ArticleACS medicinal chemistry letters2012
Optimized 5-membered heterocycle-linked pterins for the inhibition of Ricin Toxin A.
Article in ACS medicinal chemistry letters, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
What it found
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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.
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Who cites it
11 citing papers in PubMed, 22 citations in OpenAlex.
- Identification and Biological Evaluation of a Novel Small-Molecule Inhibitor of Ricin Toxin.Molecules (Basel, Switzerland) · 2024Article
- Structure-based design and optimization of a new class of small molecule inhibitors targeting the P-stalk binding pocket of ricin.Bioorganic & medicinal chemistry · 2024Article
- The Search for Antidotes Against Ricin.Mini reviews in medicinal chemistry · 2024Review
- Crystal structure of ricin toxin A chain complexed with a highly potent pterin-based small-molecular inhibitor.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Article
- Pterin-based small molecule inhibitor capable of binding to the secondary pocket in the active site of ricin-toxin A chain.PloS one · 2022Article
- Synthesis and Structural Characterization of Ricin Inhibitors Targeting Ribosome Binding Using Fragment-Based Methods and Structure-Based Design.Journal of medicinal chemistry · 2021Article
- Thermochemical and Quantum Descriptor Calculations for Gaining Insight into Ricin Toxin A (RTA) Inhibitors.ACS omega · 2021Article
- Article
- Exploring the scope of DBU-promoted amidations of 7-methoxycarbonylpterin.Beilstein journal of organic chemistry · 2020Article
- Peptide-conjugated pterins as inhibitors of ricin toxin A.Journal of medicinal chemistry · 2013Article
Corrections and comments
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
Abstract
The optimization of a series of pterin amides for use as Ricin Toxin A (RTA) inhibitors is reported. Based upon crystallographic data of a previous furan-linked pterin, various expanded furans were synthesized, linked to the pterin and tested for inhibition. Concurrently, hetero-analogs of furan were explored, leading to the discovery of more potent triazol-linked pterins. Additionally, we discuss a dramatic improvement in the synthesis of these pterin amides via a dual role by diazabicycloundecene (DBU). This synthetic enhancement facilitates rapid diversification of the previously challenging pterin heterocycle, potentially aiding future medicinal research involving this structure.
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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.