Evidence map›Paper›PMID 38142914›Full record

ArticleBioorganic & medicinal chemistry letters2024

Synthesis and structure-activity relationships of aryl fluorosulfate-based inhibitors as novel antitubercular agents.

Baiyuan Yang, Paridhi Sukheja, Bo Qin, Gencheng Li, Grant A L Bare, Alessandro Cascioferro, Melissa S Love, H Michael Petrassi, K Barry Sharpless, Case W McNamara and 1 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2024. 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

11 authors.

Baiyuan YangCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA. Electronic address: byang@scripps.edu.
Paridhi SukhejaCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.
Bo QinCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.
Gencheng LiDepartment of Chemistry, Scripps Research, La Jolla, CA 92037, USA.
Grant A L BareDepartment of Chemistry, Scripps Research, La Jolla, CA 92037, USA.
Alessandro CascioferroCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.
Melissa S LoveCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.
H Michael PetrassiCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.
K Barry SharplessDepartment of Chemistry, Scripps Research, La Jolla, CA 92037, USA.
Case W McNamaraCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.
Arnab K ChatterjeeCalibr, a Division of Scripps Research, La Jolla, CA 92037, USA.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

To identify new compounds that can effectively inhibit Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis (TB), we screened, synthesized, and evaluated a series of novel aryl fluorosulfate derivatives for their in vitro inhibitory activity against Mtb. Compound 21b exhibited an in vitro minimum inhibitory concentration (MIC) of 0.06 µM against Mtb, no cytotoxicity against both HEK293T and HepG2 mammalian cell lines, and had good in vivo mouse plasma exposure and lung concentration with a 20 mg/kg oral dose, which supports advanced development as a new chemical entity for TB treatment.

Indexed as

Mycobacterium tuberculosisTuberculosisAnimalsAntitubercular AgentsHEK293 CellsHumansMammalsMiceMicrobial Sensitivity TestsStructure-Activity RelationshipSulfuric Acid EstersAntitubercular AgentsSulfuric Acid EstersAnti-TB activityAryl fluorosulfateMycobacterium tuberculosisPharmacokineticStructure–activity relationship studiesSuFExSulfur (VI) fluoride exchange

Identifiers

PMID38142914
PMCPMC10808981

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.