Inhibition of arabinose 5-phosphate isomerase. An approach to the inhibition of bacterial lipopolysaccharide biosynthesis

J Med Chem. 1984 Jun;27(6):717-26. doi: 10.1021/jm00372a003.

Abstract

Arabinose 5-phosphate ( A5P ) isomerase is a key enzyme in the biosynthesis of lipopolysaccharide, an essential component of the outer membrane of Gram-negative bacteria. The mechanism of the isomerase is envisioned to involve an enediol intermediate. A series of compounds, which are analogues of the substrates or intermediate, were tested as inhibitors of A5P isomerase with the belief that a good inhibitor would stop bacterial growth or render the cells more susceptible to other antibiotics or natural defenses. In a series of phosphorylated sugars, the order of isomerase inhibitory activity was as follows: aldonic acids greater than alditols greater than aldoses. Nonphosphorylated sugars were much less inhibitory. The best inhibitor was erythronic acid 4-phosphate (54), which had Km/Ki = 29. None of the compounds displayed antibacterial activity in vitro.

MeSH terms

  • Aldose-Ketose Isomerases*
  • Arabinose / analogs & derivatives
  • Bacteria / enzymology*
  • Carbohydrate Epimerases / antagonists & inhibitors*
  • Kinetics
  • Lactones / pharmacology
  • Lipopolysaccharides / biosynthesis*
  • Ribose / analogs & derivatives
  • Ribose / pharmacology
  • Sugar Acids / pharmacology
  • Sugar Phosphates / pharmacology

Substances

  • Lactones
  • Lipopolysaccharides
  • Sugar Acids
  • Sugar Phosphates
  • Ribose
  • Arabinose
  • Carbohydrate Epimerases
  • Aldose-Ketose Isomerases
  • arabinose-5-phosphate isomerase