Evidence map›Paper›PMID 36037791›Full record

ArticleEuropean journal of medicinal chemistry2022

Discovery of substituted benzyloxy-benzylamine inhibitors of acetyltransferase Eis and their anti-mycobacterial activity.

Allan H Pang, Keith D Green, Nishad Thamban Chandrika, Atefeh Garzan, Ankita Punetha, Selina Y L Holbrook, Melisa J Willby, James E Posey, Oleg V Tsodikov, Sylvie Garneau-Tsodikova

Open access · greenAbstract read
PubMed Full text at PMC Publisher
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 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
1.4field-weighted citation impact, top 17% 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

6 citing papers in PubMed, 15 citations in OpenAlex.

  1. NProceedings of the National Academy of Sciences of the United States of America · 2025
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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 2 institutions in 1 country.

Allan H PangDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.
Keith D GreenDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.
Nishad Thamban ChandrikaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.
Atefeh GarzanDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.
Ankita PunethaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.
Selina Y L HolbrookDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA.
Melisa J WillbyLaboratory Branch, Division of Tuberculosis Elimination, National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention, Centers for Disease Control and Prevention, Atlanta, GA, USA.
James E PoseyLaboratory Branch, Division of Tuberculosis Elimination, National Center for HIV/AIDS, Viral Hepatitis, STD, and TB Prevention, Centers for Disease Control and Prevention, Atlanta, GA, USA.
Oleg V TsodikovDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA. Electronic address: oleg.tsodikov@uky.edu.
Sylvie Garneau-TsodikovaDepartment of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 789 South Limestone Street, Lexington, KY, 40536-0596, USA. Electronic address: sylviegtsodikova@uky.edu.
University of Kentucky · USCenters for Disease Control and Prevention · US

Funding

Novel aminoglycoside adjuvants and stand-alone agents to combat tuberculosisR01AI090048 · NIAID · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI GARNEAU-TSODIKOVA, SYLVIE · 2011 to 2021
$4.4M
Bruker AVANCE NEO 600 MHz High-Performance Digital NMR SpectrometerS10OD028690 · OD · UNIVERSITY OF KENTUCKY · PI GARNEAU-TSODIKOVA, SYLVIE · 2020 to 2020
$1.4M
NIAID NIH HHS R01 AI090048NIH HHS S10 OD028690
6 · The paper itself

Abstract

A clinically significant mechanism of tuberculosis resistance to the aminoglycoside kanamycin (KAN) is its acetylation catalyzed by upregulated Mycobacterium tuberculosis (Mtb) acetyltransferase Eis. In search for inhibitors of Eis, we discovered an inhibitor with a substituted benzyloxy-benzylamine scaffold. A structure-activity relationship study of 38 compounds in this structural family yielded highly potent (IC

Indexed as

AcetyltransferasesMycobacterium tuberculosisAminoglycosidesAnimalsAnti-Bacterial AgentsAntitubercular AgentsBacterial ProteinsBenzylaminesKanamycinMammalsAcetyltransferasesAminoglycosidesAnti-Bacterial AgentsAntitubercular AgentsBacterial ProteinsBenzylaminesKanamycinCrystal structureDrug resistanceEnhanced intracellular survivalEnzyme kineticsMycobacterium tuberculosisStructure-activity relationshipTuberculosis

Identifiers

PMID36037791
PMCPMC9481687
OpenAlexW4292212386

What OpenQuestion holds

Textmetadata
LicenceTDM
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.