Synthesis and in vitro evaluation of 12-(substituted aminomethyl) berberrubine derivatives as anti-diabetics
Synthesis and in vitro evaluation of 12-(substituted aminomethyl) berberrubine derivatives as anti-diabetics
复制标题
12-(取代氨甲基)小檗红素衍生物抗糖尿病药的合成及体外评价
DOI：
10.1016/j.bmcl.2014.02.032
复制
发表时间：
2014-04-01
影响因子：
2.7
通讯作者：
Wu, Yong
中科院分区：
文献类型：
--
作者：
Li, Renjun;Wu, Jianbo;Wu, Yong
通过在小檗红碱的12位上引入不同的氨甲基，合成了一系列12位取代氨甲基小檗红碱衍生物，并对其抗2型糖尿病活性进行了评价。结果表明，大部分化合物具有中等至良好的抗糖尿病活性，与小檗碱、阳性对照罗格列酮和胰岛素相当或更好。尤其是在C-12位具有N-甲基哌嗪-4-甲基的化合物3b，表现出最强的抗糖尿病活性。(C)2014爱思唯尔有限公司版权所有。
By introducing various amino methyl groups into 12-position of berberrubine, a series of 12-(substituted aminomethyl) berberrubine derivatives were synthesized and evaluated for their anti-diabetic activity against type 2 diabetes mellitus. The results indicated that most of the prepared compounds exhibited moderate to good anti-diabetic activity, which were comparable to or even better than the berberine, the positive control rosiglitazone and insulin. Especially, compound 3b with an N-methyl piperazine-4-methyl group at C-12, exerted the most powerful anti-diabetic activity. (C) 2014 Elsevier Ltd. All rights reserved.