α,α-Difluorophosphonohydroxamic Acid Derivatives among the Best Antibacterial Fosmidomycin Analogues.
Fiche publication
Date publication
août 2021
Journal
Molecules (Basel, Switzerland)
Auteurs
Membres identifiés du Cancéropôle Est :
Pr GROSDEMANGE-BILLIARD Catherine
Tous les auteurs :
Dreneau A, Krebs FS, Munier M, Ngov C, Tritsch D, Lièvremont D, Rohmer M, Grosdemange-Billiard C
Lien Pubmed
Résumé
Three α,α-difluorophosphonate derivatives of fosmidomycin were synthesized from diethyl 1,1-difluorobut-3-enylphosphonate and were evaluated on . Two of them are among the best 1-deoxy-d-xylulose 5-phosphate reductoisomerase inhibitors, with IC in the nM range, much better than fosmidomycin, the reference compound. They also showed an enhanced antimicrobial activity against on Petri dishes in comparison with the corresponding phosphates and the non-fluorinated phosphonate.
Mots clés
1-deoxy-dxylulose 5-phosphate reductoisomerase (DXR), 2-C-methyl-derythritol 4-phosphate (MEP) pathway, antimicrobial, deoxyxylulose phosphate reductoisomerase, fosmidomycin, isoprenoid biosynthesis, α,α-difluorophosphonate
Référence
Molecules. 2021 Aug 23;26(16):