunctional anti-Alzheimer agents

被引：46

作者：

Fang, Lei ^{[1
,2
,3
]}

Chen, Mohao ^{[1
,2
]}

Liu, Zhikun ^{[1
,2
,4
]}

Fang, Xubin ^{[1
,2
]}

Gou, Shaohua ^{[1
,2
]}

Chen, Li ^{[4
]}

机构：

[1] Southeast Univ, Jiangsu Prov Hitech Key Lab Biomed Res, Nanjing 211189, Peoples R China

[2] Southeast Univ, Sch Chem & Chem Engn, Nanjing 211189, Peoples R China

[3] China Pharmaceut Univ, State Key Lab Nat Med, Nanjing 210009, Peoples R China

[4] China Pharmaceut Univ, Dept Nat Med Chem, Nanjing 210009, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2016年 / 24卷 / 04期

关键词：

Hybrid compounds; Antioxidant; Anti-Alzheimer; AChE inhibitor; DISEASE;

D O I：

10.1016/j.bmc.2016.01.010

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：886 / 893

页数：8

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