5-Fluoro derivatives of 4-epi-isofagomine as D-galactosidase inhibitors and potential pharmacological chaperones for GM1-gangliosidosis as well as Fabry's disease

Martin Thonhofer, Andres Gonzalez Santana, Roland Fischer, Ana Torvisco Gomez, Robert Saf, Michael Schalli, Arnold Stütz, Stephen G. Withers

Publikation: Beitrag in einer FachzeitschriftArtikelBegutachtung

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.
Originalspracheenglisch
Seiten (von - bis)6-12
FachzeitschriftCarbohydrate Research
Jahrgang420
DOIs
PublikationsstatusVeröffentlicht - Dez 2015

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