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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.
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https://www.hal.inserm.fr/inserm-00323821
Contributor : Julie Charton <>
Submitted on : Tuesday, September 23, 2008 - 11:58:48 AM
Last modification on : Friday, November 29, 2019 - 6:32:04 PM

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Julie Charton, Benoît Déprez, Rébecca Déprez-Poulain. Synthesis of a 200-member library of squaric acid N-hydroxylamide amides.. Bioorganic and Medicinal Chemistry Letters, Elsevier, 2008, 18 (18), pp.4968-71. ⟨10.1016/j.bmcl.2008.08.025⟩. ⟨inserm-00323821⟩

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