Synthesis and decreasing A beta content evaluation of arctigenin-4-yl carbamate derivatives
Synthesis and decreasing A beta content evaluation of arctigenin-4-yl carbamate derivatives
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牛蒡甙元-4-基氨基甲酸酯衍生物的合成及降低Aβ含量评价
DOI：
10.1016/j.bmcl.2016.05.028
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发表时间：
2016
影响因子：
2.7
通讯作者：
Hu Lihong
中科院分区：
文献类型：
--
作者：
Xu Xingyu;Li Cong;Lei Min;Zhu Zhiyuan;Yan Jianming;Shen Xu;Hu Lihong
合成了一系列牛至皂苷元-4-氨基甲酸酯类化合物，并对其降低HEK293-APPswe细胞中β-淀粉样蛋白(A-β)含量的作用进行了评价。大多数牛至皂苷元-4-基芳烷基或芳基氨基甲酸酯的衍生物在降低A-β含量方面表现出更好的效力。在所合成的化合物中，牛至皂苷元-4-(3-氯苯基)氨基甲酸酯(20)对Aβ含量的降低效果最强，在20μM时Aβ含量降低了78.7%。此外，在μM浓度为1、10和20℃时，牛至皂素-4-基(4-氯苯基)氨基甲酸酯(19)和牛至皂素-4-基(3-氯苯基)氨基甲酸酯(20)对A DNA含量的降低效果优于牛至皂素。
A series of arctigenin-4-yl carbamate derivatives were synthesized and evaluated for potency in reducingβ-amyloid (Aβ) content in HEK293-APPswe cells. Most of the arctigenin-4-yl aralkyl or aryl carbamate derivatives showed improved potency in reducing Aβcontent. Among the synthesized compounds, arctigenin-4-yl (3-chlorophenyl)carbamate (20) exhibited the strongest potency with 78.7% Aβcontent reduction at 20 μM. Furthermore, the effect of arctigenin-4-yl (4-chlorophenyl)carbamate (19) and arctigenin-4-yl (3-chlorophenyl)carbamate (20) on lowing Aβcontent was better than arctigenin under the concentrations of 1, 10 and 20 μM.