Evidence map›Paper›PMID 32787141›Full record

ArticleJournal of medicinal chemistry2020

Optimization of Acetazolamide-Based Scaffold as Potent Inhibitors of Vancomycin-Resistant

Jatinder Kaur, Xufeng Cao, Nader S Abutaleb, Ahmed Elkashif, Amanda L Graboski, Aaron D Krabill, Ahmed Hassan AbdelKhalek, Weiwei An, Atul Bhardwaj, Mohamed N Seleem and 1 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 56 papers.

0numbers the graph read from it
0cells of the map it votes in
56citing 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

56 citing papers in PubMed.

  1. Review
  2. Article
  3. Article
  4. Article
  5. Article
  6. Drug Design of Carbonic Anhydrase Inhibitors.Sub-cellular biochemistry · 2026
    Review
  7. Article
  8. Article
  9. Antimicrobial Activity of 1,3,4-Thiadiazole Derivatives.Pharmaceuticals (Basel, Switzerland) · 2025
    Review
  10. Article
  11. Article
  12. Article
  13. Article
  14. Article
  15. Article
  16. Inhibition of pathogenic bacterial carbonic anhydrases by monothiocarbamates.Journal of enzyme inhibition and medicinal chemistry · 2023
    Article
  17. Benzenesulfonamide derivatives asJournal of enzyme inhibition and medicinal chemistry · 2023
    Article
  18. Selected strategies to fight pathogenic bacteria.Journal of enzyme inhibition and medicinal chemistry · 2023
    Review
  19. Article
  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

11 authors.

Jatinder KaurDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.ORCID 0000-0001-6565-7909
Xufeng CaoDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
Nader S AbutalebDepartment of Comparative Pathobiology, College of Veterinary Medicine, Purdue University, 625 Harrison Street, West Lafayette, Indiana 47907, United States.ORCID 0000-0003-1730-4150
Ahmed ElkashifDepartment of Comparative Pathobiology, College of Veterinary Medicine, Purdue University, 625 Harrison Street, West Lafayette, Indiana 47907, United States.
Amanda L GraboskiDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
Aaron D KrabillDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
Ahmed Hassan AbdelKhalekDepartment of Comparative Pathobiology, College of Veterinary Medicine, Purdue University, 625 Harrison Street, West Lafayette, Indiana 47907, United States.ORCID 0000-0002-3386-4070
Weiwei AnDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
Atul BhardwajDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.
Mohamed N SeleemDepartment of Comparative Pathobiology, College of Veterinary Medicine, Purdue University, 625 Harrison Street, West Lafayette, Indiana 47907, United States.ORCID 0000-0003-0939-0458
Daniel P FlahertyDepartment of Medicinal Chemistry and Molecular Pharmacology, College of Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, Indiana 47907, United States.ORCID 0000-0002-8305-0606

Funding

Repurposing novel selective drugs for treatment and decolonization of vancomycin resistant enterococciR01AI148523 · NIAID · VIRGINIA POLYTECHNIC INST AND ST UNIV · PI Daniel Patrick Flaherty, Mohamed Seleem · 2019 to 2026
$4.2M
Antibacterial inhibitors of RnpAR01AI134685 · NIAID · UNIVERSITY OF ROCHESTER · PI DUNMAN, PAUL M. · 2018 to 2022
$3.6M
NIAID NIH HHS R01 AI134685NIAID NIH HHS R01 AI148523
6 · The paper itself

Abstract

Vancomycin-resistant enterococci (VRE) are the second leading cause of hospital-acquired infections (HAIs) attributed to a drug-resistant bacterium in the United States, and resistance to the frontline treatments is well documented. To combat VRE, we have repurposed the FDA-approved carbonic anhydrase drug acetazolamide to design potent antienterococcal agents. Through structure-activity relationship optimization we have arrived at two leads possessing improved potency against clinical VRE strains from MIC = 2 μg/mL (acetazolamide) to MIC = 0.007 μg/mL (

Indexed as

Drug DesignAcetazolamideAnimalsAnti-Bacterial AgentsCaco-2 CellsCarbonic AnhydrasesHumansMiceMicrobial Sensitivity TestsModels, MolecularProtein ConformationStructure-Activity RelationshipTissue DistributionVancomycin-Resistant EnterococciAcetazolamideAnti-Bacterial AgentsCarbonic Anhydrases

Identifiers

PMID32787141
PMCPMC8317130

What OpenQuestion holds

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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.