Evidence map›Paper›PMID 33620219›Full record

ArticleJournal of medicinal chemistry2021

Novel Antimalarial Tetrazoles and Amides Active against the Hemoglobin Degradation Pathway in

Aloysus Lawong, Suraksha Gahalawat, John Okombo, Josefine Striepen, Tomas Yeo, Sachel Mok, Ioanna Deni, Jessica L Bridgford, Hanspeter Niederstrasser, Anwu Zhou and 14 more

Abstract read
In one paragraph

Article in 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 9 papers.

0numbers the graph read from it
0cells of the map it votes in
9citing 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

9 citing papers in PubMed.

  1. Incorporation of the Trifluoromethylthio Group (CFThe Journal of organic chemistry · 2026
    Review
  2. Article
  3. Article
  4. Article
  5. Review
  6. Article
  7. Fast-Killing Tyrosine Amide ((ACS infectious diseases · 2023
    Article
  8. Repurposed dihydroorotate dehydrogenase inhibitors with efficacy against drug-resistantProceedings of the National Academy of Sciences of the United States of America · 2022
    Article
  9. Current and emerging target identification methods for novel antimalarials.International journal for parasitology. Drugs and drug resistance · 2022
    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

24 authors.

Aloysus LawongDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Suraksha GahalawatDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
John OkomboDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Josefine StriepenDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Tomas YeoDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Sachel MokDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Ioanna DeniDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Jessica L BridgfordDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Hanspeter NiederstrasserDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Anwu ZhouDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Bruce PosnerDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Sergio WittlinSwiss Tropical and Public Health Institute, 4002 Basel, Switzerland.
Francisco Javier GamoMedicines Development Campus, GlaxoSmithKline, Tres Cantos, 28760 Madrid, Spain.ORCID 0000-0002-1854-2882
Benigno CrespoMedicines Development Campus, GlaxoSmithKline, Tres Cantos, 28760 Madrid, Spain.
Alisje ChurchyardDepartment of Life Sciences, Imperial College London, SW7 2AZ South Kensington, U.K.
Jake BaumDepartment of Life Sciences, Imperial College London, SW7 2AZ South Kensington, U.K.
Nimisha MittalDivision of Host-Microbe Systems and Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093, United States.
Elizabeth WinzelerDivision of Host-Microbe Systems and Therapeutics, Department of Pediatrics, University of California San Diego, La Jolla, California 92093, United States.ORCID 0000-0002-4049-2113
Benoît LaleuMedicines for Malaria Venture, 1215 Geneva, Switzerland.ORCID 0000-0002-7530-2113
Michael J PalmerMedicines for Malaria Venture, 1215 Geneva, Switzerland.
Susan A CharmanCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
David A FidockDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Joseph M ReadyDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.ORCID 0000-0003-1305-9581
Margaret A PhillipsDepartment of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.ORCID 0000-0001-5250-5578

Funding

Lead Optimization of DHODH Inhibitors for MalariaR01AI103947 · NIAID · UT SOUTHWESTERN MEDICAL CENTER · PI Margaret A. Phillips · 2013 to 2026
$9.7M
MECHANISMS OF DRUG ACTION AND DISPOSITIONT32GM007062 · NIGMS · UT SOUTHWESTERN MEDICAL CENTER · PI MANGELSDORF, DAVID J · 1985 to 2020
$7.4M
NIAID NIH HHS R01 AI103947NIGMS NIH HHS T32 GM007062Wellcome TrustWellcome Trust 100993/Z/13/Z
6 · The paper itself

Abstract

Malaria control programs continue to be threatened by drug resistance. To identify new antimalarials, we conducted a phenotypic screen and identified a novel tetrazole-based series that shows fast-kill kinetics and a relatively low propensity to develop high-level resistance. Preliminary structure-activity relationships were established including identification of a subseries of related amides with antiplasmodial activity. Assaying parasites with resistance to antimalarials led us to test whether the series had a similar mechanism of action to chloroquine (CQ). Treatment of synchronized

Indexed as

AmidesAntimalarialsDrug Resistance, MicrobialHemeproteinsHemoglobinsHep G2 CellsHumansMolecular StructureParasitic Sensitivity TestsPlasmodium falciparumSmall Molecule LibrariesStructure-Activity RelationshipTetrazolesAmidesAntimalarialsHemeproteinsHemoglobinshemozoinSmall Molecule LibrariesTetrazoles

Identifiers

PMID33620219
PMCPMC7997635

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.