Evidence map›Paper›PMID 34963068›Full record

ArticleEuropean journal of medicinal chemistry2022

Synthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis.

Hamish S Sutherland, Guo-Liang Lu, Amy S T Tong, Daniel Conole, Scott G Franzblau, Anna M Upton, Manisha U Lotlikar, Christopher B Cooper, Brian D Palmer, Peter J Choi and 1 more

Open access · hybridAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.7field-weighted citation impact, top 27% 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

2 citing papers in PubMed, 11 citations in OpenAlex.

  1. Antibiotics (Basel, Switzerland) · 2024
    Review
  2. FInternational journal of molecular sciences · 2023
    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

11 authors at 3 institutions in 2 countries.

Hamish S SutherlandAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand; Maurice Wilkins Centre, University of Auckland, Private V, Auckland, 1142, New Zealand.
Guo-Liang LuAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand.
Amy S T TongAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand.
Daniel ConoleAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand.
Scott G FranzblauInstitute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, 833 South Wood Street, Chicago, IL, 60612, USA.
Anna M UptonGlobal Alliance for TB Drug Development, 40 Wall St, New York, 10005, USA.
Manisha U LotlikarGlobal Alliance for TB Drug Development, 40 Wall St, New York, 10005, USA.
Christopher B CooperGlobal Alliance for TB Drug Development, 40 Wall St, New York, 10005, USA.
Brian D PalmerAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand; Maurice Wilkins Centre, University of Auckland, Private V, Auckland, 1142, New Zealand.
Peter J ChoiAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand; Maurice Wilkins Centre, University of Auckland, Private V, Auckland, 1142, New Zealand. Electronic address: p.choi@auckland.ac.nz.
William A DennyAuckland Cancer Society Research Centre, School of Medical Sciences, University of Auckland, Private Bag 92019, Auckland, 1142, New Zealand; Maurice Wilkins Centre, University of Auckland, Private V, Auckland, 1142, New Zealand.
University of Auckland · NZTB Alliance · USUniversity of Illinois Chicago · US

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Drug resistant tuberculsosis (TB) is global health crisis that demands novel treatment strategies. Bacterial ATP synthase inhibitors such as bedaquiline and next-generation analogues (such as TBAJ-876) have shown promising efficacy in patient populations and preclinical studies, respectively, suggesting that selective targeting of this enzyme presents a validated therapeutic strategy for the treatment of TB. In this work, we report tetrahydronaphthalene amides (THNAs) as a new class of ATP synthase inhibitors that are effective in preventing the growth of Mycobacterium tuberculosis (M.tb) in culture. Design, synthesis and comprehensive structure-activity relationship studies for approximately 80 THNA analogues are described, with a small selection of compounds exhibiting potent (in some cases MIC

Indexed as

AmidesAnimalsAntitubercular AgentsDiarylquinolinesDrug DiscoveryHumansLiverMiceMicrobial Sensitivity TestsMycobacterium tuberculosisStructure-Activity RelationshipTetrahydronaphthalenesAmidesAntitubercular AgentsbedaquilineDiarylquinolinesTetrahydronaphthalenesATP synthaseStructure-activity relationshipsSynthesisTetrahydronaphthalenesTuberculosis

Identifiers

PMID34963068
PMCPMC8811485
OpenAlexW4200588820

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.