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.
Alvarez-Dorta, D., King, D. T., Legigan, T., Ide, D., Adachi, I., Deniaud, D., Désiré, J., Kato, A., Vocadlo, D., Gouin, S. G., & Blériot, Y. (2017). Multivalency To Inhibit and Discriminate Hexosaminidases. Chemistry – A European Journal, 23(38), 9022–9025. https://doi.org/10.1002/chem.201701756
Chemistry – A European Journal
Multivalency To Inhibit and Discriminate Hexosaminidases
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