title: Synthesis of a 200-member library of squaric acid N-hydroxylamide amides.
abstract: 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.
authors.affiliation: INSERM U761, Biostructures and Drug Discovery, 3 rue du Professeur Laguesse, Nord, Lille F-59006, France. julie.charton@univ-lille2.fr
authors.forename: Julie
authors.initials: J
authors.lastname: Charton
authors.forename: Florence
authors.initials: F
authors.lastname: Leroux
authors.forename: Sylvain
authors.initials: S
authors.lastname: Delaroche
authors.forename: Valérie
authors.initials: V
authors.lastname: Landry
authors.forename: Benoît P
authors.initials: BP
authors.lastname: Déprez
authors.forename: Rébecca F
authors.initials: RF
authors.lastname: Déprez-Poulain