Synthesis and evaluation of dimeric lipophilic iminosugars as inhibitors of glucosylceramide metabolism

Tom Wennekes, Richard J. B. H. N. van den Berg, Kimberley M. Bonger, Wilma E. Donker-Koopman, Amar Ghisaidoobe, Gijsbert A. van der Marel, Anneke Strijland, Johannes M. F. G. Aerts, Herman S. Overkleeft

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Abstract

Four dimeric and four monomeric lipophilic iminosugars were synthesized and subsequently evaluated on their inhibitory potential towards mammalian glucosylceramide synthase, glucocerebrosidase, beta-glucosidase 2, sucrase and lysosomal alpha-glucosidase. Compared to their monomeric counterparts the dimeric inhibitors showed decreased inhibition of glucosylceramide synthase and generally a comparable inhibitory potency for the glycosidases. (C) 2009 Elsevier Ltd. All rights reserved
Original languageEnglish
Pages (from-to)836-846
JournalTETRAHEDRON-ASYMMETRY
Volume20
Issue number6-8
DOIs
Publication statusPublished - 2009

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