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

  作者 SASAKI HIROAKI; KITOH YUKI; MIKI KAZUHIKO; KINOSHITA KAORU; KOYAMA KIYOTAKA; KANEDA MIYUKI; TAKAHASHI KUNIO  
  选自 期刊  Heterocycles;  卷期  2012年85-11;  页码  2749-2756  
  关联知识点  
 

[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.

 
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