ArticleJournal of medicinal chemistry2011
Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice.
Article in Journal of medicinal chemistry, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 50 papers.
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.
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.
Who cites it
50 citing papers in PubMed.
- A Randomized Trial Evaluating the Prophylactic Activity of DSM265 Against Preerythrocytic Plasmodium falciparum Infection During Controlled Human Malarial Infection by Mosquito Bites and Direct Venous Inoculation.The Journal of infectious diseases · 2018Trial
- From Deep-Sea Natural Product to Optimized Therapeutics: Computational Design of Marizomib Analogs.International journal of molecular sciences · 2025Article
- Identification of a New Pentafluorosulfanyl-Substituted Chalcone with Activity Against Hepatoma and Human Parasites.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Novel pentafluorosulfanyl-containing triclocarban analogs selectively kill Gram-positive bacteria.Microbiology spectrum · 2024Article
- 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
- Direct trifluoroethylation of carbonyl sulfoxonium ylides using hypervalent iodine compounds.Beilstein journal of organic chemistry · 2024Article
- Identifying inhibitors of β-haematin formation with activity against chloroquine-resistant Plasmodium falciparum malaria parasites via virtual screening approaches.Scientific reports · 2023Article
- Repurposed dihydroorotate dehydrogenase inhibitors with efficacy against drug-resistantProceedings of the National Academy of Sciences of the United States of America · 2022Article
- Article
- Synthetic studies towards isomeric pyrazolopyrimidines as potential ATP synthesis inhibitors ofTetrahedron letters · 2022Article
- Strategies for synthesis of 1,2,4-triazole-containing scaffolds using 3-amino-1,2,4-triazole.Molecular diversity · 2022Review
- Synthesis and Physicochemical Properties of 2-SFACS organic & inorganic Au · 2021Article
- On the application of 3d metals for C-H activation toward bioactive compounds: The key step for the synthesis of silver bullets.Beilstein journal of organic chemistry · 2021Review
- Article
- Design and tests of prospective property predictions for novel antimalarial 2-aminopropylaminoquinolones.Journal of computer-aided molecular design · 2020Article
- An insight on medicinal attributes of 1,2,4-triazoles.European journal of medicinal chemistry · 2020Review
- Driving antimalarial design through understanding of target mechanism.Biochemical Society transactions · 2020Review
- Synthesis of Aryl Propionamide Scaffold Containing a Pentafluorosulfanyl Moiety as SARMs.Molecules (Basel, Switzerland) · 2019Article
- The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.Molecules (Basel, Switzerland) · 2019Review
- 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.European journal of medicinal chemistry · 2019Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
16 authors.
Funding
Abstract
Malaria is one of the leading causes of severe infectious disease worldwide; yet, our ability to maintain effective therapy to combat the illness is continually challenged by the emergence of drug resistance. We previously reported identification of a new class of triazolopyrimidine-based Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors with antimalarial activity, leading to the discovery of a new lead series and novel target for drug development. Active compounds from the series contained a triazolopyrimidine ring attached to an aromatic group through a bridging nitrogen atom. Herein, we describe systematic efforts to optimize the aromatic functionality with the goal of improving potency and in vivo properties of compounds from the series. These studies led to the identification of two new substituted aniline moieties (4-SF(5)-Ph and 3,5-Di-F-4-CF(3)-Ph), which, when coupled to the triazolopyrimidine ring, showed good plasma exposure and better efficacy in the Plasmodium berghei mouse model of the disease than previously reported compounds from the series.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
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.