ArticleJournal of medicinal chemistry2014
Structure-based design and synthesis of antiparasitic pyrrolopyrimidines targeting pteridine reductase 1.
Article in Journal of medicinal chemistry, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 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
16 citing papers in PubMed, 52 citations in OpenAlex.
- Titanium-Catalyzed Diastereoselective Keto- and Iminonitrile Cyclizations.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Design of 2-Aminobenzothiazole Derivatives Targeting Trypanosomatid PTR1 by a Multidisciplinary Fragment Hybridization Approach.Journal of medicinal chemistry · 2025Article
- Barbituric Acid Derivatives as Covalent Inhibitors ofJournal of medicinal chemistry · 2025Article
- Recent advances in the antimicrobial application of the pyrrolo[2,3-RSC advances · 2025Review
- A concise synthesis of pyrrolo[2,3-d]pyrimidine through IBMC chemistry · 2025Article
- The allure of targets for novel drugs.RSC medicinal chemistry · 2024Review
- In Silico and In Vitro Search for Dual Inhibitors of theMolecules (Basel, Switzerland) · 2023Article
- Covalent Inhibitors for Neglected Diseases: An Exploration of Novel Therapeutic Options.Pharmaceuticals (Basel, Switzerland) · 2023Review
- Crystal structures of FolM alternative dihydrofolate reductase 1 from Brucella suis and Brucella canis.Acta crystallographica. Section F, Structural biology communications · 2022Article
- Sesquiterpene Lactones with Dual Inhibitory Activity against theMolecules (Basel, Switzerland) · 2021Article
- Repurposing the Trypanosomatidic GSK Kinetobox for the Inhibition of Parasitic Pteridine and Dihydrofolate Reductases.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Synthesis ofBeilstein journal of organic chemistry · 2021Article
- Article
- Essential multimeric enzymes in kinetoplastid parasites: A host of potentially druggable protein-protein interactions.PLoS neglected tropical diseases · 2017Article
- Chroman-4-One Derivatives Targeting Pteridine Reductase 1 and Showing Anti-Parasitic Activity.Molecules (Basel, Switzerland) · 2017Article
- New class of 8-aryl-7-deazaguanine cell permeable fluorescent probes.Bioorganic & medicinal chemistry letters · 2015Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
10 authors at 4 institutions in 1 country.
Funding
Abstract
The treatment of Human African trypanosomiasis remains a major unmet health need in sub-Saharan Africa. Approaches involving new molecular targets are important; pteridine reductase 1 (PTR1), an enzyme that reduces dihydrobiopterin in Trypanosoma spp., has been identified as a candidate target, and it has been shown previously that substituted pyrrolo[2,3-d]pyrimidines are inhibitors of PTR1 from Trypanosoma brucei (J. Med. Chem. 2010, 53, 221-229). In this study, 61 new pyrrolo[2,3-d]pyrimidines have been prepared, designed with input from new crystal structures of 23 of these compounds complexed with PTR1, and evaluated in screens for enzyme inhibitory activity against PTR1 and in vitro antitrypanosomal activity. Eight compounds were sufficiently active in both screens to take forward to in vivo evaluation. Thus, although evidence for trypanocidal activity in a stage I disease model in mice was obtained, the compounds were too toxic to mice for further development.
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.