132059-11-1Relevant articles and documents
Potent benzimidazolone based human β3-adrenergic receptor agonists
Finley, Don R.,Bell, Michael G.,Borel, Anthony G.,Bloomquist, William E.,Cohen, Marlene L.,Heiman, Mark. L.,Kriauciunas, Aidas,Matthews, Donald P.,Miles, Tania,Neel, David A.,Rito, Christopher J.,Sall, Daniel J.,Shuker, Anthony J.,Stephens, Thomas W.,Tinsley, Frank C.,Winter, Mark A.,Jesudason, Cynthia D.
, p. 5691 - 5694 (2007/10/03)
The synthesis and biological evaluation of a series of benzimidazolone β3 adrenergic receptor agonists are described. A trend toward the reduction of rat atrial tachycardia upon increasing steric bulk at the 3-position of the benzimidazolone mo
4-Aminopiperidine ureas as potent selective agonists of the human β3-Adrenergic receptor
Ashwell, Mark A,Solvibile Jr., William R,Han, Stella,Largis, Elwood,Mulvey, Ruth,Tillet, Jeffrey
, p. 3123 - 3127 (2007/10/03)
The preparation and structure-activity relationships (SARs) of potent agonists of the human β3-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human β3-AR potency with selectivity over human β1-AR and/or human β2-AR agonism. Compound 29s was identified as a potent (EC50 = 1 nM) and selective (greater than 400-fold over β1- with no β2-AR agonism) full β3-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.
A simplified template approach towards the synthesis of a potent beta-3 adrenoceptor agonist at the human receptor
Beeley,Berge,Chapman,Dean,Kelly,Lowden,Kotecha,Morgan,Rami,Thompson,Vong,Ward
, p. 219 - 224 (2007/10/03)
A simplified template approach was used to delineate the structural requirements for high potency and intrinsic activity of aryloxypropanolamines as agonists at the human beta-3 adrenoceptor. The information generated was used to prepare selective beta-3 adrenoceptor agonists.
