Evidence map›Paper›PMID 26964758›Full record

ArticleJournal of medicinal chemistry2016

Antibacterial Diamines Targeting Bacterial Membranes.

Bo Wang, Boobalan Pachaiyappan, Jordon D Gruber, Michael G Schmidt, Yong-Mei Zhang, Patrick M Woster

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 32 papers.

0numbers the graph read from it
0cells of the map it votes in
32citing papers in PubMed
7.4field-weighted citation impact, top 3% 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

32 citing papers in PubMed, 78 citations in OpenAlex.

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  10. Review
  11. Article
  12. Patrick M. Woster Memorial Commentary.ACS medicinal chemistry letters · 2023
    Article
  13. Biomolecules · 2023
    Article
  14. Efflux, Signaling and Warfare in a Polymicrobial World.Antibiotics (Basel, Switzerland) · 2023
    Review
  15. Article
  16. Article
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  20. 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

6 authors at 2 institutions in 2 countries.

Bo WangDepartment of Biochemistry and Molecular Biology, Medical University of South Carolina , Charleston, South Carolina 29425, United States.
Boobalan PachaiyappanDepartment of Drug Discovery and Biomedical Sciences, Medical University of South Carolina , Charleston, South Carolina 29425, United States.
Jordon D GruberDepartment of Biochemistry and Molecular Biology, Medical University of South Carolina , Charleston, South Carolina 29425, United States.
Michael G SchmidtDepartment of Microbiology & Immunology, Medical University of South Carolina , Charleston, South Carolina 29425, United States.
Yong-Mei ZhangDepartment of Biochemistry and Molecular Biology, Medical University of South Carolina , Charleston, South Carolina 29425, United States.
Patrick M WosterDepartment of Drug Discovery and Biomedical Sciences, Medical University of South Carolina , Charleston, South Carolina 29425, United States.
Medical University of South Carolina · USChinese Academy of Medical Sciences & Peking Union Medical College · CN

Funding

South Carolina Clinical & Translational Research Institute (SCTR)UL1TR000062 · NCATS · MEDICAL UNIVERSITY OF SOUTH CAROLINA · PI BRADY, KATHLEEN T. · 2012 to 2014
$9.4M
Identification of LSD1 inhibitors targeting epigenetic regulation in tumor cellsR01CA149095 · NCI · WAYNE STATE UNIVERSITY · PI WOSTER, PATRICK M · 2010 to 2014
$1.3M
NCATS NIH HHS UL1TR000062NCI NIH HHS 5 RO1 CA149095NCI NIH HHS R01 CA149095
6 · The paper itself

Abstract

Antibiotic resistance is a growing threat to human health exacerbated by a lack of new antibiotics. We now describe a series of substituted diamines that produce rapid bactericidal activity against both Gram-positive and Gram-negative bacteria, including methicillin-resistant Staphylococcus aureus and stationary-phase bacteria. These compounds reduce biofilm formation and promote biofilm dispersal in Pseudomonas aeruginosa. The most potent analogue, 3 (1,13-bis{[(2,2-diphenyl)-1-ethyl]thioureido}-4,10-diazatridecane), primarily acts by depolarization of the cytoplasmic membrane and permeabilization of the bacterial outer membrane. Transmission electron microscopy confirmed that 3 disrupts membrane integrity rapidly. Compound 3 is also synergistic with kanamycin, demonstrated by the checkerboard method and by time-kill kinetic experiments. In human cell toxicity assays, 3 showed limited adverse effects against the HEK293T human kidney embryonic cells and A549 human adenocarcinoma cells. In addition, 3 produced no adverse effects on Caenorhabditis elegans development, survival, and reproduction. Collectively, diamines related to 3 represent a new class of broad-spectrum antibacterials against drug-resistant pathogens.

Indexed as

AnimalsAnti-Bacterial AgentsBiofilmsCaenorhabditis elegansCell MembraneCell Membrane PermeabilityChemistry Techniques, SyntheticDiaminesDrug Evaluation, PreclinicalDrug InteractionsEscherichia coliHEK293 CellsHumansMethicillin-Resistant Staphylococcus aureusMicrobial Sensitivity TestsPseudomonas aeruginosaAnti-Bacterial AgentsDiamines

Identifiers

PMID26964758
PMCPMC5927580
OpenAlexW2293816157

What OpenQuestion holds

Textmetadata
LicenceTDM
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.