H-phosphonate derivatives as novel peptide deformylase inhibitors

Bioorg Med Chem Lett. 1998 Sep 22;8(18):2479-82. doi: 10.1016/s0960-894x(98)00443-0.

Abstract

Peptide deformylase catalyzes the removal of the N-terminal formyl group from nascent polypeptides during prokaryotic protein maturation and is essential for bacterial survival. Its absence from eukaryotic organisms makes it an attractive target for designing novel antibacterial agents. Peptidyl H-phosphonates were synthesized and shown to be competitive inhibitors of the deformylase.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amidohydrolases*
  • Aminopeptidases / antagonists & inhibitors*
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / pharmacology*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Ferrous Compounds / metabolism
  • Kinetics
  • Models, Chemical
  • Organophosphonates / chemistry*
  • Zinc / metabolism

Substances

  • Anti-Infective Agents
  • Enzyme Inhibitors
  • Ferrous Compounds
  • Organophosphonates
  • Aminopeptidases
  • Amidohydrolases
  • peptide deformylase
  • Zinc