Parallel Synthesis and Biological Screening of Dopamine Receptor Ligands Taking Advantage of a Click Chemistry Based BAL Linker

Löber S, Gmeiner P, Hübner H (2005)


Publication Type: Journal article

Publication year: 2005

Journal

Publisher: American Chemical Society

Book Volume: 7

Pages Range: 309-316

DOI: 10.1021/cc049860s

Abstract

The click-chemistry-derived formyl indolyl methyl triazole (FIMT) resin 1a was evaluated for the parallel solid-phase synthesis of a series of BP-897-type arylcarboxamides. By application of a five-step sequence (including loading by reductive amination, subsequent amide coupling, deprotection, palladium-catalyzed N-arylation, and acidic cleavage), a focused library of putative dopamine D3 receptor ligands was constructed. The final products revealed good to excellent purity and were screened for binding at monoaminergic G-protein-coupled receptors when selected library members proved to show excellent binding affinity, especially toward the dopamine D3 receptor subtype. © 2005 American Chemical Society.

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How to cite

APA:

Löber, S., Gmeiner, P., & Hübner, H. (2005). Parallel Synthesis and Biological Screening of Dopamine Receptor Ligands Taking Advantage of a Click Chemistry Based BAL Linker. Journal of Combinatorial Chemistry, 7, 309-316. https://doi.org/10.1021/cc049860s

MLA:

Löber, Stefan, Peter Gmeiner, and Harald Hübner. "Parallel Synthesis and Biological Screening of Dopamine Receptor Ligands Taking Advantage of a Click Chemistry Based BAL Linker." Journal of Combinatorial Chemistry 7 (2005): 309-316.

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