Synthesis of N-alkylated noeurostegines and evaluation of their potential as treatment for Gaucher's diseaseRassmussen, T. S., Allman, S., Twigg, G., Butters, T. D. and Jensen, H. H. (2011) Synthesis of N-alkylated noeurostegines and evaluation of their potential as treatment for Gaucher's disease. Bioorganic & Medicinal Chemistry Letters, 21 (5). pp. 1519-1522. ISSN 0960-894X Full text not archived in this repository. It is advisable to refer to the publisher's version if you intend to cite from this work. See Guidance on citing. To link to this item DOI: 10.1016/j.bmcl.2010.12.106 Abstract/SummaryThe potent and selective inhibitor of β-glucosidases, noeurostegine, was evaluated as an inhibitor of glucocerebrosidase (GCase) to give an IC50 value of 0.4 μM, being 250- and 150-fold better than N-butyl and N-nonyl noeurostegine, respectively. The parent noeurostegine and its N-butyl and N-nonyl alkylated congeners were also tested as pharmacological chaperones against a N370S GCase mutant. Of these, only noeurostegine, was found to increase enzyme activity, which in potency was comparable to that previously reported for isofagomine.
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