Skip to Main content Skip to Navigation
Journal articles

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

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.
Document type :
Journal articles
Complete list of metadatas

https://www.hal.inserm.fr/inserm-00323832
Contributor : Julie Charton <>
Submitted on : Tuesday, September 23, 2008 - 12:11:16 PM
Last modification on : Friday, November 29, 2019 - 6:32:04 PM

Identifiers

Collections

Citation

Marion Flipo, Terence Beghyn, Julie Charton, Virginie 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, Elsevier, 2007, 15 (1), pp.63-76. ⟨10.1016/j.bmc.2006.10.010⟩. ⟨inserm-00323832⟩

Share

Metrics

Record views

156