Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging

Nebel N, Maschauer S, Bartuschat A, Fehler S, Hübner H, Gmeiner P, Kuwert T, Heinrich M, Prante O, Hocke C (2014)


Publication Language: English

Publication Type: Journal article, Original article

Publication year: 2014

Journal

Publisher: Elsevier

Book Volume: 24

Pages Range: 5399-5403

DOI: 10.1016/j.bmcl.2014.10.043

Abstract

A series of fluoro substituted pyridinylcarboxamides and their phenylazo analogues with high affinity and selectivity for the dopamine D3 receptor was synthesized by the use of 6-fluoropyridine-3-carbonyl chloride (1) and fluorophenylazocarboxylic ester (2). Several of these compounds (9a-e and 10a-h) have been evaluated in vitro, among which 9b, 10a, 10c and 10d proved to have at least single-digit nanomolar affinity for D3. They also exhibit considerable selectivity over the other dopamine receptor subtypes and noteworthy selectivity over the structurally related serotonin receptor subtypes 5-HT1A and 5-HT2, offering potential radiotracers for positron emission tomography.

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APA:

Nebel, N., Maschauer, S., Bartuschat, A., Fehler, S., Hübner, H., Gmeiner, P.,... Hocke, C. (2014). Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging. Bioorganic & Medicinal Chemistry Letters, 24, 5399-5403. https://dx.doi.org/10.1016/j.bmcl.2014.10.043

MLA:

Nebel, Natascha, et al. "Synthesis and evaluation of fluoro substituted pyridinylcarboxamides and their phenylazo analogues for potential dopamine D3 receptor PET imaging." Bioorganic & Medicinal Chemistry Letters 24 (2014): 5399-5403.

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