1.
Bioorg Med Chem Lett
; 12(20): 2957-61, 2002 Oct 21.
Article
in English
| MEDLINE
| ID: mdl-12270183
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.
Subject(s)
Adrenergic beta-3 Receptor Agonists , Adrenergic beta-Agonists/chemical synthesis , Adrenergic beta-Agonists/pharmacology , Piperidines/chemical synthesis , Piperidines/pharmacology , Animals , CHO Cells , Cricetinae , Humans , Indicators and Reagents , Mice , Mice, Transgenic , Receptors, Adrenergic, beta-3/genetics , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 12(20): 2963-7, 2002 Oct 21.
Article
in English
| MEDLINE
| ID: mdl-12270184
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.