Difluorotetrahydropyridothiazinone: a selective β-galactosidase inhibitor

Arch Pharm (Weinheim). 2010 Oct;343(10):577-82. doi: 10.1002/ardp.200900307.

Abstract

Selective difluorination, introducing a lactame moiety (instead of an amine) and a double bond in a trihydroxy-2-thiaquinolizidine derivative reverses the selectivity of the glycosidase inhibitor - a selective inhibitor for an α-glucosidase is altered into an excellent, competitive inhibitor for a β-galactosidase.

MeSH terms

  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / chemistry
  • Enzyme Inhibitors / pharmacology*
  • Pyridines / chemical synthesis*
  • Pyridines / chemistry
  • Pyridines / metabolism*
  • Pyridines / pharmacology*
  • Thiazines / chemical synthesis*
  • Thiazines / chemistry
  • Thiazines / metabolism*
  • Thiazines / pharmacology*
  • beta-Galactosidase / antagonists & inhibitors*

Substances

  • Enzyme Inhibitors
  • Pyridines
  • Thiazines
  • beta-Galactosidase