Charton Julie, Leroux Florence, Delaroche Sylvain, Landry Valérie, Déprez Benoît P, Déprez-Poulain Rébecca F
INSERM U761, Biostructures and Drug Discovery, 3 rue du Professeur Laguesse, Nord, Lille F-59006, France.
Bioorg Med Chem Lett. 2008 Sep 15;18(18):4968-71. doi: 10.1016/j.bmcl.2008.08.025. Epub 2008 Aug 14.
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.
