Synthesis and [alpha]-amylase inhibitory activity of glucose-deoxynojirimycin conjugates

Inhibitors of [alpha]-amylase have attracted attention for their putative effects against diabetes mellitus. Although numerous studies have explored natural small molecule inhibitors, acarbose is currently the only compound with sufficient inhibitory potency and drug-like characteristics to be consi...

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Bibliographic Details
Published in:Tetrahedron 2011-10, Vol.67 (40), p.7692-7702
Main Authors: Kato, Eisuke, Iwano, Naoya, Yamada, Akihiko, Kawabata, Jun
Format: Article
Language:English
Subjects:
Chemical compounds
Conjugates
Glucose
Glucosidase
Inhibitors
Pharmacology
Synthesis (chemistry)
Tetrahedrons
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Summary:Inhibitors of [alpha]-amylase have attracted attention for their putative effects against diabetes mellitus. Although numerous studies have explored natural small molecule inhibitors, acarbose is currently the only compound with sufficient inhibitory potency and drug-like characteristics to be considered as a potential therapeutic agent. We have synthesized conjugates of the potent glucosidase inhibitor, 1-deoxynojirimycin, and glucose, with the aim of enhancing inhibitory activity against [alpha]-amylase. This synthetic conjugate showed increased inhibition of [alpha]-amylase compared to 1-deoxynojirimycin alone, suggesting that similar modifications of existing glucosidase inhibitors may yield more potent [alpha]-amylase inhibitors.
ISSN:0040-4020
DOI:10.1016/j.tet.2011.08.012