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Thonhofer, M; Gonzalez Santana, A; Fischer, R; Torvisco Gomez, A; Saf, R; Schalli, M; Stütz, AE; Withers, SG.
5-Fluoro derivatives of 4-epi-isofagomine as D-galactosidase inhibitors and potential pharmacological chaperones for GM1-gangliosidosis as well as Fabry's disease.
Carbohydr Res. 2016; 420(5): 6-12. Doi: 10.1016/j.carres.2015.10.009
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Co-Autor*innen der Med Uni Graz
Schalli Michael
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Abstract:
Electrophilic fluorination of an exocyclic methoxymethylene enol ether derived from N-tert-butyloxycarbonyl-1,5-dideoxy-1,5-imino-3,4-O-isopropylidene-D-erythro-pent-2-ulose (11) provided the 5-fluoro derivative of the powerful β-galactosidase inhibitor 4-epi-isofagomine (8). This structural alteration, in combination with N-alkylation, led to considerably improved α-galactosidase selectivity. New compounds may serve as leads en route to new pharmacological chaperones for Fabry's disease. Copyright © 2015 Elsevier Ltd. All rights reserved.
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Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
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Fabry Disease - drug therapy
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Gangliosidosis, GM1 - drug therapy
Gangliosidosis, GM1 - enzymology
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Molecular Structure -
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Find related publications in this database (Keywords)
Iminoalditol
Fluorosugar
Galactosidase inhibitor
Pharmacological chaperone
Fabry's disease
G(M1)-gangliosidosis
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