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Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore
Journal article   Peer reviewed

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

R J Mathvink, J S Tolman, D Chitty, M R Candelore, M A Cascieri, L F Colwell, Jr, L Deng, W P Feeney, M J Forrest, G J Hom, …
Bioorganic & medicinal chemistry letters, Vol.10(17), pp.1971-1973
09/04/2000
PMID: 10987429

Abstract

Ethanolamines - chemical synthesis Sulfonamides - chemical synthesis Cricetinae Animals Thiazoles - chemical synthesis Humans Adrenergic beta-Agonists - pharmacology Structure-Activity Relationship Adrenergic beta-Agonists - chemical synthesis Adrenergic beta-3 Receptor Agonists CHO Cells
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.

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