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Multivalency To Inhibit and Discriminate Hexosaminidases
Author(s) -
AlvarezDorta Dimitri,
King Dustin T.,
Legigan Thibaut,
Ide Daisuke,
Adachi Isao,
Deniaud David,
Désiré Jérôme,
Kato Atsushi,
Vocadlo David,
Gouin Sébastien G.,
Blériot Yves
Publication year - 2017
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201701756
Subject(s) - potency , ethylene glycol , chemistry , selectivity , cyclodextrin , biochemistry , organic chemistry , in vitro , catalysis
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.