Evidence map›Paper›PMID 39303295›Full record

ArticleJournal of medicinal chemistry2024

Development of Fragment-Based Inhibitors of the Bacterial Deacetylase LpxC with Low Nanomolar Activity.

Sebastian Mielniczuk, Katharina Hoff, Fady Baselious, Yunqi Li, Jörg Haupenthal, Andreas M Kany, Maria Riedner, Holger Rohde, Katharina Rox, Anna K H Hirsch and 3 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

4 citing papers in PubMed.

  1. Article
  2. Frontiers in bioinformatics · 2026
    Review
  3. Article
  4. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

13 authors.

Sebastian MielniczukInstitute of Organic Chemistry, Universität Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg, Germany.
Katharina HoffInstitute of Organic Chemistry, Universität Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg, Germany.
Fady BaseliousInstitute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, Kurt-Mothes-Straße 3, 06120 Halle (Saale), Germany.ORCID 0000-0003-3242-8514
Yunqi LiTeam "Small Molecules for Biological Targets", Institut Convergence Plascan, Centre de Recherche en Cancérologie de Lyon, INSERM U1052-CNRS UMR5286, Centre Léon Bérard, Université de Lyon, Université Claude Bernard Lyon1, 69008 Lyon, France.ORCID 0000-0002-2841-1253
Jörg HaupenthalHelmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Campus E8.1, 66123 Saarbrücken, Germany.
Andreas M KanyHelmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Campus E8.1, 66123 Saarbrücken, Germany.
Maria RiednerTechnology Platform Mass Spectrometry, Universität Hamburg, Mittelweg 177, 20148 Hamburg, Germany.ORCID 0000-0003-4421-998X
Holger RohdeGerman Center for Infection Research (DZIF), Partner Site Hamburg-Lübeck-Borstel-Riems, 20146 Hamburg, Germany.
Katharina RoxDepartment of Chemical Biology, Helmholtz Centre for Infection Research (HZI), Inhoffenstr. 7, 38124 Braunschweig, Germany.ORCID 0000-0002-8020-1384
Anna K H HirschHelmholtz Institute for Pharmaceutical Research Saarland (HIPS), Helmholtz Centre for Infection Research (HZI), Campus E8.1, 66123 Saarbrücken, Germany.ORCID 0000-0001-8734-4663
Isabelle KrimmTeam "Small Molecules for Biological Targets", Institut Convergence Plascan, Centre de Recherche en Cancérologie de Lyon, INSERM U1052-CNRS UMR5286, Centre Léon Bérard, Université de Lyon, Université Claude Bernard Lyon1, 69008 Lyon, France.ORCID 0000-0002-5981-109X
Wolfgang SipplInstitute of Pharmacy, Martin-Luther-University of Halle-Wittenberg, Kurt-Mothes-Straße 3, 06120 Halle (Saale), Germany.ORCID 0000-0002-5985-9261
Ralph HollInstitute of Organic Chemistry, Universität Hamburg, Martin-Luther-King-Platz 6, 20146 Hamburg, Germany.ORCID 0000-0001-8511-3546

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

In a fragment-based approach using NMR spectroscopy, benzyloxyacetohydroxamic acid-derived inhibitors of the bacterial deacetylase LpxC bearing a substituent to target the uridine diphosphate-binding site of the enzyme were developed. By appending privileged fragments via a suitable linker, potent LpxC inhibitors with promising antibacterial activities could be obtained, like the one-digit nanomolar LpxC inhibitor (

Indexed as

AmidohydrolasesAnti-Bacterial AgentsEnzyme InhibitorsMolecular Docking SimulationAnimalsHumansHydroxamic AcidsMicrobial Sensitivity TestsMolecular Dynamics SimulationStructure-Activity RelationshipAmidohydrolasesAnti-Bacterial AgentsEnzyme InhibitorsHydroxamic AcidsLpxC deacetylase, PseudomonasUDP-3-O-acyl-N-acetylglucosamine deacetylase

Identifiers

PMID39303295
PMCPMC11472313

What OpenQuestion holds

Textmetadata
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.