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  4. New synthetic seven-membered 1-azasugars displaying potent inhibition towards glycosidases and glucosylceramide transferase
 
research article

New synthetic seven-membered 1-azasugars displaying potent inhibition towards glycosidases and glucosylceramide transferase

Li, Hongqing
•
Liu, Tao
•
Zhang, Yongmin
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2008
Chembiochem

Several members of a new family of seven-membered azasugars, which can be seen as 1-azasugar ring homologues, have been I obtained by simple chemical transformations starting from a sugar-derived azidolactol. Unlike their piperidine counterparts, these molecules are chemically stable when they possess a hydroxy group at the pseudo-C-2 position. Biological assays with a range of carbohydrate-processing enzymes have revealed interesting potential for these compounds. A trihydroxymethyl-substituted azepane displayed strong competitive inhibition on almond beta-glucosidase (K-i = 2.5 mu M) while a trihydroxylated corboxylic acid derivative proved to be a potent and selective L-fucosidase inhibitor K-i = 41 nM). N-Butylation of these seven-membered 1-azasugars generated derivatives with some activity towards the Gaucher's disease-related glucosylceramide transferase (IC50) 75 mu M) that did not interact significantly with digestive glucosidases.

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Type
research article
DOI
10.1002/cbic.200700496
Web of Science ID

WOS:000252880000012

Author(s)
Li, Hongqing
Liu, Tao
Zhang, Yongmin
Favre, Sylvain  
Bello, Claudia
Vogel, Pierre  
Butters, Terry D.
Oikonomakos, Nikos G.
Marrot, Jerome
Bleriot, Yves
Date Issued

2008

Published in
Chembiochem
Volume

9

Start page

253

End page

260

Subjects

azasugars

•

azepanes

•

Gaucher's disease

•

glycosidases

•

inhibitors

•

Alpha-Glucosidase-Inhibitor

•

Gem-Diamine 1-N-Iminosugars

•

Type-2 Diabetes-Mellitus

•

Hepatitis-Virus Agents

•

Gauchers-Disease

•

Imino Sugars

•

Mimicking Monosaccharides

•

Glycogen-Phosphorylase

•

Asymmetric-Synthesis

•

Biological-Activity

Editorial or Peer reviewed

REVIEWED

Written at

EPFL

EPFL units
LGSA  
Available on Infoscience
November 30, 2010
Use this identifier to reference this record
https://infoscience.epfl.ch/handle/20.500.14299/61632
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