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Bioorg Med Chem. 2007 Jan 1;15(1):63-76. Epub 2006 Oct 12.

A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.

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  • 1Inserm, U761, University of Lille 2, Faculty of Pharmacy, Institut Pasteur Lille, "Biostructures and Drug Discovery" 3 rue du Pr Laguesse F-59006 Lille cedex, France.


We report here the design and parallel synthesis of 217 compounds based on a malonic-hydroxamic acid template. These compounds are obtained via a two-step solution-phase procedure. The set of diverse building-blocks used makes this strategy suitable for the search of inhibitors of various metallo-proteases and for the investigation of the biological role of new metallo-proteases. As a proof of concept, we screened this library on Neutral Aminopeptidase (APN; EC, the prototypal enzyme of the M1 family. Several submicromolar inhibitors were identified.

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