ArticleACS medicinal chemistry letters2016
Discovery and Characterization of 2-Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Who cites it
23 citing papers in PubMed.
- Modified Julia Olefination Approach to Chiral α-Fluorovinyl Amino Alcohols and Amino Acids, via Fluorovinyl Oxazolidine Precursors, Conformational and Crystallographic Analyses.Chemistry (Weinheim an der Bergstrasse, Germany) · 2026Article
- Preclinical development of [European journal of nuclear medicine and molecular imaging · 2026Article
- Potential of Small Molecule TAAR-1 Agonists for the Therapy of Neurodegenerative Psychosis: A Medicinal Chemistry Perspective.Mini reviews in medicinal chemistry · 2026Review
- Article
- Computational Methods for the Discovery and Optimization of TAAR1 and TAAR5 Ligands.International journal of molecular sciences · 2024Review
- Discovery of a Novel Chemo-Type for TAAR1 Agonism via Molecular Modeling.Molecules (Basel, Switzerland) · 2024Article
- Unlocking the secrets of trace amine-associated receptor 1 agonists: new horizon in neuropsychiatric treatment.Frontiers in psychiatry · 2024Review
- Chemo- and enantioselective intramolecular silver-catalyzed aziridinations of carbamimidates.Chemical communications (Cambridge, England) · 2023Article
- Article
- Discovery of Guanfacine as a Novel TAAR1 Agonist: A Combination Strategy through Molecular Modeling Studies and Biological Assays.Pharmaceuticals (Basel, Switzerland) · 2023Article
- Robust aversive effects of trace amine-associated receptor 1 activation in mice.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2023Article
- Article
- Discovery of Trace Amine Associated Receptor 1 (TAAR1) Agonist 2-(5-(4'-Chloro-[1,1'-biphenyl]-4-yl)-4Biomolecules · 2022Article
- Discovery and In Vivo Efficacy of Trace Amine-Associated Receptor 1 (TAAR1) Agonist 4-(2-Aminoethyl)-International journal of molecular sciences · 2022Article
- Binding of SEP-363856 within TAAR1 and the 5HTMolecular psychiatry · 2022Review
- Therapeutic Potential of TAAR1 Agonists in Schizophrenia: Evidence from Preclinical Models and Clinical Studies.International journal of molecular sciences · 2021Review
- Progress in mechanistically novel treatments for schizophrenia.RSC medicinal chemistry · 2021Review
- Novel 1-Amidino-4-Phenylpiperazines as Potent Agonists at Human TAAR1 Receptor: Rational Design, Synthesis, Biological Evaluation and Molecular Docking Studies.Pharmaceuticals (Basel, Switzerland) · 2020Article
- Synthesis of Chiral Allylic Esters by Using the New Recyclable Chiral Heterogeneous Oxazoline-Based Catalysts.ACS omega · 2020Article
- Trace amine-associated receptor 1 (TAAR1) promotes anti-diabetic signaling in insulin-secreting cells.The Journal of biological chemistry · 2019Article
Corrections and comments
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
2-Aminooxazolines were discovered as a novel structural class of TAAR1 ligands. Starting from a known adrenergic compound 1, structural modifications were made to obtain highly potent and selective TAAR1 ligands such as 12 (RO5166017), 18 (RO5256390), 36 (RO5203648), and 48 (RO5263397). These compounds exhibit drug-like physicochemical properties, have good oral bioavailability, and display in vivo activity in a variety of animal models relevant for psychiatric diseases and addiction.
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