Evidence map›Paper›PMID 34001512›Full record

ArticleAntimicrobial agents and chemotherapy2021

Piperidine-4-Carboxamides Target DNA Gyrase in Mycobacterium abscessus.

Dereje Abate Negatu, Andreas Beuchel, Abdeldjalil Madani, Nadine Alvarez, Chao Chen, Wassihun Wedajo Aragaw, Matthew D Zimmerman, Benoît Laleu, Martin Gengenbacher, Véronique Dartois and 2 more

Open access · hybridAbstract read
In one paragraph

Article in Antimicrobial agents and chemotherapy, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.

0numbers the graph read from it
0cells of the map it votes in
16citing papers in PubMed
3.0field-weighted citation impact, top 8% of its field
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

16 citing papers in PubMed, 28 citations in OpenAlex.

  1. Article
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  7. A laboratory perspective onFrontiers in microbiology · 2024
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  9. Characterization ofMicrobiology spectrum · 2023
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  11. Why Matter Matters: Fast-TrackingMolecules (Basel, Switzerland) · 2022
    Review
  12. Article
  13. Article
  14. Structure-Activity Relationship of Anti-ACS medicinal chemistry letters · 2022
    Article
  15. Article
  16. Article
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

12 authors at 4 institutions in 4 countries.

Dereje Abate Negatu *Center for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Andreas Beuchel *Institut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, Halle, Germany.
Abdeldjalil Madani *Center for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Nadine AlvarezCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Chao ChenCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Wassihun Wedajo AragawCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Matthew D ZimmermanCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Benoît LaleuMedicines for Malaria Venture, Geneva, Switzerland.
Martin GengenbacherCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Véronique DartoisCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Peter ImmingInstitut für Pharmazie, Martin-Luther-Universität Halle-Wittenberg, Halle, Germany.
Thomas DickCenter for Discovery and Innovation, Hackensack Meridian Health, Nutley, New Jersey, USA.
Hackensack Meridian Health · USMartin Luther University Halle-Wittenberg · DEGeorgetown University · USMedicines for Malaria Venture · CH

Funding

Discovery of novel lead-target pairs and identification of all-oral bactericidal drug regimens for Mycobacterium abscessus lung diseaseR01AI132374 · NIAID · RBHS-NEW JERSEY MEDICAL SCHOOL · PI Thomas Dick · 2018 to 2026
$7.0M
A QTRAP 6500 LC-MS/MS System from SCIEX for high accuracy drug content analysisS10OD023524 · OD · RBHS-NEW JERSEY MEDICAL SCHOOL · PI DARTOIS, VERONIQUE · 2017 to 2017
$526k
HHS | National Institutes of Health (NIH) R01AI132374HHS | National Institutes of Health (NIH) S10-OD023524NIAID NIH HHS R01 AI132374NIH HHS S10 OD023524
6 · The paper itself

Abstract

New, more-effective drugs for the treatment of lung disease caused by nontuberculous mycobacteria (NTM) are needed. Among NTM opportunistic pathogens, Mycobacterium abscessus is the most difficult to cure and intrinsically multidrug resistant. In a whole-cell screen of a compound collection active against Mycobacterium tuberculosis, we previously identified the piperidine-4-carboxamide (P4C) MMV688844 (844) as a hit against M. abscessus. Here, we identified a more potent analog of 844 and showed that both the parent and improved analog retain activity against strains representing all three subspecies of the M. abscessus complex. Furthermore, P4Cs showed bactericidal and antibiofilm activity. Spontaneous resistance against the P4Cs emerged at a frequency of 10

Indexed as

Mycobacterium abscessusMycobacterium Infections, NontuberculousAnti-Bacterial AgentsDNA GyraseHumansMicrobial Sensitivity TestsNontuberculous MycobacteriaPiperidinesAnti-Bacterial AgentsDNA Gyrasepiperidine-4-carboxamidePiperidinesDNA gyraseMMV688844Mycobacterium abscessusnontuberculous mycobacteriaNTM

Identifiers

PMID34001512
PMCPMC8284461
OpenAlexW3161942250

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

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.