Synthesis and evaluation of potent and selective beta3 adrenergic receptor agonists containing heterobiaryl carboxylic acids.
The design, synthesis, and SAR of a novel series of heterobiaryl phenethanolamine beta3 adrenergic receptor agonists are described. The furan analogue 49 was shown to elicit a significant dose-dependent lowering of plasma glucose in a rodent model of type 2 diabetes.
Shearer
Barry G
BG
Department of Medicinal Chemistry, GlaxoSmithKline, Research Triangle Park, NC 27709, USA. barry.g.shearer@gsk.com
Chao
Esther Y
EY
Uehling
David E
DE
Deaton
David N
DN
Cowan
Conrad
C
Sherman
Bryan W
BW
Milliken
Tula
T
Faison
Walter
W
Brown
Kathleen
K
Adkison
Kimberly K
KK
Lee
Frank
F
D058667:Adrenergic beta-3 Receptor Agonists; D001665:Binding Sites; D002264:Carboxylic Acids / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D058667:Adrenergic beta-3 Receptor Agonists; D002264:Carboxylic Acids