Synthesis of 13-(substituted benzyl) berberine and berberrubine derivatives as antifungal agents

被引：100

作者：

Park, Ki Duk

Lee, Jong Hun

Kim, Sung Han

Kang, Tae Hoon

Moon, Jae Sun

Kim, Sung Uk ^{[1
]}

机构：

[1] Korea Res Inst Biosci & Biotechnol, Div Biomat Sci, Taejon 305333, South Korea

[2] Nutrex Technol, Seoul 137864, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 15期

关键词：

antifungal activity; 13-(substituted benzyl) berberine; 13-(substituted benzyl) berberrubine;

D O I：

10.1016/j.bmcl.2006.05.033

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

By introducing various aromatic groups in 13-C of berberine and berberrubine, a series of 13-(substituted benzyl) berberine and berberrubine derivatives were synthesized and examined for antifungal activities against various human pathogenic fungi. The synthesized compounds exhibited more potent antifungal activities than berberine and berberrubine. Among them, 13-(4-isopropyl benzyl) berberine (6e) exerted the most potent antifungal activities against Candida species (MIC = 1-8 mu g/ml) and a 4-fold stronger activity than 13-(4-isopropyl benzyl) berberrubine (7e) synthesized by pyrolysis of compound 6e. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：3913 / 3916

页数：4

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