A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening. - Archive ouverte HAL Access content directly
Journal Articles Bioorganic and Medicinal Chemistry Year : 2007

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

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Abstract

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 3.4.11.2), the prototypal enzyme of the M1 family. Several submicromolar inhibitors were identified.

Dates and versions

inserm-00323832 , version 1 (23-09-2008)

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Marion Flipo, Terence Beghyn, Julie Charton, Virginie A. Leroux, Benoit Déprez, et al.. A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.. Bioorganic and Medicinal Chemistry, 2007, 15 (1), pp.63-76. ⟨10.1016/j.bmc.2006.10.010⟩. ⟨inserm-00323832⟩
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