ArticleThe Journal of organic chemistry2012
Synthesis and profiling of a diverse collection of azetidine-based scaffolds for the development of CNS-focused lead-like libraries.
Article in The Journal of organic chemistry, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 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
42 citing papers in PubMed.
- Lewis Acid Catalyzed Dual Strain-Release Platform for Transforming Azabicyclo[1.1.0]butanes into Functionalized Azetidines with Donor-Acceptor(D-A) Cyclopropanes and Bicyclo[1.1.0]butanes.Organic letters · 2026Article
- Structural and mechanistic insights into azetidine-associated αKG-NHFe enzyme OkaE with multifunctional catalysis.Nature communications · 2026Article
- Diversity-oriented synthesis encoded by deoxyoligonucleotides.Nature communications · 2023Article
- Four-Component Strain-Release-Driven Synthesis of Functionalized Azetidines.Angewandte Chemie (International ed. in English) · 2022Article
- Arylboration of Enecarbamates for the Synthesis of Borylated Saturated N-Heterocycles.Angewandte Chemie (International ed. in English) · 2022Article
- Phenotypic Screening for Small Molecules that Protect β-Cells from Glucolipotoxicity.ACS chemical biology · 2022Article
- Intramolecular, Visible-Light-Mediated Aza Paternò-Büchi Reactions of Unactivated Alkenes.Organic letters · 2022Article
- Biocatalytic One-Carbon Ring Expansion of Aziridines to Azetidines via a Highly Enantioselective [1,2]-Stevens Rearrangement.Journal of the American Chemical Society · 2022Article
- The Use of Informer Sets in Screening: Perspectives on an Efficient Strategy to Identify New Probes.SLAS discovery : advancing life sciences R & D · 2021Article
- Structural basis of malaria parasite phenylalanine tRNA-synthetase inhibition by bicyclic azetidines.Nature communications · 2021Article
- Synthesis of azetidines via visible-light-mediated intermolecular [2+2] photocycloadditions.Nature chemistry · 2020Article
- Bicyclic azetidines kill the diarrheal pathogenScience translational medicine · 2020Article
- Modular, stereocontrolled CProceedings of the National Academy of Sciences of the United States of America · 2019Article
- Article
- Synergistic Effects of Stereochemistry and Appendages on the Performance Diversity of a Collection of Synthetic Compounds.Journal of the American Chemical Society · 2018Article
- Ring Expansion of Bicyclic Methyleneaziridines via Concerted, Near-Barrierless [2,3]-Stevens Rearrangements of Aziridinium Ylides.ACS catalysis · 2018Article
- Chemical probes and drug leads from advances in synthetic planning and methodology.Nature reviews. Drug discovery · 2018Review
- Recent updates in the discovery and development of novel antimalarial drug candidates.MedChemComm · 2018Review
- Anti-inflammatory and anti-oxidative effects of 3-(naphthalen-2-yl(propoxy)methyl)azetidine hydrochloride on β-amyloid-induced microglial activation.BMB reports · 2017Article
- Neuroprotective Effect of 3-(Naphthalen-2-Yl(Propoxy)Methyl)Azetidine Hydrochloride on Brain Ischaemia/Reperfusion Injury.Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology · 2017Article
Corrections and comments
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Authors and funding
25 authors.
Funding
Abstract
The synthesis and diversification of a densely functionalized azetidine ring system to gain access to a wide variety of fused, bridged, and spirocyclic ring systems is described. The in vitro physicochemical and pharmacokinetic properties of representative library members are measured in order to evaluate the use of these scaffolds for the generation of lead-like molecules to be used in targeting the central nervous system. The solid-phase synthesis of a 1976-membered library of spirocyclic azetidines is also described.
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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.