Multivalency To Inhibit and Discriminate Hexosaminidases

Dimitri Alvarez-Dorta (1) , Dustin King (2) , Thibaut Legigan (3) , Daisuke Ide (4, 5) , Isao Adachi (4, 5) , David Deniaud (1) , Jerome Desire (3) , Atsushi Kato (4, 5) , David Vocadlo (2) , Sébastien G. Gouin (1) , Yves Blériot (3)

1 CEISAM - Chimie Et Interdisciplinarité : Synthèse, Analyse, Modélisation
2 SFU.ca - Simon Fraser University = Université Simon Fraser
3 IC2MP [Poitiers] - Institut de chimie des milieux et matériaux de Poitiers [UMR 7285]
4 Department of Hospital Pharmacy [Toyama]
5 University of Toyama

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.

Mots clés: exo-N-acetyl-β-glucosaminidases; glycoclusters; glycosidases; iminosugars; multivalency

Domaines: Chimie; Chimie organique

Dimitri Alvarez-Dorta, Dustin King, Thibaut Legigan, Daisuke Ide, Isao Adachi, et al.. Multivalency To Inhibit and Discriminate Hexosaminidases. Chemistry - A European Journal, 2017, 23 (38), pp.9022 - 9025. ⟨10.1002/chem.201701756⟩. ⟨hal-01744683⟩