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N-acetylhexosaminidase inhibitory properties of C-1 homologated GlcNAc- and GalNAc-thiazolines

  作者 Amorelli, B; Yang, CH; Rempel, B; Withers, SG; Knapp, S  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2008年18-9;  页码  2944-2947  
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[摘要]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 beta-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. (C) 2008 Elsevier Ltd. All rights reserved.

 
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