ArticleBioorganic & medicinal chemistry letters2016
Synthesis and characterization of a series of chiral alkoxymethyl morpholine analogs as dopamine receptor 4 (D4R) antagonists.
Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Synthesis and Biological Characterization of 4,4-Difluoro-3-(phenoxymethyl)piperidine Scaffold as Dopamine 4 Receptor (DChemMedChem · 2025Article
- Recent progress in therapeutic applications of fluorinated five-membered heterocycles and their benzo-fused systems.RSC advances · 2024Review
- Computer-Aided Design and Biological Evaluation of Diazaspirocyclic DACS chemical neuroscience · 2024Article
- Pharmacology and Therapeutic Potential of Benzothiazole Analogues for Cocaine Use Disorder.Journal of medicinal chemistry · 2023Article
- From dopamine 4 to sigma 1: Synthesis, SAR and biological characterization of a piperidine scaffold of σ1 modulators.European journal of medicinal chemistry · 2022Article
- Nickel-catalyzed enantioselective α-heteroarylation of ketonesChemical science · 2022Article
- Discovery and characterization of benzyloxy piperidine based dopamine 4 receptor antagonists.Bioorganic & medicinal chemistry letters · 2022Article
- Receptor Ligands as Helping Hands to L-DOPA in the Treatment of Parkinson's Disease.Biomolecules · 2019Review
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
Herein, we report the synthesis and structure-activity relationship of a series of chiral alkoxymethyl morpholine analogs. Our efforts have culminated in the identification of (S)-2-(((6-chloropyridin-2-yl)oxy)methyl)-4-((6-fluoro-1H-indol-3-yl)methyl)morpholine as a novel potent and selective dopamine D4 receptor antagonist with selectivity against the other dopamine receptors tested (<10% inhibition at 1μM against D1, D2L, D2S, D3, and D5).
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Registered trials
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