ArticleACS infectious diseases2016
A Triazolopyrimidine-Based Dihydroorotate Dehydrogenase Inhibitor with Improved Drug-like Properties for Treatment and Prevention of Malaria.
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Article in ACS infectious diseases, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 39 papers.
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39citing papers in PubMed
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Who cites it
39 citing papers in PubMed.
- Antimalarial activity of single-dose DSM265, a novel plasmodium dihydroorotate dehydrogenase inhibitor, in patients with uncomplicated Plasmodium falciparum or Plasmodium vivax malaria infection: a proof-of-concept, open-label, phase 2a study.The Lancet. Infectious diseases · 2018Trial
- Cross-species therapeutics in Plasmodium and Babesia: erythrocyte invasion and conserved drug targets.Tropical animal health and production · 2026Review
- Virtual screening and molecular dynamics analysis of Plasmodium falciparum dihydroorotate dehydrogenase (DHODH) inhibitors targeting pyrimidine biosynthesis pathway.Folia microbiologica · 2026Article
- Repurposing of Inhibitors of Plasmodial Aspartate Transcarbamoylase Toward Trypanosoma Cruzi.ChemMedChem · 2026Article
- RL-MSVP: Reinforcement Learning and Multi-scale Validation Pipeline Investigating Azole-Fused Pyrimidines as PotentialACS omega · 2025Article
- Targeting Mitochondrial Function inInternational journal of molecular sciences · 2025Review
- Targeting Malaria's Achilles' Heels: A Review of Plasmodium Life Cycle Vulnerabilities for Drug Discovery.Current topics in medicinal chemistry · 2025Review
- To quest new targets ofJournal of parasitic diseases : official organ of the Indian Society for Parasitology · 2024Review
- The AI-driven Drug Design (AIDD) platform: an interactive multi-parameter optimization system integrating molecular evolution with physiologically based pharmacokinetic simulations.Journal of computer-aided molecular design · 2024Article
- Susceptibility of Ugandan Plasmodium falciparum Isolates to the Antimalarial Drug Pipeline.Microbiology spectrum · 2023Article
- Predicting Optimal Antimalarial Drug Combinations from a Standardized Plasmodium falciparum Humanized Mouse Model.Antimicrobial agents and chemotherapy · 2023Article
- Bioassay-Guided Isolation of Antiplasmodial Compounds fromBioMed research international · 2023Article
- Synthesis, Anti-Plasmodial Activities, and Mechanistic Insights of 4-Aminoquinoline-Triazolopyrimidine Hybrids.ACS medicinal chemistry letters · 2022Article
- Longitudinal ex vivo and molecular trends of chloroquine and piperaquine activity against Plasmodium falciparum and P. vivax before and after introduction of artemisinin-based combination therapy in Papua, Indonesia.International journal for parasitology. Drugs and drug resistance · 2021Article
- Probing the distinct chemosensitivity of Plasmodium vivax liver stage parasites and demonstration of 8-aminoquinoline radical cure activity in vitro.Scientific reports · 2021Article
- Identification of 3,4-Dihydro-2International journal of molecular sciences · 2021Article
- MalDA, Accelerating Malaria Drug Discovery.Trends in parasitology · 2021Review
- Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.Journal of medicinal chemistry · 2021Article
- Parasite-Host Dynamics throughout Antimalarial Drug Development Stages Complicate the Translation of Parasite Clearance.Antimicrobial agents and chemotherapy · 2021Article
- Clinical management of Plasmodium knowlesi malaria.Advances in parasitology · 2021Review
Corrections and comments
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Authors and funding
36 authors.
Margaret A Phillips
Karen L WhiteCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, VIC 3052, Australia.
Sreekanth KokkondaDepartments of Chemistry and Global Health, University of Washington , Seattle, Washington 98195, United States.
Xiaoyi Deng
John WhiteDepartments of Chemistry and Global Health, University of Washington , Seattle, Washington 98195, United States.
