N-Sulfonyl hydroxamate derivatives as inhibitors of class II fructose-1,6-diphosphate aldolase

Sabine Gavalda; Rémi Braga; Chantal Dax; Alain Vigroux; Casimir Blonski

doi:10.1016/j.bmcl.2005.09.006

N-Sulfonyl hydroxamate derivatives as inhibitors of class II fructose-1,6-diphosphate aldolase

Bioorg Med Chem Lett. 2005 Dec 15;15(24):5375-7. doi: 10.1016/j.bmcl.2005.09.006. Epub 2005 Oct 19.

Authors

Sabine Gavalda¹, Rémi Braga, Chantal Dax, Alain Vigroux, Casimir Blonski

Affiliation

¹ Laboratoire de Synthèse et de Physico-Chimie de Molécules d'intérêt Biologique, Groupe de Chimie Organique Biologique, UMR 5068, Université Paul Sabatier, Bât IIR1, 118 route de Narbonne, 31062 Toulouse Cedex 4, France.

PMID: 16236509
DOI: 10.1016/j.bmcl.2005.09.006

Abstract

Dihydroxyacetone-phosphate and phosphonate derivatives were synthesized bearing a N-sulfonyl hydroxamate moiety. The phosphate derivatives represent competitive inhibitors for the class II-FBP aldolase catalyzed reaction, while the phosphonate isosteres are comparatively weaker inhibitors.

MeSH terms

Animals
Enzyme Inhibitors / chemical synthesis
Enzyme Inhibitors / pharmacology
Fructose-Bisphosphate Aldolase / antagonists & inhibitors*
Hydroxamic Acids / chemical synthesis
Hydroxamic Acids / pharmacology*
Kinetics
Mammals
Organophosphonates / chemical synthesis
Organophosphonates / pharmacology*

Substances

Enzyme Inhibitors
Hydroxamic Acids
Organophosphonates
Fructose-Bisphosphate Aldolase