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Paper
Org. Biomol. Chem., 2010, 8, 433 - 441, DOI: 10.1039/b918576c
Synthesis and glycosidase inhibitory activity of noeurostegine—a new and potent inhibitor of
-glucoside hydrolasesTina Secher Rasmussen and Henrik Helligsø Jensen
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 maritima
-glucosidases, coffee bean
-galactosidase, and Asp. oryzae
-galactosidase were inhibited in the low micromolar region but significant tightening of binding to Ki 50 nM for almond
-glucosidase was found to occur after pre-incubation. Yeast
-glucosidase and E. coli
-galactosidase were not inhibited at 1 mM.
