Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines

Robert J Steffan; Mark A Ashwell; William R Solvibile; Edward Matelan; Elwood Largis; Stella Han; Jeffery Tillet; Ruth Mulvey

doi:10.1016/s0960-894x(02)00608-x

Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2963-7. doi: 10.1016/s0960-894x(02)00608-x.

Authors

Robert J Steffan¹, Mark A Ashwell, William R Solvibile, Edward Matelan, Elwood Largis, Stella Han, Jeffery Tillet, Ruth Mulvey

Affiliation

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

PMID: 12270184
DOI: 10.1016/s0960-894x(02)00608-x

Abstract

The synthesis and SAR of a series of beta3 adrenoreceptor agonists based on a novel template derived from 4-aminomethylpiperidine coupled with a common pharmacophore, arylethylamine, is described. This combination led to the identification of human beta3 adrenoreceptor agonists with in vivo activity in a transgenic mouse model.

MeSH terms

Adrenergic beta-3 Receptor Agonists*
Adrenergic beta-Agonists / chemical synthesis*
Adrenergic beta-Agonists / pharmacology*
Animals
CHO Cells
Cricetinae
Humans
Indicators and Reagents
Mice
Mice, Transgenic
Piperidines / chemical synthesis*
Piperidines / pharmacology*
Receptors, Adrenergic, beta-3 / genetics
Structure-Activity Relationship

Substances

Adrenergic beta-3 Receptor Agonists
Adrenergic beta-Agonists
Indicators and Reagents
Piperidines
Receptors, Adrenergic, beta-3