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Multivalency To Inhibit and Discriminate Hexosaminidases.

Dimitri Alvarez-DortaDustin T KingThibaut LegiganDaisuke IdeIsao AdachiDavid DeniaudJérôme DésiréAtsushi KatoDavid VocadloSébastien G GouinYves Blériot
Published in: Chemistry (Weinheim an der Bergstrasse, Germany) (2017)
A set of multivalent polyhydroxylated acetamidoazepanes based on ethylene glycol, glucoside, or cyclodextrin scaffolds was prepared. The compounds were assessed against plant, mammalian, and therapeutically relevant hexosaminidases. Multimerization was shown to improve the inhibitory potency with synergy, and to fine tune the selectivity profile between related hexosaminidases.
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