Design and synthesis of beta-carboxamido phosphonates as potent inhibitors of imidazole glycerol phosphate dehydratase

Bioorg Med Chem Lett. 1999 Jul 19;9(14):2053-8. doi: 10.1016/s0960-894x(99)00338-8.

Abstract

We describe the synthesis and enzymatic activity of a library of beta-carboxamido phosphonates as inhibitors of imidazole glycerol phosphate dehydratase (IGPD). Biological results suggest the presence of an enzymatic interaction site not previously observed for other inhibitors of IGPD.

MeSH terms

  • Computer Simulation
  • Cryptococcus / enzymology
  • Databases, Factual
  • Drug Design
  • Drug Evaluation, Preclinical
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / metabolism
  • Enzyme Inhibitors / pharmacology*
  • Hydro-Lyases / antagonists & inhibitors*
  • Hydro-Lyases / metabolism
  • Inhibitory Concentration 50
  • Phenoxyacetates / chemical synthesis*
  • Phenoxyacetates / pharmacology*
  • Software
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Phenoxyacetates
  • Hydro-Lyases
  • imidazoleglycerolphosphate dehydratase