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Literature DB >> 17070058

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

Marion Flipo¹, Terence Beghyn, Julie Charton, Virginie A Leroux, Benoit P Deprez, Rebecca F Deprez-Poulain.

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.

Entities: Chemical Gene

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Year: 2006 PMID： 17070058 DOI： 10.1016/j.bmc.2006.10.010

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

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Cited

7 in total

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2. Syntheses and evaluation of substituted aromatic hydroxamates and hydroxamic acids that target Mycobacterium tuberculosis.

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Journal: Chem Biol Drug Des Date: 2011-06-16 Impact factor: 2.817

4. Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.

Authors: Taha Y Taha; Shaimaa M Aboukhatwa; Rachel C Knopp; Naohiko Ikegaki; Hazem Abdelkarim; Jayaprakash Neerasa; Yunlong Lu; Raghupathi Neelarapu; Thomas W Hanigan; Gregory R J Thatcher; Pavel A Petukhov
Journal: ACS Med Chem Lett Date: 2017-08-01 Impact factor: 4.345

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

1. Syntheses and Biological Evaluations of Highly Functionalized Hydroxamate Containing and N-Methylthio Monobactams as Anti-Tuberculosis and β-Lactamase Inhibitory Agents.

2. Syntheses and evaluation of substituted aromatic hydroxamates and hydroxamic acids that target Mycobacterium tuberculosis.

3. Targeting metalloproteins by fragment-based lead discovery.

4. Design, Synthesis, and Biological Evaluation of Tetrahydroisoquinoline-Based Histone Deacetylase 8 Selective Inhibitors.

5. Chelator fragment libraries for targeting metalloproteinases.

6. Design and synthesis of novel chloramphenicol amine derivatives as potent aminopeptidase N (APN/CD13) inhibitors.

Review 7. Driving antimalarial design through understanding of target mechanism.