Format

Send to:

Choose Destination
See comment in PubMed Commons below
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.

Author information

  • 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.

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.

PMID:
17070058
[PubMed - indexed for MEDLINE]
PubMed Commons home

PubMed Commons

0 comments
How to join PubMed Commons

    Supplemental Content

    Full text links

    Icon for Elsevier Science
    Loading ...
    Write to the Help Desk