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4-Aminopiperidine ureas as potent selective agonists of the human beta(3)-adrenergic receptor
M A Ashwell1, W R Solvibile, S Han
1Chemical Sciences, Wyeth-Ayerst Research, PO Box CN-8000, USA. mashwell@arqule.com
Bioorganic & Medicinal Chemistry Letters
|November 27, 2001
Abstract:
The preparation and structure-activity relationships (SARs) of potent agonists of the human beta(3)-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human beta(3)-AR potency with selectivity over human beta(1)-AR and/or human beta(2)-AR agonism. Compound 29s was identified as a potent (EC(50)=1nM) and selective (greater than 400-fold over beta(1)- with no beta(2)-AR agonism) full beta(3)-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.