Document Report Card

Basic Information

ID: ALA1141698

Journal: Bioorg Med Chem Lett

Title: Synthesis of a 200-member library of squaric acid N-hydroxylamide amides.

Authors: Charton J, Leroux F, Delaroche S, Landry V, Déprez BP, Déprez-Poulain RF.

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.

CiteXplore: 18760922

DOI: 10.1016/j.bmcl.2008.08.025