title: Synthesis and biological evaluation of potential new inhibitors of the bacterial transferase MraY with a β-ketophosphonate structure.
abstract: Stable analogs of bacterial transferase MraY substrate or product with a pyrophosphate surrogate in their structure are described. β-ketophosphonates were designed as pyrophosphate bioisosteres and were investigated as UDP-GlcNAc mimics. The developed strategy allows introduction of structural diversity at a late stage of the synthesis. The biological activity of the synthesized compounds was evaluated on the MraY enzyme.
authors: Université Paris Descartes, UMR 8601 CNRS, Laboratoire de Chimie et Biochimie Pharmacologiques et Toxicologiques, 45 rue des Saints Pères, 75006 Paris, France.
authors: Nicolas
authors: N
authors: Auberger
authors: Rok
authors: R
authors: Frlan
authors: Bayan
authors: B
authors: Al-Dabbagh
authors: Ahmed
authors: A
authors: Bouhss
authors: Muriel
authors: M
authors: Crouvoisier
authors: Christine
authors: C
authors: Gravier-Pelletier
authors: Yves
authors: Y
authors: Le Merrer
mesh_terms: D001412:Bacillus subtilis / Q000201:enzymology*; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D055162:Biocatalysis; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008968:Molecular Conformation; D063065:Organophosphonates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014166:Transferases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D017855:Transferases (Other Substituted Phosphate Groups)
chemical_list: D001426:Bacterial Proteins; D004791:Enzyme Inhibitors; D063065:Organophosphonates; D014166:Transferases; D017855:Transferases (Other Substituted Phosphate Groups); C079803:mraY protein, Bacteria