Evidence map›Paper›PMID 39406121›Full record

ArticleEuropean journal of medicinal chemistry2024

Design, synthesis, and biological evaluation of imidazo[4,5-b]pyridine mitochondrial uncouplers for the treatment of metabolic dysfunction-associated steatohepatitis (MASH).

Joseph M Salamoun, Emily L Krinos, Mary A Foutz, Stefan R Hargett, Martina Beretta, Riya Shrestha, Kyle L Hoehn, Webster L Santos

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2024. 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

8 authors.

Joseph M SalamounDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States.
Emily L KrinosDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States.
Mary A FoutzDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States.
Stefan R HargettDepartment of Pharmacology, University of Virginia, Charlottesville, VA, 22908, United States.
Martina BerettaSchool of Biotechnology and Biomolecular Sciences, University of New South Wales, Kensington, NSW, 2033, Australia.
Riya ShresthaSchool of Biotechnology and Biomolecular Sciences, University of New South Wales, Kensington, NSW, 2033, Australia.
Kyle L HoehnDepartment of Pharmacology, University of Virginia, Charlottesville, VA, 22908, United States; School of Biotechnology and Biomolecular Sciences, University of New South Wales, Kensington, NSW, 2033, Australia. Electronic address: k.hoehn@unsw.edu.au.
Webster L SantosDepartment of Chemistry and Virginia Tech Center for Drug Discovery, Virginia Tech, Blacksburg, VA, 24061, United States. Electronic address: santosw@vt.edu.

Funding

Therapeutic Mitochondrial UncouplersR01DK128612 · NIDDK · VIRGINIA POLYTECHNIC INST AND ST UNIV · PI HOEHN, KYLE LEE, SANTOS, WEBSTER L · 2021 to 2024
$2.2M
NIDDK NIH HHS R01 DK128612
6 · The paper itself

Abstract

Small molecule mitochondrial uncouplers have gained traction for their potential therapeutic use against metabolic dysfunction-associated steatohepatitis (MASH). Herein, we report a novel imidazo[4,5-b]pyridine scaffold derived from iterative modifications of the potent uncoupler BAM15. Our structure-activity relationship (SAR) study demonstrated that this promising scaffold has a range of tolerated substitutions that allows for the modulation of uncoupling activity and in vivo pharmacokinetic properties. Specifically, compound SHS206 displayed an EC

Indexed as

Drug DesignImidazolesMitochondriaPyridinesAnimalsDose-Response Relationship, DrugFatty LiverHumansMaleMetabolic DiseasesMiceMice, Inbred C57BLMolecular StructureStructure-Activity RelationshipUncoupling Agentsimidazo(4,5-b)pyridineImidazolesPyridinesUncoupling AgentsMetabolic dysfunction-associated steatohepatitisMitochondrial uncouplersProtonophoreSmall moleculeStructure-activity relationship

Identifiers

PMID39406121
PMCPMC11585420

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.