ArticleJournal of medicinal chemistry2021
Potent Antimalarials with Development Potential Identified by Structure-Guided Computational Optimization of a Pyrrole-Based Dihydroorotate Dehydrogenase Inhibitor Series.
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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 20 papers, 1 of them a synthesis that pooled it.
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Who cites it
20 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Pooled it
- A Framework for Autonomous AI-Driven Drug Discovery.bioRxiv : the preprint server for biology · 2026Article
- Targeting Mitochondrial Function inInternational journal of molecular sciences · 2025Review
- Direct long-read visualization reveals hidden variation in GCH1 gene copy number and precise expansion steps.BMC genomics · 2025Article
- Recent advances in metal-free catalysts for the synthesis of N-heterocyclic frameworks focusing on 5- and 6-membered rings: a review.RSC advances · 2025Review
- Structure-Based Discovery and Development of Highly Potent Dihydroorotate Dehydrogenase Inhibitors for Malaria Chemoprevention.Journal of medicinal chemistry · 2025Article
- Antimalarial Drug Discovery from Natural and Synthetic Sources.Current medicinal chemistry · 2025Review
- Uncovering the Mechanism of Action of Antiprotozoal Agents: A Survey on Photoaffinity Labeling Strategy.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Identification of potent and reversible piperidine carboxamides that are species-selective orally active proteasome inhibitors to treat malaria.Cell chemical biology · 2024Article
- Proposition ofCombinatorial chemistry & high throughput screening · 2024Review
- Direct long read visualization reveals metabolic interplay between two antimalarial drug targets.bioRxiv : the preprint server for biology · 2023Article
- Antimalarial drug discovery: progress and approaches.Nature reviews. Drug discovery · 2023Review
- Cell death signaling inExperimental biology and medicine (Maywood, N.J.) · 2023Article
- Susceptibility of Ugandan Plasmodium falciparum Isolates to the Antimalarial Drug Pipeline.Microbiology spectrum · 2023Article
- Clauson-Kaas pyrrole synthesis using diverse catalysts: a transition from conventional to greener approach.Beilstein journal of organic chemistry · 2023Review
- The mystery of massive mitochondrial complexes: the apicomplexan respiratory chain.Trends in parasitology · 2022Review
- Roseoflavin, a Natural Riboflavin Analogue, PossessesAntimicrobial agents and chemotherapy · 2022Article
- Design of Anti-infectious Agents from Lawsone in a Three-Component Reaction with Aldehydes and Isocyanides.ACS omega · 2022Article
- Development of a biomarker to monitor target engagement after treatment with dihydroorotate dehydrogenase inhibitors.Biochemical pharmacology · 2022Article
- On drug discovery against infectious diseases and academic medicinal chemistry contributions.Beilstein journal of organic chemistry · 2022Article
Corrections and comments
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Authors and funding
44 authors.
Michael J PalmerMedicines for Malaria Venture, 1215 Geneva, Switzerland.
Xiaoyi DengDepartment of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
Shawn WattsSchrodinger, Inc., 120 West 45th St, 17th Floor, New York, New York 100036-4041, United States.
Goran KrilovSchrodinger, Inc., 120 West 45th St, 17th Floor, New York, New York 100036-4041, United States.
Aleksey GerasyutoSchrodinger, Inc., 120 West 45th St, 17th Floor, New York, New York 100036-4041, United States.
Sreekanth KokkondaDepartments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
Farah El MazouniDepartment 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.
Karen L WhiteCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Josefine StriepenDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Jade BathDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Kyra A SchindlerDepartment 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.
David M ShacklefordCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Sachel MokDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.ORCID 0000-0002-9605-0154
Ioanna DeniDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Aloysus LawongDepartment of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
Ann HuangDepartment of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
Gong ChenCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Wen WangCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Jaya JayaseelanCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Kasiram KatneniCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Rahul PatilCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Jessica SaundersCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Shatrughan P ShahiSyngene International Ltd, Bangalore 560099, India.
Rajesh ChittimallaSyngene International Ltd, Bangalore 560099, India.
Iñigo Angulo-BarturenTAD, Biscay Science and Technology Park, Astondo Bidea, BIC Bizkaia Bd 612, Derio, 48160 Bizkaia, Basque Country, Spain.
