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5-Fluoro derivatives of 4-epi-isofagomine as D-galactosidase inhibitors and potential pharmacological chaperones for GM1-gangliosidosis as well as Fabry's disease.
Thonhofer, Martin; Gonzalez Santana, Andres; Fischer, Roland; Torvisco Gomez, Ana; Saf, Robert; Schalli, Michael; Stütz, Arnold E; Withers, Stephen G.
Afiliação
  • Thonhofer M; Glycogroup, Institute for Organic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Gonzalez Santana A; Chemistry Department, University of British Columbia, 2036 Main Mall, Vancouver, BC, Canada V6T 1Z1.
  • Fischer R; Institute for Inorganic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Torvisco Gomez A; Institute for Inorganic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Saf R; Institute for Chemistry and Technology of Materials, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Schalli M; Glycogroup, Institute for Organic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • Stütz AE; Glycogroup, Institute for Organic Chemistry, Graz University of Technology, Stremayrgasse 9, A-8010 Graz, Austria. Electronic address: stuetz@tugraz.at.
  • Withers SG; Chemistry Department, University of British Columbia, 2036 Main Mall, Vancouver, BC, Canada V6T 1Z1.
Carbohydr Res ; 420: 6-12, 2016 Feb.
Article em En | MEDLINE | ID: mdl-26717544
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 ß-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.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Imino Piranoses / Galactosidases Limite: Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Inibidores Enzimáticos / Imino Piranoses / Galactosidases Limite: Humans Idioma: En Ano de publicação: 2016 Tipo de documento: Article