Evidence map›Paper›PMID 26246997›Full record

ArticleChemistryOpen2015

Optimization and Evaluation of 5-Styryl-Oxathiazol-2-one Mycobacterium tuberculosis Proteasome Inhibitors as Potential Antitubercular Agents.

Francesco Russo, Johan Gising, Linda Åkerbladh, Annette K Roos, Agata Naworyta, Sherry L Mowbray, Anders Sokolowski, Ian Henderson, Torey Alling, Mai A Bailey and 4 more

Open access · goldAbstract read
In one paragraph

Article in ChemistryOpen, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
2.5field-weighted citation impact, top 11% of its field
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

8 citing papers in PubMed, 16 citations in OpenAlex.

  1. Review
  2. Selective Phenylimidazole-Based Inhibitors of theJournal of medicinal chemistry · 2019
    Article
  3. Review
  4. The crystal structures of two isomers of 5-(phenyl-iso-thia-zol-yl)-1,3,4-oxa-thia-zol-2-one.Acta crystallographica. Section E, Crystallographic communications · 2017
    Article
  5. Crystal structure determination as part of an ongoing undergraduate organic laboratory project: 5-[(Acta crystallographica. Section E, Crystallographic communications · 2017
    Article
  6. Kunkel Lecture: Fundamental immunodeficiency and its correction.The Journal of experimental medicine · 2017
    Review
  7. Article
  8. 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

14 authors at 4 institutions in 2 countries.

Francesco RussoDepartment of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University Box 574, 751 23, Uppsala, Sweden.
Johan GisingDepartment of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University Box 574, 751 23, Uppsala, Sweden.
Linda ÅkerbladhDepartment of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University Box 574, 751 23, Uppsala, Sweden.
Annette K RoosDepartment of Cell and Molecular Biology, Science for Life Laboratory, BMC, Uppsala University Box 596, 751 24, Uppsala, Sweden.
Agata NaworytaDepartment of Cell and Molecular Biology, BMC, Uppsala University Box 596, 751 24, Uppsala, Sweden.
Sherry L MowbrayDepartment of Cell and Molecular Biology, Science for Life Laboratory, BMC, Uppsala University Box 596, 751 24, Uppsala, Sweden.
Anders SokolowskiDepartment of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University Box 574, 751 23, Uppsala, Sweden.
Ian HendersonMedivir AB PO Box 1086, 141 22, Huddinge, Sweden.
Torey AllingTB Discovery Research, Infectious Disease Research Institute Seattle, WA, 98102, USA.
Mai A BaileyTB Discovery Research, Infectious Disease Research Institute Seattle, WA, 98102, USA.
Megan FilesTB Discovery Research, Infectious Disease Research Institute Seattle, WA, 98102, USA.
Tanya ParishTB Discovery Research, Infectious Disease Research Institute Seattle, WA, 98102, USA.
Anders KarlénDepartment of Medicinal Chemistry, Organic Pharmaceutical Chemistry, BMC, Uppsala University Box 574, 751 23, Uppsala, Sweden.
Mats LarhedDepartment of Medicinal Chemistry, Science for Life Laboratory, BMC, Uppsala University Box 574, 751 23, Uppsala, Sweden.
Uppsala University · SEInfectious Disease Research Institute · USScience for Life Laboratory · SEMedivir (Sweden) · SE

Funding

High throughput assays to detect inhibition of a key M. tuberculosis proteaseR01AI095652 · NIAID · ACCESS TO ADVANCED HEALTH INSTITUTE · PI PARISH, TANYA · 2013 to 2015
$1.1M
High throughput assays to detect inhibition of a key M. tuberculosis proteaseR56AI095652 · NIAID · ACCESS TO ADVANCED HEALTH INSTITUTE · PI PARISH, TANYA · 2011 to 2011
$396k
NIAID NIH HHS R01 AI095652NIAID NIH HHS R56 AI095652
6 · The paper itself

Abstract

This is the first report of 5-styryl-oxathiazol-2-ones as inhibitors of the Mycobacterium tuberculosis (Mtb) proteasome. As part of the study, the structure-activity relationship of oxathiazolones as Mtb proteasome inhibitors has been investigated. Furthermore, the prepared compounds displayed a good selectivity profile for Mtb compared to the human proteasome. The 5-styryl-oxathiazol-2-one inhibitors identified showed little activity against replicating Mtb, but were rapidly bactericidal against nonreplicating bacteria. (E)-5-(4-Chlorostyryl)-1,3,4-oxathiazol-2-one) was most effective, reducing the colony-forming units (CFU)/mL below the detection limit in only seven days at all concentrations tested. The results suggest that this new class of Mtb proteasome inhibitors has the potential to be further developed into novel antitubercular agents for synergistic combination therapies with existing drugs.

Indexed as

5-styryl-oxathiazolonesantitubercular agentsMtb proteasome inhibitorMycobacterium tuberculosisnonreplicating Mtbrapid bactericidal activity

Identifiers

PMID26246997
PMCPMC4522185
OpenAlexW2092126930

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.