Synthesis of a 200-member library of squaric acid N-hydroxylamide amides.
We report here the parallel synthesis of 200 compounds based on squaric acid template. These compounds are obtained via a one-step solution-phase procedure starting from three squaric acid N-hydroxylamide esters precursors. The set of diverse reagents qualified (amines, anilines, amino-alcohols and amino-esters) makes this strategy suitable for the search of biologically active compounds. The library was screened on the zinc metalloenzyme ADAMTS-5 and hits with IC(50) in the range of 1-50 microM were identified.
Charton
Julie
J
INSERM U761, Biostructures and Drug Discovery, 3 rue du Professeur Laguesse, Nord, Lille F-59006, France. julie.charton@univ-lille2.fr
Leroux
Florence
F
Delaroche
Sylvain
S
Landry
Valérie
V
Déprez
Benoît P
BP
Déprez-Poulain
Rébecca F
RF