Design of an Amide N-Glycoside Derivative of β-Glucogallin: A Stable, Potent, and Specific Inhibitor of Aldose Reductase

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• 作者：Linfeng Li ; Kun-Che Chang ; Yaming Zhou ; Biehuoy Shieh ; Jessica Ponder ; Adedoyin D. Abraham ; Hadi Ali ; Anson Snow ; J. Mark Petrash ; Daniel V. LaBarbera
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：January 9, 2014
• 年：2014
• 卷：57
• 期：1
• 页码：71-77
• 全文大小：478K
• ISSN：1520-4804

文摘

尾-Glucogallin (BGG), a major component of the Emblica officinalis medicinal plant, is a potent and selective inhibitor of aldose reductase (AKR1B1). New linkages (ether/triazole/amide) were introduced via high yielding, efficient syntheses to replace the labile ester, and an original two-step (90%) preparation of BGG was developed. Inhibition of AKR1B1was assessed in vitro and using transgenic lens organ cultures, which identified the amide linked glucoside (BGA) as a stable, potent, and selective therapeutic lead toward the treatment of diabetic eye disease.