Evidence map›Paper›PMID 34520959›Full record

ArticleEuropean journal of medicinal chemistry2021

6-Fluorophenylbenzohydrazides inhibit Mycobacterium tuberculosis growth through alteration of tryptophan biosynthesis.

Sara Consalvi, Giulia Venditti, Junhao Zhu, Helena I Boshoff, Kriti Arora, Alessandro De Logu, Thomas R Ioerger, Eric J Rubin, Mariangela Biava, Giovanna Poce

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2021. 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
0.1field-weighted citation impact, top 50% 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, 3 citations in OpenAlex.

  1. Article
  2. 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

10 authors at 5 institutions in 2 countries.

Sara ConsalviDepartment of Chemistry and Technologies of Drug, Sapienza University of Rome, Piazzale A. Moro 5, 00185, Rome, Italy.
Giulia VendittiDepartment of Chemistry and Technologies of Drug, Sapienza University of Rome, Piazzale A. Moro 5, 00185, Rome, Italy.
Junhao ZhuDepartment of Immunology and Infectious Diseases, Harvard T.H. Chan School of Public Health, 677 Huntington Avenue, Boston, MA, 02115, USA.
Helena I BoshoffNational Institute of Allergy and Infectious Diseases, Laboratory of Clinical Immunology and Microbiology, 9000 Rockville Pike, Bethesda, MD, 20892, USA.
Kriti AroraNational Institute of Allergy and Infectious Diseases, Laboratory of Clinical Immunology and Microbiology, 9000 Rockville Pike, Bethesda, MD, 20892, USA.
Alessandro De LoguDepartment of Life and Environmental Sciences, University of Cagliari, via Ospedale 72, 09124, Cagliari, Italy.
Thomas R IoergerDepartment of Computer Science, Texas A&M University, 3112 TAMU, College Station, TX, 77843, USA.
Eric J RubinDepartment of Immunology and Infectious Diseases, Harvard T.H. Chan School of Public Health, 677 Huntington Avenue, Boston, MA, 02115, USA.
Mariangela BiavaDepartment of Chemistry and Technologies of Drug, Sapienza University of Rome, Piazzale A. Moro 5, 00185, Rome, Italy. Electronic address: mariangela.biava@uniroma1.it.
Giovanna PoceDepartment of Chemistry and Technologies of Drug, Sapienza University of Rome, Piazzale A. Moro 5, 00185, Rome, Italy. Electronic address: giovanna.poce@uniroma1.it.
Sapienza University of Rome · ITHarvard University · USNational Institute of Allergy and Infectious Diseases · USTexas A&M University · USUniversity of Cagliari · IT

Funding

Intramural NIH HHS Z99 AI999999
6 · The paper itself

Abstract

A major constraint in reducing tuberculosis epidemic is the emergence of strains resistant to one or more of clinically approved antibiotics, which emphasizes the need of novel drugs with novel targets. Genetic knockout strains of Mycobacterium tuberculosis (Mtb) have established that tryptophan (Trp) biosynthesis is essential for the bacterium to survive in vivo and cause disease in animal models. An anthranilate-like compound, 6-FABA, was previously shown to synergize with the host immune response to Mtb infection in vivo. Herein, we present a class of anthranilate-like compounds endowed with good antimycobacterial activity and low cytotoxicity. We show how replacing the carboxylic moiety with a hydrazide led to a significant improvement in both activity and cytotoxicity relative to the parent compound 6-FABA. Several new benzohydrazides (compounds 20-31, 33, 34, 36, 38 and 39) showed good activities against Mtb (0.625 ≤ MIC≤6.25 μM) and demonstrated no detectable cytotoxicity against Vero cell assay (CC

Indexed as

AnimalsAntitubercular AgentsChlorocebus aethiopsDose-Response Relationship, DrugHydrazinesMolecular StructureMycobacterium tuberculosisStructure-Activity RelationshipTryptophanVero CellsAntitubercular AgentsHydrazinesTryptophan6-FluorophenylbenzohydrazidesDrug developmentTryptophan biosynthesisTuberculosis

Identifiers

PMID34520959
PMCPMC10994514
OpenAlexW3198763918

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.