Evidence map›Paper›PMID 32248693›Full record

ArticleJournal of medicinal chemistry2020

Lead Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series for the Treatment of Malaria.

Sreekanth Kokkonda, Xiaoyi Deng, Karen L White, Farah El Mazouni, John White, David M Shackleford, Kasiram Katneni, Francis C K Chiu, Helena Barker, Jenna McLaren and 19 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing 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

13 citing papers in PubMed.

  1. Article
  2. Genetic analysis of pyrimidine biosynthetic enzymes inbioRxiv : the preprint server for biology · 2025
    Article
  3. Article
  4. To quest new targets ofJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2024
    Review
  5. Article
  6. Fast-Killing Tyrosine Amide ((ACS infectious diseases · 2023
    Article
  7. New targets for antimalarial drug discovery.Current opinion in microbiology · 2022
    Review
  8. Article
  9. Article
  10. Article
  11. Review
  12. Article
  13. 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

29 authors.

Sreekanth KokkondaDepartments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
Xiaoyi DengDepartments of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
Karen L WhiteCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Farah El MazouniDepartments of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
John WhiteDepartments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
David M ShacklefordCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Kasiram KatneniCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Francis C K ChiuCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Helena BarkerCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Jenna McLarenCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Elly CrightonCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Gong ChenCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.
Inigo Angulo-BarturenGSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Maria Belen Jimenez-DiazGSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Santiago FerrerGSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Leticia Huertas-ValentinGSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Maria Santos Martinez-MartinezGSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Maria Jose Lafuente-MonasterioGSK, Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Rajesh ChittimallaSyngene International Ltd, Bangalore 560 099, India.
Shatrughan P ShahiSyngene International Ltd, Bangalore 560 099, India.
Sergio WittlinSwiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.
David WatersonMedicines for Malaria Venture, 1215 Geneva, Switzerland.
Jeremy N BurrowsMedicines for Malaria Venture, 1215 Geneva, Switzerland.
Dave MatthewsMedicines for Malaria Venture, 1215 Geneva, Switzerland.
Diana TomchickDepartment of Biophysics, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
Pradipsinh K RathodDepartments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
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.
Margaret A PhillipsDepartments of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, 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
Single Crystal X-ray Diffractometer equipped with Hybrid Pixel Array Detector and In Situ Crystallization Plate Screening CapS10OD025018 · OD · UT SOUTHWESTERN MEDICAL CENTER · PI TOMCHICK, DIANA R. · 2018 to 2018
$453k
NIAID NIH HHS R01 AI103947NIH HHS S10 OD025018
6 · The paper itself

Abstract

Malaria puts at risk nearly half the world's population and causes high mortality in sub-Saharan Africa, while drug resistance threatens current therapies. The pyrimidine biosynthetic enzyme dihydroorotate dehydrogenase (DHODH) is a validated target for malaria treatment based on our finding that triazolopyrimidine DSM265 (

Indexed as

AnimalsAntimalarialsCell Line, TumorCrystallography, X-RayDihydroorotate DehydrogenaseDogsEnzyme InhibitorsFemaleHumansMalaria, FalciparumMaleMice, SCIDMicrosomes, LiverMolecular StructureOxidoreductases Acting on CH-CH Group DonorsParasitic Sensitivity TestsAntimalarialsDihydroorotate DehydrogenaseEnzyme InhibitorsOxidoreductases Acting on CH-CH Group DonorsPyrroles

Identifiers

PMID32248693
PMCPMC7394244

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.