Abstract
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.
MeSH terms
-
Adrenergic beta-3 Receptor Agonists*
-
Adrenergic beta-Agonists / chemistry*
-
Adrenergic beta-Agonists / metabolism
-
Adrenergic beta-Agonists / pharmacology
-
Animals
-
Humans
-
Oxygen Consumption / drug effects
-
Oxygen Consumption / physiology
-
Rats
-
Receptors, Adrenergic, beta-3 / metabolism
-
Sulfonamides / chemistry*
-
Sulfonamides / metabolism
-
Sulfonamides / pharmacology
Substances
-
Adrenergic beta-3 Receptor Agonists
-
Adrenergic beta-Agonists
-
Receptors, Adrenergic, beta-3
-
Sulfonamides