STRUCTURE-ACTIVITY RELATIONSHIPS OF BIFLAVONOIDS FOR β-SECRETASE (BACE-1) INHIBITORY ACTIVITY

被引：8
|
作者：
Sasaki, Hiroaki [1 ]
Kitoh, Yuki [2 ]
Miki, Kazuhiko [2 ]
Kinoshita, Kaoru [2 ]
Koyama, Kiyotaka [2 ]
Kaneda, Miyuki [1 ]
Takahashi, Kunio [2 ]
机构：
[1] Shujitsu Univ, Sch Pharm, Naka Ku, Okayama 7038516, Japan
[2] Meiji Pharmaceut Univ, Dept Pharmacognosy & Phytochem, Kiyose, Tokyo 2048588, Japan
来源：
HETEROCYCLES | 2012年 / 85卷 / 11期
关键词：
Biflavonoid; Amentoflavone; BACE-1; beta-Secretase; Alzheimer's Disease;
D O I：
10.3987/COM-12-12561
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Bioactive natural products are useful sources of new pharmaceutics. Their analogues are also important for evaluating structure-activity relationships. In this study the structure-activity relationships of 2,3-dihydro-6-methylginketin (1) for BACE-1 inhibitory activity were studied. Biflavonoids consisting of flavanone and flavone, and also the presence of a methoxy group at the C-4' position, were found to be important for strong activity. 2,3-Dihydro-6-methylbilobetin (2) showed strong activity with an IC50 value of 0.56 mu M.
引用
收藏
页码：2749 / 2756
页数：8
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