Novel substituted 4-aminomethylpiperidines as potent and selective human β 3-agonists. Part 1: aryloxypropanolaminomethylpiperidines

…, E Matelan, E Largis, S Han, J Tillet, R Mulvey

Index: Steffan, Robert J.; Ashwell, Mark A.; Solvibile, William R.; Matelan, Edward; Largis, Elwood; Han, Stella; Tillet, Jeffery; Mulvey, Ruth Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 20 p. 2957 - 2961

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Citation Number: 12

Abstract

The synthesis and SAR of a series of human β3 adrenoreceptor agonists based on a template derived from a common pharmacophore coupled with 4-aminomethylpiperidine is described. Potent and selective agents were identified such as 26 that was in vitro active in CHO cells expressing human β3-AR (EC50= 49 nM, IA= 1.1), and in vivo active in a transgenic mouse model.