Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore

A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. Incorporation of aryl and heteroaryl substitution in the 4-position of the thiazole ring resulted in a number of highly potent and selecti...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2000-09, Vol.10 (17), p.1971-1973
Main Authors: Mathvink, R J, Tolman, J S, Chitty, D, Candelore, M R, Cascieri, M A, Colwell, Jr, L F, Deng, L, Feeney, W P, Forrest, M J, Hom, G J, MacIntyre, D E, Tota, L, Wyvratt, M J, Fisher, M H, Weber, A E
Format: Article
Language:English
Subjects:
Adrenergic beta-3 Receptor Agonists
Adrenergic beta-Agonists - chemical synthesis
Adrenergic beta-Agonists - pharmacology
Animals
Benzenesulfonamides
CHO Cells
Cricetinae
Ethanolamines - chemical synthesis
Humans
Structure-Activity Relationship
Sulfonamides - chemical synthesis
Thiazoles - chemical synthesis
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Summary:A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. Incorporation of aryl and heteroaryl substitution in the 4-position of the thiazole ring resulted in a number of highly potent and selective beta3 agonists. Results of preliminary in vivo evaluation of several of these compounds is described.
ISSN:0960-894X