Novel 2-aryl-3,4,5-trihydroxypiperidines: Synthesis and glycosidase inhibition

Hui Zhao, Wu Bao Wang, Shinpei Nakagawa, Yue Mei Jia, Xiang Guo Hu, George W.J. Fleet, Francis X. Wilson, Robert J. Nash, Atsushi Kato*, Chu Yi Yu

*この論文の責任著者

研究成果: ジャーナルへの寄稿学術論文査読

10 被引用数 (Scopus)

抄録

Three pairs of novel 2-aryl-3,4,5-trihydroxypiperidines (6-8 and their enantiomers), the piperidine analogues of the pyrrolidine alkaloids radicamine A and radicamine B, were prepared from six-membered cyclic nitrones through a concise two-step procedure, i.e., Grignard reagent addition and deprotection. These novel polyhydroxylated piperidine iminosugars were assayed against 10 types of enzymes. Only compound 8 exhibited weak inhibition (IC50 1080 μmol/L) against β-galactosidase from rat intestinal lactases.

本文言語英語
ページ(範囲)1059-1063
ページ数5
ジャーナルChinese Chemical Letters
24
12
DOI
出版ステータス出版済み - 2013/12

ASJC Scopus 主題領域

  • 化学一般

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