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ID: ALA1134913
Journal: Bioorg Med Chem Lett
Title: Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.
Authors: Steffan RJ, Ashwell MA, Solvibile WR, Matelan E, Largis E, Han S, Tillet J, Mulvey R.
Abstract: The synthesis and SAR of a series of human beta3 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 beta3-AR (EC50=49 nM, IA=1.1), and in vivo active in a transgenic mouse model.
CiteXplore: 12270183