Evidence map›Paper›PMID 42593902›Full record

ArticleJournal of medicinal chemistry2026

Structure-Activity Relationship Study of Anti-Cryptosporidium Benzoxaboroles Yields Enhanced Potency and Curative Efficacy.

Soumitra Guin, José E Teixeira, Peter Miller, Ankita Sarkar, Christopher D Huston, Marvin J Meyers

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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

0 citing papers in PubMed.

No citing paper in PubMed yet.

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.

Soumitra GuinDepartment of Chemistry, Saint Louis University, Saint Louis, Missouri63103, United States.
José E TeixeiraDepartment of Medicine, University of Vermont Larner College of Medicine, Burlington, Vermont05401, United States.
Peter MillerDepartment of Medicine, University of Vermont Larner College of Medicine, Burlington, Vermont05401, United States.
Ankita SarkarDepartment of Chemistry, Saint Louis University, Saint Louis, Missouri63103, United States.
Christopher D HustonDepartment of Medicine, University of Vermont Larner College of Medicine, Burlington, Vermont05401, United States.ORCID 0000-0002-5393-139X
Marvin J MeyersDepartment of Chemistry, Saint Louis University, Saint Louis, Missouri63103, United States.ORCID 0000-0001-5484-619X

Funding

Repurposing the EMD-Serono "mini-library" for Cryptosporidium drug developmentR33AI141184 · NIAID · UNIVERSITY OF VERMONT & ST AGRIC COLLEGE · PI HUSTON, CHRISTOPHER D, MEYERS, MARVIN J · 2021 to 2023
$1.3M
National Institute of Allergy and Infectious Diseases R33 AI141184NIAID NIH HHS R33 AI141184
6 · The paper itself

Abstract

Cryptosporidiosis is a major cause of life-threatening diarrhea in children and chronic diarrhea in immunocompromised individuals. Our previous work identified pyrazolo[3,4-d]pyrimidine benzoxaborole (2) as an orally efficacious inhibitor of Cryptosporidium with a downside of relapse after 7 days post drug treatment. Here, we report a structure-activity relationship study around the benzoxaborole ring of compound 2, resulting in rac- 11 with improved in vitro potency (EC50 = 0.025 μM). Remarkably, rac- 11 is noncytotoxic and displayed curative in vivo efficacy in Cryptosporidium-infected immunocompromised NSG mice. Furthermore, resolution of rac-11 into its enantiomers demonstrated that one enantiomer is 2-fold more potent (ent2-11; EC50 = 0.011 μM), whereas the other is 400-fold less potent, highlighting the importance of the methyl group at the C3 position of benzoxaborole. The ent2-11 also had reduced adverse binding to hPDE5 compared to 2. Collectively, these findings advance new and effective candidates for the treatment of cryptosporidiosis.

Indexed as

Antiprotozoal AgentsBoron CompoundsCryptosporidiosisCryptosporidiumAnimalsHumansMiceStereoisomerismStructure-Activity RelationshipAntiprotozoal AgentsBoron Compounds

Identifiers

PMID42593902
PMCPMC13492363

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.