Synthesis of polyhydroxylated piperidines and evaluation as glycosidase inhibitors

Bioorg Med Chem. 2004 Oct 1;12(19):5091-7. doi: 10.1016/j.bmc.2004.07.039.

Abstract

A series of 16 new chiral nonracemic polyhydroxylated piperidines was synthesized utilizing several chiral beta-amino-alcohols. They act as a nitrogen source, chirality inducer and iminium stabilizer, in the desymmetrization of meso-trihydroxylated glutaraldehyde. The biological activity of these compounds towards several glycosidases (alpha-D-glucosidase, alpha-D-mannosidase, alpha-L-fucosidase) has been evaluated.

MeSH terms

  • Bacterial Proteins / antagonists & inhibitors
  • Enzyme Inhibitors / chemical synthesis
  • Enzyme Inhibitors / pharmacology
  • Geobacillus stearothermophilus / chemistry
  • Glycoside Hydrolases / antagonists & inhibitors*
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacology
  • Structure-Activity Relationship
  • alpha-L-Fucosidase / antagonists & inhibitors
  • alpha-Mannosidase / antagonists & inhibitors

Substances

  • Bacterial Proteins
  • Enzyme Inhibitors
  • Piperidines
  • Glycoside Hydrolases
  • alpha-Mannosidase
  • alpha-L-Fucosidase