4-Aminopiperidine ureas as potent selective agonists of the human β₃-Adrenergic receptor

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• 作者：Ashwell ; Mark A. ; Solvibile Jr ; William R. ; Han ; Stella ; Largis ; Elwood ; Mulvey ; Ruth ; Tillet ; Jeffrey
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2001
• 出版时间：December 17, 2001
• 年：2001
• 卷：11
• 期：24
• 页码：3123-3127
• 全文大小：151 K

文摘

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