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Bioorg Med Chem Lett. 2002 Oct 21;12(20):2957-61.

Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 1: aryloxypropanolaminomethylpiperidines.

Author information

1
Chemical Sciences, Wyeth Research, 500 Arcola Rd, Collegeville, PA 19426, USA. steffar@wyeth.com

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.

PMID:
12270183
DOI:
10.1016/s0960-894x(02)00607-8
[Indexed for MEDLINE]

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