Farah El Mazouni
Kennan MarshAbbVie Inc. , 1 North Waukegan Road, North Chicago, Illinois 60064-6104, United States.
Diana R Tomchick
Krishne ManjalanagaraSyngene International Ltd. , 560 099 Bangalore, India.
Kakali Rani RudraSyngene International Ltd. , 560 099 Bangalore, India.
Grennady WirjanataGlobal and Tropical Health Division, Menzies School of Health Research, Charles Darwin University , P.O. Box 41096, Casuarina, NT 0811, Australia.
Rintis NoviyantiEijkman Institute for Molecular Biology , Jl. Diponegoro 69, 10430 Jakarta, Indonesia.
Ric N PriceGlobal and Tropical Health Division, Menzies School of Health Research, Charles Darwin University , P.O. Box 41096, Casuarina, NT 0811, Australia.
Jutta MarfurtGlobal and Tropical Health Division, Menzies School of Health Research, Charles Darwin University , P.O. Box 41096, Casuarina, NT 0811, Australia.
David M ShacklefordCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, VIC 3052, Australia.
Francis C K ChiuCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, VIC 3052, Australia.
Michael CampbellCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, VIC 3052, Australia.
Maria Belen Jimenez-DiazGlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Santiago Ferrer BazagaGlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Iñigo Angulo-BarturenGlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Maria Santos MartinezGlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Maria Lafuente-MonasterioGlaxoSmithKline , Tres Cantos Medicines Development Campus, Severo Ochoa, Madrid 28760, Spain.
Werner KaminskyDepartments of Chemistry and Global Health, University of Washington , Seattle, Washington 98195, United States.
Kigbafori SilueCentre Suisse de Recherches Scientifiques en Côte d'Ivoire , Km17, Route de Dabou, Adiopodoumé, BP 1303 Abidjan, Ivory Coast.
Anne-Marie ZeemanBiomedical Primate Research Centre , 2288 GJ Rijswijk, The Netherlands.
Clemens KockenBiomedical Primate Research Centre , 2288 GJ Rijswijk, The Netherlands.
Didier LeroyMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Benjamin BlascoMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Emilie RossignolMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Thomas RueckleMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Dave MatthewsMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Jeremy N BurrowsMedicines for Malaria Venture , 1215 Geneva, Switzerland.
David WatersonMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Michael J PalmerMedicines for Malaria Venture , 1215 Geneva, Switzerland.
Pradipsinh K RathodDepartments of Chemistry and Global Health, University of Washington , Seattle, Washington 98195, United States.
Susan A CharmanCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, VIC 3052, Australia.
Funding
Lead Optimization of DHODH Inhibitors for MalariaR01AI103947 · NIAID · UT SOUTHWESTERN MEDICAL CENTER · PI Margaret A. Phillips · 2013 to 2026
$9.7MNIAID NIH HHS R01 AI103947Wellcome Trust 091625
Abstract
The emergence of drug-resistant malaria parasites continues to hamper efforts to control this lethal disease. Dihydroorotate dehydrogenase has recently been validated as a new target for the treatment of malaria, and a selective inhibitor (DSM265) of the Plasmodium enzyme is currently in clinical development. With the goal of identifying a backup compound to DSM265, we explored replacement of the SF
Indexed as
AnimalsAntimalarialsDihydroorotate DehydrogenaseDogsEnzyme InhibitorsHumansMalaria, FalciparumMiceOxidoreductases Acting on CH-CH Group DonorsPlasmodium falciparumProtozoan ProteinsPyrimidinesRatsStructure-Activity RelationshipAntimalarialsDihydroorotate DehydrogenaseEnzyme InhibitorsOxidoreductases Acting on CH-CH Group DonorsProtozoan ProteinspyrimidinePyrimidinesdihydroorotate dehydrogenasemalariaPlasmodiumpyrimidine biosynthesis
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