Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2

Bastien Reux; Tapio Nevalainen; Katri H. Raitio; Ari M.P. Koskinen

doi:10.1016/j.bmc.2009.05.013

Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2

Bastien Reux, Tapio Nevalainen, Katri H. Raitio, Ari M.P. Koskinen

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Abstract

A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.

Original language	English
Pages (from-to)	4441-4447
Journal	BIOORGANIC AND MEDICINAL CHEMISTRY
Volume	17
Issue number	13
DOIs	https://doi.org/10.1016/j.bmc.2009.05.013
Publication status	Published - 2009
MoE publication type	A1 Journal article-refereed

Keywords

cannabinoid
receptor CB2
quinoline
isoquinoline

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10.1016/j.bmc.2009.05.013

ms141Accepted author manuscript, 417 KB

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title = "Synthesis and agonist properties of novel quinoline and isoquinoline derivatives toward the cannabinoid receptor CB2",

abstract = "A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.",

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AU - Raitio, Katri H.

AU - Koskinen, Ari M.P.

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AB - A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB2 receptor-dependent G-protein activities were determined using the [35S]GTPcS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB2 receptor agonist activity, the most potent ligands being the 2-(Me2N)-phenyl substituted derivatives, which were also full agonists at the CB2-receptor.

KW - cannabinoid

KW - receptor CB2

KW - quinoline

KW - isoquinoline

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JO - BIOORGANIC AND MEDICINAL CHEMISTRY

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