Potent and selective, sulfamide-based human beta 3-adrenergic receptor agonists.
A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human beta(3)-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the beta(3)-AR and high selectivities versus the beta(2)- or beta(3)-AR.
Dow
Robert L
RL
Cardiovascular and Metabolic Diseases, Pfizer Global Research and Development, Groton, CT 06340, USA. robert_l_dow@groton.pfizer.com
Paight
Ernest S
ES
Schneider
Steven R
SR
Hadcock
John R
JR
Hargrove
Diane M
DM
Martin
Kelly A
KA
Maurer
Tristan S
TS
Nardone
Nancy A
NA
Tess
David A
DA
DaSilva-Jardine
Paul
P
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D000818:Animals; D006801:Humans; D010101:Oxygen Consumption / Q000187:drug effects / Q000502:physiology; D051381:Rats; D022702:Receptors, Adrenergic, beta-3 / Q000378:metabolism; D013449:Sulfonamides / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology
D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D022702:Receptors, Adrenergic, beta-3; D013449:Sulfonamides