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Bicyclic isoureas derived from 1-deoxynojirimycin are potent inhibitors of β-glucocerebrosidase.
- Source :
-
Organic & biomolecular chemistry [Org Biomol Chem] 2016 Oct 07; Vol. 14 (37), pp. 8670-3. Date of Electronic Publication: 2016 Sep 06. - Publication Year :
- 2016
-
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.
- Subjects :
- Enzyme Inhibitors metabolism
Glucosylceramidase chemistry
Glucosylceramidase metabolism
Inhibitory Concentration 50
Molecular Docking Simulation
Protein Conformation
Urease metabolism
1-Deoxynojirimycin chemistry
Bridged Bicyclo Compounds, Heterocyclic chemistry
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Glucosylceramidase antagonists & inhibitors
Urease chemistry
Urease pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1477-0539
- Volume :
- 14
- Issue :
- 37
- Database :
- MEDLINE
- Journal :
- Organic & biomolecular chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 27604065
- Full Text :
- https://doi.org/10.1039/c6ob01735e