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 IC50 in the range of 1–50 μM were identified.

We report here the parallel synthesis of 200 compounds based on squaric acid template. The library was screened on the zinc metalloenzyme ADAMTS-5 and hits with IC50 in the range of 1–50 μM were identified.Figure optionsDownload as PowerPoint slide