Evidence map›Paper›PMID 40590790›Full record

ArticleJournal of medicinal chemistry2025

Thioquinazolinones as Antituberculosis Agents Targeting Phosphopantetheinyl Transferase.

Amrita Singh, Logan T Zwerneman, Kyle Planck, Takushi Kaneko, Andrew J Perkowski, Christine M Suh, Alexander Alex, James Bean, Kristin Burns-Huang, David Zhang and 13 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2025. 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

23 authors.

Amrita SinghDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.ORCID 0000-0001-5649-8483
Logan T ZwernemanDivision of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.
Kyle PlanckDepartment of Medicine, Weill Cornell Medicine, New York, New York 10021, United States.
Takushi KanekoGlobal Alliance for TB Drug Development, 80 Pine Street, New York, New York 10005, United States.
Andrew J PerkowskiDivision of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.ORCID 0009-0000-1143-8962
Christine M SuhDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.
Alexander AlexAMG Consultants Limited, Camburgh House, 27 New Dover Road, Canterbury, Kent CT1 3DN, U.K.
James BeanImmunology Program, Sloan Kettering Institute, New York, New York 10021, United States.
Kristin Burns-HuangDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.
David ZhangDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.
Helena I M BoshoffTuberculosis Research Section, Laboratory of Clinical Immunology and Microbiology, National Institutes of Health, Bethesda, Maryland 20852, United States.ORCID 0000-0002-4333-206X
Christine RoubertEvotec ID, SAS 40 Avenue Tony Garnier, Lyon 69001, France.
Inna KriegerDepartment of Biochemistry and Biophysics, Texas Agricultural and Mechanical University, College Station, Texas 77843, United States.
Mark GardnerAMG Consultants Limited, Camburgh House, 27 New Dover Road, Canterbury, Kent CT1 3DN, U.K.
Bastien CautainEvotec ID, SAS 40 Avenue Tony Garnier, Lyon 69001, France.
Christopher B CooperGlobal Alliance for TB Drug Development, 80 Pine Street, New York, New York 10005, United States.
Zaid TanvirGlobal Alliance for TB Drug Development, 80 Pine Street, New York, New York 10005, United States.
James SacchettiniDepartment of Biochemistry and Biophysics, Texas Agricultural and Mechanical University, College Station, Texas 77843, United States.
Ben S GoldDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.ORCID 0000-0002-9562-8241
Kyu Y RheeDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.
Nader FotouhiGlobal Alliance for TB Drug Development, 80 Pine Street, New York, New York 10005, United States.
Carl F NathanDepartment of Microbiology & Immunology, Weill Cornell Medicine, New York, New York 10021, United States.
Jeffrey AubéDivision of Chemical Biology and Medicinal Chemistry, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599, United States.ORCID 0000-0003-1049-5767

Funding

X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI SELWYN M VICKERS · 1985 to 2026
$347.4M
Study of M. tuberculosis under human host selection to identify virulence and barrier lipids (Project 1)U19AI162584 · NIAID · BRIGHAM AND WOMEN'S HOSPITAL · PI WOOD, ROBIN · 2021 to 2025
$13.5M
Discovery of Phospopantetheinyl Transferse Inhibitors Against Mycobacterium tuberculosisR01AI155510 · NIAID · UNIV OF NORTH CAROLINA CHAPEL HILL · PI AUBE, JEFFREY · 2021 to 2024
$3.1M
Organic Synthesis at the Service of Biology and MedicineR50CA243895 · NCI · SLOAN-KETTERING INST CAN RESEARCH · PI Ouathek Ouerfelli · 2019 to 2026
$1.9M
Request for a 500 MHz NMR console and nitrogen-cooled cryoprobeS10OD032476 · OD · UNIV OF NORTH CAROLINA CHAPEL HILL · PI LEE, ANDREW L · 2022 to 2022
$599k
Metabolic Impact of Tryptophan Synthase Inhibition in Mycobacterium tuberculosis and Implications for Rational Combination TherapyF31AI154832 · NIAID · WEILL MEDICAL COLL OF CORNELL UNIV · PI PLANCK, KYLE · 2020 to 2022
$138k
Gates Foundation INV-002431Gates Foundation INV-004709NCI NIH HHS P30 CA008748NCI NIH HHS R50 CA243895NIAID NIH HHS F31 AI154832NIAID NIH HHS R01 AI155510NIAID NIH HHS U19 AI162584NIH HHS S10 OD032476
6 · The paper itself

Abstract

The essential mycobacterial enzyme phosphopantetheinyl transferase (PptT) is a potential target for antituberculosis drugs. We here report the identification of (pyridin-3-ylmethyl)-substituted thioquinazolinones as hits in a screen against PptT and a structure-activity relationship (SAR) study of the chemotype. The resulting thioquinazolinones exert on-target whole-cell activity against

Indexed as

Antitubercular AgentsMycobacterium tuberculosisQuinazolinonesTransferases (Other Substituted Phosphate Groups)AnimalsBacterial ProteinsHumansMacrophagesMiceMicrobial Sensitivity TestsStructure-Activity RelationshipAntitubercular AgentsBacterial Proteinsphosphopantetheinyl transferaseQuinazolinonesTransferases (Other Substituted Phosphate Groups)

Identifiers

PMID40590790
PMCPMC12765392

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.