• Publications
  • Influence
Scalable syntheses of both enantiomers of DNJNAc and DGJNAc from glucuronolactone: the effect of N-alkylation on hexosaminidase inhibition.
TLDR
Correlation of the in vitro inhibition with the cellular data, by using a free oligosaccharide analysis of the lysosomal enzyme inhibition, revealed the following structure-property relationship: hydrophobic side-chains preferentially promoted the intracellular access of iminosugars to those inhibitors with more-hydrophilic side-chain characteristics. Expand
Synthesis of 2-acetamido-1,2-dideoxy-d-galacto-nojirimycin [DGJNAc] from d-glucuronolactone: the first sub-micromolar inhibitor of α-N-acetylgalactosaminidases
Abstract 2-Acetamido-1,2-dideoxy- d -galacto-nojirimycin [DGJNAc], prepared in 20% overall yield from d -glucuronolactone, is the first potent competitive sub-micromolar inhibitor ofExpand
Synthesis of the enantiomers of XYLNAc and LYXNAc: comparison of β-N-acetylhexosaminidase inhibition by the 8 stereoisomers of 2-N-acetylamino-1,2,4-trideoxy-1,4-iminopentitols.
TLDR
Both XYLNAc and LABNAc are potent inhibitors against HexNAcases and the N-benzyl derivatives are better inhibitors than the parent compounds. Expand
2-Acetamido-N-benzyl-1,4-imino-1,2,4-trideoxy-l-xylitol (N-benzyl-l-XYLNAc)
TLDR
X-ray crystallography defines the relative configuration at the three-stereogenic centres in the title compound N-benzyl-l-XYLNAc, C14H20N2O3, using l-glucuronolactone as the starting material for the synthesis. Expand
The synthesis and biological evaluation of novel N-acetylhexosaminidase inhibitors
Abstract The synthesis and biological evaluation of novel N-acetylhexosaminidase inhibitors Elizabeth Crabtree, Exeter College, University of Oxford D.Phil., Trinity Term 2011 Iminosugars are knownExpand
The effect and mechanisms of the cag II of Helicobacter pylori on the transcription of IL-8 in gastric epithelial cells
TLDR
Results showed that multiple genes in the tag Ⅱ locus play an important role in transcription of IL-8 in L5F11 gastric epithelial cells and transcriptionIL-8 gene induced by H. pylori is mainly mediated by the protein tyrosine kinase. Expand