Literature DB >> 18760922

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

Julie Charton1, Florence Leroux, Sylvain Delaroche, Valérie Landry, Benoît P Déprez, Rébecca F Déprez-Poulain.   

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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Year:  2008        PMID： 18760922     DOI： 10.1016/j.bmcl.2008.08.025

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  4 in total

1.  Identifying chelators for metalloprotein inhibitors using a fragment-based approach.

Authors:  Jennifer A Jacobsen; Jessica L Fullagar; Melissa T Miller; Seth M Cohen
Journal:  J Med Chem       Date:  2010-12-28       Impact factor: 7.446

2.  Structure-activity relationships of imidazole-derived 2-[N-carbamoylmethyl-alkylamino]acetic acids, dual binders of human insulin-degrading enzyme.

Authors:  Julie Charton; Marion Gauriot; Jane Totobenazara; Nathalie Hennuyer; Julie Dumont; Damien Bosc; Xavier Marechal; Jamal Elbakali; Adrien Herledan; Xiaoan Wen; Cyril Ronco; Helene Gras-Masse; Antoine Heninot; Virginie Pottiez; Valerie Landry; Bart Staels; Wenguang G Liang; Florence Leroux; Wei-Jen Tang; Benoit Deprez; Rebecca Deprez-Poulain
Journal:  Eur J Med Chem       Date:  2014-12-04       Impact factor: 6.514

3.  Synthesis and evaluation of squaramide and thiosquaramide inhibitors of the DNA repair enzyme SNM1A.

Authors:  Mark Berney; William Doherty; Werner Theodor Jauslin; Manav T Manoj; Eva-Maria Dürr; Joanna Francelle McGouran
Journal:  Bioorg Med Chem       Date:  2021-08-25       Impact factor: 3.641

4.  A hydroxamic-acid-containing nucleoside inhibits DNA repair nuclease SNM1A.

Authors:  William Doherty; Eva-Maria Dürr; Hannah T Baddock; Sook Y Lee; Peter J McHugh; Tom Brown; Mathias O Senge; Eoin M Scanlan; Joanna F McGouran
Journal:  Org Biomol Chem       Date:  2019-08-05       Impact factor: 3.876
  4 in total

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