Synthesis and glycosidase inhibitory activity of noeurostegine-a new and potent inhibitor of beta-glucoside hydrolases.
Synthesis and glycosidase inhibitory activity of noeurostegine-a new and potent inhibitor of beta-glucoside hydrolases.
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Noeurostegine 的合成和糖苷酶抑制活性 - 一种新型有效的 β-葡萄糖苷水解酶抑制剂。
DOI：
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发表时间：
2010
影响因子：
3.2
通讯作者：
H. H. Jensen
中科院分区：
文献类型：
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作者：
T. S. Rasmussen;H. H. Jensen
以左旋葡聚糖为原料，经22步反应合成了一种新的稳定的半缩醛胺去甲托烷，命名为noeurostegine。甜杏仁和海栖热袍菌-葡萄糖苷酶、咖啡豆α-半乳糖苷酶和Asp。在低微摩尔区域，米β-半乳糖苷酶被抑制，但发现在预孵育后，杏仁β-葡萄糖苷酶与K（i）50 nM的结合显着收紧。酵母α-葡萄糖苷酶和E.大肠杆菌β-半乳糖苷酶在1 mM时不受抑制。
A new, stable hemi-aminal nor-tropane christened noeurostegine was synthesised in 22 steps from levoglucosan and tested for inhibitory activity against glycoside hydrolases. Sweet almond and Thermotoga maritimabeta-glucosidases, coffee bean alpha-galactosidase, and Asp. oryzaebeta-galactosidase were inhibited in the low micromolar region but significant tightening of binding to K(i) 50 nM for almond beta-glucosidase was found to occur after pre-incubation. Yeast alpha-glucosidase and E. colibeta-galactosidase were not inhibited at 1 mM.