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Issue 37, 2016
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Bicyclic isoureas derived from 1-deoxynojirimycin are potent inhibitors of β-glucocerebrosidase

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Abstract

A series of bicyclic isourea derivatives were prepared from 1-deoxynojirimycin using a concise synthetic protocol proceeding via a guanidino intermediate. Inhibition assays with a panel of glycosidases revealed that these deoxynojirimycin-derived bicyclic isoureas display very potent inhibition against human recombinant β-glucocerebrosidase with IC50 values in the low nanomolar range.

Graphical abstract: Bicyclic isoureas derived from 1-deoxynojirimycin are potent inhibitors of β-glucocerebrosidase

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Publication details

The article was received on 10 Aug 2016, accepted on 30 Aug 2016 and first published on 30 Aug 2016


Article type: Communication
DOI: 10.1039/C6OB01735E
Citation: Org. Biomol. Chem., 2016,14, 8670-8673
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    Bicyclic isoureas derived from 1-deoxynojirimycin are potent inhibitors of β-glucocerebrosidase

    A. Sevšek, M. Čelan, B. Erjavec, L. Quarles van Ufford, J. Sastre Toraño, E. E. Moret, R. J. Pieters and N. I. Martin, Org. Biomol. Chem., 2016, 14, 8670
    DOI: 10.1039/C6OB01735E

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