1-氨基-3,6-脱水-1-脱氧-D-山梨醇衍生物的合成及糖苷酶抑制活性。
Synthesis and glycosidase inhibitory activity of 1-amino-3,6-anhydro-1-deoxy-D-sorbitol derivatives.
机构信息
UCO2M, UMR CNRS 6011, Université du Maine, Avenue O. Messiaen, 72085 Le Mans Cedex 09, France.
出版信息
Bioorg Chem. 2010 Apr;38(2):43-7. doi: 10.1016/j.bioorg.2009.12.002. Epub 2009 Dec 5.
PMID:20060997
Abstract
3,6-Anhydro-1-(aryl or alkylamino)-1-deoxy-D-sorbitol derivatives have been prepared in four steps from isosorbide, a by-product from the starch industry. The inhibitory activities of these new compounds have been evaluated towards 13 glycosidases. A first lead-compound was identified, which inhibited beta-N-acetylglucosaminidase from bovine kidney (82% inhibition at 1mM).
摘要
3,6-脱水-1-(芳基或烷基氨基)-1-去氧-D-山梨糖醇衍生物已从淀粉工业的副产物异山梨醇出发，经四步反应制备得到。这些新化合物对 13 种糖苷酶的抑制活性进行了评估。鉴定出了第一个先导化合物，它抑制牛肾的β-N-乙酰氨基葡萄糖苷酶（在 1mM 时抑制率为 82%）。
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