María Belén Jiménez-DíazTAD, Biscay Science and Technology Park, Astondo Bidea, BIC Bizkaia Bd 612, Derio, 48160 Bizkaia, Basque Country, Spain.
Sergio WittlinSwiss Tropical and Public Health Institute, Socinstrasse 57, 4002 Basel, Switzerland.
Patrick K TumwebazeInfectious Diseases Research Collaboration, Kampala, Uganda.
Philip J RosenthalDepartment of Medicine, University of California, San Francisco, California 94143, United States.
Roland A CooperDepartment of Natural Sciences and Mathematics, Dominican University of California, San Rafael, California 94901, United States.
Anna Caroline Campos AguiarUniversity of Sao Paulo, Sao Carlos Institute of Physics, Sáo Carlos, SP 13560-970, Brazil.
Rafael V C GuidoUniversity of Sao Paulo, Sao Carlos Institute of Physics, Sáo Carlos, SP 13560-970, Brazil.
Dhelio B PereiraTropical Medicine Research Center of Rondonia, Av. Guaporé, 215, Porto Velho, RO 76812-329, Brazil.
Nimisha MittalDepartment of Pediatrics, Division of Host-Microbe Systems and Therapeutics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.
Elizabeth A WinzelerDepartment of Pediatrics, Division of Host-Microbe Systems and Therapeutics, School of Medicine, University of California San Diego, La Jolla, California 92093, United States.ORCID 0000-0002-4049-2113
Diana R TomchickDepartment of Biochemistry, University of Texas Southwestern Medical Center at Dallas, 5323 Harry Hines Blvd, Dallas, Texas 75390-9135, United States.
Benoît LaleuMedicines for Malaria Venture, 1215 Geneva, Switzerland.
Jeremy N BurrowsMedicines for Malaria Venture, 1215 Geneva, Switzerland.ORCID 0000-0001-8448-6068
Pradipsinh K RathodDepartments of Chemistry and Global Health, University of Washington, Seattle, Washington 98195, United States.
David A FidockDepartment of Microbiology and Immunology, Columbia University Irving Medical Center, New York, New York 10032, United States.
Susan A CharmanCentre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, VIC 3052, Australia.
Margaret A PhillipsDepartment 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
Shared TechnologyU19AI089688 · NIAID · UNIVERSITY OF WASHINGTON · PI RATHOD, PRADIPSINH K. · 2010 to 2023
$22.4MTRAINING GRANTS IN ENVIROMENTAL TOXICOLOGYT32ES007020 · NIEHS · MASSACHUSETTS INSTITUTE OF TECHNOLOGY · PI ESSIGMANN, JOHN M · 1985 to 2024
$13.1MLead Optimization of DHODH Inhibitors for MalariaR01AI103947 · NIAID · UT SOUTHWESTERN MEDICAL CENTER · PI Margaret A. Phillips · 2013 to 2026
$9.7MMechanisms of varied sensitivity of P. falciparum field isolates to the antimalarial drug pipelineR01AI139179 · NIAID · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI Philip Jon Rosenthal · 2018 to 2026
$6.3MDefining P. falciparum resistance to artemisinin-based combination therapiesR01AI109023 · NIAID · COLUMBIA UNIVERSITY HEALTH SCIENCES · PI FIDOCK, DAVID A · 2014 to 2025
$4.4MMalaria Topoisomerase inhibitorsR01AI093380 · NIAID · UNIVERSITY OF WASHINGTON · PI RATHOD, PRADIPSINH K. · 2011 to 2020
$3.4MSingle 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
$453kNIAID NIH HHS R01 AI093380NIAID NIH HHS R01 AI103947NIAID NIH HHS R01 AI109023NIAID NIH HHS R01 AI139179NIAID NIH HHS U19 AI089688NIEHS NIH HHS T32 ES007020NIH HHS S10 OD025018
Abstract
Dihydroorotate dehydrogenase (DHODH) has been clinically validated as a target for the development of new antimalarials. Experience with clinical candidate triazolopyrimidine DSM265 (
Indexed as
Drug DesignAnimalsAntimalarialsDihydroorotate DehydrogenaseEnzyme InhibitorsMiceOxidoreductases Acting on CH-CH Group DonorsPlasmodium falciparumPyrrolesStructure-Activity RelationshipAntimalarialsDihydroorotate DehydrogenaseEnzyme InhibitorsOxidoreductases Acting on CH-CH Group DonorsPyrroles
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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.