Title of article
N-Acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines
Author/Authors
Benjamin Amorelli، نويسنده , , Chunhua Yang، نويسنده , , Brian Rempel، نويسنده , , Stephen G. Withers and Pedro M. Alzari، نويسنده , , Spencer Knapp، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
2944
To page
2947
Abstract
Several C-1 homologated GlcNAc- and GalNAc-thiazolines, as well as a related GalNAc-thiazole, have been prepared. The compounds are analogues of GlcNAc-thiazoline, a potent transition-state-mimicking inhibitor of retaining β-N-acetylglycosaminidases. Kinetic evaluation of these fused pyranose-heterocycles against the bacterial N-acetylhexosaminidase SpHex suggests active site steric restrictions around the substrate anomeric carbon.
Keywords
Transition state mimic , Streptomyces plicatus , Glycosidase , O-GlcNAcase , Pyranose conformation
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799478
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