Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity

A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified. A high-throughput screening campaign resulted in the discovery of a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2008-03, Vol.18 (5), p.1725-1729
Main Authors: Ermann, Monika, Riether, Doris, Walker, Edward R., Mushi, Innocent F., Jenkins, James E., Noya-Marino, Beatriz, Brewer, Mark L., Taylor, Malcolm G., Amouzegh, Patricia, East, Stephen P., Dymock, Brian W., Gemkow, Mark J., Kahrs, Andreas F., Ebneth, Andreas, Löbbe, Sabine, O’Shea, Kathy, Shih, Daw-Tsun, Thomson, David
Format: Article
Language:English
Subjects:
Agonists
Arylsulfonamide
Biological and medical sciences
Cannabinoid receptor
CB1
CB2
Medical sciences
Miscellaneous
Molecular Structure
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Receptor, Cannabinoid, CB1 - agonists
Receptor, Cannabinoid, CB2 - agonists
Selectivity
Structure-Activity Relationship
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Summary:A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified. A high-throughput screening campaign resulted in the discovery of a highly potent dual cannabinoid receptor 1 (CB1) and 2 (CB2) agonist. Following a thorough SAR exploration, a series of selective CB2 full agonists were identified.
ISSN:0960-894X
0968-0896
1464-3405
1464-3391
DOI:10.1016/j.bmcl.2008.01.042