Multivalency To Inhibit and Discriminate Hexosaminidases.

Authors :: Alvarez‐Dorta, Dimitri
King, Dustin T.
Legigan, Thibaut
Ide, Daisuke
Adachi, Isao
Deniaud, David
Désiré, Jérôme
Kato, Atsushi
Vocadlo, David
Gouin, Sébastien G.
Blériot, Yves
Source :: Chemistry - A European Journal; 7/6/2017, Vol. 23 Issue 38, p9022-9025, 4p
Publication Year :: 2017
Abstract: 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. [ABSTRACT FROM AUTHOR]