Evidence map›Paper›PMID 28187957›Full record

ArticleBioorganic & medicinal chemistry2017

Discovery of N-(2-aminoethyl)-N-benzyloxyphenyl benzamides: New potent Trypanosoma brucei inhibitors.

Andriy Buchynskyy, J Robert Gillespie, Matthew A Hulverson, Joshua McQueen, Sharon A Creason, Ranae M Ranade, Nicole A Duster, Michael H Gelb, Frederick S Buckner

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing 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

4 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
  4. 1-Benzyl-3-aryl-2-thiohydantoin Derivatives as New Anti-ACS medicinal chemistry letters · 2017
    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

9 authors.

Andriy BuchynskyyDepartment of Chemistry, University of Washington, Seattle, WA 98195, USA.
J Robert GillespieDepartment of Medicine, University of Washington, Seattle, WA 98109, USA.
Matthew A HulversonDepartment of Medicine, University of Washington, Seattle, WA 98109, USA.
Joshua McQueenDepartment of Chemistry, University of Washington, Seattle, WA 98195, USA.
Sharon A CreasonDepartment of Medicine, University of Washington, Seattle, WA 98109, USA.
Ranae M RanadeDepartment of Medicine, University of Washington, Seattle, WA 98109, USA.
Nicole A DusterDepartment of Medicine, University of Washington, Seattle, WA 98109, USA.
Michael H GelbDepartment of Chemistry, University of Washington, Seattle, WA 98195, USA. Electronic address: gelb@chem.washington.edu.
Frederick S BucknerDepartment of Medicine, University of Washington, Seattle, WA 98109, USA. Electronic address: fbuckner@uw.edu.

Funding

Biochemistry of Protein PrenylationR01AI054384 · NIAID · UNIVERSITY OF WASHINGTON · PI BUCKNER, FREDERICK SIMMONS, GELB, MICHAEL H · 2003 to 2012
$5.3M
Rational Development of Anti-Trypanosoma Cruzi DrugsR01AI070218 · NIAID · UNIVERSITY OF WASHINGTON · PI BUCKNER, FREDERICK SIMMONS, GELB, MICHAEL H · 2006 to 2014
$4.4M
Drug Discovery for Human African TrypanosomiasisR01AI106850 · NIAID · UNIVERSITY OF WASHINGTON · PI BUCKNER, FREDERICK SIMMONS, GELB, MICHAEL H · 2013 to 2017
$3.7M
NIAID NIH HHS R01 AI054384NIAID NIH HHS R01 AI070218NIAID NIH HHS R01 AI106850
6 · The paper itself

Abstract

A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-phenyl benzamides as a starting point for hit-to-lead medicinal chemistry. Eighty two analogues were prepared, which led to the identification of a set of highly potent N-(2-aminoethyl)-N-benzyloxyphenyl benzamides with the most potent compound 73 having an in vitro EC

Indexed as

Administration, OralAnimalsAntiprotozoal AgentsBenzamidesBiological AvailabilityDrug DiscoveryMiceStructure-Activity RelationshipTrypanosoma brucei bruceiTrypanosomiasisAntiprotozoal AgentsBenzamidesHit-to-lead optimizationHuman African Trypanosomiasis“Sleeping Sickness”Trypanosoma brucei inhibitor

Identifiers

PMID28187957
PMCPMC5419589

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.