title: Novel substituted 4-aminomethylpiperidines as potent and selective human beta3-agonists. Part 2: arylethanolaminomethylpiperidines.
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.
authors.affiliation: Chemical Sciences, Wyeth Research, 500 Arcola Rd, Collegeville, PA 19426, USA. steffar@wyeth.com
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Steffan
authors.forename: Mark A
authors.initials: MA
authors.lastname: Ashwell
authors.forename: William R
authors.initials: WR
authors.lastname: Solvibile
authors.forename: Edward
authors.initials: E
authors.lastname: Matelan
authors.forename: Elwood
authors.initials: E
authors.lastname: Largis
authors.forename: Stella
authors.initials: S
authors.lastname: Han
authors.forename: Jeffery
authors.initials: J
authors.lastname: Tillet
authors.forename: Ruth
authors.initials: R
authors.lastname: Mulvey
mesh_terms: D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D016466:CHO Cells; D006224:Cricetinae; D006801:Humans; D007202:Indicators and Reagents; D051379:Mice; D008822:Mice, Transgenic; D010880:Piperidines / Q000138:chemical synthesis* / Q000494:pharmacology*; D022702:Receptors, Adrenergic, beta-3 / Q000235:genetics; D013329:Structure-Activity Relationship
chemical_list: D058667:Adrenergic beta-3 Receptor Agonists; D000318:Adrenergic beta-Agonists; D007202:Indicators and Reagents; D010880:Piperidines; D022702:Receptors, Adrenergic, beta-3