Potent, selective 3-pyridylethanolamine β3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore

Robert J Mathvink,J.Samuel Tolman,Dawn Chitty,Mari R Candelore,Margaret A Cascieri,Lawrence F Colwell,Liping Deng,William P Feeney,Michael J Forrest,Gary J Hom,D.Euan MacIntyre,Laurie Tota,Matthew J Wyvratt,Michael H Fisher,Ann E Weber

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（2000）

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摘要

A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human β3 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 β3 agonists. Results of preliminary in vivo evaluation of several of these compounds is described.

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