Potent and selective, sulfamide-based human β 3-adrenergic receptor agonists
…, NA Nardone, DA Tess, P DaSilva-Jardine
文献索引：Dow, Robert L.; Paight, Ernest S.; Schneider, Steven R.; Hadcock, John R.; Hargrove, Diane M.; Martin, Kelly A.; Maurer, Tristan S.; Nardone, Nancy A.; Tess, David A.; DaSilva-Jardine, Paul Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 12 p. 3235 - 3240
A series of sulfamide-based analogs related to L-796568 were prepared and evaluated for their biological activity at the human β3-adrenergic receptor (AR). This modification allows for a significant reduction in molecular weight, while maintaining single-digit nanomolar potencies at the β3-AR and high selectivities versus the β1-or β2-AR.
