Evidence map›Paper›PMID 28873428›Full record

ArticlePloS one2017

Evaluation of robenidine analog NCL195 as a novel broad-spectrum antibacterial agent.

Abiodun D Ogunniyi, Manouchehr Khazandi, Andrew J Stevens, Sarah K Sims, Stephen W Page, Sanjay Garg, Henrietta Venter, Andrew Powell, Karen White, Kiro R Petrovski and 10 more

Open access · goldAbstract read
In one paragraph

Article in PloS one, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.

0numbers the graph read from it
0cells of the map it votes in
23citing papers in PubMed
3.9field-weighted citation impact, top 5% 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

23 citing papers in PubMed, 75 citations in OpenAlex.

  1. Microbiology spectrum · 2026
    Article
  2. Article
  3. Article
  4. Article
  5. Ultrastructural Alterations of the Human PathogenPathogens (Basel, Switzerland) · 2023
    Review
  6. Anti-Frontiers in microbiology · 2023
    Review
  7. Article
  8. Article
  9. Impact of a Novel Anticoccidial Analogue on SystemicAntibiotics (Basel, Switzerland) · 2022
    Article
  10. Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Isopropoxy Benzene Guanidine KillsFrontiers in microbiology · 2021
    Article
  16. Frontiers in microbiology · 2020
    Article
  17. Article
  18. Article
  19. Aminoguanidines: New leads for treatment of Giardia duodenalis infection.International journal for parasitology. Drugs and drug resistance · 2019
    Article
  20. Discovery of 4,6-bis(2-((ChemistryOpen · 2019
    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

20 authors at 6 institutions in 2 countries.

Abiodun D OgunniyiAustralian Centre for Antimicrobial Resistance Ecology, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.ORCID http://orcid.org/0000-0001-9308-5629
Manouchehr KhazandiAustralian Centre for Antimicrobial Resistance Ecology, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
Andrew J StevensChemistry, School of Environmental & Life Sciences, The University of Newcastle, Callaghan, New South Wales, Australia.
Sarah K SimsSchool of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
Stephen W PageNeoculi Pty Ltd, Burwood, Victoria, Australia.
Sanjay GargCentre for Pharmaceutical Innovation and Development, School of Pharmacy and Medical Sciences, Sansom Institute for Health Research, University of South Australia, Adelaide, South Australia, Australia.
Henrietta VenterSchool of Pharmacy and Medical Sciences, Sansom Institute for Health Research, University of South Australia, Adelaide, South Australia, Australia.
Andrew PowellCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.
Karen WhiteCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.
Kiro R PetrovskiAustralian Centre for Antimicrobial Resistance Ecology, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
Geraldine Laven-LawSchool of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
Eliane G TótoliDepartment of Drugs and Medicines, School of Pharmaceutical Sciences, São Paulo State University, Araraquara, São Paulo, Brazil.
Hérida R SalgadoDepartment of Drugs and Medicines, School of Pharmaceutical Sciences, São Paulo State University, Araraquara, São Paulo, Brazil.
Hongfei PiAustralian Centre for Antimicrobial Resistance Ecology, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
Geoffrey W CoombsDepartment of Microbiology, Path West Laboratory Medicine-WA, Fiona Stanley Hospital, Murdoch, Western Australia, Australia.
Dean L ShinabargerMicromyx LLC, Kalamazoo, Michighan, United States of America.
John D TurnidgeAustralian Centre for Antimicrobial Resistance Ecology, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
James C PatonResearch Centre for Infectious Diseases, Department of Molecular and Cellular Biology, School of Biological Sciences, The University of Adelaide, Adelaide, South Australia, Australia.
Adam McCluskeyChemistry, School of Environmental & Life Sciences, The University of Newcastle, Callaghan, New South Wales, Australia.
Darren J TrottAustralian Centre for Antimicrobial Resistance Ecology, School of Animal and Veterinary Sciences, The University of Adelaide, Roseworthy, South Australia, Australia.
The University of Adelaide · AUMonash University · AUUniversidade Estadual Paulista (Unesp) · BRUniversity of Newcastle Australia · AUUniversity of South Australia · AUMurdoch University · AU

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

The spread of multidrug resistance among bacterial pathogens poses a serious threat to public health worldwide. Recent approaches towards combating antimicrobial resistance include repurposing old compounds with known safety and development pathways as new antibacterial classes with novel mechanisms of action. Here we show that an analog of the anticoccidial drug robenidine (4,6-bis(2-((E)-4-methylbenzylidene)hydrazinyl)pyrimidin-2-amine; NCL195) displays potent bactericidal activity against Streptococcus pneumoniae and Staphylococcus aureus by disrupting the cell membrane potential. NCL195 was less cytotoxic to mammalian cell lines than the parent compound, showed low metabolic degradation rates by human and mouse liver microsomes, and exhibited high plasma concentration and low plasma clearance rates in mice. NCL195 was bactericidal against Acinetobacter spp and Neisseria meningitidis and also demonstrated potent activity against A. baumannii, Pseudomonas aeruginosa, Escherichia coli, Klebsiella pneumoniae and Enterobacter spp. in the presence of sub-inhibitory concentrations of ethylenediaminetetraacetic acid (EDTA) and polymyxin B. These findings demonstrate that NCL195 represents a new chemical lead for further medicinal chemistry and pharmaceutical development to enhance potency, solubility and selectivity against serious bacterial pathogens.

Indexed as

AnimalsAnti-Bacterial AgentsCell LineCell MembraneDrug Resistance, BacterialEnterococcusHemolysisHumansMiceMicrobial Sensitivity TestsMicrosomes, LiverRobenidineStaphylococcus aureusStreptococcus pneumoniaeStructure-Activity RelationshipTime FactorsAnti-Bacterial AgentsRobenidineVancomycin

Identifiers

PMID28873428
PMCPMC5584945
OpenAlexW2753289010

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.