Evidence map›Paper›PMID 40878880›Full record

ArticleJournal of medicinal chemistry2025

Hit-to-Lead Optimization of Acetazolamide-Based Bacterial Carbonic Anhydrase Inhibitors with Efficacy In Vivo for Treatment of Vancomycin-Resistant Enterococci Septicemia.

Katrina J Holly, Prabhakara R Tharra, Nader S Abutaleb, Alessio Nocentini, Ahmed A Abouelkhair, Molly S Youse, Anil Kumar Marapaka, Abdallah S Abdelsattar, Weiwei An, Faith L Drummond and 4 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2025. 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. Article
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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

14 authors.

Katrina J HollyBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.
Prabhakara R TharraBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.
Nader S AbutalebDepartment of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, United States.
Alessio NocentiniDepartment of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Firenze 50019, Italy.ORCID 0000-0003-3342-702X
Ahmed A AbouelkhairDepartment of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, United States.
Molly S YouseBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.
Anil Kumar MarapakaBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.ORCID 0000-0001-8872-0552
Abdallah S AbdelsattarDepartment of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, United States.
Weiwei AnBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.
Faith L DrummondBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.
Olivia C SnellBorch Department of Medicinal Chemistry and Molecular Pharmacology, West Lafayette, Indiana 47907, United States.
Claudiu T SupuranDepartment of NEUROFARBA, Section of Pharmaceutical and Nutraceutical Sciences, University of Florence, Polo Scientifico, Firenze 50019, Italy.ORCID 0000-0003-4262-0323
Mohamed N SeleemDepartment of Biomedical Sciences and Pathobiology, Virginia-Maryland College of Veterinary Medicine, Virginia Polytechnic Institute and State University, Blacksburg, Virginia 24061, United States.ORCID 0000-0003-0939-0458
Daniel P FlahertyBorch Department of Medicinal Chemistry and Molecular Pharmacology, 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
Development of novel anti-Neisseria gonorrhoeae therapeutic agentsR01AI153264 · NIAID · PURDUE UNIVERSITY · PI FLAHERTY, DANIEL PATRICK · 2022 to 2025
$3.1M
NIAID NIH HHS R01 AI148523NIAID NIH HHS R01 AI153264
6 · The paper itself

Abstract

As one of the leading causes of hospital-acquired infections reported by the National Healthcare Safety Network, vancomycin-resistant enterococci (VRE) continue to afflict patients in healthcare facilities, with limited FDA-approved drugs available for treating systemic infections. Our group previously showed the 1,3,4-thiadiazole acetazolamide human carbonic anhydrase inhibitor scaffold can be repositioned with potent

Indexed as

AcetazolamideAnti-Bacterial AgentsCarbonic Anhydrase InhibitorsSepsisVancomycin-Resistant EnterococciAnimalsHumansMiceMicrobial Sensitivity TestsStructure-Activity RelationshipTriazolesAcetazolamideAnti-Bacterial AgentsCarbonic Anhydrase InhibitorsTriazoles

Identifiers

PMID40878880
PMCPMC12527224

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.