4-Aminopiperidine ureas as potent selective agonists of the human β 3-Adrenergic receptor

…, WR Solvibile, S Han, E Largis, R Mulvey…

文献索引：Ashwell, Mark A; Solvibile Jr., William R; Han, Stella; Largis, Elwood; Mulvey, Ruth; Tillet, Jeffrey Bioorganic and Medicinal Chemistry Letters, 2001 , vol. 11, # 24 p. 3123 - 3127

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被引用次数: 17

摘要

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= 1nM) and selective (greater than 400-fold over β1-with no β2-AR agonism) full β3-AR agonist with in vivo ...