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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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Article information


Submitted
10 Aug 2016
Accepted
30 Aug 2016
First published
30 Aug 2016

Org. Biomol. Chem., 2016,14, 8670-8673
Article type
Communication

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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