Evidence map›Paper›PMID 37599793›Full record

ArticleACS bio & med chem Au2023

Thiazolide Prodrug Esters and Derived Peptides: Synthesis and Activity.

Andrew V Stachulski, Jean-Francois Rossignol, Sophie Pate, Joshua Taujanskas, Jonathan A Iggo, Rudi Aerts, Etienne Pascal, Sara Piacentini, Simone La Frazia, M Gabriella Santoro and 5 more

Abstract read
In one paragraph

Article in ACS bio & med chem Au, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. 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

15 authors.

Andrew V StachulskiDonnan and Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K.ORCID https://orcid.org/0000-0002-5100-8884
Jean-Francois RossignolRomark Laboratories, L.C., Tampa, Florida 33609, United States.
Sophie PateDonnan and Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K.
Joshua TaujanskasDonnan and Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K.
Jonathan A IggoDonnan and Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K.ORCID https://orcid.org/0000-0001-8070-1226
Rudi AertsRomark Belgium BVBA, Roosveld 6, 3400 Landen, Belgium.
Etienne PascalRomark Belgium BVBA, Roosveld 6, 3400 Landen, Belgium.
Sara PiacentiniDepartment of Biology, University of Rome Tor Vergata, 00133 Rome, Italy.
Simone La FraziaDepartment of Biology, University of Rome Tor Vergata, 00133 Rome, Italy.
M Gabriella SantoroDepartment of Biology, University of Rome Tor Vergata, 00133 Rome, Italy.
Lieven van VoorenArdena Gent NV, Kleimor 4, 9030 Mariakerke, Belgium.
Liesje SintubinArdena Gent NV, Kleimor 4, 9030 Mariakerke, Belgium.
Mark CooperBio-Techne, Avonmouth, Bristol BS11 9QD, U.K.
Karl SwiftBio-Techne, Avonmouth, Bristol BS11 9QD, U.K.
Paul M O'NeillDonnan and Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, U.K.ORCID https://orcid.org/0000-0003-4338-0317

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Amino acid ester prodrugs of the thiazolides, introduced to improve the pharmacokinetic parameters of the parent drugs, proved to be stable as their salts but were unstable at pH > 5. Although some of the instability was due to simple hydrolysis, we have found that the main end products of the degradation were peptides formed by rearrangement. These peptides were stable solids: they maintained significant antiviral activity, and in general, they showed improved pharmacokinetics (better solubility and reduced clearance) compared to the parent thiazolides. We describe the preparation and evaluation of these peptides.

Identifiers

PMID37599793
PMCPMC10436260

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.